U.S. patent application number 13/870845 was filed with the patent office on 2013-11-21 for sunscreen compositions comprising uniform, rigid, spherical, nanoporous calcium phosphate particles and methods of making and using the same.
This patent application is currently assigned to Laboratory Skin Care, Inc.. The applicant listed for this patent is Laboratory Skin Care, Inc.. Invention is credited to Rodica-Tatiana Canelide, Zahra Mansouri, Tetsuro Ogawa, Douglas Thomas.
Application Number | 20130309305 13/870845 |
Document ID | / |
Family ID | 43992384 |
Filed Date | 2013-11-21 |
United States Patent
Application |
20130309305 |
Kind Code |
A1 |
Mansouri; Zahra ; et
al. |
November 21, 2013 |
Sunscreen Compositions Comprising Uniform, Rigid, Spherical,
Nanoporous Calcium Phosphate Particles and Methods of Making and
Using the Same
Abstract
Aspects of the invention include sunscreen formulations that
include uniform, rigid, spherical nanoporous calcium phosphate
particles. Also provided are methods of making the sunscreen
formulations. The sunscreen formulations find use in sunblocking
applications.
Inventors: |
Mansouri; Zahra; (Tahoe
City, CA) ; Canelide; Rodica-Tatiana; (Menlo Park,
CA) ; Thomas; Douglas; (Tahoe City, CA) ;
Ogawa; Tetsuro; (Tahoe City, CA) |
|
Applicant: |
Name |
City |
State |
Country |
Type |
Laboratory Skin Care, Inc.; |
|
|
US |
|
|
Assignee: |
Laboratory Skin Care, Inc.
Tahoe City
CA
|
Family ID: |
43992384 |
Appl. No.: |
13/870845 |
Filed: |
April 25, 2013 |
Related U.S. Patent Documents
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Application
Number |
Filing Date |
Patent Number |
|
|
12943887 |
Nov 10, 2010 |
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13870845 |
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61259935 |
Nov 10, 2009 |
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Current U.S.
Class: |
424/489 ;
424/59 |
Current CPC
Class: |
A61K 8/37 20130101; A61K
8/29 20130101; A61K 2800/60 20130101; A61K 8/24 20130101; A61K
8/025 20130101; A61K 8/0279 20130101; A61K 2800/412 20130101; A61K
2800/5922 20130101; A61K 8/27 20130101; A61Q 17/04 20130101; A61K
8/40 20130101; A61K 2800/56 20130101 |
Class at
Publication: |
424/489 ;
424/59 |
International
Class: |
A61K 8/02 20060101
A61K008/02; A61Q 17/04 20060101 A61Q017/04 |
Claims
1. A sunscreen composition comprising: uniform, rigid, spherical,
nanoporous calcium phosphate particles; and a sunscreen delivery
vehicle.
2. The sunscreen composition according to claim 1, wherein the
uniform, rigid, spherical, nanoporous calcium phosphate particle is
ceramic.
3. The sunscreen composition according to claim 1, wherein the
uniform, rigid, spherical, nanoporous calcium phosphate particle
has a diameter ranging from 0.05 to 50 .mu.m.
4. The sunscreen composition according to claim 1, wherein the
uniform, rigid, spherical, nanoporous calcium phosphate particle
have a surface area ranging from 10 m.sup.2/g to 150 m.sup.2/g.
5. The sunscreen composition according to claim 1, wherein the
uniform, rigid, spherical, nanoporous calcium phosphate particle
comprises pores are sintered.
6. The sunscreen composition according to claim 1, wherein the
uniform, rigid, spherical, nanoporous calcium phosphate particle
comprises pores are loaded with anti-oxidants.
7. The sunscreen composition according to claim 1, wherein the
uniform, rigid, spherical, nanoporous calcium phosphate particle
comprises pores are loaded with additional sunscreens.
8. The sunscreen composition according to claim 1, wherein the
sunscreen delivery vehicle is an oil-in-water or water-in-oil
emulsion.
9. The sunscreen composition according to claim 1, wherein the
sunscreen delivery vehicle comprises inorganic UV shielding
particles; organic UV absorbers; a polymeric water-proof component
and a lipophilic component.
10. A sunscreen composition comprising by weight: (a) from 0.001%
to 10% of uniform rigid spherical nanoporous calcium phosphate
particles; (b) from about 0.1% to about 50% of inorganic UV
shielding particles; (c) from about 0.1% to about 15% of organic UV
absorbers; (d) from about 0.1% to about 10% of a polymeric
water-proof component; (e) 30% or more lipophilic component; and
(f) water.
11. The sunscreen composition according to claim 10, wherein the
uniform, rigid, spherical, nanoporous calcium phosphate particle is
ceramic.
12. The sunscreen composition according to claim 10, wherein the
uniform, rigid, spherical, nanoporous calcium phosphate particle
has a diameter ranging from 0.05 to 50 .mu.m.
13. The sunscreen composition according to claim 10, wherein the
uniform, rigid, spherical, nanoporous calcium phosphate particle
have a surface area ranging from 10 m.sup.2/g to 150 m.sup.2/g.
14. The sunscreen composition according to claim 10, wherein the
uniform, rigid, spherical, nanoporous calcium phosphate particle
comprises pores are sintered.
15. The sunscreen composition according to claim 10, wherein the
uniform, rigid, spherical, nanoporous calcium phosphate particle
comprises pores are loaded with anti-oxidants.
16. The sunscreen composition according to claim 10, wherein the
uniform, rigid, spherical, nanoporous calcium phosphate particle
comprises pores are loaded with organic or inorganic UV absorbers
and/or blockers.
17. A method comprising: applying a sunscreen composition
comprising: (a) uniform, rigid, spherical, nanoporous calcium
phosphate particles; and (b) a sunscreen delivery vehicle; to a
topical region of a subject.
18. The method according to claim 17, wherein the topical region is
a keratinized skin surface.
Description
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] Pursuant to 35 U.S.C. .sctn.119 (e), this application claims
priority to the filing date of U.S. Provisional Patent Application
Ser. No. 61/259,935 filed Nov. 10, 2009; the disclosure of which
application is herein incorporated by reference.
INTRODUCTION
[0002] It is well recognized that solar ultraviolet (UV) radiation
poses a serious threat to human skin, which may range from the
short term hazard like erythema, i.e., sunburn, to long term
hazards like skin cancer and/or premature aging of the skin. UV
radiation having a wavelength of 290 nm to 320 nm, generally
referred to as UVB radiation, is known to cause erythema. In
addition, numerous studies point to exposure of unprotected skin to
UV radiation having a wavelength of from 320 nm to 400 nm,
generally referred to as UVA radiation, as being the primary cause
of skin cancer. It is important therefore, that skin is protected
from both UVA and UVB radiations to avoid the long and short term
deleterious effects of solar radiation.
[0003] The sun protection factor (SPF) rating system has been
developed to help consumers select the appropriate sun protection
product for any given outdoor activity involving exposure to the
sun. The SPF rating corresponds to a multiplying factor by which
the duration of protection by a properly applied sunscreen exceeds
the exposure time that causes unprotected skin to darken. Thus,
with proper application of an SPF 8 product, a person should be
able to remain in the sun without skin darkening for eight times
the usual unprotected duration.
[0004] In recent years, due to the increased public awareness of UV
radiation hazards, the use of sun protection products has grown
considerably, with consumers preferring products that have high SPF
ratings and offer protection over the entire range of UV radiation,
i.e., from 290 nm to 400 nm. These products typically contain
certain UV-absorbers that are approved for use in sunscreen
compositions by regulatory agencies (for example, US Food and Drug
Administration (FDA) in the USA and COLIPA in the European Union).
These approved UV-absorbers are either organic compounds, referred
to in the art as organic UV-absorbers or sunscreens, or inorganic
compounds, referred to in the art as inorganic UV-absorbers or
sunscreens. At present, approved inorganic UV-absorbers are
inorganic oxides such as titanium dioxide (TiO.sub.2) and zinc
oxide (ZnO). Among these inorganic oxide sunscreens, ZnO is capable
of absorbing substantial amounts of UVA-radiation, and hence is
often used as a UVA-sunscreen.
SUMMARY
[0005] Aspects of the invention include sunscreen formulations that
include uniform, rigid, spherical nanoporous calcium phosphate
particles. Also provided are methods of making the sunscreen
formulations. The sunscreen formulations find use in sunblocking
applications.
DETAILED DESCRIPTION
[0006] Aspects of the invention include sunscreen formulations that
include uniform, rigid, spherical nanoporous calcium phosphate
particles. Also provided are methods of making the sunscreen
formulations. The sunscreen formulations find use in sunblocking
applications.
[0007] Before the present invention is further described, it is to
be understood that this invention is not limited to particular
embodiments described, as such may vary. It is also to be
understood that the terminology used herein is for the purpose of
describing particular embodiments only, and is not intended to be
limiting, since the scope of the present invention will be limited
only by the appended claims.
[0008] Where a range of values is provided, it is understood that
each intervening value, to the tenth of the unit of the lower limit
unless the context clearly dictates otherwise, between the upper
and lower limit of that range and any other stated or intervening
value in that stated range, is encompassed within the invention.
The upper and lower limits of these smaller ranges may
independently be included in the smaller ranges and are also
encompassed within the invention, subject to any specifically
excluded limit in the stated range. Where the stated range includes
one or both of the limits, ranges excluding either or both of those
included limits are also included in the invention.
[0009] Certain ranges are presented herein with numerical values
being preceded by the term "about." The term "about" is used herein
to provide literal support for the exact number that it precedes,
as well as a number that is near to or approximately the number
that the term precedes. In determining whether a number is near to
or approximately a specifically recited number, the near or
approximating unrecited number may be a number which, in the
context in which it is presented, provides the substantial
equivalent of the specifically recited number.
[0010] Methods recited herein may be carried out in any order of
the recited events which is logically possible, as well as the
recited order of events.
[0011] Unless defined otherwise, all technical and scientific terms
used herein have the same meaning as commonly understood by one of
ordinary skill in the art to which this invention belongs. Although
any methods and materials similar or equivalent to those described
herein can also be used in the practice or testing of the present
invention, the preferred methods and materials are now
described.
[0012] All publications mentioned herein are incorporated herein by
reference to disclose and describe the methods and/or materials in
connection with which the publications are cited.
[0013] It must be noted that as used herein and in the appended
claims, the singular forms "a", "an", and "the" include plural
referents unless the context clearly dictates otherwise. It is
further noted that the claims may be drafted to exclude any
optional element. As such, this statement is intended to serve as
antecedent basis for use of such exclusive terminology as "solely,"
"only" and the like in connection with the recitation of claim
elements, or use of a "negative" limitation.
[0014] The publications discussed herein are provided solely for
their disclosure prior to the filing date of the present
application. Nothing herein is to be construed as an admission that
the present invention is not entitled to antedate such publication
by virtue of prior invention. Further, the dates of publication
provided may be different from the actual publication dates which
may need to be independently confirmed.
Sunscreen Formulations Comprising Uniform, Rigid, Spherical,
Nanoporous Calcium Phosphate Particles
[0015] Aspects of the invention include sunscreen compositions.
While the SPF value of sunscreen compositions of the invention may
vary, in some instances the compositions have an SPF value of 4 or
more, e.g., 8 or more, 15 or more, 20 or more, 30 or more, 40 or
more, 50 or more, 60 or more, including 70 or more. The
compositions may have a UV-A protection value of 1 or more, such as
2 or more, e.g., 2.25 or more, etc., such as 4 or more, e.g., 8 or
more, 15 or more, 20 or more, 30 or more, 40 or more, 50 or more,
60 or more, including 70 or more. SPF and UV-A protection values
may be determined using any convenient protocol, such as the
protocols reported in the Experimental Section, below.
[0016] As summarized above, aspects of the invention include
sunscreen formulations. Sunscreen formulations of the invention
include uniform, rigid, spherical, nanoporous calcium phosphate
particles in a sunscreen delivery vehicle, where the sunscreen
delivery vehicle may or may not include additional sunscreens,
e.g., organic or inorganic sunscreens. Each of these components is
now described separately in greater detail.
Uniform, Rigid, Spherical, Nanoporous Calcium Phosphate
Particles
[0017] The calcium phosphate particles of the sunscreen
formulations described herein are uniform, rigid, spherical,
nanoporous calcium phosphate particles. By "uniform" is meant that
the shape of the particles does not vary substantially, such that
the particles have substantially the same spherical shape. By
"rigid" is meant that the particles are hard, such that they are
not pliant. The term "spherical" is employed in its conventional
sense to mean a round body whose surface is at all points
substantially equidistant from the center. Of interest are calcium
phosphate particles in which the median diameter is 100 .mu.m or
less, such as 75 .mu.m or less, including 50 .mu.m or less, e.g.,
25 .mu.m or less, such as 20 .mu.m or less, such as 10 .mu.m or
less, including 5 .mu.m or less, where in some instances the medium
diameter is 4 .mu.m or less, such as 3 .mu.m or less, including 2
.mu.m or less, including 1 .mu.m or less, including 0.1 .mu.m or
less. In a given calcium phosphate particulate composition, a
distribution of diameters may be present, where in some instances
the majority (such as 60% or more, 75% or more, 90% or more, 95% or
more) of the particles have diameters that range from 0.01 to 20
.mu.m, such as from 0.1 to 10 .mu.m, and including from 0.1 to 2
.mu.m. In some instances, the proportion of the particles that have
an average particle diameter of 2 .mu.m or less is 50% or more by
number, such as 70% or more by number, including 90% or more by
number. In some instances, the compositions includes two more
distinct populations of particles that differ from each other in
terms if diameter, e.g., where the magnitude of the difference may
be 10% or more, such as 20% or more. The number of distinct
population sizes may vary, and in some instances may be 2 or more,
such as 3 or more, 4 or more, 5 or more, 6 or more, etc. In such
embodiments, each distinct population may be present in varying
amounts with respect to the total amount of calcium phosphate
particles, e.g., where each distinct population is present in an
amount ranging from 0.5 to 99.5% by weight, such as 1 to 75% by
weight, including 1 to 50% by weight of the total weight of the
calcium phosphate particles.
[0018] The particles are nanoporous. By "nanoporous" is meant that
the particles have a porosity of 30% or more, such as 40% or more,
including 50% or more, where the porosity may range from 30% to
85%, such as from 40% to 70%, including from 45% to 55%, as
determined using a mercury intrusion porosimeter porosity
determination protocol as described in ASTM D 4284-88 "Standard
Test Method for Determining Pore Volume Distribution of Catalysts
by Mercury Intrusion Porosimetry". Porosity is also described by
"pore volume (ml/g)" and in such instances many range from 0.1 ml/g
to 2.0 ml/g. In some cases, the particles have a porosity such that
their internal surface area ranges from 10 m.sup.2/g to 150
m.sup.2/g, such as from 20 m.sup.2/g to 100 m.sup.2/g, including 30
m.sup.2/g to 80 m.sup.2/g, as determined using a BET gas adsorption
surface area determination protocol as described in ASTM D3663-03
Standard Test Method for Surface Area of Catalysts and Catalyst
Carriers. The pore diameter may vary, ranging in certain instances
from 2 to 100 nm, such as 5 to 80 nm, including 10 to 60 nm. In
addition, the particles may have a tapping density ranging from 0.2
g/cm.sup.3 to 0.5 g/cm.sup.3, such as from 0.25 g/cm.sup.3 to 0.45
g/cm.sup.3, including from 0.3 g/cm.sup.3 to 0.4 g/cm.sup.3. The
tap density can be measured by using standard ASTM WK13023--New
Determination of Tap Density of Metallic Powders by a Constant
Volume Measuring Method.
[0019] The particles are, in some instances, not activated with
trace elements, such that they do not include amounts of trace
elements such as Zn, Mn, or Mg. In some instances, the particles do
no include at least partial substitution of an organic anion, e.g.,
lactate, for the hydroxide anion. In some instances, the particles
are not apalight, i.e., the chemical formula of the particles is
not (Zn, Mn, Mg)Ca.sub.5(PO.sub.4).sub.3(OH)(Lactate). The
particles are, in some instances, chemically pure. By chemically
pure is meant that the particles are made up of substantially one
type of calcium phosphate mineral. In some instances, the calcium
phosphate particles are described by the molecular formula
Ca.sub.10(PO.sub.4).sub.6(OH).sub.2.
[0020] In some instances, the particles are ceramic particles. By
ceramic is meant that the particles are produced using a method
which includes a step of subjecting the particles to high
temperature conditions, where such conditions are illustrated
below. High temperatures may range from 200 to 1000.degree. C.,
such as 300 to 900.degree. C. and including 300 to 800.degree. C.
In some embodiments, the particles have a compression rupture
strength ranging from 20 to 200 MPa, such as from 50 to 150 MPa,
and including 75 to 90 MPa, as determined using a SHIMADZU MCT-W500
micro-compression testing machine particle strength determination
protocol with a particle sintered at temperature of 400.degree. C.
to 900.degree. C., as described in European Patent EP1840661.
[0021] In some embodiments, the particles are biodegradable, by
which is meant that the particles degrade in some manner, e.g.,
dissolve, over time under physiological conditions. As the
particles of these embodiments are biodegradable under
physiological conditions, they at least begin to dissolve at a
detectable rate under conditions of pH of 5 or less, such as 4.5 or
less, including 4.3 or less. As such, the particles exhibit
solubility under acidic environments of pH 5 or less, such as upon
application to the skin.
[0022] The calcium phosphate particles are non-toxic, e.g., as
determined via US-FDA 21 CFR Part 58, non-mutagenic, e.g., as
determined by Mutagenicity Ames Test, and non-irritating, e.g., as
determined via Skin Sensitization RIPT (Human).
[0023] While the uniform, rigid, spherical, nanoporous calcium
phosphate particles of the sunscreen compositions may vary in a
variety of different parameters, including as reviewed above, in
some embodiments the particles employed in the sunscreen
compositions are chemically pure particles that have a mean
diameter of 2 .mu.m.
[0024] The uniform, rigid, spherical, nanoporous calcium phosphate
particles of the sunscreen compositions of the invention may be
prepared using any convenient protocol. Examples of fabrication
protocols of interest include, but are not limited to, those
described in U.S. Pat. Nos. 4,781,904; 5,039,408; 5,082,566; and
5,158,756; the disclosures of which are herein incorporated by
reference. In one protocol of interest, the particles are
manufactured by spray drying a slurry that includes nano calcium
phosphate (e.g., hydroxyapatite) crystals (which may range from 2
nm to 100 nm size range) to produce uniform spherical nanoporous
calcium phosphate particles. The resultant particles are then
sintered for a period of time sufficient to provide mechanically
and chemically stable rigid spheres. In this step, the sintering
temperatures may range from 200.degree. C. to 1000.degree. C., such
as 300.degree. C. to 900.degree. C. and including 300.degree. C. to
800.degree. C. for a period of time ranging from 1 hour to 10
hours, such as 2 hours to 8 hours and including 3 hours to 6 hours.
Additional details regarding this method of manufacturing the
uniform, rigid, spherical, nanoporous calcium phosphate particles
are provided in U.S. Provisional Application Ser. No. 61/108,805,
the disclosure of which is herein incorporated by reference.
[0025] Where desired, initially porous particles, e.g., as
described above, may be rendered non-porous prior to combination
with the sunscreen delivery vehicle in preparing the sunscreen
compositions. Accordingly, in some instances the calcium phosphate
particles present in the sunscreen compositions are non-porous. In
these embodiments, initially porous particles may be combined with
a suitable filler, e.g., an inert filler, so that the porosity of
the pores is reduced by a desired amount. In such applications,
loading protocols described in copending application Ser. No.
12/565,687 (the disclosure of which is herein incorporated by
reference), may be employed.
[0026] In addition, as further described below, the particles may
also be loaded with one or more components of the sunscreen
composition, e.g., organic or inorganic sunscreen blocking agents,
antioxidants, etc.
Sunscreen Delivery Vehicle
[0027] Sunscreen compositions of the invention include a suitable
amount of the above described particles present in a sunscreen
delivery vehicle (i.e., topical delivery vehicle) that is
configured for application to a topical site of a living subject,
such as a human. As such, sunscreen compositions of the invention
are compositions that are formulated for application to a
keratinized skin surface of a mammalian subject, such as a human
subject. By keratinized skin surface is meant a skin location of a
subject, i.e., a location of the external covering or integument of
an animal body. Because the topical compositions of the invention
are formulated for delivery to topical location, they are
formulated so as to be physiologically compatible with the topical
location for which they are formulated. Accordingly, when contacted
with the target keratinized skin surface for which they are
formulated, the topical compositions do not cause substantial, if
any, physiological responses (such as inflammation or irritation)
that would render the use of the topical compositions unsuitable
for topical application.
[0028] As indicated above, the sunscreen compositions include an
amount of uniform, rigid, spherical nanoporous calcium phosphate
particles, e.g., as described above. In a given sunscreen
composition, a distribution of diameters for the particles thereof
may be present, where in some instances the majority (such as 60%
or more, 75% or more, 90% or more, 95% or more) of the particles
have diameters that range from 0.01 to 20 .mu.m, such as 0.05 to 15
.mu.m such as from 0.1 to 10 .mu.m, and including from 0.1 to 2
.mu.m. In some instances, the proportion of the particles that have
an average particle diameter of 2 .mu.m or less is 50% or more by
number, such as 70% or more by number, including 90% or more by
number. In some instances, formulations are manufactured to include
two or more, including 3 or more, 4 or more, 5 or more, etc.,
discrete particle size populations, where each particle size
population has a different average particle size. For example, a
composition may include a first particle size population having an
average particle size ranging from 0.1 to 2 .mu.m and a second
particle size population having an average particle size ranging
from 2 to 20 .mu.m. Where two or more different particle size
populations are present, the difference in average particle size
between any two particle size populations may vary, and in certain
embodiments is 1 .mu.m or greater, such as 2 .mu.m or greater,
including 3 .mu.m or greater, 5 .mu.m or greater, and 10 .mu.m or
greater.
[0029] The total amount of a particles that is present in a given
sunscreen composition and therefore combined with a sunscreen
delivery vehicle may vary. In some instances, the total amount of
calcium phosphate particles present in the composition is
sufficient to increase the SPF factor of the composition as
compared to a control (i.e., the same formulation lacking the
calcium phosphate particles) by a magnitude of 1 or more, such as 2
or more, e.g., 3 or more, 4 or more, 5 or more, 6 or more, 7 or
more, 8 or more, 9 or more, 10 or more, where in some instances the
magnitude increase in SPF factor ranges from 0.5 to 5, such as 1 to
4, e.g., 2 to 3. In some instances, the total amount of calcium
phosphate particles present in the composition is sufficient to
increase the UV-A protection value of the composition as compared
to a control (i.e., the same formulation lacking the calcium
phosphate particles) by a magnitude of 0.1 or more, such as 0.2 or
more, e.g., 0.3 or more, 0.4 or more, 0.5 or more, 0.6 or more, 0.7
or more, 0.8 or more, 0.9 or more, 1.0 or more. In some
embodiments, the amount of particles present in the delivery
vehicle ranges from 0.01 to 200 mg/g, such as 0.1 to 100 mg/g and
including 1 to 50 mg/g active agent loaded particles per gram of
delivery vehicle. In certain embodiments the particles are present
in compositions in an amount ranging from about 0.001 to about 80%
by weight, such as from about 0.01 to about 70% by weight, and
including from about 0.05 to about 60% by weight, e.g., 0.1 to 10%
by weight, such as 0.1 to 5% by weight, including 1% by weight.
[0030] As indicated above, the sunscreen compositions of the
invention further include a sunscreen delivery vehicle. The
sunscreen delivery vehicle (i.e., topical delivery component)
refers to that portion of the sunscreen composition that is not the
calcium phosphate particles, where this portion of the sunscreen
composition may include a number of different and varying
components, as reviewed below. Sunscreen delivery vehicles of
interest include vehicles formulated for application to a topical
region or surface of a subject, such as a keratinized skin surface.
The subject compositions may be formulated as stable solutions or
suspensions of the components, e.g., in an aqueous solvent. Where
desired, the components may be combined with one or more carrier
materials to form a solution, suspension, gel, lotion, cream,
ointment, aerosol spray or the like, as desired. In some instances,
the sunscreen delivery vehicle is an oil-in-water or water-in-oil
emulsion composition.
[0031] Sunscreen delivery vehicles of interest include, optionally,
one or more additional sunscreens and a carrier.
Additional Sunscreens
[0032] In some instances, the sunscreen composition of the
invention may include an amount of an additional sunscreen
component, e.g., UV absorber or UV scatterer, which may be
inorganic or organic. The additional sunscreen component (such as
UV absorber) may absorb and/or physically block UV-B radiation,
e.g., UV-B and/or both UV-A radiation. In some instances, one or
more additional sunscreen components may be present in type and
amount that provides for more UV-B screening than UV-A screening,
e.g., in compositions configured or formulated to provide for the
occurrence of a "natural" tan. In some instances, the sunscreen
compositions of the present invention will be effective against
both UV-A and UV-B and have either strong UV-A/UV-B sunblock
actives or the presence of an additional UV-A sunblock active,
e.g., to provide a balanced UV-A/UV-B blocking composition. Of
interest are inorganic actives that work by reflecting the UV light
and organic actives that work, predominately, by absorbing UV
energy. The amount of the sunblock active to be incorporated into
the sunscreen formulations, when present, may vary.
[0033] Organic sunscreen components of interest include, but are
not limited to, avobenzone, butyl methoxydibenzoylmethane,
cinoxate, benzophenone-8, dioxybenzone, homosalate, octylsalate,
menthyl anthranilate, octocrylene, ethyhexyl methoxycinnamate,
octyl methoxycinnamate, octyl salicylate, oxybenzone, padimate O,
ethylhexyl salicylate, benzophenone-3, p-aminobenzoic acid (PABA),
ethylhexyl dimethyl PABA, glyceryl PABA, phenylbenzimidazole
sulfonic acid, sulfisobezone, trolamine salicylate,
4-methylbenzylidene camphor, bisoctrizole, bemotrizinol, ecamsule,
drometrizole trisiloxane, disodium phenyl dibenzimidazole
tetrasulfonate, diethylamine hydroxybenzoyl hexyl bezoate, octyl
triazone, hexyl benzoate, benzophenone-4, ethyhexyl triazone,
diethylhexyl butamido triazone, bisimidazylate, polysilicone-15,
2-ethylhexyl 2-cyano-3,3-diphenyl-2-propenoate (octrocrylene),
etc.
[0034] Inorganic sunscreens of interest include, but are not
limited to, titanium oxide, e.g., microfine surface treated
titanium dioxide, and zinc oxide, e.g., microfine untreated and
surface treated zinc oxide. The titanium dioxide in the sunscreen
compositions may have a mean primary particle size of between 5 and
150 nm, preferably between 10 and 100 nm. Titanium oxide may have
an anatase, rutile, or amorphous structure. The zinc oxide in the
sunscreen compositions preferably has a mean primary particle size
of between 5 nm and 150 nm, preferably between 10 nm and 100
nm.
[0035] In some instances, the sunscreen compositions of the present
invention will comprise a combination of such sunblock actives. As
such, in some instances the sunscreen composition include, in
addition to the calcium phosphate particles described above,
combinations of both inorganic and organic sunscreen components. In
some instances, the sunscreen components are chosen from the
following list of agents: p-aminobenzoic acid (PABA); padimate O
(OD-PABA, octyldimethyl-PABA, .sigma.-PABA); phenylbenzimidazole
sulfonic acid (Ensulizole, Eusolex 232, PBSA, Parsol H); cinoxate
(2-Ethoxyethyl p-methoxycinnamate), dioxybenzone (Benzophenone-8),
oxybenzone (Benzophenone-3, Eusolex 4360, Escalol 567), homosalate
(Homomethyl salicylate, HMS), menthyl anthranilate (Meradimate),
octocrylene (Eusolex OCR, 2-cyano-3,3diphenyl acrylic acid,
2-ethylhexylester), octylmethoxycinnamate (Octinoxate, EMC, OMC,
Ethylmethoxycinnamate, Escalol 557,
2-ethylhexyl-paramethoxycinnamate, Parsol MCX), octyl salicylate
(Octisalate, 2-Ethylhexyl salicylate, Escalol 587), sulisobenzone
(2-Hydroxy-4-Methoxybenzophenone-5-sulfonic acid,
3-benzoyl-4-hydroxy-6-methoxybenzenesulfonic acid, Benzophenone-4,
Escalol 577), trolamine salicylate (Triethanolamine salicylate),
avobenzone
(1-(4-methoxyphenyl)-3-(4-tert-butylphenyl)propane-1,3-dione, Butyl
methoxy dibenzoylmethane, BMDBM, Parsol 1789, Eusolex 9020),
ecamsule (Mexoryl SX, Terephthalylidene Dicamphor Sulfonic Acid),
titanium dioxide, zinc oxide, 4-methylbenzylidene camphor
(Enzacamene, Parsol 5000, Eusolex 6300, MBC), tinosorb M
(Bisoctrizole, Methylene Bis-Benzotriazolyl Tetramethylbutylphenol,
MBBT), tinosorb S (Bis-ethylhexyloxyphenol methoxyphenol triazine,
Bemotrizinol, BEMT, anisotriazine), neo heliopan AP (Bisdisulizole
Disodium, Disodium phenyl dibenzimidazole tetrasulfonate,
bisimidazylate, DPDT), mexoryl XL (Drometrizole Trisiloxane),
benzophenone-9 (Uvinul DS 49, CAS 3121-60-6, Sodium Dihydroxy
Dimethoxy Disulfobenzophenone), uvinul T 150 (Octyl triazone,
ethylhexyl triazone, EHT), uvinul A plus (Diethylamino
Hydroxybenzoyl Hexyl Benzoate), uvasorb HEB (Iscotrizinol,
Diethylhexyl butamido triazone, DBT), parsol SLX
(Dimethico-diethylbenzalmalonate, Polysilicone-15),
isopentenyl-4-methoxycinnamate (Isoamyl p-Methoxycinnamate, IMC,
Neo Heliopan E1000, Amiloxate)
[0036] The amounts of sunscreens which are employed in any given
composition will vary, e.g., depending upon the sunscreen chosen
and the desired Sun Protection Factor (SPF) to be achieved.
Carrier
[0037] The sunscreen delivery vehicles include a carrier, which is
that component of the vehicle which is not the inorganic or organic
sunscreen components, e.g., as described above (it is noted that in
those instances where the vehicle does not include an additional
sunscreen component, the carrier and the vehicle are the same, such
that the carrier is not a component of the vehicle but is the
entire vehicle). The carrier is that material or combination of
materials that is used to essentially carry or deliver the calcium
phosphate particles, sunblock active(s) when present) to the skin.
The specific carrier material that is present in a given sunscreen
composition will depend upon the desired delivery method for the
composition, e.g., spray one, rub on, etc. For example, as
mentioned earlier, the sunscreen compositions may be in the form of
lotions, creams, gels, foams, emulsions, dispersions, sprays,
liposomes, coacervates, etc. Each composition may include any
convenient topical excipient and like agents desirable for
achieving the particular form. Of interest are carriers that
include an amount of water, e.g., 30% by weight or more, such as
40% by weight or more. Excipients of interest may include, e.g.,
mineral oils and emulsifying agents. In its most simplest of
embodiments, the carrier may be water, alcohol or water/alcohol
combinations, or other solvent(s) or solvent systems in which the
aforementioned actives may be, e.g., soluble, dispersed,
emulsified, etc. In some instances, sunscreen compositions of
interest will include excipients and the like that create a
substantially stable, homogenous sunscreen composition and/or
provide body and viscosity to the sunscreen composition so that the
actives do not merely run off the skin once applied. In some
instances, the carrier will comprise from 30 to 99% by weight of
the sunscreen composition. Any known carrier or base composition
may be present in the sunscreen compositions of the invention.
Suitable carriers and carrier compositions of interest include, but
are not limited to: those described in U.S. Pat. Nos. 7,186,404;
7,175,834; 7,172,754; 7,175,835; 7,101,536; 7,078,022; 5,175,340;
5,567,418, 5,538,716; 5,951,968; 5,670,140; 6,831,191; 6,602,515;
7,166,273; 6,936,735; 6,699,463; 6,165,450; 7,150,876; 6,962,692;
5,830,441.
[0038] Though a carrier by itself is sufficient, the sunscreen
compositions may contain various other components typically
associated with skin care products. For example, various skin care
agents including, but not limited to, skin care excipients as well
as additional photoprotective agents and skin lightening agents may
be present. Such agents include, but are not limited to
antioxidants, vitamins, anti-inflammatory agents, self-tanning
agents, moisturizers, emollients, humectants, and the like, and
mixtures thereof, in their conventional amounts. Agents and
additive materials of interest include those described in U.S. Pat.
No. 7,078,022.
[0039] Suitable antioxidants include, but are not limited to,
water-soluble antioxidants such as sulfhydryl compounds and their
derivatives (e.g., sodium metabisulfite and N-acetyl-cysteine),
lipoic acid and dihydrolipoic acid, resveratrol, lactoferrin, and
ascorbic acid and ascorbic acid derivatives (e.g., ascorbyl
palmitate, ascorbyl polypeptide and ascorbyl phosphate).
Oil-soluble antioxidants suitable for use in the compositions of
this invention include, but are not limited to, butylated
hydroxytoluene, retinoids (e.g., retinol and retinyl palmitate),
tocopherols (e.g., tocopherol acetate), sodium tocopheryl
phosphate, tocotrienols, alkylresorcinols, curcurmin and its
derivatives and ubiquinone. Natural extracts containing
antioxidants suitable for use in the compositions of this
invention, include, but not limited to, extracts containing
flavonoids and isoflavonoids and their derivatives (e.g., genistein
and diadzein), extracts containing resveratrol and the like.
Examples of such natural extracts include grape seed, green tea,
pine bark, Phyllanthus emblica and propolis. Other examples of
antioxidants may, be found on pages 1612-13 of the ICI Handbook as
well as in U.S. Pat. No. 6,124,268.
[0040] The sunscreen compositions of the present invention may also
include one or more vitamins and/or their derivatives. Vitamins and
vitamin derivatives include, for example, vitamin A, vitamin A
propionate, vitamin A palmitate, vitamin A acetate, retinol,
vitamin B, thiamine chloride hydrochloride (vitamin B.sub.1),
riboflavin (vitamin B.sub.2), nicotinamide, vitamin C and
derivatives (for example ascorbyl palmitate, magnesium ascorbyl
phosphate, ascorbyl acetate), vitamin D, ergocalciferol (vitamin
D.sub.2), vitamin E, DL-.alpha.-tocopherol, tocopherol E acetate,
tocopherol hydrogensuccinate, vitamin K.sub.1, esculin (vitamin P
active ingredient), thiamine (vitamin B.sub.1), nicotinic acid
(niacin), pyridoxine, pyridoxal, pyridoxamine, (vitamin B.sub.6),
pantothenic acid, biotin, folic acid and cobalamine (vitamin
B.sub.12). Preferred vitamins are, for example, vitamin A
palmitate, vitamin C and derivatives thereof,
DL-.alpha.-tocopherol, tocopherol E acetate, nicotinic acid,
pantothenic acid and biotin.
[0041] Suitable emollients include those agents known for softening
the skin which may be selected from hydrocarbons, fatty acids,
fatty alcohols, e.g., cetyl alcohol and stearyl alcohol, and
esters. Petrolatum is a common hydrocarbon type of emollient
conditioning agent. Other hydrocarbons that may be employed include
alkyl benzoate, mineral oil, polyolefins such as polydecene, and
paraffins, such as isohexadecane. Fatty acids and alcohols
typically have from about 10 to 30 carbon atoms. Illustrative are
myristic, isostearic, hydroxystearic, oleic, linoleic, ricinoleic,
behenic and eruicie acids and alcohols. Oily ester emollients may
be those selected from one or more of the following, triglyceride
esters, acetoglyceride esters, ethoxylated glycerides, all esters
of fatty acids, ether esters, polyhydric alcohol esters and wax
esters. Additional emollients or hydrophobic agents include
C.sub.12 to C.sub.15 alkyl benzoate, dioctyladipate, octyl
stearate, octyldodecanol, hexyl laurate, octyldodecyl
neopentanoate, cyclomethicone, dicapryl ether, dimethicone, phenyl
trimethicone, isopropyl myristate, capriylic/capric triglycerides,
siloxanes, e.g., cyclotetrasiloxane and cyclopentasiloxane,
propylene glycol dicaprylate/dicaprate and decyl oleate.
[0042] Suitable humectants include various polyhydric alcohols,
especially polyalkylene glycols and, more preferably, alkylene
polyols and their derivatives. Exemplary humectants include
propylene glycol, dipropylene glycol, polypropylene glycol,
polyethylene glycol, sorbitol, 2-pyrrolidone-5-carboxylate,
hydroxypropyl sorbitol, hexylene glycol, ethoxydiglycol
1,3-butylene glycol, 1,2,6-hexanetriol; glycerin, ethoxylated
glycerin, propoxylated glycerin, compatible solutes, such as
ectoin, hydroxectoin, taurines, carnithine, acetyl carnithine and
mixtures thereof. Also of interest are urea; guanidine; glycolic
acid and glycolate salts (e.g. ammonium and quaternary alkyl
ammonium); lactic acid and lactate salts (e.g. sodium, ammonium,
and quaternary alkyl ammonium); aloe vera in any of its variety of
forms (e.g., aloe vera gel); pyrrolidone carboxylic acids and their
salts (e.g., sodium pyrrolidone carboxylic acid); sugars and
starches; sugars and starches and their derivatives (e.g., honey
extract, alkoxylated glucose);
6-(N-acetylamino)-4-oxahexyltrimonium chloride; hyaluronic acid;
chitin, lactamide monoethanolamine; acetamide monoethanolamine;
propoxylated glycerol; etc. In some instances, humectants of
interest include, but are not limited to: C.sub.3-C.sub.6 diols and
triols, such as the C.sub.3-C.sub.6 diols and triols selected from
the group consisting of propylene glycol, 1,3-dihydroxypropane,
glycerin, urea; honey extract, butylene glycol, hexylene glycol,
1,4-dihydroxyhexane, 1,2,6-hexanetriol, and mixtures thereof. In
some instances, the humectants are those selected from the group
consisting of glycerin, urea, honey extract, butylene glycol,
hexylene glycol, and mixtures thereof. When employed in effective
amounts, generally from 1 to 30%, preferably from 2 to 20%, by
weight of the sunscreen composition, these additives serve as skin
moisturizers as well as reduce scaling and stimulate the removal of
built-up scale from the skin.
[0043] In some instances, the compositions include one or more skin
conditioning agents, where skin conditioning agents of interest
include occlusive skin condition agents, emollient skin
conditioning agents and miscellaneous skin conditioning agents, as
well as combinations thereof.
[0044] Occlusive skin conditioning agents of interest include, but
are not limited to: avena sativa (oat) kernel oil, behenyl
isostearate, caprylic/capric triglyceride,
caprylic/capric/myristic/stearic triglyceride, caprylyl methicone,
caprylyl trimethicone, safflower seed oil, cetyl palmitate, cetyl
stearate, coconut oil, dimethicone PEG-8 olivate, emu oil, glycol
distearate, hydrogenated avocado oil, hydrogenated rice bran oil,
propylene glycol diistearate, sweet almond oil, jojoba oil,
squalane, stearyl beewax, stearyl dimethicone, cocoa seed butter,
wheat germ oil, vegetable oil, etc.
[0045] Also of interest as skin conditioning agents are emollients.
The compositions may include one or more emollients, which
typically act to soften, soothe, and otherwise lubricate and/or
moisturize the skin. Suitable emollients that can be incorporated
into the compositions include, but are not limited to: oils such as
petrolatum based oils, petrolatum, vegetable based oils, mineral
oils, natural or synthetic oils, alkyl dimethicones, alkyl
methicones, alkyldimethicone copolyols, phenyl silicones, alkyl
trimethylsilanes, dimethicone, dimethicone crosspolymers,
cyclomethicone, cyclotetrasiloxane, cyclopentasiloxane, lanolin and
its derivatives, fatty esters, glycerol esters and derivatives,
propylene glycol esters and derivatives, alkoxylated carboxylic
acids, alkoxylated alcohols, fatty alcohols, and combinations
thereof. Suitable esters could include, but not be limited to,
cetyl palmitate, stearyl palmitate, cetyl stearate, isopropyl
laurate, isopropyl myristate, isopropyl palmitate, glyceryl
caprylate and combinations thereof. The fatty alcohols could
include but not be limited to octyldodecanol, lauryl, myristyl,
cetyl, stearyl, behenyl alcohol, and combinations thereof. Ethers
such as eucalyptol, ceteraryl glucoside, dimethyl isosorbic
polyglyceryl-3 cetyl ether, polyglyceryl-3 decyltetradecanol,
propylene glycol myristyl ether, and combinations thereof can also
suitably be used as emollients.
[0046] Also of interest are miscellaneous skin conditioning agents.
Examples of miscellaneous skin conditioning agents of interest
include, but are not limited to: alanine, algae extract, allantoin,
aloe vera extract, aluminum PCA, apricot kernel amino acids,
arbutin, arginine, asorbic acid, bisabolol, biotin, caffeine,
calcium ascorbate, calendula oil, carnitine, carnosine, lime oil,
orange oil, grapefruit oil, cucumber extract, tumeric extract,
carrot seed oil, dipalmitoyl glutathione, dipalmitoyl
hydroxyproline, dipotassium glycyrrhizate, disodium adenosine
phosphate, disodium adenosine triphosphate, elastin; fennel
extract, ginko biloba extract, beta-glucan, glutamine, glycolipids,
glycerrhizic acid, histidine, hyaluronic acid, hydrogenated
polydecene, hydrolyzed algae extract, hydrolyzed collagen,
hydrolyzed DNA, hydrolyzed oat protein, kinetin, lactic acid,
linoleic acid, lysine, magnesium ascorbate, niacin, oat amino
acids, oligopeptide-5, oligopeptide-6, oligopeptide-10, palmitoyl
oligopeptide, papain, pea extract, sweet almond oil, apple extract,
retinyl palmitate, resveratrol, soluble collagen, etc.
[0047] In some instances, the compositions include an emulsifying
agent. Emulsifying agents of interest include, but are not limited
to, sorbitan esters, glyceryl esters, polyglyceryl esters, methyl
glucose esters, sucrose esters, ethoxylated fatty alcohols,
hydrogenated castor oil ethoxylates, sorbitan ester ethoxylates,
polymeric emulsifiers, silicone emulsifiers, glyceryl monoesters,
preferably glyceryl monoesters of C.sub.16-C.sub.22 saturated,
unsaturated and branched chain fatty acids such as glyceryl oleate,
glyceryl monostearate, glyceryl monopalmitate, glyceryl
monobehenate, and mixtures thereof; polyglyceryl esters of
C.sub.16-C.sub.22 saturated, unsaturated and branched chain fatty
acids, such as polyglyceryl-4 isostearate, polyglyceryl-3 oleate,
diglycerol monooleate, tetraglycerol monooleate and mixtures
thereof; methyl glucose esters, preferably methyl glucose esters of
C.sub.16-C.sub.22 saturated, unsaturated and branched chain fatty
acids such as methyl glucose dioleate, methyl glucose
sesquiisostearate, and mixtures thereof; sucrose fatty acid esters,
preferably sucrose esters of C.sub.12-C.sub.22 saturated,
unsaturated and branched chain fatty acids such as sucrose
stearate, sucrose trilaurate, sucrose distearate, C.sub.12-C.sub.22
ethoxylated fatty alcohols such as oleth-2, oleth-3, steareth-2,
and mixtures thereof; hydrogenated castor oil ethoxylates such as
PEG-7 hydrogenated castor oil; sorbitan ester ethoxylates such as
PEG-40 sorbitan peroleate, polysorbate-80, and mixtures thereof;
polymeric emulsifiers such as ethoxylated dodecyl glycol copolymer;
and silicone emulsifiers such as laurylmethicone copolyol,
cetyldimethicone, dimethicone copolyol, and mixtures thereof. (e.g.
apricot kernel oil PEG-6 esters, beeswax, behenoyl stearic acid,
ceteareth-2, cetearyl glucoside, cetyl alcohol, cetyl phosphate,
glyceryl palmitate, glyceryl caprylate, glyceryl stearate,
hydrogenated lecithin, hydrolyzed beeswax, isostearyl glucoside,
palmitic acid, palm kernel acid, glyceride, PEG-20 stearate,
PEG-100 stearate, oleic acid, stearic acid, stearyl alcohol,
stearyl phosphate, sucrose cocoate, sucrose palmitate, sucrose
stearate, TEA stearate, tocopheryl phosphate, wheat germ oil PEG-8
esters, xanthan gum, corn oil), etc.
[0048] The compositions of the disclosure can also include natural
fats and oils. As used herein, the term "natural fat or oil" is
intended to include fats, oils, essential oils, essential fatty
acids, non-essential fatty acids, phospholipids, and combinations
thereof. These natural fats and oils can provide a source of
essential and non-essential fatty acids to those found in the
skin's natural barrier. Suitable natural fats or oils can include
citrus oil, olive oil, avocado oil, apricot oil, babassu oil,
borage oil, camellia oil, canola oil, castor oil, coconut oil, corn
oil, cottonseed oil, emu oil, evening primrose oil, hydrogenated
cottonseed oil, hydrogenated palm kernel oil, jojoba oil, maleated
soybean oil, meadowfoam oil, palm kernel oil, peanut oil, rapeseed
oil, grapeseed oil, safflower oil, sphingolipids, sweet almond oil,
tall oil, lauric acid, palmitic acid, stearic acid, linoleic acid,
stearyl alcohol, lauryl alcohol, myristyl alcohol, behenyl alcohol,
rose hip oil, calendula oil, chamomile oil, eucalyptus oil, juniper
oil, sandlewood oil, tea tree oil, sunflower oil, soybean oil, and
combinations thereof. The composition of the invention may include
fats and oils in an amount of from about 0.01% (by weight of the
composition) to about 40% (by weight of the composition), such as
from about 0.05% (by weight of the composition) to about 25% (by
weight of the composition), and including from about 0.1% (by
weight of the composition) to about 10% (by weight of the
composition).
[0049] Suitable preservatives for use in the formulation of the
present invention include, but are not limited to, one or more of
phenoxyethanol, ethylhexylglycerin; caprylyl glycol, sorbic acid,
sodium hydroxymethylglycinate, disodium salt of
ethylenediaminetetraacetic acid, chloroxylenol, sodium benzoate,
DMDM Hydantoin, 3-iodo-2-propylbutyl carbamate, potassium sorbate,
chlorhexidine digluconate, the alkyl esters of para-hydroxybenzoic
acid (the parabens, e.g. butylparaben, methylparaben and
propylparaben), lonicera caprifolium (honeysuckle) flower extract
& lonicera japonica (honeysuckle) flower extract.
[0050] Examples of anti-inflammatory ingredients include, but are
not limited to, bisabolol, curcurmin and its derivatives,
retinoids, flavonoids and other polyphenolics etc. These and other
anti-inflammatory agents, as well as additional anti-oxidants and
the like, are disclosed--US 2005/0048008A1.
[0051] Examples of self-tanning ingredients include, but are not
limited to, dihydroxyacetone and erythrulose.
[0052] The sunscreen compositions of the present invention may also
include one or more skin penetrants. These are additives that, when
applied to the skin, have a direct effect on the permeability of
the skin barrier: increasing the speed with which and/or the amount
by which certain other compounds are able to penetrate into the
skin layers. Exemplary organic penetration enhancers include
dimethyl sulfoxide; isopropyl myristate; decyl, undecyl or dodecyl
alcohol; propylene glycol; polyethylene glycol, C.sub.9-11,
C.sub.12-13 or C.sub.12-15 fatty alcohols; none; alkyl
pyrrolidones; lecithin; etc. Surfactants can also be used as
penetration enhancers.
[0053] Other optional adjunct ingredients for the sunscreen
compositions of the present invention include preservatives,
waterproofing agents, fragrances, anti-foam agents, plant extracts
(Aloe vera, witch hazel, cucumber, etc), opacifiers, stabilizers,
skin conditioning agents colorants, and the like, each in amounts
effective to accomplish their respective functions.
[0054] The carrier may also contain other physiologically
acceptable excipients or other minor additives, particularly
associated with organoleptic properties, such as fragrances, dyes,
buffers, cooling agents (e.g. menthol), stabilizers or the like.
The excipients and minor additives will be present in conventional
amounts, e.g., ranging from about 0.001% to 5%, such as 0.001-2%,
by weight, and in some instances not exceeding a total of 10% by
weight.
Loaded Calcium Phosphate Particles
[0055] Where desired, the calcium phosphate particles may be loaded
with an amount of one or more of the above components, e.g.,
anti-oxidants, UV absorbers/blockers, etc. In such applications,
loading protocols described in co-pending application Ser. No.
12/565,687 (the disclosure of which is herein incorporated by
reference), may be employed.
Emulsion Formulations
[0056] As indicated above, in some instances the sunscreen
compositions are emulsions, e.g., wherein the emulsion may be
oil-in-water or water-in-oil emulsion compositions. Of interest are
oil-in-water emulsified sunscreen compositions that include by
weight:
[0057] (a) from 0.001% to 10% of Uniform Rigid Spherical Nanoporous
Calcium Phosphate Particles as an ultra violet (UV) blocking and
scattering agent, e.g., as described above;
[0058] (b) from about 0.1% to about 50% of inorganic sunscreen
component (e.g., UV shielding particles) such as described
above;
[0059] (c) from about 0.1% to about 15% of organic sunscreen
component (e.g., UV absorbers) such as described above;
[0060] (d) from about 0.1% to about 10% of solid wax or polymer
film former for the water proof function;
[0061] (e) 30% or more of the entire composition of a lipophilic
component (e.g., made up of fats, oils, other lipophilic
ingredients, etc.), e.g., as described above;
[0062] (f) from 30 to 80%, such as 40 to 50% water.
[0063] In some instances, the above formulation includes one or
more of the following additional components:
[0064] (g) From about 0.01% to about 10% of Skin Conditioning
Agent--Miscellaneous: Ex: Botanivera 1-200C (INCI: Aloe barbadensis
Leaf Juice);
[0065] (h) One or more viscosity enhancers (e.g Xanthan Gum) in an
amount of from about 0.01% (by weight of the composition) to about
25% (by weight of the composition), such as from about 0.05% (by
weight of the composition) to about 10% (by weight of the
composition), and including from about 0.1% (by weight of the
composition) to about 5% (by weight of the composition);
[0066] (i) From about 0.5% to about 25% of Humectant: e.g.,
Glycerin;
[0067] (j) From about 0.5% to about 20% of Skin Conditioning
Agent--Occlusive: e.g., (INCI: Caprylic/Capric Triglyceride);
Caprylyl Trimethicone;
[0068] (k) From about 0.01% to about 20% of Emulsifier and emulsion
stabilizer: e.g. Lipomulse 165 (INCI: Glyceryl Stearate &
PEG-100 Stearate); Capmul 708 G (Glyceryl Caprylate); Cetyl
Alcohol; Stearyl Alcohol;
[0069] (l) From about 0.5% to about 25% of Skin Conditioning
agent--Emollient: e.g., Capmul 708 G (Glyceryl Caprylate);
Botanisil CM-70 (Cyclotetrasiloxane and Cyclopentasiloxane);
Botanisil GB-20 (INCI: Cyclopentasiloxane & Dimethicone/Vinyl
Dimethicone Crosspolymer;
[0070] (m) From about 0.5% to about 5% of Skin Conditioning Agent
Viscosity Increasing agent--nonaqueous: e.g., Botanisil GB-20
(INCI: Cyclopentasiloxane & Dimethicone/Vinyl Dimethicone
Crosspolymer);
[0071] (n) From about 0.5% to 1.1% of Preservative: e.g., Euxyl PE
9010 (INCI: Phenoxyethanol & Ethylhexylglycerin);
[0072] (o) From about 0.001% to about 10% of Antioxidant; Skin
Conditioning Agent--Miscellaneous; e.g., Sodium Tocopheryl
Phosphate; Tocopheryl Acetate
[0073] (p) From about 0.01% to about 10% of Skin Conditioning
Agent--Miscellaneous; Viscosity Increasing Agent--Aqueous; e.g.,
Hyaluronic Acid
Container
[0074] In some instances, the sunscreen composition is present in
container. The container may be configured to hold a desired amount
of sunscreen and provide for storage stability of the sunscreen. In
some instances, the container is configured to contain from 0.5 to
100 oz of sunscreen composition, such as 1 to 50 oz of sunscreen
composition.
[0075] As such, aspects of the invention include a container
delimiting at least one compartment, the container being closed by
means of a closing member; and a composition as described above and
placed inside said compartment. The container may be in any
appropriate form. It may in particular be in the form of a bottle,
a tube, a jar, a case, a box, a sachet or a carton. The closing
member may be in the form of a removable stopper, a lid, a cap, a
tear-off strip or a capsule, in particular of the type comprising a
body attached to the container and a cover cap articulated on the
body. It may also be in the form of a member for selectively
closing the container, in particular a pump, a valve or a flap
valve. The product may be contained directly in the container, or
indirectly. By way of example, the product may be arranged on an
impregnated carrier, in particular in the form of a wipe or of a
pad, and arranged (individually or in plurality) in a box or in a
sachet. Such a carrier incorporating the product is described, for
example, in WO 01/03538. The closing member may be coupled to the
container by screwing. Alternatively, the coupling between the
closing member and the container is done other than by screwing, in
particular via a bayonet mechanism, by click-fastening, gripping,
welding, bonding or by magnetic attraction. The term
"click-fastening" is in particular intended to mean any system
involving the crossing of a bead or cord of material by elastic
deformation of a portion, in particular of the closing member,
followed by return to the elastically unconstrained position of
said portion after the crossing of the bead or cord. The container
may be at least partially made of thermoplastic material. By way of
examples of thermoplastic materials, mention may be made of
polypropylene or polyethylene. Alternatively, the container is made
of non-thermoplastic material, in particular of glass or of metal
(or alloy). The container may have rigid walls or deformable walls,
in particular in the form of a tube or of a tubular bottle. The
container may comprise means for distributing or facilitating the
distribution of the composition. By way of example, the container
may have deformable walls so as to cause the composition to exit in
response to a positive pressure inside the container, this positive
pressure being caused by elastic (or non-elastic) squeezing of the
walls of the container.
Fabrication Methods
[0076] Aspects of the invention further include methods of making
the sunscreen formulations that include the uniform, rigid,
spherical, nanoporous calcium phosphate particles and topical
compositions that include the same. With respect to methods of
making the formulations, aspects of these methods include combining
an amount of uniform, rigid, spherical, nanoporous calcium
phosphate particles comprising a porous structure that defines an
internal space; and a desired sunscreen delivery vehicle.
Utility and Methods
[0077] The sunscreen compositions of the invention find use in a
variety of different application, including sunblocking
applications. The compositions are effective in reducing or
preventing skin damage due to UV exposure, such as exposure to the
sun. As such, aspects of the invention include methods of
protecting skin from damage due to UV exposure, where the methods
include the step of applying sunscreen compositions according to
embodiments of the invention to skin. In some instances, the
present invention provides a method of reducing or preventing
erythema resulting from exposure to UV light. Methods of the
invention may include applying the sunscreen composition to areas
of the skin that are or may be exposed to the sun. In some
instances, the sunscreen composition is applied to areas that are
not typically exposed to the sun but that nevertheless have
exposure to the penetrating UV rays. For example, tee shirts and
other light fabrics offer minimal protection against sun exposure,
especially to UV rays. Thus, in some instances the sunscreen
compositions may be applied to essentially all areas of the body,
including those typically covered by clothing.
[0078] The amount of the sunscreen composition that is to be
applied to the skin may vary, so long as it is sufficient to
provide the desired sun protection. To some extent, the amount
depends upon the form of the sunscreen composition and its mode of
application. For example, a spray formulation may be applied so as
to provide a light, even coat on the skin. Lotions, creams, gels
and the like may be applied at a rate of about 1 to 2 ounces for
the entire body, i.e., for the exposed skin of a "average
individual" wearing a swimsuit and standing 5 feet 4 inches tall,
weighing 150 pounds, and having a 32 inch waist. This translates to
an application rate of about 2 mg/cm.sup.2 of skin. On the face, an
application rate of interest is 1/4 to 1/3 of a teaspoon. In some
instances, the application rate will be from about 0.1 to about 10
mg/cm.sup.2, preferably from about 1 to about 3 mg/cm.sup.2, of
skin.
[0079] In certain embodiments, the sunscreen composition is applied
before sun exposure, such as at least 15 minutes before, and
reapplied every 2 hours or more frequently, e.g., if the individual
engages in activities/actions that may cause the sunscreen
composition to wear or wipe off, e.g., swimming; washing dishes,
windows, etc., washing hands and/or face; contact sports
activities; activities that promote substantial sweating; etc.
[0080] In addition to the above-mentioned photo-protective benefits
of the sunscreen compositions, the continual, e.g., daily, use of
the sunscreen compositions of the present invention, regardless of
whether one anticipates UV exposure or not, provides in some
instances a number of additional benefits to skin. For example, the
continual use of these sunscreen compositions may delay the
appearance of fine lines, enhance extracellular matrix cohesion,
reduce the appearance of spider veins, improving skin firmness and
elasticity: skin effects that are not only a result of exposure to
the sun but also the natural aging process. For example, the
long-term use of the inventive sunscreen compositions may help with
thickening the keratinous tissue (i.e., building the epidermis
and/or dermis layers of the skin), thereby preventing and/or
retarding atrophy of human skin; preventing and/or retarding the
appearance of spider veins and/or red blotchiness on human skin;
preventing and/or retarding the appearance of dark circles under
the eye; preventing and/or retarding sallowness and/or sagging of
human skin; soften and/or smooth lips; preventing and/or relieving
itch of human skin, regulating skin texture (e.g. wrinkles and fine
lines), improving skin color (e.g. redness, freckles); and the
like.
[0081] The following examples are offered by way of illustration
and not by way of limitation.
EXPERIMENTAL
I. Formulations
[0082] The following formulas were prepared. Formula 10090 lacks
calcium phosphate particles and formulation 10091 includes an
amount of calcium phosphate particles.
TABLE-US-00001 Raw Material % w/w Function LSC.RNB010091 Purified
Water 47.325% Skin Conditioning Agent - Miscellaneous; Solvent
Botanivera 1-200C 0.100% Skin Conditioning Agent - Miscellaneous
(INCI: Aloe barbadensis Leaf Juice) Xanthan Gum 0.400% Viscosity
Increasing Agent -Aqueous; Binder; Emulsion stabilizer Glycerin
8.000% Humectant Neo Heliopan .RTM. 303 (INCI: 6.000% Sunscreen
agent Octocrylene) Ethylhexyl Salicylate 1.600% Sunscreen agent
TiO2 (INCI: Titanium 1.750% Sunscreen agent Dioxide) Zinc Oxide
6.000% Sunscreen agent CCT (INCI: Caprylic/Capric 7.000% Skin
Conditioning Agent - Occlusive Triglyceride) Lipomulse 165 (INCI:
2.500% Emulsifier and emulsion stabilizer Glyceryl Stearate &
PEG-100 Stearate) Capmul 708 G (INCI: 3.000% Skin Conditioning
agent - Emollient: Glyceryl Caprylate) Surfactant - Emulsifying
agent Cetyl Alcohol 2.000% Emulsion stabilizer; Opacifying Agent;
Surfactant Emulsifying Agent Stearyl Alcohol 2.000% Emulsion
stabilizer; Opacifying Agent; Surfactant Emulsifying Agent
Botanisil CM-70 5.000% Skin Conditioning Agent - Emollient (INCI:
Cyclotetraxsiloxane and Cyclopentasiloxane) Botanisil GB-20 2.000%
Skin Conditioning Agent - Emollient & (INCI: Cyclopentasiloxane
& Viscosity Increasing agent - nonaqueous Dimethicone/Vinyl
Dimethicone Crosspolymer) Caprylyl Trimethicone 3.000% Skin
Conditioning Agent - Occlusive Euxyl PE 9010 1.100% Preservative
(INCI: Phenoxyethanol & Ethylhexylglycerin) Tocopheryl Acetate
0.100% Antioxidant; Skin Conditioning Agent - Miscellaneous
Hyauronic Acid 0.120% Skin Conditioning Agent - Miscellaneous;
Viscosity Increasing Agent -Aqueous Sodium Tocopheryl 0.005%
Antioxidant; Skin Conditioning Agent - Phosphate Miscellaneous
Hydroxysomes .TM. calcium 1.000% Sunscreen phosphate particles
(Laboratory Skin Care) LSC.RNB010090 Purified Water 48.325% Skin
Conditioning Agent - Miscellaneous; Solvent Botanivera 1-200C
0.100% Skin Conditioning Agent - Miscellaneous (INCI: Aloe
barbadensis Leaf Juice) Xanthan Gum 0.400% Viscosity Increasing
Agent -Aqueous; Binder; Emulsion stabilizer Glycerin 8.000%
Humectant Neo Heliopan .RTM. 303 (INCI: 6.000% Sunscreen agent
Octocrylene) Ethylhexyl Salicylate 1.600% Sunscreen agent TiO2
(INCI: Titanium 1.750% Sunscreen agent Dioxide) Zinc Oxide 6.000%
Sunscreen agent CCT (INCI: Caprylic/Capric 7.000% Skin Conditioning
Agent - Occlusive Triglyceride) Lipomulse 165 (INCI: 2.500%
Emulsifier and emulsion stabilizer Glyceryl Stearate & PEG- 100
Stearate) Capmul 708 G (INCI: 3.000% Skin Conditioning agent -
Emollient: Glyceryl Caprylate) Surfactant - Emulsifying agent Cetyl
Alcohol 2.000% Emulsion stabilizer; Opacifying Agent; Surfactant
Emulsifying Agent Stearyl Alcohol 2.000% Emulsion stabilizer;
Opacifying Agent; Surfactant Emulsifying Agent Botanisil CM-70
5.000% Skin Conditioning Agent - Emollient (INCI:
Cyclotetraxsiloxane and Cyclopentasiloxane) Botanisil GB-20 2.000%
Skin Conditioning Agent - Emollient & Viscosity (INCI:
Cyclopentasiloxane & Increasing agent - nonaqueous
Dimethicone/Vinyl Dimethicone Crosspolymer) Caprylyl Trimethicone
3.000% Skin Conditioning Agent - Occlusive Euxyl PE 9010 1.100%
Preservative (INCI: Phenoxyethanol & Ethylhexylglycerin) Sodium
Tocopheryl 0.005% Antioxidant; Skin Conditioning Agent - Phosphate
Miscellaneous Tocopheryl Acetate 0.100% Antioxidant; Skin
Conditioning Agent - Miscellaneous Hyauronic Acid 0.120% Skin
Conditioning Agent - Miscellaneous; Viscosity Increasing Agent
-Aqueous
II. Procedure
[0083] The following procedure was employed to prepare the above
formulations:
Phase A
[0084] Add the required amount of Purified Water of Phase A into a
clean, sanitized vessel. Add the required amount of Botanivera
1-200 C, Xanthan Gum and Glycerin. Start heating of Phase A to
65.degree. C.-70.degree. C. and mix with propeller-type mixing. Mix
until dissolve and uniform. Hold temperature for phase
combination.
Phase B
[0085] Prepare Phase B by combining into a suitably-sized clean and
sanitized vessel, Neo Heliopan 303, Ethylhexyl Salicylate,
Caprylic/Capric Triglyceride, Lipomulse 165, Capmul 708G, Cetyl
Alcohol, Stearyl Alcohol, Botanisil CM-70, Botanisil GB-20,
Caprylyl Trimethicone. Heat to 65.degree. C.-70.degree. C. with
mixing until melted and uniform. Add ZnO powder and TiO2 powder.
Homogenized until uniform.
Phase Combination
[0086] When both phases are at 65.degree. C.-70.degree. C., start
adding Phase B into Phase A in the main batching vessel. Homogenize
to achieve a very fine emulsion.
[0087] When the batch is free of air, commence cooling to
40.degree. C. with propeller-type mixing. Add the required amounts
of Euxyl PE 9010, Tocopheryl Acetate, Hyaluronic Acid, Sodium
Tocopheryl Phosphate. Mix until uniform.
[0088] For formula 10091, in a separate vessel at R.T. add Purified
Water (Part II), sodium Tocopheryl Phosphate. Mix until Sodium
Tocopheryl Phosphate is dissolved. Add Hydroxysomes.TM. and mix for
30 minutes. Add D to C. Homogenize until uniform.
III. Testing
[0089] Formulations 10090 and 10091 were tested by Helioscreen
(Marseilles, France) for SPF and UV-A blocking ability, according
to the following protocols.
A. SPF
[0090] The method employed is based on the protocol initially
described in B. L. Diffey and J. Robson (J.S.C.C. 40, 127-133
May/June 1989) modified and improved to evaluate the skin
protection against UVB. The method consists of evaluating the Sun
Protection Factor (SPF) which expresses the protection level a sun
protection product brings through the full UV spectrum, using an
adequate substrate on which the product has been spread, by means
of a spectrophotometric method. The employed method consists in
measuring the flow of UV energy through a test product (transmitted
energy) and in comparing this flow to the initial flow according to
the spectrophotometric method:
T(.lamda.)=I/I.sub.0, with .lamda. as the wavelength.
The wave function represented by this ratio is not sufficient to
express the level of protection of the spread on the skin product
as it also depends on two others wavelength functions: [0091]
Spectral irradiance of the "Standard Sun" as defined by "Commission
Internationale de l'Eclairage", wave function noted S(.lamda.).
[0092] Erythemal action spectrum which expresses the relationship
between cutaneous or subcutaneous reactions and energy of
excitation light, wave function noted E(.lamda.). S(.lamda.) and
E(.lamda.) are known and tabulated values.
[0093] A "KONTRON 930" spectrophotometer equipped with an UV source
and a double monochromator able to deliver a flow of energy between
250 and 800 nm was used. A 10.sup.-4 g precision laboratory balance
to control deposited product weight was employed, where the
products were deposited with a spatula. The following PMMA plates
were used: HELIOPLATE.RTM. HD6 guaranteed roughness, from
HelioScreen.RTM. Labs. as substrate.
[0094] Deposition of the test sample was performed as small lined
up spots all over the surface of the substrate. As deposited on the
substrate, product quantity was checked by weighing. Application
rate was determined in such a way that the actual quantity of
product left on the substrate before equilibration was 1.2
mg/cm.sup.2. The application area was greater than 16 cm.sup.2, in
fact about 25 cm.sup.2. A PMMA plate containing UV filter was used
as a reference so as to check the equipment was in good working
order and to assess the relevance of carried out measures.
[0095] The in vitro SPF was expressed from the whole residual UVB
and UVA spectrum having crossed the spread composition on substrate
product layer. This led to a wave function T(.lamda.) which was
multiplied by: [0096] A first wave function S(.lamda.), spectral
irradiance of the Standard Sun. [0097] A second wave function
E(.lamda.), erythemal action spectrum. The SPF was calculated from
the ratio:
[0097] In vitro SPF = .intg. 290 n m 400 n m E ( .lamda. ) S (
.lamda. ) .lamda. .intg. 290 nm 400 nm E ( .lamda. ) S ( .lamda. )
T ( .lamda. ) .lamda. ##EQU00001##
[0098] The SPF of the tested product was obtained by the
calculation of the arithmetical average of the different measures:
all measures corresponding to selected samples were taken into
account for the calculation of the statistical dispersion.
B. UVA
[0099] The determination of the UVA protection factor or UVAPF was
made using a spectrophotometric method as initially described by B.
L. Diffey and J. Robson "A new substrate to measure sunscreen
protection factors throughout the ultraviolet spectrum", J. Soc.
Cosmet. Chem., 40, 127-133 (1989) for the SPF determination, then
modified and adapted by Colipa (as reported at
http://www.colipa.com/site/index.cfm?SID=15588&OBJ=26783&back=1,
n.degree. 20) to evaluate the skin protection against UVA
irradiation.
[0100] The employed method consisted of evaluating the protection
brought by a sun protection product within the UVA range, by means
of a spectrophotometric method, using an adequate substrate on
which the product has been spread. The test was based on the
assessment of UV transmittance through a thin film of the sun
product sample, spread on a roughened substrate, before and after
exposure to a controlled dose of UV radiation, from a defined UV
source. Due to the possible lack of inter-laboratory
reproducibility of in vitro SPF protection factor measurement, this
SPF value was adjusted to the lapelled in vivo SPF through the use
of a multiplying coefficient C. The sunscreen sample was exposed to
an irradiation dose proportional to the initial UVA protection
factor (UVAPF0), calculated from the adjusted absorbance data of
the non exposed sample. The final in vitro UVA protection factor
(UVAPF) is calculated from the adjusted absorbance data of the UV
exposed sample.
[0101] The method used consisted of measuring the flow of UV energy
through the product, expressed in transmitted energy and in
comparing this flow to the initial flow according to the principle
of any spectrophotometric method:
T(.lamda.)=I/I.sub.0, with .lamda. as the wavelength.
Absorbance at wavelength .lamda. is related to Transmittance
by:
A(.lamda.)=-log(T(.lamda.)
Absorbance values were then multiplied by different irradiances and
action spectrums so as to be correlated to biological responses of
in vivo methods: For the SPF calculation: [0102] By the source
irradiance. This is the spectral irradiance of the UV source
I(.lamda.). [0103] And by the action spectrum related to the skin.
This is the Erythema action spectrum which expresses the
relationship between cutaneous or subcutaneous reactions and energy
of excitation light E(.lamda.) (as defined by "Commission
Internationale de l'Eclairage"). For the UVAPF calculation: [0104]
By the source irradiance. This is the spectral irradiance of the UV
source I(.lamda.). [0105] And by the action spectrum related to the
skin. This is the persistent pigment darkening [0106] (PPD) action
spectrum which expresses the relationship between cutaneous or
[0107] subcutaneous reactions and energy of excitation UV light
P(.lamda.). [0108] I(.lamda.), E(( ) and P(( ) are known and
tabulated values. The determination of the UVAPF was made through
the following steps: [0109] Step 1: In vitro measurement of
absorbance A.sub.0(.lamda.) through the spread on PMMA plate
product prior to any UV irradiation. [0110] Step 2: Mathematical
adjustment of the initial UV spectrum using coefficient `C` to
achieve an in vitro SPF (0% UV dose) equal to the labeled (in vivo)
SPF. Then initial UVA protection (UVAPF.sub.0) is calculated using
A.sub.0(.lamda.) and C. [0111] Step 3: A single UV dose D is
calculated, proportional to UVAPF.sub.0. (D=UVAPF.sub.0.times.1.2)
[0112] Step 4: UV exposure of the sample to the calculated UV dose
D. [0113] Step 5: In vitro transmission measurement of the sun
product after UV exposure. Acquisition of second UV spectrum with
A(.lamda.) data. [0114] Step 6: Mathematical adjustment of the
second spectrum (following UV exposure) according to the same C
coefficient previously determined in step 2, then calculation of
the in vitro UVA protection factor UVAPF.
[0115] A "KONTRON 930" spectrophotometer equipped with an UV source
and a double monochromator able to deliver a flow of energy between
250 and 800 nm was employed. A single spot area about 1.2 cm.sup.2
was evaluated. A 10.sup.-4 g precision laboratory balance was
employed to control deposited product weight. A spatula or syringe
was employed deposit the product. A UV source for pre-irradiation:
a CPS+SUNTEST (ATLAS) with standard and Schott WG320 filters were
used. In this appliance the temperature regulation of the samples
was maintained in the 20.degree. C.-40.degree. C. range. The
following PMMA plates have been used: HELIOPLATE.RTM. HD2
guaranteed roughness, from HelioScreen.RTM. Labs. as substrate.
[0116] Deposition of the test sample was performed as small lined
up spots all over the surface. As deposited on the substrate, the
sample quantity was checked by weighing. Application rate was
determined in such a way that the actual quantity of product left
on the substrate before equilibration was 1.2 mg/cm.sup.2. The
application area was greater than 16 cm.sup.2, in fact about 25
cm.sup.2.
[0117] The spectral irradiance at the exposure plane of the
artificial UV source that was used for radiation was as similar as
possible to the irradiance at ground level under a standard zenith
sun, as defined by COLIPA (1994) or in DIN 67501 (1999). The UV
irradiance was within the following acceptance limits (measured at
sample distance).
TABLE-US-00002 Light source specifications Total UV
irradiance.sub.(290 to 400 nm) 50-140 W/m.sup.2 Irradiance ratio of
UVA.sub.(320 to 400 nm) to UVB.sub.(290 to 320 nm) 8-22
The reference standard sun has a total irradiance of 51.4 to 63.7
W/m.sup.2 (Colipa 1994/DIN67501) and a UVA to UVB irradiance ratio
of 16.9 to 17.5. The device had the ability to maintain samples
below 40.degree. C. by using air conditioning. The sample was
exposed to full spectrum UV radiation but the dose is being defined
by the UVA content.
[0118] For the pre-irradiation dose calculation, the Mean
UVAPF.sub.0 value found was 2.97 and was calculated as shown below.
The single UVA applied dose was calculated to be 4 (j/cm.sup.2)
according to the formula:
D=UVAPF.sub.0.times.D.sub.0 in J/cm.sup.2
D.sub.0 being fixed at 1.2 J/cm.sup.2 UVA (in j/cm.sup.2).
[0119] A PMMA plate containing UV filter was used as a reference so
as to check the equipment was in good working order and to assess
the relevance of carried out measures.
[0120] The in vitro SPF was calculated using the following
formula:
SPF in vitro = .intg. .lamda. = 290 nm .lamda. = 400 nm E ( .lamda.
) * I ( .lamda. ) * .lamda. .intg. .lamda. = 290 nm .lamda. = 400
nm E ( .lamda. ) * I ( .lamda. ) * 10 - A 0 ( .lamda. ) * .lamda.
##EQU00002##
where: E(.lamda.)=see above I(.lamda.)=see above
A.sub.0(.lamda.)=mean monochromatic absorbance of the test product
layer before UV exposure d.lamda.=wavelength step (1 nm)
[0121] Calculation of the adjusted in vitro SPF and determination
of the coefficient of adjustment C':
[0122] C is the coefficient of adjustment, iteratively determined
to adjust the calculated in vitro SPF value to the labeled (in
vivo) SPF value. It is recommended that C falls within a range
between 0.8 and 1.2.
SPF in vitro , ad j = SPF labelled = .intg. .lamda. = 290 nm
.lamda. = 400 nm E ( .lamda. ) * I ( .lamda. ) * .lamda. .intg.
.lamda. = 290 nm .lamda. = 400 nm E ( .lamda. ) * I ( .lamda. ) *
10 - .LAMBDA. 0 ( .lamda. ) * C * .lamda. ##EQU00003##
The mean value of SPF in vivo was previously evaluated at: 11.70
Therefore, the value of the (C) coefficient was calculated at:
1.00
[0123] UVAPF.sub.0 is calculated for each plate individually,
according to formula:
UVAPF 0 = .intg. .lamda. = 320 nm .lamda. = 400 nm P ( .lamda. ) *
I ( .lamda. ) * .lamda. .intg. .lamda. = 320 nm .lamda. = 400 nm P
( .lamda. ) * I ( .lamda. ) * 10 - .LAMBDA. 0 ( .lamda. ) * C *
.lamda. ##EQU00004## [0124] where: P(.lamda.)=see above Calculation
of UVAPF of plates after UV irradiation of the sample The in vitro
UVAPF was calculated using the following formula:
[0124] UVAPF = .intg. .lamda. = 320 n m .lamda. = 400 nm P (
.lamda. ) * I ( .lamda. ) * .lamda. .intg. .lamda. = 320 nm .lamda.
= 400 nm P ( .lamda. ) * I ( .lamda. ) * 10 - .LAMBDA. ( .lamda. )
* C * .lamda. ##EQU00005##
[0125] Where:
[0126] A(.lamda.) is the mean monochromatic absorbance of the test
product layer after UV exposure.
[0127] Mean UVAPF0 and UVAPF Calculation:
[0128] Each plate was measured at 3 different sites to ensure that
a total area of at least 2 cm.sup.2 was measured. UVAPF.sub.0 or
UVAPF of one plate was calculated from the mean absorbance value
from the 3 individual spots. When coefficient of variation of
absorbance between spots exceeded 50%, then the plate was rejected
and a new plate prepared. UVAPF.sub.0 or UVAPF of the product was
the mean of the UVAPF.sub.0 or UVAPF's of three individual plates.
When the coefficient of variation between the UVAPF.sub.0 or
UVAPF's of the individual plates exceeded 20%, then further plates
have been measured until the coefficient of variation requirement
was reached.
[0129] All tests corresponding to selected samples were taken into
account for the calculation of the statistical dispersion.
C. CONCLUSION
TABLE-US-00003 [0130] UVA SPF With HAX 3-5 2.80 11.69 .+-. 2.40
Without HAX 3-5 2.50 9.48 .+-. 2.27
[0131] The above results demonstrate that inclusion of calcium
phosphate particles in sunscreen formulations increases both the
UV-A protection factor and sun protection factor of sunscreen
compositions.
[0132] Although the foregoing invention has been described in some
detail by way of illustration and example for purposes of clarity
of understanding, it is readily apparent to those of ordinary skill
in the art in light of the teachings of this invention that certain
changes and modifications may be made thereto without departing
from the spirit or scope of the appended claims.
[0133] Accordingly, the preceding merely illustrates the principles
of the invention. It will be appreciated that those skilled in the
art will be able to devise various arrangements which, although not
explicitly described or shown herein, embody the principles of the
invention and are included within its spirit and scope.
Furthermore, all examples and conditional language recited herein
are principally intended to aid the reader in understanding the
principles of the invention and the concepts contributed by the
inventors to furthering the art, and are to be construed as being
without limitation to such specifically recited examples and
conditions. Moreover, all statements herein reciting principles,
aspects, and embodiments of the invention as well as specific
examples thereof, are intended to encompass both structural and
functional equivalents thereof. Additionally, it is intended that
such equivalents include both currently known equivalents and
equivalents developed in the future, i.e., any elements developed
that perform the same function, regardless of structure. The scope
of the present invention, therefore, is not intended to be limited
to the exemplary embodiments shown and described herein. Rather,
the scope and spirit of present invention is embodied by the
appended claims.
* * * * *
References