BRPI0819683B1 - topical cosmetic composition and non therapeutic cosmetic method for whitening skin pigmentation - Google Patents

Description

"TOPICAL COSMETIC COMPOSITION AND NON-THERAPEUTIC COSMETIC METHOD FOR SKIN PIGMENTATION" FIELD OF THE INVENTION The subject matter described herein refers to cosmetic, topical or dermatological compositions comprising plant extracts. These compositions are employed for cosmetic, topical applications specifically for treating unwanted skin pigmentation.

BACKGROUND OF THE INVENTION

Safe, effective topical skin-lightening compositions are specifically desired for treatment of unwanted skin pigmentation, including, for example, regional hyperpigmentation caused by melanocytic hyperactivity, such as idiopathic melas occurring during pregnancy (pregnancy mask). or estrus asthma) or secondary to estrogen-progesterone contraception, local hyperpigmentation caused by benign melanocytic hyperactivity and proliferation such as senile macula, known as senile lentigo; accidental hyperpigmentation, such as photosensitivity after injury and scarring; skin aging (eg senile lentigines); and certain forms of leukoderma, such as vitiligo where, if injured skin cannot be repigmented, the residual areas of normal skin are lightened or depigmented to provide a homogeneous color to the entire skin. Various active ingredients and preparations that lighten the skin, that is, inhibit skin pigmentation are currently known. These products that are routinely employed contain hydroquinone, but such products have recently been found to be unacceptable for toxicological reasons. In fact, RDG 215 prohibited the use of hydroquinone in cosmetic products after December 2007. US Patent Application Published Number 2008/0050459 describes a cosmetic composition comprising Phyianthus emblica extract. a Bellis Perrenis extract, a Glycyrrhiza Glabra extract and needing at least one oligopeptide to achieve its cosmetic effect for the combined cosmetic treatment of fine lines and wrinkles, and / or skin lightening. Oligopeptides are described as having an appropriate molecular weight, so that they are able to act as Pbyliantbus emblica extract carriers and penetrate the skin to maximize efficacy. The only oligopeptides described in the publication for obtaining the cosmetic composition are oligopeptide-4 (pro-collagen oligopeptide) and oligopeptide-5 (pro-elastin oligopeptide).

There remains a need in the art for improved, topical, cosmetic compositions containing skin-clearing agents safely and effectively.

SUMMARY OF THE INVENTION The present subject matter generally relates to topical cosmetic compositions useful for the treatment of various skin disorders or conditions associated with unwanted skin pigmentation. Additionally, the present subject matter relates to topical, cosmetic compositions useful for cosmetic whitening of skin areas, the pigmentation of which is unsuitable for the individual skin type.

In one embodiment, the present target subject refers to the cosmetic, topical composition comprising and consisting essentially of or consisting of a Phyllanthus® extract, a Bellis- extract, and a licorice extract. In one embodiment, the cosmetic composition does not comprise at least one oligopeptide. In another embodiment, the cosmetic composition does not comprise at least one oligopeptide not normally present in Phyllanthus extract, Bellis extract or licorice extract. In a further embodiment, the cosmetic composition does not comprise oligopeptide-4 (pro-collagen oligopeptide) or oligopeptide-5 (pro-elastin oligopeptide). In another embodiment, the cosmetic composition does not comprise at least one oligopeptide having an appropriate molecular weight, so that it is capable of acting as an emblica Phyllanthus extract vehicle and penetrates the skin in maximizing efficacy.

In one embodiment, the present subject matter relates to a topical cosmetic composition comprising, consisting essentially of or consisting of a Phyllanthus emblica- extract, a Bellis perennis extract and a licorice extract.

In another embodiment, the present subject matter relates to a topical cosmetic composition comprising, consisting of or consisting of an active skin lightening component comprising, consisting essentially of or consisting of a Phyllanthus extract, a Bellis extract and an extract. of licorice, at least one sunscreen; and a cosmetically acceptable vehicle.

In another embodiment, the present subject matter relates to a topical cosmetic composition comprising, consisting essentially of, or consisting of an active skin lightening component comprising, consisting essentially of, or consisting of an extract of Phyllanthus emblica, an extract from Bellis perennis, and a licorice extract; at least one sunscreen; and a cosmetically acceptable vehicle.

In one embodiment, the present subject matter relates to a topical cosmetic composition comprising, consisting essentially of, or consisting of an active skin lightening component comprising, consisting essentially of, or consisting of a Phyllanthus extract, a Bellis and a licorice extract; and a skin lightening component comprising at least one sunscreen.

In one embodiment, the present subject matter relates to a topical cosmetic composition comprising, consisting essentially of, or consisting of an active skin-sealing component comprising, consisting essentially of, or consisting of an extract of Phyllanthus emblica, an extract from Bellis perennis, and a licorice extract; and a non-skinning component comprising at least one sunscreen.

In another embodiment, the present subject matter is directed to a method for screening an individual's skin pigmentation, comprising topically administering to the skin of an individual in need thereof a therapeutically effective amount of a topical cosmetic composition according to the invention. matter described herein.

In yet another embodiment the present subject matter relates to a method for treating a skin disorder or condition in an individual in need thereof of a therapeutically effective amount of a topical cosmetic composition according to the presently described subject matter.

BRIEF DESCRIPTION OF THE DRAWINGS Figure 1 illustrates progressive splicing over time which becomes statistically significant after 21 days for Site B treated with 2% hydroquinone. Figure 2 illustrates progressive splicing over time which becomes statistically significant after 14 days for Site E treated with the present topical cosmetic composition. Figure 3 illustrates progressive splicing (natural degradation of synthesized melamine) without any significance over experimental times for the untreated control site (Site F). Figure 4 illustrates the comparison between the mean colorimetric values in treatments 1 (Site B) and 2 (Site E) and control (Site F) over the course of the evaluation times. Figure 5 illustrates photographs of the clinical data supporting the colorimetric results in treatments 1 (Site B) and 2 (Site E) and control (Site F) comparing the TO and T21 assessment times.

DETAILED DESCRIPTION

Definitions As used herein, the terms "administering", "administration" and similar terms refer to any method which in medicine or cosmetic practice releases composition to an individual in such a way as to provide a positive effect on a dermatological disorder. condition, or appearance. The compositions may be administered such that they cover the entire area to be treated.

As used herein "aqueous solvent" refers to a solvent such as water or containing water. Other dissolved components may be present in small amounts, such as, for example, salts, buffers and other components understood by one of skill in the art to be optionally present in an aqueous solution. "Anhydrous formulation" refers to any formulation of the present topical cosmetic composition that does not contain water. "Cosmetically acceptable" refers to a non-toxic, inert and / or physiologically compatible composition.

As used herein, the phrase "effective amount" or "therapeutically effective amount" of an active agent or ingredient, which is synonymous herein, refers to an amount of the active agent sufficient enough to have a positive effect on application area. Consequently, these amounts are sufficient to modify the disorder, condition or appearance of the skin to be treated, but low enough to prevent serious side effects within the medical scope or dermatological recommendation.

As used herein, "extract" refers to one or more components isolated from a plant source in a fluid or powder form. The plant source may comprise or consist of the plant all or one or more parts of the plant, for example the plant fruit, flower, root, leaves, stems and / or bark. A fluid or liquid extract may be dried, for example, spray dried or dissected to form a powder. The extract may be a mixture of one or more components of a plant in fluid and / or powder form. "Non-skin lightening" means any compound, substance or composition, agent or component comprising, consisting essentially of or consisting of one or more agents, substances, compounds and compositions in which topical application to the skin does not depigment or lighten the skin. Such agents may include, for example, one or more active agents, for example, a sunscreen, an anti-acne agent, an antimicrobial agent, an anti-wrinkle agent, an anti-pediatric agent, an anti-inflammatory agent and an optical brightener; and / or one or more cosmetically acceptable excipients, for example a thickener, chelating agent, humidifier, emollient, humectant, gelling agent, pH adjuster, surfactant, stabilizer, vitamin, penetration enhancer, a perfume, a coloring agent and a solvent; and / or combinations thereof as described herein.

As used herein, "pharmaceutically acceptable free bases, salts, esters or solvates" refer to the free bases, salts, esters or solvates of the target compound (s) having the same biological activity as ( non-biological or otherwise undesirable target compound (s) A salt, ester or solvate may be formed, for example, with organic and inorganic acids Dispersible or water-soluble products are obtained. thus.

As used herein, "oligopeptide" refers to a peptide having an appropriate molecular weight so as to be able to act as a vehicle for the Phyllanthus emblica extract and to penetrate the skin. Oligopeptides that may act as carriers of Phyllanthus emblica extract and penetrate the skin include oligopeptide-4 (pro-collagen oligopeptide) and oligopeptide-5 (pro-elastin oligopeptide). As used herein, "oligopeptide" does not refer to any peptide that is normally present in Phyllanthus extract, Bellis extract or licorice extract. It is observed that in one embodiment of the present target matter, the cosmetic composition does not comprise at least one oligopeptide not normally present in Phyllanthus extract, Bellis extract or licorice extract.

As used herein, "serum" refers to the hydrophilic liquid formulation. A serum may optionally be free of one or more emollient, wax and a silicone.

As used herein "skin whitening agent" refers to any compound, substance or composition which, upon topical application to the skin, brightens or depigments it. Such bleaching agents may include, but are not limited to, pigmentation inhibitors, tyrosinase inhibitors, and melanocyte melanogenesis inhibitors.

As used herein, "synergistic skin lightening system" or "synergistic skin lightening component" refers to an active skin lightening component comprising, consisting essentially of, or consisting of an extract of Phyllanthus emblica, an extract Bellis perennis, and a licorice extract, which exhibits synergistic efficacy for skin whitening compared to the skin whitening effectiveness of each individual active skin whitening agent. In this regard, the combination of these ingredients provides a greater skin lightening effect than additive.

As used herein, a "treatment" of a skin disease, disorder or condition encompasses alleviation of at least one symptom thereof, a reduction in their severity or a delay, prevention or inhibition of their progression. Treatment does not mean that the disease, disorder or condition is fully cured. A composition useful herein need only reduce the severity of a skin disease, disorder or condition, reduce the severity of the symptoms associated with it, provide improvement of the patient's quality of life or delay, prevent or inhibit the onset of a skin disease. skin, disorder or condition. It is noted that, as used in the specification and claims only, the singular forms "one, one" and "the, a" include references to the plural unless the context clearly shows otherwise. Unless otherwise defined all technical and scientific terms employed herein have the same meaning as known to one of ordinary skill in the art to which the subject matter described herein refers.

Where a wide range of values is provided, for example concentration ranges, percentage ranges or other forms, it is understood that each intervening value is one tenth of the lower bound unit, unless the context clearly dictates otherwise, between the upper and lower limit of that range and any other intervening or stated value within that range is encompassed within the present subject matter. The upper and lower limits of these minor bands may be independently included in the minor bands, and such embodiments are also encompassed within the described subject matter, subject to any specifically excluded limit in the stated range. Where the stated range includes one or both limits, the bands excluding either or both of these included limits are also included in the described target matter.

Throughout the application, descriptions of the various embodiments employ the "comprising" language, however, it is understood by one skilled in the art that, in some specific instances, one embodiment may be described alternatively by employing the "consisting essentially of" or "language". consisting of ”.

For purposes of better understanding of the present teachings and in no way limiting the scope of the teachings, unless otherwise indicated, all numbers expressing quantities, percentages or proportions and other numerical values used in the descriptive report and claims should be understood to be modified in all instances by the term "about." Accordingly, unless otherwise indicated, the numerical parameters set forth in the following specification and appended claims are approximations which may vary depending upon the desired properties to be obtained. , each numerical parameter shall at a minimum be constructed according to the number of significant digits reported and by applying common rounding techniques.

Cosmetic Compositions, Topical The present subject matter relates to a topical cosmetic composition comprising, consisting essentially of, or consisting of a Phyüanthus extract, Beiiis extract or licorice extract.

Active Agents for Primary Skin Whitening According to the target subject matter described herein, the present topical cosmetic compositions may comprise or consist of a Phyllanthus extract, Betlis extract i.e. a Beiiis perennis extract; and a licorice extract. "Phyüanthus extract" means an extract obtained from the fruit of an element of the genus Phyllanthus including, for example, Phyllanthus emirica L., Phyllanthus elegans Wall, Phyllanthus reticulatus, Phyllanthus urinaria L., Phyllanthus reticulatus Poir Phyllanthus conami Sw, Phyllanthus lathyroides Η. BK, Phyllanthus casticum Soy-Will and Phyllanthus madagascariensis. Phyllanthus extract is a safe and effective natural antioxidant. "Phyllanthus emblica extract" means a standardized extract of Phyllanthus emblica, including, for example , EMBLICA® (Merck KGaA, Darmstadt, Germany and EM industries, Inc., USA, an affiliate of Merck KGaA). Phyllanthus emblica is also commonly known as "Emblica officinalis Gaertn" and is an element of the family "Euphorbiaceae." Phyllanthus emblica is a very rich source of vitamin C, having ascorbic acid content in the range of 1,000 to 1,800 mg per 100 grams of fruit. . Phyllanthus emblica extract is a safe and effective natural antioxidant that has no pro-oxidation activity and can exhibit dual functionality, namely chelation and antioxidanate. Unlike most antioxidants that go from active to inactive, Phyllanthus emblica extract can exhibit a cascading effect that provides stable and long-lasting antioxidant activity. Phyllanthus emblica extract can be produced by extracting high quality fruits using a water based process as described in US Patent No. 6,124,268 incorporated herein by reference in its entirety. Phyllanthus emblica extract typically contains low molecular weight tannins, namely Emblicanin A and Emblicanin B, along with Pedunculagin and Puniglyconine, Rutin and Gallo-elagitanoids. "Bellis extract" means an extract obtained from an element of the genus Bellis including, for example, extract obtained from flowers of an element of the genus Bellis, for example, flowers of Bellis perennis and / or flowers of Bellis rotundifolia L. Bellis extract may comprise or consist of one or more bioactive molecules including saponins (triterpene glycosides), polyphenols (phenolic acid), flavonoid glycosides, polysaccharides and inulin. “Bellis perennis extract means the extract obtained from Bellis perennis flowers. which may comprise or consist of one or more bioactive molecules including saponins (triterpene glycosides), polyphenols (phenolic acid), flavonoid glycosides, polysaccharides and inulin Bellis perennis extract may include BELIDES® available from CLR Chemisches Laboratorium, Berlin, Germany Bellis perennis is also commonly known as Bellis alpina Hegetschw., Bellis hortensis Mill., Bellis hybrida Ten., Bellis integrifolia DC., and Bellis scaposa Gilib. “Licorice extract” means an extract obtained from an element of the genus Glycyrrhiza, for example, obtained from the root of an element of the genus Glycyrrhiza. The genus Glycyrrhiza is an element of the Fabaceae family. Suitable Glycyrrhiza extracts may include the oil-soluble licorice extract available from Bioland, Korea. Other suitable Glycyrrhiza extracts may be obtained from one or more of the following elements of the genus Glycyrrhiza including Glycyrrhiza echinata L. (Chinese licorice), Glycyrrhiza glabra L., Glycyrrhiza lepidota L., Glycyrrhiza gutinosa glutodium, Glycyrrhiza brachycarpa Boiss., Glycyrrhiza germanica Tourn., Glycyrrhiza glandulifera Waldst. et Kit., Glycyrrhiza hirsuta L., Glycyrrhiza laevis Rali., Glycyrrhiza officinalis Lepech., Glycyrrhiza pallida Boiss., Glycyrrhiza siliquosa Tourn., Glycyrrhiza violacea Boiss., Glycyrrhiza viscosa Turc. ex Ledeb., Glycyrrhiza vulgaris Gueldenst. ex Ledeb, Liquiritia officinalis Moench, and Liquiritia officinarum Medik.

In one embodiment, the present topical cosmetic composition may comprise or consist of an active skin lightening component which may comprise or consist of a Phyllanthus extract, a Bellis extract and a licorice extract.

In one embodiment, the present topical cosmetic composition may comprise or consist of an active skin lightening component which may comprise or consist of a Phyllanthus emblica extract, a Bellis perennis extract and a licorice extract.

In one embodiment, the present target subject refers to a topical cosmetic composition wherein the total active skin lightening component is present in the topical cosmetic composition in an amount of from about 0.5% to about 43% by weight. about 1% to about 30% by weight, about 1.5% to about 23% by weight, about 1.5% to about 15% by weight, about 3% to about 10% by weight. weight, about 6% to about 8% by weight, or about 7.05% by weight, based on the total weight of the composition.

In another embodiment, the present subject matter relates to a topical cosmetic composition wherein Phyllanthus extract, for example Phyllanthus emblica extract, is present in the topical cosmetic composition in an amount of from about 0.1% to about 1%. 8% by weight, about 0.25% to about 4% by weight, about 0.5% to about 3% by weight, about 0.5% to about 2% by weight, about 1% to about 2% by weight, or about 2% by weight, based on the total weight of the composition.

In a further embodiment, the present subject matter relates to a cosmetic composition, wherein Bellis extract, for example Bellis perennis extract, is present in the topical cosmetic composition in an amount of from about 0.5% to about 30% by weight, about 1% to about 20% by weight, about 2% to about 10% by weight, about 3% to about 7% by weight, about 4% to about 6%. % by weight, or about 5.0% by weight, based on the total weight of the composition.

In still another embodiment, the present subject matter relates to a topical cosmetic composition wherein the licorice extract is present in the topical cosmetic composition in an amount from about 0.005% to about 5% by weight, about 0.01%. % to about 2% by weight, about 0.01% to about 1% by weight, about 0.02% to about 0.08% by weight, about 0.03% to about 0, 07% by weight, or about 0.05% by weight, based on the total weight of the composition.

In another embodiment, the present subject matter relates to a topical cosmetic composition wherein Phyllanthus extract, for example Phyllanthus emblica extract, is present in the topical cosmetic composition in an amount from about 0.50% by weight to about 2% by weight; Bellis extract, for example Bellis perennis extract, is present in the topical cosmetic composition in an amount from about 1 wt% to about 20 wt%; and the licorice extract is present in the topical cosmetic composition in an amount from about 0.01 wt% to about 1 wt%.

In still another embodiment, the present subject matter relates to a topical cosmetic composition, wherein the Phyllanthus emblica extract is present in the topical cosmetic composition in an amount of about 2% by weight; Bellis perennis extract is present in an amount of about 5% by weight; and licorice extract is present in the topical cosmetic composition in an amount of about 0.05% by weight.

In one embodiment, the present subject matter relates to a topical cosmetic composition comprising, consisting essentially of, or consisting of an active skin lightening component comprising, consisting essentially of, or consisting of a Phyllanthus extract, for example, a Phyllanthus emblica · extract, a Bellis extract, for example, a Bellis perennis extract; and a licorice extract; at least one sunscreen; and a cosmetically acceptable vehicle. The vehicle is a cosmetically acceptable vehicle. The cosmetically acceptable carrier may comprise or consist of one or more cosmetically acceptable excipients.

In another embodiment, the present subject matter relates to a topical cosmetic composition comprising, consisting essentially of or consisting of an active skin lightening component comprising, consisting essentially of, or consisting of a Phyllanthus extract, for example, a Phyllanthus emblica- extract, a Bellis extract, for example, a Bellis perennis- extract, and a licorice extract; and a skin lightening component. The skin lightening component may comprise or consist of one or more of an active agent, for example a sunscreen; a cosmetically acceptable vehicle; and / or a cosmetically acceptable excipient as described herein.

In a further embodiment, the present target subject refers to a topical, cosmetic composition according to the target subject disclosed herein which may comprise one or more active skin lightening agents.

In yet another embodiment, the cosmetic, topical composition and / or cosmetically acceptable carrier and / or one or more cosmetically acceptable excipients may be free of any skin whitening agents other than Phyllanthus extract, for example a Phyllanthus extract. emblica; a Bellis extract, for example, a Beilis perennis extract; and licorice extract. The cosmetic, topical composition and / or cosmetically acceptable carrier and / or one or more physically acceptable excipients may be free from any plant derived skin bleaching agents other than a Phyllanthus extract, for example a Phyllanthus emblica extract, a Bellis extract, for example, a Bellis perennis extract; and licorice extract. The cosmetic, topical composition and / or the cosmetically acceptable carrier and / or one or more cosmetically acceptable excipients may be free of any non-plant derived skin whitening agents.

In one embodiment, the present subject matter relates to a topical cosmetic composition, wherein the composition and / or an active skin lightening component and / or a skin non-lightening component do not comprise hydroquinone or a derivative thereof and / or does not comprise a polyorganosiloxane-containing epsilon-polylysine compound, and / or does not comprise a flavane.

Synergistic Component for Skin Whitening In another embodiment, the present subject matter relates to a topical, cosmetic composition which may comprise or consist of a synergistic active component for skin whitening comprising, consisting essentially of, or consisting of a skin extract. Phyllanthus, for example, an extract of Phyllanthus emblica] a Bellis extract for example, a Bellis perennis extract; and licorice extract, where the synergistic active ingredient for skin whitening exhibits synergistic efficacy in skin whitening compared to the skin whitening effectiveness of each individual active skin whitening agent.

In one embodiment, the present subject matter relates to a synergistic skin lightening component for use in a topical cosmetic composition comprising, consisting essentially of, or consisting of a Phyllanthus extract, for example, an Phyllanthus emblica extract; a Bellis extract, for example, a Beilis perennis extract; and licorice extract.

In another embodiment, the present subject matter relates to a synergistic skin lightening component for use in a topical cosmetic composition comprising, consisting essentially of, or consisting of a Phyllanthus extract, for example, an Phyllanthus emblica extract; a Bellis extract, for example, a Beilis perennis extract; and licorice extract, where the synergistic skin lightening component demonstrates improved skin whitening efficacy. The synergistic skin lightening component may be hydroquinone free.

In one embodiment, the topical cosmetic composition according to the presently disclosed target matter may comprise or consist of an active skin lightening component which exhibits synergistic efficacy for skin lightening.

In a further embodiment, the topical cosmetic composition according to the subject matter described herein may comprise or consist of an active skin whitening component which exhibits synergistic efficacy for skin whitening, wherein the topical cosmetic composition is free from hydroquinone.

In one embodiment, the cosmetic, topical composition or synergistic skin lightening system according to the presently described target matter may comprise or consist of an active skin lightening component which exhibits synergistic efficacy for skin lightening where Topical, cosmetic composition is free of hydroquinone and / or a flavane and / or a polyorganosiloxane-containing epsilon-polylysine compound.

Cosmetically Acceptable Vehicle Any cosmetically acceptable, topical, effective, inert, non-toxic vehicle may be used to formulate the compositions described herein. Well-known carriers employed to formulate other topical therapeutic compositions for administration to humans are useful in such compositions. Examples of such components which are well known to those skilled in the art are described in The Merck Index, Thirteenth Edition, Budavari et al., Eds., Merck & Co., Inc., Rahway, N.J. (2001); the CTFA (Cosmetic, Toiletry, and Fragrance Association) International Cosmetic Ingredient Dictionary and Handbook, Tenth Edition (2004); and the Inactive Ingredient Guide, U.S. Food and Drug Administration (FDA) Center for Drug Evaluation and Research (CDER) Office of Management, January 1996, the contents of which are hereby incorporated by reference in their entirety. Examples of such cosmetically acceptable excipients, vehicles and diluents include distilled water, physiological brine, Ringer's solution, dextrose solution, Hank's solution, and DMSO, which are within the range suitable for use herein.

These other additional inactive components as well as effective formulations and administration procedures are well known in the art and are described in standard textbooks such as Goodman and Gillman's: The Pharmacological Bases of Therapeutics, 8-Ed., Gilman et al. Eds. Pergamon Press (1990) and Remington's Pharmaceutical Sciences, M-Ed., Mack Publishing Co., Easton, Pa. (1990), both of which are incorporated herein by reference in their entirety.

Solar Filters In another embodiment, the present subject matter relates to a topical cosmetic composition which may comprise at least one sunscreen. The at least one sunscreen may be present in an amount from about 0.5% to about 30% by weight based on the total weight of the topical cosmetic composition, about 1% by weight to about 20% by weight. or about 1 wt% to about 10 wt% based on the total weight of the composition.

Suitable sunscreens may include broad spectrum sunscreens that protect against UVA and UVB radiation or sunscreen agents that protect against UVA or UVB radiation.

In one embodiment, the present topical cosmetic compositions may comprise a sunscreen comprising or consisting of one or more of methylene bis-benzotriazolyl tetramethylphenol, diethylamino hydroxybenzoyl hexyl benzoate, coated zinc oxide, ethylhexyl methoxycinnamate, ethyl homosalate salicylate hexyl, octocrene, polysilicone-15, butyl methoxydibenzoylmethane, menthyl anthranilate and dimethyl ethylhexyl PABA.

In a further embodiment, the present topical cosmetic compositions may comprise a sunscreen consisting of one or more of methylene bis-benzotriazolyl tetramethylphenol (TINOSORB M available from CIBA), diethylamino hydroxybenzoyl hexyl benzoate and a zinc oxide in an amount from about 1% to about 20% by weight, about 2% to about 10% by weight or about 5% by weight, based on the total weight of the composition. For example, topical cosmetic compositions may comprise a sunscreen comprising methylene bis-benzotriazolyl tetramethylphenol in an amount from about 1% to about 20%, from about 2% to about 10% by weight or about 5% by weight based on the total weight of the composition.

In a further embodiment, the present topical cosmetic compositions may comprise a sunscreen comprising or consisting of one or more of ethylhexyl methoxycinnamate (available from BASF), isoamyl methoxycinnamate, ethyl hexyl homosalate salicylate, octocrylene, polysilicone-15. butyl methoxydibenzoylmethane, menthyl anthranilate and dimethyl ethylhexyl PABA in an amount from about 1% to about 10%, from about 5% to about 9% or about 7.5% by weight, based on total weight of the composition.

In one embodiment, the present topical cosmetic compositions may comprise one or more sunscreens in an amount from about 0.5 wt% to about 30 wt%, about 1 wt% to about 20 wt% or about 1 wt% to about 10 wt% based on the total weight of the composition.

In one embodiment, at least one sunscreen may comprise or consist of a first sunscreen selected from the group consisting of methylene bis-benzotriazolyl tetramethylphenol, diethylamino hydroxybenzoyl benzoate and coated zinc oxide; and a second sunscreen selected from the group consisting of ethylhexyl methoxycinnamate, isoamyl methoxycinnamate, ethylhexyl homosalate salicylate, octocrylene, polysilicone-15, butyl methoxybenzylamide, menthyl anthranylate and dimethyl pABA . The first sunscreen may be present in an amount from about 1% to about 20% by weight and the second sunscreen may be present in an amount from about 1% to about 10% by weight total cosmetic topical composition. The first sunscreen may comprise or consist of methylene bis-benzotriazolyl tetramethylphenol and the second sunscreen may comprise or consist of ethylethyl methoxycinamate.

In one embodiment, the present subject matter relates to a topical cosmetic composition having an SPF greater than about 10, an SPF greater than about 15, an SPF of at least about 15, an SPF of about 15 , an SPF from about 10 to about 45, an SPF from about 15 to about 45, or an SPF from about 15 to about 25, Aqueous Solvent The present topical cosmetic compositions may additionally comprise a solvent. aqueous. In one embodiment, the present compositions comprise an aqueous solvent, for example water, in an amount from about 5% to about 95% by weight, about 10% to about 90% by weight, about 25% to about 100%. about 80% by weight, about 55% to about 75% by weight, about 60% to about 70% by weight, or about 63% by weight, based on the total weight of the composition.

Cosmetically Acceptable Excipients In yet another embodiment, the present subject matter relates to a topical cosmetic composition which may comprise water and at least one cosmetically acceptable excipient. Cosmetically acceptable excipients include those generally known to one of ordinary skill in the art as being useful in topical compositions.

In one embodiment, the at least one cosmetically acceptable excipient may comprise or consist of one or more elements selected from the group consisting of an antioxidant, chelating agent, pH adjuster, emollent, thickening agent, gelling agent, radical scavenger. free, a preservative, an emulsifier, a humectant, a humectant, a wetting agent, a suspending agent, a surfactant, a stabilizer, a vitamin, a penetration enhancer, a perfume or fragrance, coloring agent, fluid alkyl alcohols, polysiloxanes , modified polyoxyoxanes and combinations thereof.

Topical Formulations In one embodiment, the present topical cosmetic compositions are formulated in a serum, a creamy gel, a lotion, a cream, an ointment, a gel, an aerosol, a foam, a foamable liquid, a solution (solubilized system). , a paste, a suspension, a dispersion, an emulsion, a skin cleanser, a milk, a mask, a solid stick, a bar (such as soap), an encapsulated formulation, a microencapsulated formulation, microspheres or nanospheres or dispersions. vesicular, or other cosmetically acceptable topical dosage form. In the case of vesicular dispersions, the lipids from which the vehicles are manufactured may be of the ionic or nonionic type or mixtures thereof. The formulation may comprise one or more of an aqueous formulation and / or anhydrous formulation.

In another embodiment, the present topical cosmetic composition according to the target matter described herein may comprise or consist of an anhydrous formulation, an aqueous formulation or an emulsion.

In yet another embodiment, the present topical cosmetic compositions according to the subject matter described herein are formulated in a cream or a gel.

Optional Additional Active Agents The presently described topical cosmetic compositions may additionally and optionally comprise one or more cosmetic active agents or dermatological active agents in addition to the described skin whitening active agents. Such agents may include, for example, additional active skin whitening agents including plant derived and non-plant derived skin whitening agents, including, for example, pigmentation inhibitors, tyrosinase inhibitors, and / or melanchocyte melanocyte inhibitors , and / or active skin lightening agents, including, for example, optical brightening agents, sunscreen agents, anti-inflammatory agents, antimicrobial agents, antifungal agents, anti-wrinkle agents, an antiopathic agent, anti-acne agents, free radical cleansers, keratolytic agents, vitamins, antielastase and / or anticolagenase agents, peptides, fatty acid derivatives, steroids, trace elements of algae and / or plankton, enzymes and coenzymes, flavonoids and / or acids, hydroxy acids, and combinations thereof. Treatment Methods In one embodiment, the present subject matter relates to a method for lightening skin pigmentation in an individual, comprising topically administering to the skin of an individual in need a therapeutically effective amount of the topical cosmetic composition according to the invention. with the target matter described herein.

In another embodiment, the present subject matter relates to a method for treating a skin disorder or condition in an individual comprising topical administration to the skin of an individual in need of a therapeutically effective amount of the topical cosmetic composition according to the present invention. the target matter described herein. The skin disorder or condition may be a disorder or condition associated with unwanted skin pigmentation.

In another embodiment, the present subject matter relates to a method for lightening skin pigmentation in an individual or treating a skin disorder or condition in an individual comprising topical administration at least once a day for at least three days. days, for at least five days, for at least seven days, for at least ten days, or for at least 14 days, to the skin of an individual in need of a therapeutically effective amount of the subject matter topical cosmetic composition. target described herein. In this regard, after three days, five days, seven days, ten days or fourteen days, respectively, of administration of the present topical compositions the skin is visibly altered.

In one embodiment, the present subject matter relates to a method for lightening skin pigmentation in an individual or treating a skin disorder or condition in an individual comprising topical administration at least once a day for at least three weeks to the skin of an individual in need of an amount of the topical cosmetic composition according to the subject matter described herein, where after three weeks the skin is visibly lightened.

The present topical, cosmetic compositions are effective in treating a variety of skin disorders or conditions characterized by undesirable skin pigmentation. Non-limiting examples of such disorders and / or conditions may include regional hyperpigmentation caused by melanocytic hyperactivity, such as idiopathic melasma occurring during pregnancy (pregnancy mask or chloasma) or secondary to estrogen-progesterone contraception; local hyperpigmentation caused by benign melanocytic hyperactivity and proliferation, such as senile macula, known as senile lentigo; accidental hyperpigmentation, such as photosensitization after injury and scarring; freckles; Poor pigmentation and certain forms of leukoderma, such as vitiligo where, if injured skin cannot be repigmented, the residual areas of normal skin are lightened or depigmented to provide a homogeneous color to all skin. The skin may be treated according to the methods described herein for purely cosmetic whitening of areas, for example large areas of skin whose pigmentation, although unwanted, is suitable for the individual skin type. In one embodiment, the skin disorder or condition to be treated according to the present methods is unwanted pigmentation of the skin. Administration of the topical cosmetic composition to areas of the skin containing unwanted pigmentation brightens those areas.

In a further embodiment, the present subject matter relates to a method for treating skin disorder or condition in an individual, or a method for lightening skin pigmentation in an individual, wherein topical administration to the skin comprises administering at least once a day or at least twice a day for a period of at least two weeks, at least three weeks or at least four weeks, where skin pigmentation is lightened. Methods of Production Various formulations of the present topical cosmetic compositions according to the presently described target matter may be readily produced by one of ordinary skill in the art according to known methods for producing such formulations including, for example, a cream, a gel a serum, lotion or other formulation described herein without undue experimentation.

A process for producing an emulsion cream or formulation may separately comprise producing an aqueous phase and an oil phase, adding the oil phase to the aqueous phase, for example by mixing and / or homogenizing (high shear) in an emulsion. After the emulsion is produced, one or more of the following components may optionally be added thereto, for example, in the following order, to produce the final emulsion or cream: one or more skin lightening actives; one or more pH adjusters; one or more emollients; one or more skin lightening active; one or more sunscreen actives; one or more thickening agents; one or more antioxidants; and one or more fragrances. Prior to formulation of the emulsion, the aqueous phase and the oil phase may be separately heated to a temperature of from about 70 to about 99 ° C; about 75 ° C to about 95 ° C; about 80 ° C to about 90 ° C; or about 85 ° C. After heating the oil phase may be slowly added to the aqueous phase, for example with high shear mixing and homogenization. The resulting emulsion may then be cooled while maintaining high shear mixing and homogenization, for example, at a temperature of about 47 ° C to about 27 ° C, about 42 ° C to about 30 ° C, about 39 ° C to about 35 ° C Thereafter, one or more of the optional components described above may then be added to the cooled emulsion, for example, by mixing and / or homogenizing with high shear. The emulsion or cream may have a pH of about 4.5 to 6.5 and / or a viscosity of about 5,000 cP to about 15,000 cP and / or a density of about 1.01 to about 1.06. Cosmetic, topical compositions are further contemplated. as being within the scope of the present target matter being produced in accordance with the described above. If produced according to these processes, these compositions exhibit appropriate chemical and physical stability for topical administration.

Topical cosmetic compositions produced according to those processes may be placed in a suitable containment container comprising a product contact surface composed of a material selected from the group consisting of glass, plastic, steel, stainless steel, aluminum, teflon, polymeric structure, ceramic structure, alloys and mixtures thereof. These containment containers are employed to facilitate the manufacture, handling, processing, packaging, storage and administration of said topical cosmetic composition. Suitable containment containers in this regard may be selected from the group consisting of plastic tubes, bottles, metal tubes and any combination thereof.

Routes of Administration / Dosaaem To be effective, the route of administration of the topical cosmetic compositions used in the present methods should readily affect the active areas of the skin. Effective results in most cases are obtained by topically applying a thin layer over the affected area, or the area where the desired effect is desired. Effective results can be obtained with application rates once every two or three days to four or more applications per day. Appropriate dosage levels for the active agents contemplated in the present cosmetic, topical compositions and methods are well known to those skilled in the art and are selected to maximize treatment of the above skin conditions. Dosage levels in the range of about 0.001 mg to about 5,000 mg per kilogram body weight of the active skin whitening components are known to be useful in treating the diseases, disorders and conditions contemplated herein. Typically, this effective amount of the skin whitening active ingredients will generally comprise from about 0.001 mg to about 100 mg per kilogram of patient body weight per day. In addition, it will be understood that this dosage of ingredients may be administered. in single or multiple dosage units to provide the desired therapeutic effect.

If desired, other therapeutic agents may be employed in conjunction with those provided in the compositions described above. The amount of active ingredients that may be combined with the carrier materials to produce a single dosage form will vary depending on the host treated, the nature of the disease, disorder or condition and the nature of the active ingredients.

The present compositions may be provided in single or multiple doses daily. It is a strategy to start with a low dose one or more times a day and work slowly to the highest dose if necessary. The amount of active ingredients that may be combined with the carrier materials to produce a single dosage form will vary depending upon the host treated, the nature of the disease, disorder or condition and the nature of the active ingredients. In one embodiment, topical cosmetic compositions may be applied topically once or several times a day. In one embodiment, the present topical cosmetic compositions are applied topically one to four times a day. For example, it is a strategy to start with once a day and progress to more frequent applications if necessary.

In one embodiment, topical cosmetic compositions as described herein may be administered one or more times a day for a period of at least one week, for a period of at least two weeks, for a period of at least four weeks. weeks or for a period of at least eight weeks. Cosmetic, topical compositions may be administered one or more times a day, for a period of up to one year, up to six months, up to three months or up to two months.

It should be understood, however, that a specific dosage level for any patient will vary depending upon a number of factors, including specific active agent activity; age, body weight, general health, gender and diet of the patient; of administration time; excretion rate; possible drug combinations; the severity of the specific condition being treated; and the form of administration. One skilled in the art would appreciate the variability of such factors and would be able to establish dosage levels using no more than routine experimentation.

Pharmacokinetic parameters such as bioavailability, absorption rate constant, apparent volume of distribution, unbound fraction, total disappearance, unchanged excreted fraction, first pass metabolism, elimination rate constant, half life and mean residence time are well known in the art.

Optical cosmetic formulations may be determined by one of skill in the art, depending upon considerations such as the specific ingredients and desired dosage. See, for example, Remington's Pharmaceutical Sciences, 18th ed. (1990, Mack Publishing Co., Easton, PA 18042), pages 1435-1712, and "Harry's Cosmeticology", 8th ed. (2000, Chemical Publishing Co., Inc., New York, N.Y. 10016), the disclosure of each being incorporated herein by reference in its entirety. Such formulations may influence physical state, stability, in vivo release rate and in vivo disappearance rate.

In one embodiment, the present topical cosmetic composition according to the target matter described herein may be a creamy gel packaged, for example, in a tube, or a serum packaged, for example, in a non-pump type container. foam and not aerosol or bottle, wherein the amount of the composition contained in the container may be in the range of from about 10 gm to about 60 gm, from about 20 gm to about 50 gm or about 30 gm or about 40 gm .

Simple dosage kits and packs containing a one-day amount of the composition can be prepared. Disposable single dose, unit dose or once daily containers of the present compositions are contemplated to be within the scope of the present subject matter.

The present topical cosmetic compositions according to the target matter described herein may be formulated for storage in a substantially non-reactive laminated package to improve the stability of the package. This storage method provides improved packaging stability compared to other paper-based packaging. The amount of composition per single package may range from about 0.1 mL to about 20 mL, from about 0.5 to about 5.0 mL, or from about 1 to about 3 mL.

Specifically, the ability to formulate compositions capable of long term storage without premixing or composting prior to application is also contemplated. Specifically, the present compositions remain unexpectedly stable in storage for periods of time including between about 3 months and about 3 years, about 3 months and about 2.5 years, between about 3 months and about 2 years, between about 3 months to about 20 months and alternatively any time period from about 6 months to about 18 months.

In one embodiment, the topical cosmetic formulation presently described according to the target matter described herein remains stable for at least three years at a temperature below 30 ° C. In one embodiment, the presently described topical cosmetic formulation remains stable for at least two years at a temperature of less than or equal to 30 ° C. In one embodiment, the presently described topical cosmetic formulation remains stable for at least two years at or below 25 ° C.

EXAMPLES

The following examples are illustrative of the present topical cosmetic compositions and are not intended for limitations. Any polymer molecular weights are average molecular weights. All percentages are based on the percentage by weight of the final release system or prepared formulation unless otherwise indicated and all totals equal to 100% by weight.

Example 1 The following example illustrates the whitening effectiveness of the present topical cosmetic composition as compared to a 2% hydroquinone composition determined by the instrumental colorimetry methodology.

In a comparative, double-blind, monocentric clinical trial for a period of six (6) weeks, the whitening efficacy of each of the two topical products was evaluated on the previously pigmented skin of 10 (ten) volunteers. Dermatological evaluations were performed at the beginning and end of the study. Skin color was measured by kidney etría, together with photographic documentation on ΤΟ, T07, TI 5 and T21. UVB pigmentation was induced in the previously pigmented skin of volunteers using a light emission source, ie the 601/300 W xenon arc light solar simulator produced by Solar Light CO.

A Minolta CR400 Saturation Meter using a CIE standard color system (The Commission International de PEclairage) was used to determine skin color. The color is expressed by a three-dimensional coordinate system where the L * axis corresponds to the brightness of the skin, the a ”axis corresponds to the green and red colors and the b * axis to the blue and yellow colors. The 601/300 W Xenon Arc Light Solar Simulator, produced by Solar Light CO, was used as a light source. This equipment provides continuous light emission in the UVB and UVA spectrum, ranging from 290 to 400 nm. The device includes a set of lenses and filters that absorb or scatter irradiation at less than 320 nm or more than 400 nm. Irradiation occurs through a set of six "orifice" fiber optic branches programmed to deliver pre-established individual doses of irradiation. Irradiation monitoring was performed using a Dose Control System (DCS), which utilizes a UVB irradiation and an electronic monitor In this study, only three “holes” were used for each application site of the tested compositions.

Assay Samples 1. Hydroquinone 2% (positive control): Component Function% Weight / Weight Citric acid pH adjuster 0.08 Purified water Vehicle 67.08 Benzophenone-3 filter I aryl 1.5 Octyl methoxinamate filter active solar 6 Hydroquinone bleaching agent 2 Lanette "emulsifier 13 Antioxidant sodium metabisulphite 0.14 Isopropyl palmitate in situ 5 Softening glycol propylene 5 Methylparaben preservative 0.15 Propylparaben preservative 0.0.5 100.0% 2. A present cosmetic topical composition comprising: Component Function% Weight / Weight Purified Water Vehicle 62,250 Cetyl Alcohol Thickener 2.2 Antioxidant Butylated Hydroxytoluene 0.050 (C14-22 Alcohol and C12-20 Alkyl Emulsifying Glycoside 5) PEG / PPG Emollient Cyclopentassiloxane -18 / 1S dimethicone Crosslinked emollient polymer 1 diclopentasiloxane dimethicone EDTA sodium chelating agent 0.2 Beilis flower extract antioxidant / active 5 perennis Extract of fr Phyllanthus uto antioxidant / active 2 emblica Antioxidant licorice extract / active 0.050 Phenoxyethanol and preservative 0.6 methylisothiazolinone Perfume fragrance 0.3 Hydroxyethyl acrylate, thickening agent 5 Sodium methyldisulfite acryloyl dimethyltaurate copolymer 60 0.3 Bis-benzotriazolyl active sunscreen 5 methylene tetramethylphenol Ethylhexyl methoxycinnamate active sunscreen 7.5 Propylene glycol emollient 2 Triethanolamine pH adjuster 0.55 100.0% Formulation: Manufacturing method 1. In a suitable container disperse the Methylene bis-benzotriazolyl tetramethylphenol in a small amount of Purified Water, Mix to Uniformity, 2. In a suitable container, combine until uniformly the PEG / PPG-18/18 dimethicone cyclopentasiloxane and cyclopentasiloxane dimethicone cross-linked polymer. 3. In a suitable container, place the propylene glycol. Add and disperse Licorice Extract. Mix until uniform. 4. In a suitable container, disperse Phyianthus emblica fruit extract in a small amount of Purified Water. Mix until uniform. 5. In a suitable container, disperse Triethanolamine in a small amount of Purified Water. Mix until uniform. 6. In a suitable container, disperse the Sodium Metabasulphite in a small amount of Purified Water. Mix until uniform. 7. Add the remaining Purified Water to the main manufacturing container. While mixing add and disperse EDTA Sodium. Heat the contents to about 85 * 0. 8. Add to a suitable container cetyl alcohol, C-14-22 alcohols and C-12-29 alkyl glycoside, Cetyl Alcohol, Ethylhexyl Methoxycinnamate and Subtle Hydroxytoluene. Heat about 85 * 0 and mix until uniform. 9. Add the Step 8 mixture to the Step 7 mixture with stirring. Mix until uniform. 10. While mixing, cool the batter to about 37 ° C. 11. While mixing add the mixture from Step 4 and then add the mixture from Step 5. Mix until uniform. 12. While mixing, add Phenoxyethanol and Methylisothiazolinone. 13. While combining add a mixture from Step 2, then the mixture from Step 3. Mix until uniform. 14. Add Betiis Perennis flower extract and mix until uniform. 15. While combining add the mixture from Step 1 and mix until uniform. 16. Add Hydroxyethyl Acriate, Sodium Acrylyldimethyltaurate Copolymer, Squalene and Polysorbate 60. Mix until uniform. 17. While combining add the mixture from Step 6. Mix until uniform. 18. While mixing add Perfume. Mix until uniform. 19. This formulation has a pH ranging from 4.5-6.5; a viscosity ranging from 5,000 to 15,000 cP and a density ranging from 1.01 to .06.

Cosmetic, topical, alternative composition comprising:% Function Component Weight / Weight 01. 1a Portion of vehicle purified water 46,470 02.2a Portion of vehicle purified water 5,000 03.3a Portion of vehicle purified water 5,000 04,4a Portion of vehicle purified water 5,000 05,5a Portion of purified water vehicle 2,000 06. Thickener cetyl alcohol 2,000 07. Butylhydroxytoluene antioxidant 0.050 08. EDTA disodium chelating agent 0.200 09- Sodium antioxidant metabisulphite 0.300 10. Ethyloxy methoxynaate sunscreen ?, 500 11. Propylene glycol solubilizer 2,000 12. Triethanolamine 99W pH adjustment 0.550 13. Methylene bis-benzotriazolyl tetramethylbutylphenol sunscreen 5,000 (e) Decyl glycoside (e) Xanthan gum <e) Propylene glycol (e) and water (Ciba) 14. Cyclopentassiloxane / PEG / PPG-18 / 18 Emollient Dimethicone 2,000 (Dow Corning) 15. Cross-linked Polymer of Dimethicone (e) Emollient 2,000 Cyclomethicone (Dow Corning) 16. HY Acrylate droxyethyl (e) Thickener polymer 5,000 Acryloyl dimethyl Sodium Taurate (e) Squalene (e) Polysorbate 60 (Chemyunion) 17. Phenoxyethanol (e) Methylisothiazolinone (Rohm & preservative 0.570 Haas) 18. Alcohol C14 / C22 (e) alkyl glycoside Emulsifier C12 / C20 2,000 (Chemy union) 19. Licorice Extract (Bioland Ltd.) active 0.060 20. Beilis Perennis Extract (Chemisches Active 5,000 Laboratorium Dr. Kurt Richter GmBh) 21. Emblica (Merck KGaA) Active 2,000 22. Fragrance FAV 22000 (FAV105) perfume 0.300 100% Alternative Method for Manufacturing the Alternative Composition This alternative method achieved a change in formulation pH from a pH ranging from 4.0 to 6.5 to a pH ranging from 5.0 to 6.5 . Licorice extract, Betiis perennis extract and Emblica were generally kept in yellow light and / or protected from exposure to white light. In one embodiment, the entire process, including packaging, is preferably performed under yellow light. In another embodiment, the resulting formulation is stored without exposure to white light and air. Premixes 1. Premix A: In an appropriate additional container add Tinosorb M® (Bis-Benzotriazolyl Methylene Tetramethylbutylphenol (e) Decyl Glycoside (e) Xanthan Gum (e) Propylene Glycol (e) Water and Purified Water 2 * Portion, Shake until fully dispersed Reserve 2. Premix B: In an appropriate additional container add DC9040® {Crosslinked Dimethyl Polymer (e) Cyclomethicone and DC5225C® (Cyclopentasiloxane / PEG / PPG-18/18 Dimethic), Shake until fully dispersed. Reserve, 3. Premix C: In an appropriate additional container add Propylene Glycol and Licorice Extract. Shake until fully dispersed, Reserve, 4. Premix D; In an appropriate additional container add Embiica and Purified Water 3 * Portion. Shake until completely dispersed. Reserve, 5. Premix E: In an appropriate additional container add Trietanoamine 99W and Purified Water 4 'Portion, Shake until fully diluted. 6. Premix F; In an appropriate additional container add Sodium Metabisulfite and Purified Water 5 "Portion. Stir until fully dispersed. Set aside.

Preparation of the Oily Phase 7. In an appropriate container prepare the Oily Phase by adding Cetyl Alcohol, Montanov L® (C14 / G22 Alcohol, C12 / G20 Alkyl Glycoside), Ethylhexyl Methoxycinnamate and Butylhydroxytoluene. Heat while stirring at 75 ° C ± 2eC.

Preparation of Aauosa Phase 8. Add Purified Water 1st Portion and disodium EDTA to the main reactor. Heat to 75aC i 2a G during stirring and homogenization.

Emulsion 9. When both phases reach 75s ± 2a C, pour the oil phase over the aqueous phase during intense stirring and homogenization. Check to see if the emulsion formed is homogeneous after 15 minutes of homogenization. If necessary, shake and homogenize longer. 10. Cool to 37s C ± 2® C „11. Add Premix D and stir until complete homogenization, 12. Add Premix E and shake and mix thoroughly for at least 15 minutes. 13. Add Premix A under intense agitation, 14. Add Neolone PE ® (Phenoxyethanol (e) Methylisothiazolinone), Premix B, Premix G and Belides® (Beilis Perennis Extract). Shake and homogenize until smooth. . 15. Add Simugel NS® (Hydroxyethyl Acrylate (e) Acrylethymethyl Copolymer (e) Sodium Taurate (e) Squalene (e) Polysorbate 60) to the main reactor under intense homogenization and incorporate agitation when all materials are in the tank, Shake and homogenize well for at least 15 minutes, 16. Add FAV 22000® Fragrance and homogenize. 17. Add Premix F, shake and mix thoroughly for at least 15 minutes. 18. Take one sample from the top and one from the bottom, measure the pH (range 5.0 to 6.5). No variation in pH results between samples should be greater than 0.3 arbitrary pH units, which shows homogeneity. If necessary, continue stirring until the previously mentioned parameter is obtained, Classification of Volunteers 1. POPULATION SAMPLING: Ten (10) volunteers of both sexes, aged between 18 and 60 years, were classified to perform the study. Participating individuals were given a personal identification number for the first four letters of the first name and the first letter of the last name (electronically generated) and a protocol number. 2. INCLUSION CRITERIA: * Age level: 18 to 60 years old; * Phototypes II and III, according to the Fitzpatric classification; # Total skin at the test site; * Agree to follow the test procedures and go to the clinic on the days and times set for the evaluations; • Assi natu re of the com m e rm e rm e rm e rm e r. 3. EXCLUSION CRITERIA; * Pregnancy or breastfeeding; • Use of anti-inflammatory or immunosuppressive drugs; * Personal history of atopy; • Use of photosensitizing systemic medication; • History of phototoxic or photo allergic reactions; * History of sensitization or irritation to topical production; Photo-induced pathologies such as sun-induced urticaria, lupus erythematosus, polyiform cracking in light, recurrence of herpes simplex; • Presence of active inflammatory dermatoses at the test site; • Presence of nevus lesions at the test site; • Active skin pathologies; * History of sensitization or irritation to topical production; • Frequent sun exposure or tanning chambers; • Using innovative new medicines in the last 6 months.

Methodology 1, METHODOLOGICAL PROCEDURES

After the initial procedures, the minimum erythematosis dose to conduct pigmentation in each volunteer was determined as described below. The. Minimum Erythematous Dose Calculation: Each volunteer underwent a pretest to assess the minimum erythematosis dose (MED). A series of six exposures was applied to the unprotected skin of each volunteer, each being 12% larger than the previous one, in geometric progression. The mean dose was previously determined according to Fitzpatric Phototype, shown in Table 1, below.

TABLE I

After irradiation, volunteers were dismissed and instructed to return after 24 hours. Exposure data were recorded for each volunteer. B. Reading: After irradiation, each volunteer was released and instructed to return within 24 hours, whereby the exposure site was read with the volunteer in a vertical position at a predetermined distance and illumination that was kept constant for each volunteer. The MED was then determined for each volunteer. Individual Minimum Erythematosis Dose (iMED) is defined as the minimum ultraviolet radiation (UV) dose required to produce clear, well-defined contour erythema at the exposure site, which was used as a reference during the test stage.

Consequently, subsites without erythema were a necessary criterion for the evaluation of the test. If this does not occur, new applications must be performed to determine iMED. ç. Pigmentation Induction After determining the iMED of each test site, located on the back, between the pelvis and the scapular, lateral to the midline of the spine, it was marked with the volunteer in a horizontal position and using a marker. Three sites indicated for application of the products were delineated, namely Site B, Site E and Site F. Each site was 35 cm2 (7x5 cm). Radiation equivalent to 1.5 times the minimum erythematosis dose previously calculated for each volunteer was applied to each of the delimited sites. This application was repeated twice, so each site was irradiated a total of three times. d. Product Application;

After irradiation, volunteers were dismissed and instructed to return after 72 hours for photographic documentation and colorimetric evaluation of the sites. Subjects were tested in triplicate with each of Sites B, E, and F corresponding to three distinct irradiation areas to provide a total of three Test sites and nine designation areas per individual. After evaluation, 2 mg of each test material was applied to a designated irradiation area of a test site in each individual, one per day according to the following sequence. Site B: 2% Hydroquinone; Site E; The present topical cosmetic composition; Site F; Negative Control: Site without product application. In order to optimize product permeation and avoid product migration, handling or UV exposure, product application sites were occluded with a paper filter supported by a semipermeable adhesive tape. The volunteer returned to the clinic for application, readings and evaluations according to Table II below.

TABLE II e. Colorimetric Evaluation: The colorimetric evaluation was performed using a Saturation Meter. All measurements were performed three times, the mean L * a * b "parameters were recorded for each volunteer. The L * parameter was analyzed statistically and separately as its value decreases. F. Statistics;

To verify whether there is a statistically significant difference between treated and control sites and between experimental time points, the L * parameter was compared. This comparison was performed using Student's t-tests for paired data.

Treatments were clinically and colorimetrically evaluated on days T7, T14 and T21. Site B containing the positive control (2% Hydroquinone) showed the colorimetric average for each experimental time, as shown in Figure 1. Figure 1 illustrates progressive bleaching with time that becomes statistically significant after 21 days. Table III below shows the results of the comparison test between the L * means of TO means and the other experimental times for area 1 (Site B). Table IV shows the raw data for individual results for area 1 (Site B) for each volunteer within L *, a * and b * for each ΤΟ, T07, T14 and T21.

Table III * Significant level: 5% ** Hypothesis: There are no differences between the treated area and the control area. TABLE IV: Individual Results of the Hydroquinone Treatment Area Figure 2 illustrates the results obtained for Site E, ie the site of application of the present evaluated topical cosmetic composition. Figure 2 illustrates that there is progressive bleaching with time that becomes statistically significant after 14 days. Table V below illustrates the results of the comparison test between the L * means of TO and the other experimental times for area 2 (Site E). Table VI shows the raw data for the individual results for area 2 (Site E). ) of each volunteer within L *, a * and b * for each of TO, TQ7, T14 and T21, TABLE V * Significant level: 5% ** Hypothesis: there are no differences between the treated area and the control area. . TABLE VI: Individual results of the present topical cosmetic composition Figure 3 illustrates, for the Site F control site, that is, where there is no treatment for irradiation, progressive bleaching (natural degradation of synthesized melamine) without any significance with respect to Experimental times, Table VII below illustrates the results of the comparison test between the L * means of TO and the other experimental times for the control area (Site F). Table VIII shows the raw data for individual results for the control area (Site F). Table VIII shows the raw data for individual results for the control area (Site F) for each volunteer within L ', a * and b * for each of ΤΟ, T07, T14 and T21.

TABLE VII * Significant level: 5% ** Hypothesis: There are no differences between the treated area and the control area. TABLE VIII: Individual results from the control area Figure 4 illustrates the comparison between the mean colorimetric values in treatments 1 and 2 and the control in relation to the evaluation times. Table IX illustrates that only the present topical cosmetic formulation exhibited a statistically significant reduction in pigmentation compared to the spontaneous reduction in pigmentation observed in the control group. TABLE IX * Significant level: 5% ** Hypothesis: no differences between areas .

Discussion In an experimental model with UV-induced pigmentation (melanogenesis) and no pre-existing pigmental dysfunction, clinical pigmentation will be spontaneously reduced over time in the treated areas. All sites, including the untreated control, exhibited a significant reduction in pigmentation up to T21 as assessed using a colorimeter.

Therefore, this experiment was performed to comparatively evaluate which treatments could cause the fastest and most significant depigmentation. Since all treatments were applied simultaneously to each volunteer, the melanization capacity variable was significantly reduced. Consequently, depigmentation would occur at the same rate in all sites tested in each volunteer.

Starting from this premise, the whitening effect was clinically observed over time for each location, which had already been provided by visual assessment and comparative analysis.

To improve the accuracy of these observations and to allow objective, consistent and reproducible assessment, the colorimeter was used as a complementary instrumental assessment, allowing the detection of differences that the human eye cannot detect.

According to colorimetry, the parameter L * provided by the colorimetric measurement is the index directly related to the luminosity of the skin. The higher the value of L *, the brighter the evaluated region.

Clinically and colorimetrically evaluating the treatments, progressive depigmentation was expected as it deals with an experimental melanization phenomenon. Irradiated but untreated control sites showed significant colorimetric improvement of L * as T21 with hydroquinone; however, the bleaching levels when compared to hydroquinone in T07 and T14 were statistically lower.

Still considering the data over time, the results differ as follows: Hydroquinone: significantly improved as from T21; The present topical cosmetic composition: significantly improves as T14, with higher lightening levels, statistically significant when compared to the control.

Accordingly, the present topical cosmetic composition provided a faster and more significant whitening effect (provides a higher whitening index) compared to hydroquinone. Figure 5 shows photographs of clinical data supporting colorimetric results where the highest average whitening effect was obtained on site with the new formula. Hydroquinone treatment and the new formulation were similar at the end of the study, although the new formulation is faster and provides a higher whitening index.

Example 6 The following example illustrates the preparation of a cream according to the presently described target matter: Component Function% Weight / Weight Purified Water Vehicle 62,250 Skeptic Alcohol Thickening Agent 2 Xanthan Gum Thickening Agent 0.2 Hydroxytoluene Antioxidant Butt 0.050 (Alcohols) C14-22 and C12-20 alkyl glycoside) emulsifier 2 Getyl potassium phosphate emulsifier 1 Glyceryl stearate and PEG-100 emulsifier stearate 2 Softening Giclomethicone 2 Disodium edetate chelating agent 0.2 Beliis perennis flower extract antioxidant / active 5 Antioxidant Emblica Phylíanthus Fruit Extract / Active 2 Antioxidant Licorice Extract / Active 0.050 Phenoxyethanol and Methylisothiazolinone Preservative 0.6 Pe rfu me FAV220Q 0-With B i nion of O esi es Fragrance 0.3 Hydroxyethyl Acrylate Sodium Acryloyl Dimethyltaurate Thickener Copolymer, Squalene and Polysorbate 60 Antioxidant Sodium Metabisulfite 0.3 Bis-b enzotriazolyl methylene tetramethylphenol active sunscreen 5 Ethylhexyl methoxycinnamate active sunscreen 7.5 Propylene glycol emollient 2 pH 0.55 adjusted triethanolamine 100.0% The composition is prepared as in Example 1. More specifically after premixing And to be added to the emulsion, Neolone PE (Phenoxyethanol and Methylisothiazolinone) and cyclomethicone are added under high shear homogenization and mixing for about 15 minutes. Thickening agents including xanthan gum are added in the oil phase.

Example 3 The following example illustrates the preparation of a cream according to the presently described target matter: Component Function% Weight / Weight Purified Water Vehicle 62.43 Antioxidant Hydroxytoluene 0.05 Disodium Edetate Chelating Agent 0.20 Propylene Glycol Emollient 2.00 Antioxidant / active Phyltanthus Embiica Fruit Extract 2.00 Hydroxyethyl Acylate, Thickening Agent Copolymer 5.00 Sodium Acrylhydimethylturate, Squalene and Polysorbate 60 Methylene Bisbenzothiazolyl Tetramethylphenol Active Sunscreen 5.00 Bellis Perennis Extract Antioxidant / active 5.00 Emollient cyclopentasiloxane crosslinked polymer 2.00 dimethicone Cyclopentasiloxane PEG / PPG-18/18 emollient dimethicone 2.00 Phenoxyethanol and methylisothiazolinone preservative 0.60 Triethanolamine pH adjuster 0.57 Perfume perfume 0.30 Cetyl alcohol agent thickener 2.00 C14-22 alcohols and C12-20 alkyl glycoside emulsifier 2.00 Ethylhexyl methoxyamate filtr Active Solar 7.50 Antioxidant Sodium Metabisulphite 0.30 Licorice Extract Antioxidant / Active 0.05 100.0% Example 4 The following example illustrates a generally applicable method for administering a composition according to the present subject matter described;

A topical cosmetic composition is administered topically to the skin of an individual being treated by conventional means. This is preferably accomplished by the use of a creamy serum or gel formulation. The topical preparation may thus be applied to the desired skin surface area, for example with the use of fingertips.

For topical administration of the cosmetic composition, the subject is instructed to first gently clean the affected area and dry it. The topical, cosmetic composition can then be applied directly to the affected area or placed in the palm or appropriate container, from which the material can be removed and manually applied to the area of skin to be treated.

Example 5 An individual is suffering from unwanted pigmentation of the skin. A cosmetic composition as described herein is topically administered to the undesirable pigmented areas of the subject's skin. The undesirablely pigmented areas of the subject's skin are expected to be lightened.

Example 6 An individual is suffering from vitiligo. A topical cosmetic composition as described herein is topically administered to the residual areas of the subject's normal skin. Residual areas of the individual's normal skin are expected to be lightened to provide a homogeneous color to the entire skin.

Example 7 An individual suffering from age spots. A topical cosmetic composition as described herein is administered topically to the affected areas of the subject's skin. The age spots are expected to be cleared.

All publications cited in the descriptive report are indicative of the level of practice of those skilled in the art to which this subject matter refers. All these publications are hereby incorporated by reference herein just as if each individual publication were specifically and individually indicated as being incorporated by reference.

With the present subject matter having thus been described, it will be clear that it can be modified or altered in various ways. Such modifications or changes should not be deemed to be outside the spirit and scope of the present subject matter, and all such modifications and changes should be included within the scope of the following claims.

Claims (12)

1, Topical cosmetic composition, characterized in that it comprises: a Phyllanthus extract which is present in an amount from 0.5 wt% to 2 wt%; a Beliis extract which is present in an amount from 1 wt% to 20 wt%; and a Glycyrrhiza extract which is present in an amount from 0.01 wt% to 1 wt%, based on the total weight of the composition. Topical cosmetic composition according to claim 1, characterized in that the Phyllanthus extract comprises an Phyllanthus emblica extract. Topical cosmetic composition according to claim 1, characterized in that the Phyllanthus emblica extract comprises a Phyllanthus emblica fruit extract: the Beliis extract comprises a Beliis perennis flower extract and the Glycyrrhiza extract. comprises an extract of Glycyrrhiza root. Topical cosmetic composition according to claim 1, characterized in that it further comprises a sunscreen. Topical cosmetic composition according to claim 4, characterized in that the sunscreen is present in an amount of 0.5 wt.% To 30 wt.%, Based on the total weight of the topical cosmetic composition. Topical cosmetic composition according to Claim 4, characterized in that the sunscreen comprises: a first sunscreen selected from the group consisting of bis-benzotriazolyl tetramethylphenol, diethylamino hydroxybenzoyl hexyl benzoate, zinc oxide and their combinations; and a second sunscreen selected from the group consisting of ethylhexyl methoxycinnamate, isoamyl methoxycinnamate, ethylhexyl homosatate salicylate, octocrene, polysilicone-15, butyl methoxydibenzoylmethane, menthyl anthranilate and dimethyl PAB combinations. Topical cosmetic composition according to claim 6, characterized in that the first sunscreen is present in an amount from 1 wt.% To 20% by weight and the second sunscreen is present in an amount of 1%. by weight to 10% by weight based on the total weight of the topical cosmetic composition. Topical cosmetic composition according to claim 6, characterized in that the first sunscreen is bis-benzotriazolyl tetramethylphenol methylene and the second sunscreen is ethylhexyl methoxycinnamate, Topical cosmetic composition according to claim 1, characterized in that it further comprises water and a cosmetically acceptable excipient. Topical cosmetic composition according to claim 9, characterized in that water is present in an amount from 3 wt.% To 95 wt.%, Based on the total weight of the composition. Topical cosmetic composition according to claim 9, characterized in that a cosmetically acceptable excipient comprises one or more elements selected from the group consisting of an antioxidant, a chelating agent, a pH adjuster, an emollient, a thickening agent. , a preservative, an emulsifier, a wetting agent, a wetting agent, a suspending agent, an optical brightener, a stabilizer, a penetration enhancer, a perfume, a coloring agent and combinations thereof. A non-therapeutic cosmetic method for whitening skin pigmentation in an individual, characterized in that it comprises topically administering an effective amount of the topical cosmetic composition as defined in claim 1 to the skin of an individual in need thereof.