WO2017143138A1

WO2017143138A1 - Multi-functional, structured, glycidic / non-glycidic matrices

Info

Publication number: WO2017143138A1
Application number: PCT/US2017/018301
Authority: WO
Inventors: John O'keefe; Sara LAMPARD; Maureen Iannucci; Mark Becker; Jon A. GIBERSON; Nicholas GREENFIELD; Tyler MCINTYRE; Clayton ROZIC
Original assignee: Aak Usa Inc.; Sonneborn, Llc
Priority date: 2016-02-17
Filing date: 2017-02-17
Publication date: 2017-08-24
Also published as: BR112018016905A2; EP3416492A4; JP2019505557A; CN109475138B; CN109475138A; BR112018016905A8; EP3416492A1; TW201729796A; JP7246926B2

Abstract

A topically-applied product comprising (i) at least one triglyceride and (ii) at least one petrolatum, wherein the topically-applied product contains, on a weight/weight basis, at least 2% triglyceride and at least 6% petrolatum. Further embodiments are wherein the topical product does not over time exhibit graininess, bloom, discoloration, or separation, or change in viscosity. Even further embodiments are wherein the triglyceride is interesterified and non-fractionated. In other embodiments, the triglyceride is interesterified and has a final melting point above or significantly above body temperature. Within this embodiment, the interesterified triglyceride having a final melting point above or significantly above body temperature may be fractionated or may be non-fractionated.

Description

Multi-Functional, Structured, Glycidic / Non-Glycidic Matrices Field of Invention

The invention in certain embodiments is directed to topical and hair care products - including, stable, multi-functional dermatocosmetic and conditioning ingredients and externally applied products (i.e., finished formulations) that provide skin and hair health benefits including improved protection of the skin and hair from environmental stress, increased moisture retention, improved skin barrier function and/or hair conditioning.

Background of the Invention

Constantly barraged by environmental stressors - heat, cold, atmospheric and airborne pollutants, and ultraviolet radiation, among others - human skin protects the body by repairing damage and restoring and maintaining homeostasis. It does so through a series of inflammatory responses that can also have adverse skin health effects. By breaking down the skin's extracellular matrix proteins (collagen and elastin), inflammation can result in thinner, less elastic and wrinkled skin. To counter environmental stress, formulators of personal care and dermatologic products have relied on safe, effective, proven emollients and barrier-protecting ingredients - petrolatum and triglyceride butters, notably shea butter.

Use of petrolatum as an emollient for relieving dry skin conditions, including flaking skin, chapping, windburn and sunburn has long history of use in the personal care and medical arts. See, e.g., 43 Fed. Reg. 34628, 34639.

Where petrolatum is the sole moisturizing ingredient, moisturization benefits typically require that petrolatum be included in a finished formulation at a concentration of at least about 3% by weight of the formulation (3%+ petrolatum).

At certain use levels (30 percent or higher) petrolatum is approved by the US Food and Drug Administration in a monograph as an over-the-counter (OTC) skin protectant agent, useful for providing temporary protection of minor cuts, scrapes, and burns as well as drying effects of wind and cold weather. Additionally, when used at OTC concentrations, petrolatum can temporarily protect and help relieve chapped or cracked skin and lips.

A variety of grades (i.e., types) of petrolatum suitable for use in topical formulations are commercially available, including from Sonneborn LLC (Parsippany, NJ). In cosmetic applications, petrolatum can be found at any usage level up to 100% in skin care, body care and hair care for moisturization, TEWL function, emolliency, and texture effects. Petrolatum is an effective, economical, versatile, safe, and inert emollient used widely in mass market products, and has limited application for active skin care claims within the anti-aging or natural/plant based market. At high use levels required for monographed skin protectant claims (30%), petrolatum has a low sensory appeal.

Vegetal-derived "butters" are triglyceride-based emollients used in topical products and have a melting point of typically in the range of from 20 to 40.5°C. Butters are generally described in terms of the fatty acid composition of the constituent triglycerides. Longer fatty acid chain lengths increase melting points; higher degrees of unsaturation translate to lower melting points.

Vegetal Butters have long been recognized and used for emolliency and moisturization in cosmetic and personal care applications. However, use levels of vegetal butters in emulsions and anhydrous systems can often be limited by their complex mix of various fatty acids and inherent polymorphic crystallization behavior. At higher concentrations (at least 2%), inclusion of a vegetal butter that has been minimally refined, bleached and deodorized (i.e., an "RBD" butter) in a finished formulation can result in grainy emulsion structures or greyish formations - so-called "bloom". Additionally, when RBD vegetal butters are used in a finished product at a concentration that provides meaningful functionality, which concentration is at least 2%, the product can, over time, exhibit changes in one or more of viscosity, color and/or gloss. In many instances, emulsion products containing high levels of RBD vegetal butter(s), greater than 2%, are observed to separate.

A mixture of petrolatum and an RBD vegetal-derived butter is likewise subject to formulation limitations, including instability and undesirable sensory properties. Prior to the present invention, suitable petrolatum-based topical products could not be formulated with more than about two percent RBD vegetal butter; at concentrations in excess of 2% wt/wt RBD shea butter in a formulation containing 3%+ petrolatum, grains are perceptible - both on visual inspection and by touch. Moreover, adding more than 2% wt/wt RBD vegetal butter to a 3%+ petrolatum formulation is known to result in gloss and/or discoloration.

Shea butter, like petrolatum, provides emolliency and moisturization and has been used in a wide range of personal care applications. See, e.g., J. Alander "Shea butter with improved moisturisation properties" Personal Care (September 2009).

The unsaponifiable content of shea butter - as much as 7% to 10% - has been shown in both in vitro and ex vivo skin models to possess anti-inflammatory, collagen- protecting/stimulating, and fibroblast-proliferating properties. Idem; see also, A-C Anderson, "Protection against stress by natural triterpene esters" Personal Care (June 2011). Triterpene esters constitute 2% to 5% of RBD shea butter. In order for triterpene esters in shea butter to have a clinically meaningful effect in a 3%+ petrolatum formulation - such as protecting against stress-related breakdown of skin extracellular matrix proteins (collagen and elastin) by reducing expression of matrix metalloproteinases or inhibition of the release of pro-inflammatory mediators like PGE2, TNF-a and IL-Ιβ - shea butter must be included at a concentration of at least about 2% - a level that commonly results in bloom, graininess, discoloration or other organoleptic deficiencies.

Interesterified, non-fractionated vegetal butters - especially shea butter - are known to be superior to their RBD counterparts in several respects. First, interesterification raises the melting point of the shea butter almost twenty degrees - from 33°C (for RBD) to 51°C (for interesterified, non-fractionated). Second, interesterified, non-fractionated shea butter crystallizes more rapidly (in less than 24 hours) than its RBD counterpart (which takes 5 to 7 days). Third, at higher temperatures, interesterified, non-fractionated shea butter retains more of its solid content than RBD shea butter.

International Patent Application Publication WO 2006/037341 discloses low- lauric, low-trans fat, cocoa butter substitutes useful for food and other

applications. The compositions in WO 2006/037341 are a specific type of inter- esterified and fractionated fat - with a low melting fat fraction that has a final melting point around and below body temperature, and a steep SFC-melting profile. (As used in the present application the term "body temperature" is to be understood as about 37°C.) Comparative Example 7 in WO 2006/037341 lists two lip balm formulations. The two formulations in Example 7 both contain 55% white petrolatum and are identical except with respect to triglyceride component. The first formulation in Example 7, "Test Composition," is made with 6% of a low melting inter-esterified and fractionated triglyceride as described immediately above. The second formulation, "Reference Composition" is made with 6% Illexao 30-61, a palm glyceride having a melting point of 34°C.

In marked contrast to the formulations in Example 7 of WO 2006/037341, compositions of certain embodiments of the present invention are created from an inter-esterified, non-frationated triglyceride component that has a final melting point above or significantly above body temperature (e.g., 51°C), as well as a very slow (i.e., flat) SFC-melting profile. By "significantly above body temperature" is meant a temperature at least 10%, at least 20%, or at least 25% above body temperature. The physical properties of a melting point above or significantly above body temperature and a very slow (i.e., flat) SFC-melting profile are central to achieving inventive properties of certain embodiments of the present invention - such as, achieving superior skin barrier protection and moisturization as measured by TEWL (i.e., by reducing trans-epidermal water loss), and/or durable protective coating on hair. The Illexao 30-61 palm triglyceride used in Example 7 of WO 2006/037341and the interesterified, non-fractionated, shea butter used in certain embodiments of the present invention differ in another functionally important respect to the inventive claims. Ilexao 30-61 contains less than about 1% unsaponifiables, and, consequently, a very low content of functional triterpene esters. The

interesterified, non-fractionated shea butter used in certain embodiments of the present invention has an unsaponifiable content of about 7% to about 10%. At this level of unsaponifiables, triterpene esters are present in amount to provide anti-inflammatory, collagen-protecting/stimulating, and fibroblast-proliferating and other skin health benefits. In combination, the above properties make the interesterified, non-fractionated shea butter that is a component of certain embodiments of the present invention more crystalline and thermally stable than its RBD counterpart. For example, if a finished formulation containing certain interesterified, non-fractionated shea butter of the present invention were to be exposed to an elevated temperature sufficient to melt its crystals (e.g., during storage), when the product was placed in cooler conditions that would allow the crystals to recrystallize, the crystals would do so achieve a stable form (transforming into β polymorphs) within 24 hours. In contrast, RBD shea butter crystals begin to melt not only at a lower temperature than interesterified, non-fractionated shea butter crystals but also more quickly. Moreover, when RBD shea butter crystals begin to recrystallize, a considerably longer period of time (5 to 7 days) is required to stabilize as β polymorphs.

In summary, there has been a long-existing and unmet commercial need within the Personal Care Industry for stable, cosmetically elegant (i.e., not unctuous), 3%+ petrolatum-based products that can incorporate triglyceride-based butters at functional threshold concentrations, e.g., of at least 2% wt/wt without reducing crystalline stability and reducing the functional TEWL performance of externally applied skin and hair treatment formulations. This need is demonstrably present for petrolatum-based products that contain 30% or more petrolatum (meeting OTC monograph requirements for "skin protectant"); evidenced by the commercial absence of OTC "skin protectant" compliant formulations (with 30% or more petrolatum) which also contain triglyceride-based vegetal-derived butters at functional threshold concentrations of at least 2%. The multifunctional structured, glycidic / non-glycidic matrices of certain embodiments of the present invention meet these needs by overcoming physical instability and eliminating the reduction of TEWL performance expected to be present in 3%+ petrolatum-based products that incorporate triglyceride-based vegetal-derived butters at functional threshold concentrations of at least 2%. Summary of the Invention

In one aspect the present invention relates to a topically-applied product comprising (i) at least one triglyceride and (ii) at least one petrolatum, wherein the topically-applied product contains, on a weight/weight basis, at least 2% triglyceride and at least 6% petrolatum.

Further embodiments are wherein the topical product does not over time exhibit graininess, bloom, discoloration, or separation, or change in viscosity.

Even further embodiments are wherein the triglyceride is interesterified and non- fractionated. In other embodiments, the triglyceride is interesterified and has a final melting point above or significantly above body temperature. Within this embodiment, the

interesterified triglyceride having a final melting point above or significantly above body temperature may be fractionated or may be non-fractionated.

In certain embodiments, the at least one triglyceride may be a combination of two (or more) interesterified fractions from one (or more) triglyceride(s), where some or all of the said fractions may be recombined.

In other embodiments, the triglyceride is interesterified, non-fractionated and has a final melting point above or significantly above body temperature.

In even further embodiments, the triglyceride is interesterified, non-fractionated and is selected from the group consisting of Butyrospermum Parkii (Shea) Butter, Theobroma Cacao (Cocoa) Seed Butter, Shorea Stenoptera (Illipe) Seed Butter, Astrocaryum

Murumuru Seed Butter, Theobroma Grandiflorum (Capuacu) Butter and Magnifera Indigo (Mango) Seed Butter.

In still even further embodiments, the at least one interesterified, non-fractionated triglyceride is Butyrospermum Parkii (Shea) Butter.

Still even further embodiments comprise at least 30% petrolatum and at least one interesterified, non-fractionated triglyceride, wherein the ratio of the at least one interesterified, non-fractionated triglyceride to the at least one petrolatum is from 1 :39 to 7: 13.

Still even further embodiments comprise at least 30% petrolatum and at least one interesterified triglyceride having a final melting point above or significantly above body temperature, wherein the ratio of the at least one interesterified triglyceride having a final melting point above or significantly above body temperature to the at least one petrolatum is from 1 :39 to 7: 13.

Still even further embodiments are comprised at least 30% petrolatum and at least one interesterified, non-fractionated triglyceride wherein the ratio of the at least one interesterified, non-fractionated triglyceride to the at least one petrolatum is from 1 : 19 to 1 :3.

Still even further embodiments are comprised at least 30% petrolatum and at least one interesterified triglyceride having a final melting point above or significantly above body temperature wherein the ratio of the at least one interesterified triglyceride having a final melting point above or significantly above body temperature to the at least one petrolatum is from 1 : 19 to 1 :3.

A further aspect of the present invention relates to a multi-functional chemical ingredient used in the manufacture of cosmetic, personal care, and/or dermatologic products comprising (i) at least one interesterified, non-fractionated triglyceride and (ii) at least one petrolatum.

A further aspect of the present invention relates to a multi-functional chemical ingredient used in the manufacture of cosmetic, personal care, and/or dermatologic products comprising (i) at least one interesterified triglyceride having a final melting point above or significantly above body temperature and (ii) at least one petrolatum.

In further embodiments, a cosmetic, personal care, and/or dermatologic product is comprised of a multi-functional chemical ingredient wherein the ratio of the at least one interesterified, non-fractionated triglyceride to the at least one petrolatum is from 1 :39 to 7: 13.

In further embodiments, a cosmetic, personal care, and/or dermatologic product is comprised of a multi-functional chemical ingredient wherein the ratio of the at least one interesterified triglyceride having a final melting point above or significantly above body temperature to the at least one petrolatum is from 1 :39 to 7: 13.

In still further embodiments, a cosmetic, personal care, and/or dermatologic product is comprised of a multi-functional chemical ingredient wherein the ratio of the at least one interesterified, non-fractionated triglyceride to the at least one petrolatum is from 1 : 19 to 1 :3.

In still further embodiments, a cosmetic, personal care, and/or dermatologic product is comprised of a multi-functional chemical ingredient wherein the ratio of the at least one interesterified triglyceride having a final melting point above or significantly above body temperature to the at least one petrolatum is from 1 : 19 to 1 :3.

In even further embodiments, the cosmetic, personal care, and/or dermatologic product is comprised of a multi-functional chemical ingredient wherein the interesterified, non- fractionated triglyceride and is selected from the group consisting of Butyrospermum Parkii (Shea) Butter, Theobroma Cacao (Cocoa) Seed Butter, Shorea Stenoptera (Illipe) Seed Butter, Astrocaryum Murumuru Seed Butter, Theobroma Grandiflorum (Capuacu) Butter and Magnifera Indigo (Mango) Seed Butter.

In further embodiments, the source of the interesterified, non-fractionated triglyceride component of the cosmetic, personal care, and/or dermatologic product is

Butyrospermum Parkii (Shea) Butter. A further aspect of the present invention relates to a dermatocosmetic product comprising (i) at least one triglyceride and (ii) at least one petrolatum, wherein the dermatocosmetic product (a) contains, on a weight/weight basis, at least 2% triglyceride and at least 6% petrolatum and (b) does not over time exhibit graininess, bloom, discoloration, separation, or change in viscosity. In certain such embodiments, the at least one triglyceride is non-fractionated and/or has a final melting point above or significantly above body temperature.

A further aspect of the present invention relates to a topical product comprising, consisting essentially of, or consisting of (i) at least one interesterified, non-fractionated triglyceride and (ii) at least one petrolatum and (iii) an optional active ingredient.

A further aspect of the present invention relates to a topical product comprising, consisting essentially of, or consisting of (i) at least one interesterified triglyceride with a final melting point above or significantly above body temperature and (ii) at least one petrolatum and (iii) an optional active ingredient.

Accordingly, the present invention further relates to a multi-functional chemical ingredient used in the manufacture of cosmetic, personal care, and dermatologic products, comprised of or consisting essentially of one (or more) interesterified, non-fractionated triglyceride(s) and an effective moisturizing amount of one (or more) petrolatum(s), more preferably in a ratio of interesterified, non-fractionated triglyceride(s) to petrolatum(s) ranging from about 7: 13 to about 1 :39 and topical formulations containing the matrix. Further embodiments are directed to multi-functional chemical ingredient used in the manufacture of cosmetic, personal care, and dermatologic products, comprised of or consisting essentially of one (or more) interesterified triglyceride(s) having a final melting point above or significantly above body temperature and an effective

moisturizing amount of one (or more) petrolatum(s), more preferably in a ratio of interesterified triglyceride(s) having a final melting point above or significantly above body temperature to petrolatum(s) ranging from about 7: 13 to about 1 :39 and topical formulations containing the matrix. In topical formulations, the effective moisturizing amount of one (or more) petrolatum(s) is at least about 3%, preferably at least about 5%, and more preferably at least about 30% by weight of the formulation. In preferred embodiments, the multifunctional chemical ingredient is present in a finished

formulation in an amount such that the interesterified, non-fractionated triglyceride or the triglyceride having a final melting point above or significantly above body temperature is at least 2% by weight of the formulation. In particularly preferred embodiments, the inter-esterified, non-fractionated triglyceride is selected from the group consisting of Butyrospermum Parkii (Shea) Butter, Theobroma Cacao (Cocoa) Seed Butter and Shorea Stenoptera (Illipe) Seed Butter.

Brief Description of the Drawings Figure 1 graphically represents the melting profile curve of a topically-applied product according to the present invention that is a mixture of 25% interesterified, non- fractionated shea butter and 75% of petrolatum.

Figure 2 graphically represent the melting profile curve of a topically-applied product according to the present invention that is a mixture of 25% RBD shea butter and 75% of petrolatum.

Figure 3 graphically represents the melting profile curve of petrolatum. Figure 4 combines the melting profile curves from Figures 1 - 3. Detailed Description of the Invention

Definitions "Dermatocosmetic" means suitable for inclusion in a cosmetic, personal care or dermatologic product for topical application on mammalian skin (epidermis, dermis, hypodermis) or other keratinous tissue [i.e., hair (including hair follicles, hair roots, and hair bulbs), and nails (i.e., ventral epithelial layer of the nail bed)], as well as the sebaceous and perspiratory glands (eccrine and apocrine), which is intended to improve the condition and/or appearance of the skin, keratinous tissue, or sebaceous/perspiratory gland, or otherwise provide a skin health benefit.

"Topical" means the surface of the skin, other keratinous tissue, or sebaceous and perspiratory glands.

"Skin health benefit" means regulating and/or improving a skin condition, non-limiting examples of which include: improving the hydration status or moisturization of the skin; improving skin barrier function; improving skin appearance by reducing the appearance of one or more of fine lines and/or wrinkles, dyschromia, redness or blotches; imparting more even skin tone; increasing skin elasticity, resiliency or firmness; improving skin feel and texture by increasing smoothness or softness; reducing levels of inflammation; reducing degradation of extracellular skin matrix proteins; increasing the quantity and quality of extracellular skin matrix proteins; increasing the thickness of one or more layers of the skin.

"Dermatocosmetic products" (also referred to herein as "finished products") include but are not limited to, creams, moisturizers, lotions, ointments, gels, serums, color cosmetics (e.g., foundation, blush, lip stick/gloss, eye shadow, concealer), masks, and cleansers and washes, that may contain one or more active ingredients, including prescription and nonprescription pharmaceutical agents.

"Interesterified, non-fractionated triglyceride" means an ester formed from glycerol and three fatty acid groups that is transformed by "interesterification," a process involving the exchange of acyl radicals between (i) the triacylglycerol ester and an acid or

(ii) the triacylglycerol ester and an alcohol, and not further fractionated. The exchanges can be within the same triacylglycerol ester or between the triacylglycerol ester and a second ester, including another triacylglycerol ester. Interesterification is accomplished by techniques known in the art, altering the physical characteristics (molecular packing and melting points) of triglycerides, and generating more stable crystalline forms. "Petrolatum" means a purified mixture of semisolid hydrocarbons obtained from petroleum. In certain embodiments, the petrolatum contains both mineral oil,

microcrystalline and paraffin wax components and is further defined with references to the following properties: specific gravity (at 60°C) according to US Pharmacopeia ("USP") Physical Test 841 from 0.815 to 0.880; drop melting point according to ASTM International Standard D127from 38.0 to 75.0°C; consistency according to ASTM

International Standard D937 between 10-300 dmm (1/lOth of 1 mm = 1 dmm).

The term "petrolatum" is also to be understood in certain embodiments to include mineral oil (an oily liquid or tar-like hydrocarbonaceous material from a solid mineral source), a petroleum waxes (microcrystalline or paraffin), or a hydrocarbon produced from a non- petroleum source that has the following characteristics: specific gravity (at 60°C) according to US Pharmacopeia ("USP") Physical Test 841 from 0.815 to 0.880; drop melting point according to ASTM International Standard D127from 38.0 to 75.0°C; consistency according to ASTM International Standard D937 between 10-300 dmm (1/lOth of 1 mm = 1 dmm).

The multi-functional chemical ingredient of the present invention - also described in the application as a "multi-functional structured, glycidic / non-glycidic matrix" (referred to by the acronym "MFSG/NGM") - is comprised of or consists essentially of, or consists of, two component parts: (i) petrolatum(s) and (ii) and interesterified, triglyceride(s) that are non-fractionated and/or have a final melting point above or significantly above body temperature. In certain embodiments, the ingredient is described as a "structured glycidic / non-glycidic matrix" because the crystalline components of the interesterified, non-fractionated triglyceride(s) is/are oriented (i.e., "packed") with respect to

petrolatum(s) in a lower-energy, more stable configuration than a system comprised of non-interesterified triglyceride(s) and petrolatum(s). The nature of the structured glycidic / non-glycidic matrix can be more particularly described based on one or more analytical methods known in the art including, but not limited to, x-ray diffraction, differential scanning calorimetry (DSC), and scanning electron microscopy.

In certain embodiments, the petrolatum(s) in the MFSG/NGM meet(s) all current USP and FDA requirements (21 CFR §172.880).

In certain embodiments of the invention, the petrolatum part comprises USP-Grade White Petrolatum, a purified mixture of semisolid hydrocarbons obtained from petroleum that is wholly or nearly decolorized and may contain a stabilizer.

In preferred embodiments, the petrolatum part has the following physical properties: specific gravity at 60°C, per USP 841 of 0.815 - 0.880; drop melting point according to ASTM D127 between 51.6-60.0°C; consistency according to ASTM D937 between 170- 200 dmm; viscosity according to ASTM D445/D2161 between 40.0- 50.0 SUS @ 210°F; and Lovibond^® color of less than 1.0 yellow when measured according to Institute of Petroleum Standard Method IP 17. In certain preferred embodiments, the multi-functional, structured glycidic / non-glycidic matrix is present in a finished product at a concentration such that total petrolatum content is at least 30% on a weight/weight basis of the finished product.

In preferred embodiments, the triglyceride that is interesterified, non-fractionated is selected from the group consisting of Butyrospermum Parkii (Shea) Butter, Theobroma Cacao (Cocoa) Seed Butter, Shorea Stenoptera (Illipe) Seed Butter, Astrocaryum

Murumuru Seed Butter, Theobroma Grandiflorum (Capuacu) Butter and Magnifera Indigo (Mango) Seed Butter. (Interesterifed shea butter, cocoa butter and Illipe butter are available from AAK Sweeden AB and AAK USA Inc., as LIPEX^® Sheasoft, LIPEX^® Cocoasoft, and LIPEX^® Illipesoft.) The melting point of Lipex Sheasoft^® is about 51°C. The slope of the solid fat content (SFC) melting profile of LIPEX^® Sheasoft from 20°C to 35°C is less than 1, where percent change in SFC is plotted on the y axis, and temperature is plotted on the x axis.

In more preferred embodiments, the triglyceride that is interesterified, non-fractionated is selected from the group consisting of Butyrospermum Parkii (Shea) Butter, Theobroma Cacao (Cocoa) Seed Butter, and Shorea Stenoptera (Illipe) Seed Butter.

In one especially preferred embodiment, the triglyceride that is interesterified, non- fractionated is shea butter having from about 7% to about 10% unsaponifiables.

The unsaponifiable fraction of interesterified, non-fractionated shea butter is comprised of triterpene esters and highly unsaturated isoprenoidal hydrocarbons. Among the triterpene esters are cinnamic and acetic acid esters of a- and β-Amyrin, Butyrospermol, Lupeol, and Parkeol.

In especially preferred embodiments, the interesterified, non-fractionated shea butter contains at least about 2% triterpene esters; and, in even more preferred embodiments, the interesterified, non-fractionated shea butter contains from about 2% to about 5% triterpene esters; and in still more preferred embodiments above about 5% triterpene esters. In a first non-limiting aspect of the invention, the petrolatum component and the interesterified, non-fractionated ester component are combined to form a multi-functional structured, glycidic / non-glycidic matrix that is thermostable in comparison to petrolatum. "Thermostable" means that the Solid Fat Content (SFC) of the MFSG/NGM of the present invention is within about 3% of the SFC of petrolatum at the same temperature. Comparing the areas under the respective melting profile curves between 20°C and 45°C of the two materials further demonstrates that the MFSG/NGM

embodiments of the present invention is equivalently thermostable to petrolatum - within about one percent (1.3%). The area under the melting profile curve of petrolatum (20°C - 45°C) is 137; the area under the melting profile curve of the MFSG/NGM of the present invention (25% interesterified, non-fractionated shea butter; 75% petrolatum) is 138.8. In contrast, the area under the melting profile curve of a blend of 25% non-interesterified (i.e., RBD) shea butter and 75% petrolatum is 101.62; this represents an over 25% difference (25.82%). Table 1 below presents the SFC and area under the curve over a temperature range from 20°C to 45°C of a topically-applied product according to the present invention that is a mixture of 25% interesterified, non-fractionated shea butter and 75% of petrolatum.

_^ Area Under Curve (AUC)

Temperature SFC _ · . . -_{» «}■ .

Trapezoidal Method

20 12.9 30.125

22.5 11.2 26

25 9.6 21.875

27.5 7.9 17.75

30 6.3 13.625

32.5 4.6 10.5

35 3.8 7.75

37.5 2.4 5

40 1.6 5.75

45 0.7

Total AUC 138.375

Table 2 below presents the SFC and area under the curve over a temperature range from 20°C to 45°C of a topically-applied product according to the present invention that is a mixture of 25% RBD shea butter and 75% of petrolatum. Table 2

Area Under Curve (AUC)

Temperature SFC

Trapezoidal Method

20 10.7 24

22.5 8.5 19.75

25 7.3 16.5

27.5 5.9 13.375

30 4.8 10

32.5 3.2 7

35 2.4 4.625

37.5 1.3 2.625

40 0.8 3.75

45 0.7

Total AUC: 101.625 le 3 below and shows the melting profile curve of neat petrolatum

Area Under Curve (AUC)

Temperature SFC

Trapezoidal Method

20 13 30.125

22.5 11.1 25.5

25 9.3 21.375

27.5 7.8 17.875

30 6.5 13.75

32.5 4.5 10.375

35 3.8 7.5

37.5 2.2 4.75

40 1.6 5.75

45 0.7

Total AUC: 137

The above area under the curve calculations demonstrate the difference in solid fat content between otherwise equivalent blends of two different shea butters with petrolatum.

In preferred embodiments of the first aspect of the invention, the thermostable

MFSG/NGM is a binary, homogenous mixture of one or more interesterified, non- fractionated triglyceride(s) and petrolatum(s) in the following ratios: 1:39; 1:38; 1:37; 1:36; 1:35; 1:34; 1:33; 1:1:32; 1:31; 1:30; 1:29; 1: 28; 1:27; 1:26; 1:25; 1:24; 1:23; 1:22; 1:21; 1:20; 1:19; 1:18; 1:17; 1:16; 1:15; 1:14; 1:13; 1:12; 1:11; 1:10; 1:9; 1:8; 1:7; 1:6; 1:5; 1:4; 1:3; 1:2; or 7:13. In preferred embodiments of the first aspect of the invention, the interesterified, non- fractionated triglyceride(s) is/are present at a concentration of from about 2% to about 50% by weight of the thermostable MFSG/NGM; from about 2.5% to about 35% by weight of the thermostable MFSG/NGM; from about 5% to about 25% by weight of the thermostable MFSG/NGM; or from about 10% to about 20% by weight of the

thermostable MFSG/NGM .

In more preferred embodiments of the first aspect of the invention, interesterified, non- fractionated triglyceride(s) is at least 10% by weight of the thermostable MFSG/NGM, but not more than 35% by weight of the thermostable MFSG/NGM. In one highly preferred embodiment of the first aspect of the invention, the

interesterified, non-fractionated triglyceride is shea butter, which is present at a concentration of greater than 2%, more preferably greater than 2.5%, but less than 35% by weight of the thermostable MFSG/NGM.

The thermostable MFSG/NGM embodiments are "multi-functional", providing multiple skin health benefits (as defined above).

In certain embodiments of the present invention, it was surprisingly and unexpectedly found that while the MFSG/NGM of the invention had substantially the same physico- sensory properties as "neat" petrolatum (i.e., petrolatum without the addition of interesterified, non-fractionated shea butter), at four hours post-application to the skin the MFSG/NGM of the invention provided a reduction in transepidermal water loss and greater improvement in skin barrier function versus neat petrolatum.

By the phrase "substantially the same physico-sensory properties as 'neat' petrolatum" is meant, a difference of less than 5% from neat petrolatum in sensory panel test that measures seven parameters on a scale of 0 - 5, where neat petrolatum is assigned as score of 3. The seven parameters are spreadability; greasiness; cushion; tack; absorption; gloss; and graininess.

A second non-limiting aspect of the invention is directed to a multifunctional, skin barrier protecting dermatocosmetic product comprising the MFSG/NGM described in the first aspect of the invention, where the product does not separate, or exhibit bloom, graininess (sometimes also referred to as "sandiness") or discernible change in viscosity during the established shelf life of the product, as perceived by a trained observer/technician or instrumentally using analytical techniques known to the skilled artisan in the field. "Bloom" occurs when two crystalline materials are mixed, and unstable crystals form. Bloom is visible to the naked eye, and can manifest as a coating on the surface of the product.

"Graininess" is a tactile property that can be perceived when a product is applied (e.g., rubbed) onto the skin. A change in viscosity is determined instrumentally. The viscosity of a product is measured with the same type of viscometer (e.g., Brookfield RVT) configured with the same type of spindle (spindle number 4) at the same rotation speed (RPM) as specified in a certificate of analysis for the product.

In the case of a dermatocosmetic product comprising the MFSG/NGM of the present invention that is an emulsion, stability (i.e., not separating into oil and water phases) may be assessed as follows. Glass jars and, preferably, finished packaging (i.e., packaging in which the product is planned to be sold to consumers) are filled with the product. The filled containers (glass jars and finished packaging) are stored at different temperatures and under different light conditions for time periods of varying lengths. Temperatures include 50°C, 45°C, 37°C, 25°C (often described in the art as "room temperature"), and 4°C. Different lighting conditions may include fluorescent light and light emitted from a solar simulator, a device that provides illumination approximating natural

sunlight. Preferably, the solar simulator is calibrated and operated in accordance with the criteria set out int the following standards: ASTM E927-10(2015) published by ASTM International (West Conshohocken, Pennsylvania); or Standard IEC 60904-9 Edition2 published by the International Electrotechnical Commission (Geneva, Switzerland). If the product is a sunscreen, the solar simulator will comply with the then current standard promulgated by the applicable governmental or industry body: in the United States, the Food and Drug Administration; in Europe, the European Cosmetics Association (COLD³ A); in Japan, Japan Cosmetics Industry Association (JCIA). Samples can, and preferably, are evaluated at the following time intervals: 2 weeks, 4 weeks, 8 weeks, 12 weeks. Additionally, samples stored at evaluated at 25°C, 37°C and 4°C are evaluated after one year. The highest temperature samples and the light exposed samples are preferably evaluated for the first three test intervals. Before testing, samples are preferably kept at room temperature for about 8 hours to equilibrate.

Separation of emulsion embodiments of the invention may occur over days or weeks. Appearance of bloom or change in color (discoloration) or developing a sandy or grainy texture may likewise occur over days or weeks. A third, non-limiting aspect of the invention is directed to a multifunctional, skin barrier protecting dermatocosmetic product that does not exhibit bloom, graininess or discernable change in viscosity during the established shelf life of the product, as perceived by a trained observer/technician or instrumentally using analytical techniques known to the skilled artisan in the field, where the product comprises a moisturizing amount of petrolatum - e.g., at least 3% by weight of the product;

preferably at least 5% by weight of the product; still more preferably at least 10% by weight of the product; and even more preferably at least 30% by weight of the product - and one (or a combination of) triglyceride butter(s) at a concentration of at least 2%. In preferred embodiments, the triglyceride butter(s) are interesterified, non-fractionated. In one preferred embodiment of the third aspect of the invention, the dermatocosmetic product is comprised of (i) at least 2%, preferably at least 5%, and still more preferably at least 10%) of an interesterified, non-fractionated triglyceride and (ii) at least 5%, preferably at least 10%, and still more preferably at least 30% of a petrolatum. An especially preferred interesterified, non-fractionated triglyceride is shea butter. Formulas containing the topical product or MFSG/NGM of the invention may also contain additional ingredients and function as a "topical delivery system" that deposits a wide range of cosmetic and dermatologic ingredients, include prescription active pharmaceutical agents and non-prescription drugs to the skin for purposes of providing a skin health benefit, as well as systemically through the skin. The International Cosmetic Ingredient Dictionary and Handbook published by the Personal Care Products Council and the U.S. Pharmacopoeia describe a wide provide a listing of many ingredients that may be delivered from (i.e., formulated in) the topical delivery systems of the present invention, non-limiting examples of which are enumerated below. It is to be understood that in certain embodiments the topical delivery system per se is a finished product.

The term "non-prescription" is to be understood as including ingredients generally recognized as safe and effective under an applicable over-the-counter monograph issued by the U.S. Food and Drug Administration ("FDA"). "Prescription" agents include drugs for which approval of the FDA, or a comparable agency responsible for the regulation of pharmaceutical actives outside the US, is required.

Both steroidal and non-steroidal anti-inflammatory agents may be formulated in, and delivered from, compositions of the present invention. Non-limiting examples of antiinflammatory agents are listed below, with corresponding doses indicated in parenthesis: Alcometasone dipropionate (0.05%); Amcinonide (0.1%>); Betamethasone dipropionate (0.05%o); Betamethasone valerate (0.01%>); Clobetasol propionate (0.05%>); Clocortolone pivalate (0. 1%>); Desometasone (0.05%>); Desonide (0.05%>); Diflorasone diacetate (0.05%o); Diflorasone diacetate (0.25%); Flocinonide (0.05%>); Fluocinolone acetonide (0.025%o); Fluoranenolide (0.05%>); Fluticasone (0.05%>); Fluticasone propionate

(0.005%); Halbetasol propionate (0.05%); Halcinonide (0.1%); Hydrocortisone (0.5%); Hydrocortisone valerate (0.1%>); Hydrocortisone butyrate (0. 1%>); Hydrocortisone valerate (0.2%); Mometasone furoate (0.1%>); Mometasone furoate (0.1%>); Prednicarbate (0.025%); Triamcinolone acetonide (0.5%).

Antipruritic agents known to those of skill in the art, including those listed below, may be delivered to the skin in topically-applied products comprising the topical delivery systems of the present invention. Non-limiting examples of antipruritic agents include Doxepin and Pramoxine.

Compositions of the present invention alone (i.e., blend of inter-esterified triglyceride and petrolatum, without additional active ingredients), may be used in the treatment of diaper dermatitis. In certain embodiments of the invention, these compositions may serve as delivery systems for one or more active ingredients useful in the treatment of diaper dermatitis, including but not limited to an antifungal (preferably nystatin cream;

clotrimazole; econazole nitrate; miconazole; or amphotericin) or an anti-inflammatory agent (preferably hydrocortisone).

Compositions of the present invention alone may also serve as delivery systems for one or more active ingredients useful in the treatment of hemorrhoids, including one or more of a topical analgesic agent, an anti-inflammatory agent and/or an antipruritic agent, each, as described in more detail, elsewhere in this application. Topical delivery systems of the present invention may be employed to deliver to the skin ingredients useful in the treatment of acne including, but not limited to, the following: Adapalene; Alpha-hydroxy acids (AHAs as defined below); Azelaic acid; Benzoyl peroxide; Cimetidine; Clindamycin; Erythromycin; Resorcinol; Salicylic Acid;

Tazarotene; Tretinoin. Hydrophilic hydroxy carboxylic acids suitable actives for use in compositions of the present invention include alpha hydroxy acids (AHAs) and polyhydroxyacids (PHAs). AHAs are acids having 1-29 carbon atoms and conforming to the structure

(Rl)(R2)C(OH)COOH, where Rl and R2 are selected from the group consisting of hydrogen, alkyl, aralkyl and aryl groups, and wherein the alkyl, aralkyl and aryl groups may be saturated or unsaturated, isomeric or non-isomeric, straight or branched chain or cyclic, and the alkyl, aralkyl and aryl groups may contain as substituents OH, CHO, COOH and alkoxy groups having 1 to 9 carbon atoms.

The "AHA" term is to be understood to include not only the free acid, but also its corresponding ester (formed by reaction of the AHA with an alcohol), its corresponding lactone (formed by the reaction of the carboxylic acid and hydroxyl groups of the AHA), as well as its corresponding salt (formed by reaction of the AHA with an organic base or an inorganic alkali). Rl and R2 may be the same or different. In the latter case, the AHAs may be stereoisomers in the D, L, and DL forms. AHAs suitable for use in the present invention may be grouped into (i) alkyl AHAs, (ii) aralkyl and aryl AHAs, (iii) polyhydroxy AHAs, and (iv) polycarboxylic AHAs.

Among the preferred hydrophilic hydroxycarboxylic acids are (a) 2-hydroxyethanoic acid (glycolic acid, hydroxyacetic acid) and 2-hydroxypropanoic acid (lactic acid); and 2- hydroxybutane-l,4-dioic acid (malic acid); 2-phenyl 2-hydroxyethanoic acid (mandelic acid); 2,3-dihydroxybutane-l,4-dioic acid (tartaric acid); and 2-hydroxy-2- carboxypentane-l,5-dioic acid (citric acid). Other preferred polyhydroxy acids include gluconolactone and lactobionic acid.

Hydrophilic hydroxycarboxylic acids may be used in the delivery systems of the present invention at concentrations ranging from about 0.1% to about 6%, preferably from about 0.2% to about 4%, and more preferably from about 0.5% to about 3%.

Hydrophobic hydroxycarboxylic acids, including orthohydroxybenzoic acid (salicylic acid), may also be delivered to the skin in the topical delivery system of the present invention, preferably at a concentration of at least about 0.5%. Topical delivery systems of the present invention can include one or more active ingredients useful in treating warts including, but not limited to Salicylic Acid.

Topical delivery systems of the present invention can include one or more active ingredients useful in treating various types of rosacea, including erythemato- telangiectatic rosacea, papulopustular rosacea, phymatous rosacea, and ocular rosacea. Non-limiting examples of such ingredients include the following: Azelaic acid; Benzoyl peroxide; Clindamycin; Doxycycline or Minocycline; Erythromycin; Isotretinoin;

Metronidazole; Permethrin; Sodium sulfacetamide; Sulfur; Tacrolimus; Tetracycline; Tretinoin.

Other dermatoses, including psoriasis, eczema, contact dermatitis, atopic dermatitis and seborrheic dermatitis may be treated by applying a topical product comprising the delivery system of the present invention and at least one anti-inflammatory or antipruritic ingredient to itchy/inflamed skin. Another aspect of the present invention is directed to the topical delivery of active ingredient(s) useful in treating erythema multiforme. These include the steroidal and nonsteroidal anti-inflammatory agents listed above.

One or more sunscreens - active ingredients which absorb, block or otherwise attenuate ultraviolet radiation - may be included in the delivery system of the present invention.

Benign photodamage manifested as hyperpigmentation may be treated by using the topical delivery systems of the present invention to deposit one or more of the following lightening (also known as bleaching) ingredients on the skin: hydroquinone, kojic acid, glycolic acid and other alpha-hydroxy acids, ascorbic acid, magnesium ascorbyl phosphate, ascorbyl glucosamine and artocarpin.

Compositions of the present invention may be used to deliver to the scalp ingredients useful in the treatment of alopecia areata and androgenic alopecia, or otherwise helping to reduce hair loss, stop hair loss or stimulate hair growth. These include, but are not limited to, the following: 5-alpha-reductase inhibitors and other anti androgenic compounds such as Flutamide, Cyproterone and Spironolactone; Cimetidine; Finasteride; and Minoxidil.

Delivery systems of the present invention may also include one or more ingredients that remove hair including, but not limited to, thioglycolates.

Compositions of the present invention may also be used to deliver therapeutically effective amounts of pharmaceutical ingredients used to treat cancerous and pre- cancerous conditions associated with exposure to ultraviolet radiation, including actinic keratoses; basal cell carcinoma; squamous cell carcinoma; melanoma. Non-limiting examples of pharamaceutical ingredients useful in the treatment of actinic keratoses that may be included in the topical delivery systems of the present invention include:

Aciretin; Adapalene; Diclofenac in combination with Hyaluronic Acid; Fluourouracil; and Imiquimod.

The present application is also directed to the topical delivery of active ingredients known to the skilled artisan that promoting wound healing, non-limiting examples of which include one or more topical antiseptic or antibiotic agents, including in combinations with one or more topical antioxidants. Non-limiting examples of such ingredients include Vitamin K and silver particles.

Compositions of the present invention may also be used to deliver topical analgesic agents including, but not limited to, corticosteroids, lidocaine, benzocaine, prilocaine, dibucaine tetracaine, butamben, pramoxine, benzyl alcohol, menthol, wintergreen oil, eucalyptus oil, capsaicin, trolamine salicylate, and mixtures thereof.

Another aspect of the present invention is directed to topical antifungal and antimicrobial agents known to those of skill in the art, including those listed below, which may be delivered to the skin in topically-applied products comprising the compositions of the present invention. Non-limiting examples of antimicrobial and antifungal agents suitable for use in the present invention include: β-lactam agents, quinolone agents, ciprofloxacin, norfloxacin, tetracycline, erythromycin, amikacin, 2,4,4'-trichloro-2'-hydroxy diphenyl ether, 3,4,4'-trichlorobanilide, phenoxyethanol, phenoxy propanol, phenoxyisopropanol, doxycycline, capreomycin, chlorhexidine, chlortetracycline, oxytetracycline,

clindamycin, ethambutol, hexamidine isethionate, metronidazole, pentamidine, gentamicin, kanamycin, lincomycin, methacycline, methenamine, minocycline, neomycin, netilmicin, paromomycin, streptomycin, tobramycin, miconazole, tetracycline hydrochloride, erythromycin, zinc erythromycin, erythromycin estolate, erythromycin stearate, amikacin sulfate, doxycycline hydrochloride, capreomycin sulfate, chlorhexidine gluconate, chlorhexidine hydrochloride, chlortetracycline hydrochloride, oxytetracycline hydrochloride, clindamycin hydrochloride, ethambutol hydrochloride, metronidazole hydrochloride, pentamidine hydrochloride, gentamicin sulfate, kanamycin sulfate, lineomycin hydrochloride, methacycline hydrochloride, methenamine hippurate, methenamine mandelate, minocycline hydrochloride, neomycin sulfate, netilmicin sulfate, paromomycin sulfate, streptomycin sulfate, tobramycin sulfate, miconazole hydrochloride, ketaconazole, amanfadine hydrochloride, amanfadine sulfate, octopirox, parachlorometa xylenol, nystatin, tolnaftate, zinc pyrithione and clotrimazole.

Compositions of the present invention may also be used to deliver agents that reduce cellulite including xanthine compounds such as caffeine, theophylline, theobromine, and aminophylline. Non-limiting examples of antioxidants/radical scavengers which may be topically delivered in the present invention include: retinoids - natural and/or synthetic analogs of Vitamin A or retinol-like compounds which possess the biological activity of Vitamin A in the skin as well as the geometric isomers and stereoisomers of these compounds, including of retinol, retinal, C₂-C₂₂ alkyl esters of retinol (e.g., retinyl palmitate, retinyl acetate, retinyl propionate), and/or retinoic acid; ascorbic acid (vitamin C) and its salts; ascorbyl esters of fatty acids, ascorbic acid derivatives (e.g., magnesium ascorbyl phosphate, sodium ascorbyl phosphate, ascorbyl sorbate); tocopherol (vitamin E), tocopherol sorbate, tocopherol acetate, other esters of tocopherol; butylated

hydroxybenzoic acids and their salts; 6-hydroxy-2,5,7,8-tetramethylchroman-2- carboxylic acid; gallic acid and its alkyl esters, especially propyl gallate; uric acid and its salts and alkyl esters; sorbic acid and its salts; lipoic acid; amines (e.g., N,N- diethylhydroxylamine, amino-guanidine); sulfhydryl compounds (e.g., glutathione); coenzyme Q10 and its analogues, including without limitation, idebenone;

dihydroxyfumaric acid and its salts; lycine pidolate; arginine pilolate;

nordihydroguaiaretic acid; bioflavonoids; curcumin, lysine; 1 -methionine; proline;

superoxide dismutase; silymarin; tea extracts; grape skin/seed extracts; melanin; and rosemary extracts.

Non-limiting examples of skin soothing and/or healing agents suitable for use in the present invention include: panthenol and derivatives, aloe vera and its derivatives, pantothenic acid and its derivatives, allantoin, bisabolol, and dipotassium glycyrrhizinate.

Steroidal reproductive agents can also be delivered in compositions of the present invention, non-limiting examples of which include: androgens, such as, for example, androstenediol and androisoxazole (for anabolic disorders), testosterone (hypogonadism, muscle wasting, male impotence, postmenopausal symptoms in women),

dihydrotestosterone (hypogonadism, muscle wasting), dehydroepiandro-sterone (muscle wasting, fat reduction, fitness); estrogens (postmenopausal symptoms, birth control), such as, for example, 17 beta-estradiol, estradiol-3, 17-diacetate, estradiol-3 -acetate, estradiol- 17-acetate, estradiol-3, 17-valerate, estradiol-3 -valerate, estradiol- 17-valerate, ethinyl estradiol, estrone; progesterones (prevent endometriosis, prevent endometrial cancer, control habitual abortion, suppress or synchronize ovulation, promote hair growth), such as, for example, progesterone (preg-4-ene-3,20-dione), norethindrone, norgestrieone, norgestadienone, norgestrel, norgestimate, progestogenic acid, dihydroprogesterol, nomagesterol. In other embodiments, a muscle-relaxant drug (non-limiting examples of which include pharmaceutically-acceptable salts of cinnamedrine, cyclobenzaprine, flavoxate, orphenadrine, papaverine and mebeverine) may be delivered using the compositions of the present invention. Further non-limiting aspects of the invention are directed to methods for providing skin health benefits, including, but not limited to, (a) protecting or relieving chapped or cracked skin and lips from the drying effects of wind and cold weather, (b) reducing transepidermal water loss and strengthening the skin moisture barrier, (c) reducing levels of the expression of one or more genes that code for IL-6 or IL-8, (d) inhibiting the release of pro-inflammatory mediators such as PGE2, TNF-aand IL-Ιβ, (e) increasing the expression of one or more genes that code for extra-cellular matrix proteins (elastin, fibronectin), (f) reducing the expression of one or more genes that code for matrix metalloproteinases.

Examples

Raw Material Examples Raw Material Example 1 Petrolatum 75%

Interesterified, non-fractionated Butyrospermum Parkii (Shea) Butter

25%

Raw Material Example 2

Petrolatum 80%

Interesterified, non-fractionated Butyrospermum Parkii (Shea) Butter

20% Raw Material Example 3

Petrolatum 90%

Interesterified, non-fractionated Theobroma Cacao (Cocoa) Seed Butter

10%

Any of the above three raw material examples could also be used as a finished product that would comply with the OTC skin protectant monograph. Finished Product Examples

Finished Product Example 1 - Hand Cream

Phase I NCI Name % wt/wt

A Shea Butter Ethyl Esters (Lipex SheaLight™) 5

A Raw Material Example 1 (MFSG/NGM of Invention 10

Petrolatum (and) Interesterified, non-fractionated

Butyrospermum

Parkii (Shea) Butter

A Canola Oil 2

A Polyglyceryl-3 Stearate 3.5

A Glyceryl Stearate 1

A Cetearyl Alcohol 2

A Dimethicone 5

B Aqua Q.S.

B Glycerin 3

B Preservative Q.S.

C Xanthan Gum 0.3

D Aluminum Starch Octenyl succinate 3

Heat ingredients in each of Phases A and B separately to 75°C. Add Phase C to Phase A; add A/C to Phase B while stirring. Homogenize. Cool to 30°C while stirring. Adjust pH to 5.5 with Citric Acid. Add Phase D while stirring to form homogeneous product. In other embodiments, Shea Butter Ethyl Esters can be added to the MFSG/NGM of the present invention to form a three-part system - interesterified, non-fractionated shea butter, shea butter ethyl esters and petrolatum. In these embodiments, shea butter ethyl esters constitute from about 1% to 25% of the MFSG/NGM. Finished Product Example 2 - Anhydrous Facial and Body Treatment Cream

At 70°C, blend and melt the following ingredients until a clear liquid is formed: (i) 20 parts Lipex^® SheaLight (INCI: Shea Butter Ethyl Esters) with (ii) 78 parts of the Dermatocosmetic Structured Glycidic / non-glycidic Matrix of the invention (INCI: Petrolatum (and) Butyrospermum Parkii (Shea) Butter) with (iii) 2 parts Lipex^® PreAct (INCI Canola Oil). Cool to 22°C.

Finished Product Example 3 - Lip Balm

INCI Name % wt/wt

1. Raw Material Example 1 (MFSG/NGM of Invention) -

Petrolatum (and) Interesterified, non-fractionated 35.0 Butyrospermum Parkii (Shea) Butter

2. Butyrospermum Parkii Butter Extract 0.5

3. Canola Oil 2.0

4. Olus Oil (and) Camelina Sativa Oil 5.0

5. Olus Oil 45.5

6. Soybean Glycerides (and) Butyrospermum Parkii (Shea)

Butter Unsaponifiables

7. Polyglyceryl-3 Polyricinoleate 5.0

8. Beeswax 5.0

9. Petrolatum (and) Butyrospermum Parkii (Shea) Butter 35.0

10. Butyrospermum Parkii Butter Extract 0.5

11. Canola Oil 2.0

12. Olus Oil (and) Camelina Sativa Oil 5.0

13. Olus Oil 45.5 I NCI Name % wt/wt

14. Soybean Glycerides (and)

15. Butyrospermum Parkii 2.0

16. Butter Unsaponifiables

17. Polyglyceryl-3 Polyricinoleate 5.0

18. Beeswax 5.0

Combine all eighteen ingredients at 75°C. Cool mixture to 30°C while stirring. Fill into tubes.

Testing Examples Improved Skin Barrier Function (TEWL)

Ten female subjects, ages 36-58, were enrolled and completed a clinical study to evaluate the efficacy of topical product comprising the Dermatocosmetic Structured Glycidic / non-glycidic Matrix of the present invention in improving skin barrier function.

Transepidermal water loss (TEWL), a measure of skin barrier function, was measured using DermaLab Evaporimeter (Cortex Technology, Hadsund, Denmark). An absence of change in TEWL at post-treatment intervals compared to baseline is indicative that the treatment had not disturbed barrier function. A decrease in TEWL indicates an improvement in skin barrier function (i.e., less water is lost through the skin barrier).

For a "washout" period of at least three days prior to commencement of the study, subjects used a neutral soap bar for cleansing (i.e. bathing) the test sites - namely, the volar surface of forearms of their forearms. Subjects were instructed not to use of any personal care products (e.g., lotions, creams, cleansers) except for those provided by the test facility.

Subjects returned to the test site facility following the washout period. As instructed, subjects wore clothing that did not cover their forearms. The volar surface of the forearms were gently wiped with a damp disposable washcloth and patted dry with a paper towel by trained staff. Staff then marked four test sites on the volar surfaces of the forearms - two sites on one forearm; two sites on the other forearm. Each test site was 4cm X 4cm; adjacent test sites were separated by at least 3cm. Test sites were placed at least 2cm from the wrist joint and at least 2cm from elbow joint, and were identified as Test Sites 1-4. Designation of test vs. untreated (control) sites was random. Next, subjects equilibrated for first time for a minimum of thirty minutes in a room maintained at approximately 22 ±2°C and 40 ± 10% relative humidity. (Temperature and humidity was verified and recorded throughout the study - before and after equilibration, and before each TEWL measurement.)

Following equilibration, baseline TEWL readings were taken at each test site by trained staff using an Evaporimeter. Approximately 2 mg/cm² of the test product (the dermatocosmetic product according to Formulation Example 1) was then pipetted directly onto the sites and rubbed in gently using a fingercot. (The fingercot was examined after application to ensure that the majority of the test material does not adhere to the fingercot.) Subjects were sequestered at the testing facility for the remainder of the study visit.

During this time, subjects were instructed to keep their volar forearms uncovered/exposed and were not allowed to cover, wet or wipe the test sites.

At 3 hours and 30 minutes post-treatment (± 10 minutes), subjects equilibrated for a second time under the above conditions. Following equilibration (4 hours ± 10 minutes post treatment), TEWL readings were taken as described above. At 7 hours and 30 minutes post-treatment (± 10 minutes), subjects equilibrated for a third and final time. Following equilibration (8 hours ± 10 minutes post treatment), TWEL measurements were made. Subjects were dismissed after the 8 hour measurements had been completed.

Sites to which the test product was applied demonstrated statistically significantly better skin barrier function than the control untreated sites when compared to baseline after 4 hours.

Sensory Panel An eight person panel compared the MFSG/NGM of the present invention (25% interesterified, non-fractionated shea butter + 75% petrolatum) with (i) a blend of 25% RBD shea butter and 75% petrolatum and (ii) "neat" petrolatum. The same grade of petrolatum was used in all three products - namely White Protoline^® Petrolatum available from Sonneborn, LLC (Parsippany, NJ). The sensory evaluation was performed on the basis of spreadability, greasiness, cushion, tack, absorption, gloss, and graininess.

Ratings for each parameter were assessed based on a 5 -point system, with neat Protoline^® being assigned a score of "3".

75% Petrolatum + 75% Petrolatum +

Parameter Petrolatum 25% Interesterified, 25% RBD

NF Shea Butter Shea Butter

Spreadability 3.0 2.9 3.6

Greasiness 3.0 3.0 4.0

Cushion 3.0 3.3 3.3

Tack 3.0 3.0 3.1

Absorption 3.0 3.1 2.0

Gloss 3.0 3.2 3.9

Graininess 3.0 3.2 3.3

Average

Difference 0.0 .1 .314 Additional Skin Benefit Testing

Skin firmness is measured using the Cutometer^®. An increase in Cutometer^®

measurements is observed after using the dermatocosmetic product according to

Example 1, indicating improvement (increase) in skin firmness.

Skin flakiness is measured by using D-Squame® Skin Surface Sampling Discs (CuDerm Corporation, Dallas, TX). A clear adhesive disc is applied to clean, dry skin prior to step 2. The disc is pressed firmly to the skin for several seconds, then removed from the skin. Before and after D-Squame® scores are assigned based on the following scale: 1 = very slight flakiness; 2 = mild flakiness; 3 = moderate flakiness; 4 = marked flakiness; 5 = severe flakiness. A decrease in D-Squame^® score indicates an improvement (decrease) in flaky skin; an increase in D-Squame^® score represents worsening of flakiness. Skin firmness is measured using the Cutometer . An increase in Cutometer

measurements is observed after using the product of Example 1 indicating an

Subjects exhibiting signs of skin aging - uneven skin tone/texture (brown patches, erythema) and visible facial fine lines and wrinkles - are recruited to participate in a clinical study to assess the effectiveness of dermatocosmetic products according to the invention in improving the appearance of these signs of skin aging. Digital images of the face are taken before and after practicing the method of the present invention. The images are captured, processed and analyzed using the VISIA^® CR Imaging System (Canfield Scientific, Inc. Fairfield, NJ). Each image is scanned horizontally and vertically; the intensity of red, green and blue pixels are determined using the proprietary VISIA^® CR mathematical algorithms, and a texture score is assigned. The same algorithms calculate the number and depth of fine lines and wrinkles.

Decreases in texture score and the wrinkle/line count and depth are observed, representing an improvement in these skin aging parameters. Skin Barrier Function Testing

TEWL was measured using a TEWL Probe - a DermaLab^® Evaporimeter (Cortex Technology, Hadsund, Denmark). Decreases in TEWL indicate an improvement in skin barrier function, such that less water is lost through the skin barrier.

Subjects were arrived at the test facility three days prior to the scheduled start date, and were enrolled per inclusion and exclusion criteria. Subjects received a "neutral" soap bar (Neutrogena) to use for cleansing (i.e. bathing) their volar forearms (which would serve as the test sites) for a 3 -day washout period. Subjects were given specific instructions prohibiting use of all personal care products (e.g., lotions, creams, cleansers) on the test sites (volar forearms) for the entirety of the study, except for products provided by the test facility.

Following the washout period, subjects returned to the testing facility. Subjects were instructed to wear clothing that did not cover their volar forearms on the evaluation day. The surface of the volar forearms was gently wiped with a damp disposable washcloth and patted dry with a paper towel by trained staff. Staff then marked six (6) test sites on the volar surfaces of the forearms (three sites on each forearm). Each test site was 4 cm x 4 cm. Test sites were placed centrally on the volar forearms (at least 2c m from the wrist and at least 2 cm from elbow) and identified at Test Sites A-F. The treatment sites and control sites (untreated) were randomly assigned using a computer generated

randomization code. Measurements were made with the TEWL Probe within these test sites throughout the study period.

Prior to measurement, subjects underwent an equilibration prcess in which they remained quietly seated for a minimum of twenty (20) minutes in a room maintained at 20-24°C and 30-50% relative humidity. During this time, subjects were instructed to keep their volar forearms uncovered/exposed by resting their hands, palms up, on their thighs.

Packaging tape was applied to the tape-stripped treated sites and control (untreated) sites. TEWL readings (by Evaporimeter) were performed and repeat tape stripping were made on the test sites until a TEWL measurement greater than 20 g/m²/h was reached. Following baseline measurements (post-tape stripping), test products - MFSG/NGM of the present invention (identified in the table below as "SF£EA XP") and "neat petrolatum" - were each applied (pipetted) onto the designated test sites at a concentration of

2mg/cm², and rubbed into the skin by stagg using a fingercot until fully absorbed. (The fingercot was examined after application to ensure that the test material did not adhere to the fingercot. One site served as a control (untreated).

For the duration of a 12-hour study period, subjects were sequestered in a temperature and humidity controlled room at the testing. Subjects were instructed to keep their volar forearms uncovered/exposed. Subjects were not allowed to cover, wet or wipe their volar forearms until dismissed from the testing. No eating or drinking was allowed 30 minutes prior to a measurement being performed.

At 3 hours and 30 minutes post-treatment (± 10 minutes), subjects equilibrated by remaining quietly seated for a minimum of 20 minutes in a room maintained at approximately 20-24°C and 30-50% relative humidity. TEWL measurement were taken at 4 hours (± 10 min) post-treatment. At 7 hours and 30 minutes post-treatment (± 10 minutes), subjects again equilibrated by remaining quietly seated for a minimum of 20 minutes in a room maintained at approximately 20-24°C and 30-50% relative humidity. TEWL measurement were taken at 8 hours (± 10 min) post-treatment. At 11 hours and 30 minutes post-treatment (± 10 minutes), subjects equilibrated by remaining quietly seated for a minimum of 20 minutes in a room maintained at approximately 20-24°C and 30-50%) relative humidity. TEWL measurement were taken at 11 hours (± 10 min) post-treatment.

Following the measurements over an initial 12-hour period, subjects were dismissed from the testing facility and were instructed to return approximately 23 hours and 30 minutes (±30 minutes) post-application. Subjects were instructed not to wet (i.e., no showering, bathing or swimming) or apply products to their volar forearms until after the 24 hour measurements. At 23 hours and 30 minutes post-treatment (± 30 minutes), subjects equilibrated by remaining quietly seated for a minimum of 20 minutes in a room maintained at approximately 20-24°C and 30-50%> relative humidity. TEWL

measurement were taken at 24 hours (± 30 min) post-treatment. Subjects were dismissed after 24 hour post-treatment measurements were obtained.

There was a directional improvement in TEWL using Shea XP vs. neat petrolatum, ranging from 2.25% to 2.69%>, within an almost 3% directional improvement at 12 hours post-application.

Results of this study are presented in the table below:

BOLS valaes ifidkase s& ϊίϊ5¾ί,·ΐίί ssgHifi &acs (» S 0.85).

Analysis of Skin Barrier Function for Shea XP versus "Neat" Petrolatum

Note. Negative difference indicates Shea.XP site has be-tec skin i •airier iliac iio»

Claims

1. A topically-applied product comprising (i) at least one interesterified, non- fractionated triglyceride and (ii) at least one petrolatum, wherein the topically- applied product contains, on a weight/weight basis, at least 2% triglyceride and at least 6% petrolatum.

2. The topical product according to claim 1 which does not over time exhibit

graininess, bloom, discoloration, or separation, or change in viscosity.

3. The topically-applied product according to any of claims 1-2 wherein the slope of the solid fat content melting profile of the triglyceride from 20°C to 35°C is less than 1.

4. The topically-applied product according to any of claims 1 - 3 wherein the

interesterified, non-fractionated triglyceride is selected from the group consisting of Butyrospermum Parkii (Shea) Butter, Theobroma Cacao (Cocoa) Seed Butter, Shorea Stenoptera (Illipe) Seed Butter, Astrocaryum Murumuru Seed Butter, Theobroma Grandiflorum (Capuacu) Butter and Magnifera Indigo (Mango) Seed Butter.

5. The topically-applied product according to any of claims 1 - 4 comprising at least 30% petrolatum and at least one interesterified, non-fractionated triglyceride, wherein the ratio of the at least one interesterified, non-fractionated triglyceride to the at least one petrolatum is from 1 :39 to 7: 13.

6. The topically-applied product according to any of claims 1 - 5 wherein the ratio of the at least one interesterified, non-fractionated triglyceride to the at least one petrolatum is from 1 : 19 to 1 :3.

7. A multi-functional chemical ingredient used in the manufacture of cosmetic, personal care, and dermatologic products comprising (i) at least one

interesterified, non-fractionated triglyceride and (ii) at least one petrolatum.

8. The multi-functional chemical ingredient according to claim 7, wherein the ratio of the at least one interesterified, non-fractionated triglyceride to the at least one petrolatum is from 1 :39 to 7: 13.

9. The multi-functional chemical ingredient according to any of claims 7 or 8,

wherein the ratio of the at least one interesterified, non-fractionated triglyceride to the at least one petrolatum is from 1 : 19 to 1 :3

10. The multi-functional chemical ingredient according to any of claims 7 - 9

wherein the interesterified, non-fractionated triglyceride and is selected from the group consisting of Butyrospermum Parkii (Shea) Butter, Theobroma Cacao (Cocoa) Seed Butter, Shorea Stenoptera (Illipe) Seed Butter, Astrocaryum

Murumuru Seed Butter, Theobroma Grandiflorum (Capuacu) Butter and

Magnifera Indigo (Mango) Seed Butter.

11. The multi-functional chemical ingredient according to any of claims 7 - 10

wherein the interesterified, non-fractionated triglyceride is Butyrospermum Parkii (Shea) Butter.

12. A multi-functional chemical ingredient used in the manufacture of cosmetic, personal care, or dermatologic products consisting essentially of (i) at least one interesterified, non-fractionated triglyceride and (ii) at least one petrolatum.

13. A dermatocosmetic product comprising (i) at least one triglyceride and (ii) at least one petrolatum, wherein the dermatocosmetic product (a) contains, on a weight/weight basis, at least 2% triglyceride and at least 6% petrolatum and (b) does not exhibit graininess, bloom, discoloration, separation, or change in viscosity.

14. A topical product comprising (i) at least one interesterified, non-fractionated

triglyceride and (ii) at least one petrolatum and (iii) an optional active ingredient.

15. The product or ingredient of any of claims 1-14, which after application to the skin of at least 10 test subjects produces an improvement in skin barrier function, as measured by reduction in trans-epidermal water loss (TEWL), after 8 hours in at least 70% of the subjects.

16. The product or ingredient of any of claims 1-14, which after application to the skin of at least 10 test subjects produces an improvement in skin barrier function, as measured by reduction of TEWL, after 8 hours in at least 80% of the subjects.

17. The product or ingredient of any of claims 1-14, which after application to the skin of at least 10 test subjects produces an improvement in skin barrier function, as measured by reduction of TEWL, after 8 hours in at least 90% of the subjects.

18. The product or ingredient of any of claims 1-14 having a shea triterpene

concentration of at least about 10 ppm.

19. The product or ingredient of any of claims 1-14 having a shea triterpene

concentration of from about 100 ppm to about 10,000 ppm.

20. The product or ingredient of any of claims 1-14 having a shea triterpene

concentration of about from 300 ppm to about 3,000 ppm.

21. The product or ingredient of any of claims 1-14 having a shea triterpene

concentration of from about 5,000 ppm to about 10,000 ppm.

22. The product or ingredient of any of claims 1-14 having a shea triterpene

concentration of about 6,000 ppm to about 9,000 ppm.

23. The product or ingredient of any of claims 1-14 which produces an increase of at least 10%) in epidermal thickness in an ex vivo study.

24. The product or ingredient of any of claims 1-14 which produces an increase of at least 20%) in epidermal thickness in an ex vivo study.

25. The product or ingredient of any of claims 1-14 which produces an increase of at least 25% in epidermal thickness in an ex vivo study.

26. The product or ingredient of any of claims 1-14 which produces an increase in dermal collagen of at least 3% in an ex vivo study.

27. The product or ingredient of any of claims 1-14 which produces an increase of at least 5%> in dermal collagen in an ex vivo study.

28. The product or ingredient of any of claims 1-14 which produces an increase of at least 6%> in dermal collagen in an ex vivo study.

29. A product of any of claims 1-6 or 13-29 comprising from about 8% to about 80% of triglyceride and petrolatum.

30. The product of claim 30 in the form of a baby lotion, a diaper rash cream, a body balm, a face cream, a lip gloss or a lip butter.

31. The product of claim 31 which is a baby lotion and contains from from about 8% to about 15%) of triglyceride and petrolatum.

32. The product of claim 31 which is a diaper rash cream and contains from from about 40%) to about 60%> of triglyceride and petrolatum.

33. The product of claim 31 which is a body balm and contains from about 60%> to about 80%) of triglyceride and petrolatum.

34. The product of claim 31 which is a face cream and contains from from about 8%> to about 15%) of triglyceride and petrolatum.

35. The product of claim 31 which is a lip gloss and contains from about 20% to about 40% of triglyceride and petrolatum.

36. A topically-applied product comprising (i) at least one interesterified triglyceride having a final melting point above or significantly above body temperature and

(ii) at least one petrolatum, wherein the topically-applied product contains, on a weight/weight basis, at least 2% triglyceride and at least 6% petrolatum.