Skin barrier protection delivery system and method thereof

Abstract

The present disclosure relates to compositions and methods for treating topical skin conditions. Topically applied compositions and delivery systems are also provided. Methods of using the compositions and delivery systems in cosmetic, personal care, and dermatological applications are also provided. There is also provided a sprayable composition comprising Vaseline.

Description

[0001] Cross-references

[0002] This application claims the benefit of U.S. Provisional Application No. 63 / 333,768, filed on April 22, 2022, the contents of which are incorporated herein by reference in their entirety. 1. Technical Field

[0003] The present disclosure relates to topical application products and delivery systems for cosmetic, personal care and dermatological applications. Topically applied compositions and delivery systems are also provided. Methods of using the compositions and delivery systems in cosmetic, personal care and dermatological applications are further provided. Compositions in the form of sprayable gels are also provided. 2. Background technology

[0004] The skin is the largest organ of the body and protects mammals from both aqueous and dry environments. It is now generally accepted that the intercellular lamellar bilayer of stratum corneum lipids is a key component of a functional barrier. Maintaining a barrier that prevents excessive transepidermal water loss to the environment is essential for the survival of all terrestrial animals. Local or systemic perturbations of the epidermal barrier occur in a variety of skin and mucosal diseases and conditions. These perturbations not only have a significant effect on the morphology of skin lesions, but also activate certain skin diseases.

[0005] Active agents are used for skin treatment of various dermatological conditions, such as psoriasis, photoaging, age spots, skin aging due to intrinsic and extrinsic causes, skin wrinkles, acne, pigmentation and skin cancer. Active agents are usually prescription active agents and over-the-counter active agents. The solvent used in the dermatological formulation with skin treatment active agents can be a strong solvent, such as acetone; it can also be a gentle, i.e. mild solvent. However, it is understood that strong solvents can cause the effects of skin conditions that require additional treatments including damage to the skin barrier, and may interfere with the patient's compliance with the skin treatment regimen. On the other hand, mild solvents are known to be ineffective in the delivery of active agents in transdermal and dermal use. In addition, with the trend of extended use of dermatological preparations in current skin care products, the demand for local preparations of active agents for various skin treatments continues to exist.

[0006] Common moisturizers and emollients also lead to the destruction of barrier function. There is a need for an elegant, non-greasy, safe and effective topical composition that not only protects the skin barrier but also effectively and safely delivers other functional and / or pharmaceutical active ingredients to the skin.

[0007] The application of topical products by the user placing their hands or an inanimate applicator (brush, spatula, swab, sponge, puff) into a container can be unhygienic and may have potentially harmful health consequences. Even if "clean" (e.g., free of foreign contaminants or disease-carrying organisms), hands may contain microorganisms present in the skin microbiome. Applicators are typically not cleaned between uses and may become colonized with microorganisms.

[0008] There has been and remains a need for cosmetically elegant, non-greasy, sprayable compositions that apply a safe and effective concentration of at least 30% by weight of petrolatum and other ingredients in a manner that not only protects the skin barrier, but also effectively and safely delivers other functional and / or pharmaceutically active ingredients to the skin. The skin barrier protective delivery system of the present disclosure meets those needs. 3. Summary of the invention

[0009] One of the objects of the present disclosure is to provide a cost-effective composition, such as a smooth and non-sticky sprayable composition, which is easy to apply and hygienic. In one embodiment, the composition of the present invention increases water retention and improves skin roughness (moisturization), repairs and protects the skin from harmful conditions.

[0010] Certain skin care formulations of the present disclosure provide surprising, unexpected results. In certain embodiments, the disclosed delivery systems comprise certain components that provide additive or synergistic results.

[0011] The present disclosure provides compositions useful as skin moisturizers, skin softeners, skin debriding agents, and the like, as well as base compositions for cosmetic preparations, compositions for treatment, such as pharmacological preparations. In cosmetic preparations, the compositions may be used with additional ingredients that have only cosmetic effects. Alternatively, cosmetic preparations may contain ingredients that have both cosmetic and therapeutic effects, such as "cosmeceutical" ingredients.

[0012] In one embodiment, disclosed herein are compositions for correcting a defective epidermal barrier in a skin or mucosal disease or condition. The disclosed compositions and methods strengthen the barrier to prevent damage caused by environmental damage. The disclosed compositions can be used as moisturizers for softening and hydrating the epidermis and have a neutral effect on the barrier function, and in some cases improve the barrier function or increase its recovery rate.

[0013] Due to its effect on the epidermal barrier function, the disclosed compositions improve epidermal hyperproliferation and reduce inflammation. This results in significantly prolonged or complete remission and prevention of recurrence of skin diseases.

[0014] In certain embodiments, the skin barrier protection delivery system comprises sprayable vaseline, which can maintain a higher concentration of active ingredients without separation. It is unexpectedly found that the composition comprising at least about 30% vaseline by weight can be formulated into a spray. It is further unexpectedly found that the preparation with such a high concentration of vaseline in the present disclosure can be easily sprayed and effectively provide uniform coverage on the skin. In certain embodiments, the sprayable formulation does not include propellant gas as an additive, which may be harmful to the subject. In one embodiment, the composition forms a closed film on the skin.

[0015] In some embodiments, a skin barrier protection delivery system is provided comprising, and preferably consisting essentially of: coconut alkanes and / or coconut oil alcohol-caprylate / caprate, preferably a mixture of the two, more preferably a ratio of coconut alkanes to coconut oil alcohol-caprylate / caprate of about 3:1 to about 9:1, and (b) petrolatum at a concentration of at least about 30%; and the ratio of (a) to (b) is about 7:3 to about 1:3. In some embodiments, the skin barrier protection delivery system is sprayable.

[0016] Optionally, the skin barrier protection delivery system of the present disclosure comprises at least one, at least two, at least three, or at least four of ceramides, triglycerides, phytosterols, phytosterol esters, terpenes (e.g., squalene), plant-based esters or waxes (e.g., jojoba esters), tocopherols, and / or phospholipids.

[0017] Optionally, the skin barrier protection delivery system of the present disclosure includes at least one, at least two, at least three, or at least four of ceramides, phytosterols, squalene, plant-based esters or waxes (e.g., jojoba esters), and / or phospholipids.

[0018] In some embodiments, the skin barrier protection delivery system of the present disclosure comprises a mixture of coconut alkanes and coconut caprylate / caprate, petrolatum, ceramide NP, ceramide AP, jojoba esters, squalene, phytosterols, phytosteryl macadamiate, tocopherol, C18-C36 acid triglycerides, C12-18 acid triglycerides, sweet potato root extract, Acacia Senegal gum, a buffer (e.g., citric acid), and a sugar (e.g., maltodextrin).

[0019] In some embodiments, the skin barrier protection delivery system of the present disclosure comprises (i) at least 30 wt% of petrolatum; (ii) coconut alkanes in the range of 30-70 wt%; (iii) coconut oil alcohol-caprylate / caprate in the range of 3-7 wt%; (iv) ceramide NP in the range of 0.01-0.1 wt%; (v) ceramide AP in the range of 0.01-0.1 wt%; (vi) jojoba esters in the range of 0.1-1.5 wt%; (vii) squalene in the range of 0.1-1 wt%; (viii) phytosteryl macadamia oleate in the range of 0.01-0.1 wt%; (ix) phytosterols in the range of 0.005-0.1 wt%; (x) tocopherols in the range of 0.001-0.1 wt%; (xi) C18-36 acid triglycerides in the range of 0.5-5 wt%; (xii) C12-18 acid triglycerides in the range of 0.1-1 wt%; (xiii) sweet potato root extract in the range of 0.01-0.1 wt%; (xiv) citric acid in the range of 0.001-0.01 wt%; (xv) acacia gum in the range of 0.001-0.1 wt%; and (xvi) maltodextrin in the range of 0.001-0.1 wt%. In some embodiments, the delivery system is a sprayable formulation. In some embodiments, petrolatum is present in a concentration of 40 wt%. In some embodiments, petrolatum is present in a concentration of 50 wt%.

[0020] In some embodiments, the skin barrier protection delivery system of the present disclosure comprises (i) 50 wt% of petrolatum; (ii) 42-43 wt% of coconut alkanes; (iii) 4-5 wt% of coconut oil alcohol-caprylate / caprate; (iv) 0.05 wt% of ceramide NP; (v) 0.05 wt% of ceramide AP; (vi) 0.75 wt% of jojoba esters; (vii) 0.3-0.4 wt% of squalene; (viii) 0.05-0.06 wt% of phytosteryl macadamia oleate; (i x) 0.01-0.02 wt% of phytosterols; (x) 0.0045 wt% of tocopherol; (xi) 1-2 wt% of C18-36 acid triglycerides; (xii) 0.4-0.5 wt% of C12-18 acid triglycerides; (xiii) 0.03-0.04 wt% of sweet potato root extract; (xiv) 0.003-0.004 wt% of citric acid; (xv) 0.03-0.04 wt% of acacia gum; and (xvi) 0.03-0.04 wt% of maltodextrin. In some embodiments, the delivery system is a sprayable formulation.

[0021] In some embodiments, the skin barrier protection delivery system has a viscosity of about 500 cps to about 10,000 cps.

[0022] In some embodiments, an emulsion is provided that includes the skin barrier protection delivery system described herein.

[0023] In some embodiments, the present disclosure provides a pharmaceutical composition comprising a skin barrier protection delivery system as described herein. In some embodiments, the composition is sprayable.

[0024] In some embodiments, the present disclosure provides a pharmaceutical composition in the form of a sprayable gel comprising a skin barrier protection delivery system as described herein.

[0025] In some embodiments, the present disclosure provides a method for protecting the skin of a subject in need thereof, comprising applying a skin barrier protection delivery system as described herein, or a pharmaceutical composition comprising a skin barrier protection delivery system, to the skin of the subject.

[0026] In some embodiments, the present disclosure provides a method for preparing the skin barrier protection delivery system of any one of the preceding claims, comprising: (a) mixing petrolatum, coconut alkanes, and coconut oil alcohol-caprylate / caprate in a reactor to produce a mixture; (b) heating the mixture until a melt is obtained; and (c) cooling the mixture. 4. Specific implementation methods

[0027] Disclosed are stable, non-irritating formulations containing skin treatment active agents and delivery systems for topical application to the skin. The disclosed topical formulations and delivery systems provide controlled, gentle release of active agents into the skin for acceptable (amenable) treatment of skin disorders and improvement of aesthetic skin properties. Also provided are methods for preparing, manufacturing and using the disclosed formulations and delivery systems. Due to its high viscosity, petrolatum was not previously considered to be useful in non-aerosol (non-propellant-based) spray formulations intended to be dispensed by a manual spray pump dispenser. In addition, the percentage of petrolatum necessary to achieve skin protection benefits is too high; therefore, the use of petrolatum will clog the spray pump. The result will be a liquid or semisolid (e.g., gel) composition that cannot be sprayed at all or sprays inefficiently through the nozzle, and leaves very uneven coverage on the skin. If any formulation does contain petrolatum, the formulation does not contain enough petrolatum to provide the necessary skin protectant benefits. It has now been unexpectedly discovered that formulations such as those of the present disclosure having such high concentrations of petrolatum (e.g., 30% or more by weight) can be easily sprayed and effectively provide uniform coverage on the skin. In certain embodiments, the sprayable formulations do not contain a propellant gas as an additive that may be harmful to the subject.

[0028] In certain embodiments, the formulations disclosed herein: i) allow for a 10- to 50-fold reduction in the amount of the main ingredient used; ii) are thus environmentally friendly; iii) for the same or better therapeutic effect, the formulation leaves a silky, smooth feel on the skin, whereas the use of known formulations and pure petrolatum jelly results in a sticky, greasy, and messy feel; and iv) the formulation is a spray, which significantly provides: 1) increased ease of use (at home and in hospital & nursing home settings (e.g., one nurse vs. two nurses)) and 2) increased protection against cross-bacterial contamination (no finger-scraper required in the can). Sprayable formulations can be applied to the skin surface without touching or rubbing the skin surface. Thus, the risk of infection or contamination is reduced. In certain embodiments, the present invention provides a surprising discovery that compositions containing high concentrations of petrolatum (e.g., 30% or more by weight) in a sprayable form have improved sprayability compared to existing compositions containing petrolatum.

[0029] In some embodiments, a skin barrier protection delivery system is provided, which includes coconut alkane and / or coconut oil alcohol-caprylate / caprate, preferably a mixture of the two, more preferably a ratio of coconut alkane to coconut oil alcohol-caprylate / caprate of about 3:1 to about 9:1, and (b) petrolatum at a concentration of at least about 30%; and the ratio of (a) to (b) is about 7:3 to 1:3. In some embodiments, the skin barrier protection delivery system is sprayable.

[0030] In some embodiments, a skin barrier protection delivery system is provided, which consists essentially of: coconut alkanes and / or coconut oil alcohol-caprylate / caprate, preferably a mixture of the two, more preferably a ratio of coconut alkanes to coconut oil alcohol-caprylate / caprate of about 3:1 to about 9:1, and (b) petrolatum at a concentration of at least about 30%; and the ratio of (a) to (b) is about 7:3 to 1:3. In some embodiments, the skin barrier protection delivery system is sprayable.

[0031] In some embodiments of the skin barrier protection delivery system of the present disclosure, the ratio of (a) coconut alkanes and / or coconut caprylate / caprate, preferably a mixture of both, to (b) petrolatum is from about 2:1 to about 1:2.

[0032] In some embodiments of the skin barrier protection delivery system of the present disclosure, the ratio of (a) coconut alkanes and / or coconut caprylate / caprate, preferably a mixture of both, to (b) petrolatum is from about 3:2 to about 2:3.

[0033] In other embodiments of the skin barrier protection delivery system of the present disclosure, the ratio of (a) coconut alkanes and / or coconut oil alcohol-caprylate / caprate, preferably a mixture of the two, to (b) petrolatum is from about 5:4 to about 4:5, and even more preferably from about 10:9 to about 9:10, and most preferably about 1:1.

[0034] In these embodiments, the ratio of (i) coconut alkanes to (ii) coconut caprylate / caprate is from about 3:1 to about 9:1.

[0035] Vaseline

[0036] Petrolatum is a composition of hydrocarbons obtained in semisolid form from dewaxed paraffin residue oil. Petrolatum mainly includes saturated crystalline and liquid hydrocarbons, which mainly have carbon chain lengths of C25 and longer.

[0037] Petrolatum has a long history as a safe and effective topical agent for a wide range of topical applications including, but not limited to: moisturizing creams and lotions; makeup; hand and foot creams and lotions; skin protectants; wound care agents; lip balms and lipsticks; salves and liniments; baby care agents; hair care agents. In the pharmaceutical industry, petrolatum is a common base for medicinal analgesic creams, ointments and creams.

[0038] In 1983, the U.S. Food and Drug Administration approved petrolatum for inclusion in its final monograph for over-the-counter human skin protection drug products. In public comments published as part of the rulemaking process, FDA included the following rationale: "The use of petrolatum as an emollient has been well accepted for dry skin conditions, especially with flaking skin such as sunburn, and chapping," 43 Fed. Reg. 34628-34639. The FDA's assessment of the safety and effectiveness of topical petrolatum is further confirmed: "Petrolatum is not absorbed through intact or injured skin and isneither sensitizing nor irritating…Clinical and marketing experience has confirmed that petrolatum is safe in the OTC dosage range used as a skinprotectant," 43 Fed. Reg. at 33372.

[0039] Under U.S. law, cosmetic, personal care, and dermatological products containing more than 30% petrolatum make skin protection "labeling" claims - that is, the product temporarily protects injured or exposed skin or mucosal surfaces from harmful or annoying irritants and may help relieve such surfaces. More specifically, such products may claim to have the following benefits: Helps prevent (or temporarily protect; and optionally, helps relieve) chafed, chapped, or cracked skin.

[0040] Lip products containing petrolatum in concentrations deemed safe and effective by the FDA in its final Skin Protectant Monograph can claim benefits of temporarily preventing dryness and helping to reduce chapped lips on the exposed surfaces.

[0041] Skin and lip products containing more than 30% petrolatum may also claim to help protect the skin / lips from the drying effects of wind and cold weather.

[0042] Despite their long history of safety and effectiveness, petrolatum-based topical formulations are known to have certain limitations - they can be greasy and cosmetically inelegant.

[0043] Coconut Alkane and Coco-Caprylate / Caprate

[0044] Coconut alkanes are produced by reducing and hydrogenating a mixture of fatty acids derived from coconut oil. Different carbon chain lengths and distributions of different carbon chain lengths are commercially available, including products from Biosynthis Ltd. (Saint-Cyr-sous-Dourdan, France), ranging from C5-C14, including C8-C10, C9-C12 and C12-C14, and mixtures thereof. Coconut alkanes are described in U.S. pre-grant patent application publications Nos. 2012 / 0027702, 2017 / 0143610, 2018 / 0256479, 2019 / 0343753, 2019 / 0343753 and 2021 / 0154110, the disclosures of each of which are incorporated herein in their entirety in relevant parts.

[0045] Coco-caprylate / caprate (CAS#95912-86-0) is a mixture of coconut alcohol (a mixture of fatty alcohols derived from coconut oil) with esters of caprylic and capric acids. Non-limiting examples of commercially available coconut-caprylate / caprate esters include LC (BASF Corporation, Florham Park, NJ), Dub 810C (Stearinerie Dubois Fils, Boulogne Billancourt, France) and Lanol TM 2681 (Seppic, Paris, France).

[0046] Coconut alkanes and coconut oil caprylate / caprate mixtures are commercially available from specialty raw material manufacturers (and their distributors) including 1214 (from Biosynthis) and Vesgesil TM Coconut alkane and coconut oil-caprylate / caprate ratios may vary.

[0047] Other excipients

[0048] In some embodiments, the skin barrier protection delivery system of the present disclosure further comprises at least one of ceramide, triglyceride, phytosterol, phytosterol ester, terpene (e.g., squalene), plant-based ester or wax, tocopherol and / or phospholipid. In some embodiments, the skin barrier protection delivery system of the present disclosure comprises at least two of ceramide, triglyceride, phytosterol, phytosterol ester, terpene, plant-based ester or wax, tocopherol and / or phospholipid. In some embodiments, the skin barrier protection delivery system of the present disclosure comprises at least three of ceramide, triglyceride, phytosterol, phytosterol ester, terpene, plant-based ester or wax, tocopherol and / or phospholipid. In some embodiments, the skin barrier protection delivery system of the present disclosure comprises at least four of ceramide, triglyceride, phytosterol, phytosterol ester, terpene, plant-based ester or wax, tocopherol and / or phospholipid. In some embodiments, the skin barrier protection delivery system of the present disclosure comprises ceramide, triglyceride, phytosterol, phytosterol ester, terpene, plant-based ester or wax, tocopherol and / or phospholipid.

[0049] In some embodiments, the skin barrier protection delivery system of the present disclosure comprises plant-based esters or waxes. Plant oils, esters and waxes derived from plants, sterols, and esters of plant sterols and fatty acids (e.g., derived from plant seed oils) can be used in cosmetic, personal care, and dermatological products.

[0050] Plant oils, esters and waxes derived from plants, sterols, and esters of plant sterols and fatty acids (e.g., derived from plant seed oils) are widely used in cosmetic, personal care, and dermatological products. In some embodiments, the plant-based oil, ester, or wax comprises jojoba esters.

[0051] Simmondsia Chinensis (Jojoba) Seed Oil is a fixed oil expressed or extracted from the seeds of the desert shrub Simmondsia Chinensis (Jojoba).

[0052] Macadamia Seed Oil is a fixed oil obtained from the kernel of the macadamia nut.

[0053] Jojoba / Macadamia Seed Oil Esters (CAS#97593-46-9) are a mixture of esters formed by transesterification of jojoba seed oil and macadamia seed oil. In some embodiments, the skin barrier protection delivery system of the present disclosure comprises at least one ceramide, preferably at least two ceramides. Ceramides are a group of sphingolipids, comprising derivatives of sphingoid bases linked to various fatty acids with amide bonds. Together with other stratum corneum lipids, ceramides play a vital role in building and maintaining the barrier function of the skin. When at least one ceramide is present in the skin barrier protection delivery system of the present disclosure, the concentration range of the ceramide is preferably from about 0.05% to about 0.5%.

[0054] Preferably, ceramide is one or both of ceramide AP and / or ceramide NP. Ceramide AP is an N-acylated sphingolipid, which is composed of phytosphingosine with a D-erythro structure connected to α-hydroxy saturated or unsaturated fatty acids. Ceramide NP is an N-acylated sphingolipid, which is composed of phytosphingosine with a D-erythro structure connected to normal saturated or unsaturated fatty acids.

[0055] Many dermatological conditions and disorders in which the skin barrier function is impaired are characterized by reduced ceramide content. Topical formulations that provide lipids identical to or mimicking those in the skin have been reported to improve skin conditions. See, e.g., Coderch, L., López, O., de la Maza A., Parra J. "Ceramides and skin function" Am. J. Clin. Dermatol. 2003; 4(2): 107-29.

[0056] In some embodiments, the skin barrier protection delivery system of the present disclosure comprises at least one phytosterol. Phytosterol (C17H28O; CAS#949109-75-5) is a family of alcohols of steranes of tetracyclic hydrocarbons without double bonds derived from plants. More specifically, the hydrogen atom at position 3 of steranes is substituted by a hydroxyl group.

[0057] In some embodiments, the skin barrier protection delivery system of the present disclosure includes at least one terpene. In some embodiments, the terpene is squalene. Squalene (CAS#111-02-4) is an unsaturated branched isoprene hydrocarbon found in a variety of plant oils or by fermentation. When squalene is present, it is preferably included in the skin barrier protection delivery system of the present disclosure in a concentration of up to 5%, such as less than about 2%, at a concentration of less than about 1%, or at a concentration of less than about 0.5%.

[0058] In some embodiments, the skin barrier protection delivery system includes vitamin E or any form thereof, such as tocopherol. Vitamin E is a fat-soluble substance derived from plants, comprising a chromanol ring with a side chain at the C2 position. Tocopherol (CAS#10191-41-0) is a form of vitamin E, named α, β, γ and δ based on the number and position of methyl groups on the chromanol ring. Some embodiments of the skin barrier protection delivery system disclosed herein include at least one ceramide, at least two ceramides, at least one phytosterol and / or squalene.

[0059] Some implementations of the skin barrier protection delivery system of the present disclosure include at least one ceramide, at least two ceramides, at least one phytosterol, and squalene.

[0060] Each of the two embodiments described above may include one or a mixture of plant-derived esters.

[0061] Exemplary plant-derived esters include jojoba / macadamia seed oil esters and / or phytosteryl macadamia oleate. Phytosteryl macadamia oleate (CAS# 68990-51-2) is an ester of phytosterols with fatty acids from macadamia seed oil.

[0062] In some embodiments, the skin barrier protection delivery system of the present disclosure comprises jojoba / macadamia seed oil esters and phytosteryl macadamia oleate.

[0063] When present, the plant-based esters may be included in the skin barrier protection delivery system of the present disclosure alone or in combination with one or more plant oils or waxes at a combined concentration of up to about 20%, preferably up to about 15%, still more preferably up to about 10%, and even more preferably up to about 5%.

[0064] Various functional ingredients, including natural, plant-derived, and algae-derived ingredients as well as active pharmaceutical ingredients, may be incorporated into the skin barrier protection delivery system of the present disclosure.

[0065] Skin lipid content, especially triglycerides, wax esters, squalene, phospholipids, sterols and sterol esters, can and does vary with age. Cotterill, JA, WJ Cunliffe, B. Williamson, and L. Bulusu. "Age and Sex Variation in Skin Surface Lipid Composition and Sebum Excretion Rate." Br. J. Dermatol. (1972); 87: 333-40.

[0066] Designed to mimic the skin lipid profile found in "younger skin", (Flora Technologies, Ltd., Chandler, AZ) contains jojoba / macadamia esters, squalene, phytosteryl macadamia oleate, phytosterols, and tocopherols. The major components of L22 are jojoba / macadamia esters (about 85%) and squalene (12.5%). The combined concentration of phytosteryl macadamia oleate and phytosterols in L22 is about 2.5%.

[0067] The "active ingredients" may be incorporated into (i.e., contained in) the skin barrier protection delivery system of the present disclosure at a concentration range of about 0.001% to about 20% by weight, preferably about 0.005% to about 10%, more preferably about 0.01% to about 5%, even more preferably about 0.1% to about 2.0% by weight, and include: steroidal and nonsteroidal agents for treating inflammatory skin diseases (including acne, eczema, psoriasis, rosacea, and inflammatory skin diseases caused by radiation exposure); antimicrobial and antifungal active substances; antipruritic agents; local anesthetics; sunscreens; emollients and skin soothing agents; humectants and moisturizers, including hyaluronic acid; skin barrier protectants (such as the U.S. FDA OTC Final Monograph (FDA OTC Final Monograph) Monograph); lipids, including oils and butters derived from plants; antioxidants and agents that reduce the appearance of fine lines and wrinkles, including vitamins, proteins and peptides; skin bleaching and whitening agents; agents that aid in wound healing / wound beauty; agents that reduce inflammation (including erythema) and / or edema; active pharmaceutical ingredients (over-the-counter or prescription) that are used to prevent or treat (or aid in the prevention or treatment of) pathological conditions (e.g., diseases), including but not limited to ulcerative skin.

[0068] One non-limiting "active" ingredient included in the skin barrier protection delivery system of the present disclosure is sweet potato root extract, which, when applied according to the present disclosure, can be shown to reduce edema in the extremities.

[0069] The novel and essential feature of the disclosed embodiments of the skin barrier protection delivery system is that the skin barrier protection delivery system consists essentially of: (a) coconut alkanes and / or coconut caprylate / caprate, preferably a mixture of the two, more preferably a ratio of coconut alkanes to coconut caprylate / caprate of about 3:1 to about 9:1; and (b) petrolatum at a concentration of at least about 30%; and the ratio of (a) to (b) is from about 7:3 to about 1:3, and the skin barrier protection delivery system is sprayable.

[0070] The skin barrier protection delivery system of the present disclosure is preferably applied by spraying or atomization, and preferably has a viscosity (TE@10) of from about 500 cps to 10,000 cps. Devices that can be used for spraying or atomization are known to those of ordinary skill in the art, and include pump sprayers, trigger sprayers, atomizers, aerosol containers (pressurized with propellants, preferably non-fluorocarbon propellants, including valve bag dispensers).

[0071] The numbers used in describing quantities of ingredients are to be understood as modified in all instances by the term "about".

[0072] Unless otherwise indicated, percentages are understood to be based on the total weight of the skin barrier protection delivery system.

[0073] Numerical ranges are intended to include combinations of numbers within the recited ranges and sub-ranges between given ranges. For example, a range of 1-5 includes 1, 2, 3, 4, and 5, as well as sub-ranges such as 2-5, 3-5, 2-3, 2-4, 1-4, etc.

[0074] "At least one" means one or more and also includes single components as well as mixtures / combinations.

[0075] The following examples are for illustrative purposes only. Modifications will be apparent to those skilled in the art without departing from the spirit and scope of the present disclosure and can be readily made. The scope of the appended claims is not limited to these examples.

[0076] 5. Examples

[0077] Example 1 - Skin Protectant Spray

[0078] INCI name Wt% Wt% Wt% Snow White Vaseline USP 30.0 65.0 50.0 Coconut Alkane and Coco-Caprylate / Caprate 65.0 30.0 45.0-47.5 Ceramide 0.05-0.5 0.05-0.5 0.05-0.5 Jojoba / Macadamia Seed Oil Esters <5.0 <5.0 2.5 Squalene <2.0 <1.0 ﹤0.5 Phytosteryl Macadamia Oleate 0.01-0.1 0.01-0.1 0.01-0.1 Phytosterols 0.05-0.3 0.05-0.3 <0.2 Tocopherol 0.01-0.25 0.01-0.25 <0.05 Sweet Potato Root Extract 0.01-5 0.01-5 <0.1

[0079] Example 2 - Skin Protectant Spray

[0080]

[0081]

[0082] Example 3 - Skin Protectant Spray

[0083]

[0084] Example 4 - Skin Protectant Spray

[0085]

[0086]

[0087] Example 5 - Skin Protectant Spray

[0088]

[0089]

[0090] Example 6 - Skin Protectant Spray

[0091] INCI Name / Specific Wt% Minimum wt% Specific wt% Maximum wt% Snow White Vaseline USP 30.0 65.0 50.0 Coconut Alkane and Coco-Caprylate / Caprate 65.0 30.0 45.0-47.5 Ceramide 0.05-0.5 0.05-0.5 0.05-0.5 Jojoba / Macadamia Seed Oil Esters <5.0 <5.0 2.5 Squalene <2.0 <1.0 <0.5 Phytosteryl Macadamia Oleate 0.01-0.1 0.01-0.1 0.01-0.1 Phytosterols 0.05-0.3 0.05-0.3 <0.2 Tocopherol 0.01-0.25 0.01-0.25 <0.05 Sweet Potato Root Extract 0.01-5 0.01-5 <0.1

[0092] Example 7 - Skin Protectant Spray

[0093] INCI name / wt% range and specific examples Minimum Wt% Specific Wt% Max Wt% Snow White Vaseline USP 30 50.0 70 Coconut Alkane and Coco-Caprylate / Caprate 30 47.5 65 Ceramide 0.05 0.25 0.5 Jojoba / Macadamia Seed Oil Esters 0.1 0.75 1.5 Squalene 0.1 0.37 1 Phytosteryl Macadamia Oleate 0.01 0.063 0.1 Phytosterols 0.005 0.015 0.1 Tocopherol 0.001 0.0045 0.1 Sweet Potato Root Extract 0.01 0.033 0.1

[0094] Example 8 - Method of preparing the formulation

[0095] Weigh and measure individual ingredients and place in separate, clean, properly labeled, appropriately sized tare containers.

[0096] Step 1: Add Snow White Vaseline USP to a main reaction vessel equipped with a propeller stirrer. The power and temperature of the main reaction vessel are controlled by variable speed control. Heat Snow White Vaseline USP to 50°C-55°C under high speed stirring and maintain at this temperature.

[0097] Step 2: In a separate container, Vegesil and ceramide are mixed and heated to 85°C-90°C until homogeneous. After Vegesil and ceramide are melted and well mixed, slowly add the mixture to the main reaction vessel in step 1 and stir until homogeneous. The temperature is maintained at 50°C-55°C.

[0098] Step 3: In a separate container, mix L22 and Natpure Xfine Potato until uniform and keep at 50℃-55℃. Then slowly add the mixture to the main reaction vessel in step 1 and stir until uniform. Then remove the mixture in the main reaction vessel from the heat source and homogenize until Natpure Xfine Potato SP313 is evenly dispersed.

[0099] Step 4: Continue stirring the mixture in the main reaction vessel and cool the mixture to 35° C. Samples of the mixture are then tested and approved.

[0100] The following items list exemplary products, systems, and methods:

[0101] 1. A skin barrier protection delivery system comprising: (a) a mixture of coconut alkanes and coconut oil alcohol-caprylate / caprate and (b) petrolatum, wherein the petrolatum is present in a concentration of at least 30% and the ratio of (a) to (b) is 7:3 to 1:3.

[0102] 2. A skin barrier protection delivery system consisting essentially of: (a) a mixture of coconut alkanes and coconut oil caprylate / caprate and (b) petrolatum, wherein the petrolatum is present in a concentration of at least 30% and the ratio of (a) to (b) is from 7:3 to 1:3.

[0103] 3. The skin barrier protection delivery system of item 1 or 2, wherein the ratio of coconut alkane to coconut oil alcohol-caprylate / caprate is about 7:3 to about 1:3.

[0104] 4. The skin barrier protection delivery system of any one of items 1 to 3, further comprising at least one of ceramides, triglycerides, phytosterols, phytosterol esters, terpenes, plant-based esters or waxes, tocopherols and / or phospholipids.

[0105] 5. The skin barrier protection delivery system according to any one of items 1 to 4, further comprising at least one of ceramide, phytosterol, squalene, plant-based esters or waxes and / or phospholipids.

[0106] 6. The skin barrier protection delivery system according to any one of items 1 to 4, further comprising at least two of ceramide, phytosterol, squalene, plant-based esters or waxes and / or phospholipids.

[0107] 7. An emulsion comprising the skin barrier protection delivery system according to any one of items 1 to 6.

[0108] 8. The skin barrier protection delivery system of any one of items 1 to 7, which is sprayable.

[0109] 9. The skin barrier protection delivery system of any one of items 1 to 8, having a viscosity of about 500 cps to about 10,000 cps.

[0110] 10. A skin barrier protection delivery system comprising: a mixture of coconut alkanes and coconut oil alcohol-caprylate / caprate, petrolatum, ceramide NP, ceramide AP, jojoba esters, squalene, phytosterols, phytosteryl macadamia oleate, tocopherol, C18-C36 acid triglycerides, C12-18 acid triglycerides, sweet potato root extract, acacia gum, citric acid and maltodextrin.

[0111] 11. A skin barrier protection delivery system comprising (i) at least 30 wt % of petrolatum;

[0112] (i) at least 30 wt % of petrolatum;

[0113] (ii) coconut alkanes in the range of 30-70 wt %;

[0114] (iii) Coconut oil alcohol caprylate / caprate in the range of 3-7 wt%;

[0115] (iv) ceramide NPs in the range of 0.01-0.1 wt %;

[0116] (v) ceramide AP in the range of 0.01-0.1 wt %;

[0117] (vi) jojoba esters in the range of 0.1-1.5 wt %;

[0118] (vii) squalene in the range of 0.1-1 wt %;

[0119] (viii) phytosteryl macadamia oleate in the range of 0.01-0.1 wt %;

[0120] (ix) phytosterols in the range of 0.005-0.1 wt %;

[0121] (x) tocopherol in the range of 0.001-0.1 wt %;

[0122] (xi) C18-36 acid triglycerides in the range of 0.5-5 wt %;

[0123] (xii) C12-18 acid triglycerides in the range of 0.1-1 wt%;

[0124] (xiii) sweet potato root extract in the range of 0.01-0.1 wt %;

[0125] (xiv) citric acid in the range of 0.001-0.01 wt %;

[0126] (xv) acacia gum in the range of 0.001-0.1 wt %; and

[0127] (xvi) 0.001-0.1 wt% maltodextrin,

[0128] Wherein the delivery system is a sprayable formulation.

[0129] 12. The skin barrier protection delivery system of item 9, comprising:

[0130] (i) 50 wt% of petrolatum;

[0131] (ii) 42-43 wt% coconut alkanes;

[0132] (iii) 4-5 wt% of coconut oil caprylate / caprate;

[0133] (iv) 0.05 wt % ceramide NPs;

[0134] (v) 0.05 wt% ceramide AP;

[0135] (vi) 0.75 wt % jojoba esters;

[0136] (vii) 0.3-0.4 wt% squalene;

[0137] (viii) 0.05-0.06 wt % phytosteryl macadamia oleate;

[0138] (ix) 0.01-0.02 wt % of phytosterols;

[0139] (x) 0.0045 wt % tocopherol;

[0140] (xi) 1-2 wt% C18-36 acid triglyceride;

[0141] (xii) 0.4-0.5 wt% C12-18 acid triglyceride;

[0142] (xiii) 0.03-0.04 wt % of sweet potato root extract;

[0143] (xiv) 0.003-0.004 wt % citric acid;

[0144] (xv) 0.03-0.04 wt% acacia gum; and

[0145] (xvi) 0.03-0.04 wt% maltodextrin.

[0146] 13. A pharmaceutical composition comprising any one of the aforementioned skin barrier protection delivery systems.

[0147] 14. A pharmaceutical composition in the form of a sprayable gel, comprising any of the aforementioned skin barrier protection delivery systems.

[0148] 15. A method for protecting the skin of a subject in need thereof, comprising applying the skin barrier protection delivery system of any one of items 1 to 12, the pharmaceutical composition according to item 13 or 14 to the skin of the subject.

[0149] 16. A method for preparing any of the aforementioned skin barrier protection delivery systems, comprising: (a) mixing petrolatum, coconut alkanes and / or coconut oil alcohol-caprylate / caprate in a reactor to produce a mixture; (b) heating the mixture until a melt is obtained; and (c) cooling the mixture.

Claims

1. A skin barrier protection delivery system comprising: (a) a mixture of coconut alkane and coconut oil alcohol-caprylate / caprate and (b) vaseline, wherein: Petrolatum is present in a concentration of at least 30%, and the ratio of (a) to (b) is from 7:3 to 1:

3.

2. A skin barrier protection delivery system consisting essentially of: (a) a mixture of coconut alkanes and coconut caprylate / caprate and (b) petrolatum, wherein the petrolatum is present in a concentration of at least 30% and the ratio of (a) to (b) is from 7:3 to 1:

3.

3. The skin barrier protection delivery system according to claim 2, wherein: The ratio of the coconut alkanes to the coconut caprylate / caprate is from about 7:3 to about 1:

3.

4. The skin barrier protection delivery system according to any one of claims 1 to 3, further comprising at least one of ceramides, triglycerides, phytosterols, phytosterol esters, terpenes, plant-based esters or waxes, tocopherols and / or phospholipids.

5. The skin barrier protection delivery system according to any one of claims 1 to 4, further comprising at least one of ceramide, phytosterol, squalene, plant-based esters or waxes, and / or phospholipids.

6. The skin barrier protection delivery system according to any one of claims 1 to 4, further comprising at least two of ceramide, phytosterol, squalene, plant-based esters or waxes, and / or phospholipids.

7. An emulsion comprising the skin barrier protection delivery system according to any one of claims 1 to 6.

8. The skin barrier protection delivery system according to any one of claims 1 to 7, which is sprayable.

9. The skin barrier protection delivery system according to claim 1, having a viscosity of about 500 cps to about 10,000 cps.

10. A skin barrier protection delivery system comprising: a mixture of coconut alkanes and coconut oil alcohol-caprylate / caprate, petrolatum, ceramide NP, ceramide AP, jojoba esters, squalene, phytosterols, phytosteryl macadamia oleate, tocopherol, C18-C36 acid triglycerides, C12-18 acid triglycerides, sweet potato root extract, acacia gum, citric acid and maltodextrin.

11. A skin barrier protection delivery system comprising (i) at least 30 wt % of petrolatum; (i) at least 30 wt % of petrolatum; (ii) coconut alkanes in the range of 30-70 wt %; (iii) Coco-caprylate / caprate in the range of 3-7 wt %; (iv) ceramide NPs in the range of 0.01-0.1 wt %; (v) ceramide AP in the range of 0.01-0.1 wt %; (vi) jojoba esters in the range of 0.1-1.5 wt %; (vii) squalene in the range of 0.1-1 wt %; (viii) phytosteryl macadamia oleate in the range of 0.01-0.1 wt %; (ix) phytosterols in the range of 0.005-0.1 wt %; (x) tocopherol in the range of 0.001-0.1 wt %; (xi) C18-36 acid triglycerides in the range of 0.5-5 wt %; (xii) C12-18 acid triglycerides in the range of 0.1-1 wt%; (xiii) sweet potato root extract in the range of 0.01-0.1 wt %; (xiv) citric acid in the range of 0.001-0.01 wt %; (xv) acacia gum in the range of 0.001-0.1 wt %; and (xvi) 0.001-0.1 wt% maltodextrin, in, The delivery system is a sprayable formulation.

12. The skin barrier protection delivery system according to claim 9, comprising: (i) 50 wt% of petrolatum; (ii) 42-43 wt% coconut alkanes; (iii) 4-5 wt% of coconut oil caprylate / caprate; (iv) 0.05 wt % ceramide NPs; (v) 0.05 wt% ceramide AP; (vi) 0.75 wt % jojoba esters; (vii) 0.3-0.4 wt% squalene; (viii) 0.05-0.06 wt % phytosteryl macadamia oleate; (ix) 0.01-0.02 wt % of phytosterols; (x) 0.0045 wt % tocopherol; (xi) 1-2 wt% C18-36 acid triglyceride; (xii) 0.4-0.5 wt% C12-18 acid triglyceride; (xiii) 0.03-0.04 wt % of sweet potato root extract; (xiv) 0.003-0.004 wt % citric acid; (xv) 0.03-0.04 wt% acacia gum; and (xvi) 0.03-0.04 wt% maltodextrin.

13. A pharmaceutical composition comprising the skin barrier protection delivery system according to any one of the preceding claims.

14. A pharmaceutical composition in the form of a sprayable gel comprising the skin barrier protection delivery system according to any one of the preceding claims.

15. A method for protecting the skin of a subject in need thereof, comprising applying the skin barrier protection delivery system according to any one of claims 1 to 10, or the pharmaceutical composition according to claim 11 or 12 to the skin of the subject.

16. A method for preparing the skin barrier protection delivery system according to any one of the preceding claims, comprising: (a) mixing petrolatum, coconut alkanes and coconut caprylate / caprate in a reactor to produce a mixture; (b) heating the mixture until a melt is obtained; and (c) cooling the mixture.

Images