Skin barrier protection delivery system and method

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. Sprayable compositions comprising petrolatum are also provided.

Description

[Technical field]

[0001] cross reference This application claims the benefit of U.S. Provisional Application No. 63 / 333,768, filed April 22, 2022, the contents of which are incorporated herein by reference in their entirety.

[0002] 1. Field The present disclosure relates to topical products and delivery systems for use in cosmetics, personal care and dermatology applications. Topically applied compositions and delivery systems are also provided. Methods of using the compositions and delivery systems in cosmetics, personal care and dermatology applications are also provided. Compositions in the form of sprayable gels are also provided. [Background technology]

[0003] 2.Background Skin is the largest organ of the body and protects mammalian organisms from both aqueous and dry surrounding environments. It is now generally accepted that the intercellular lamellar bilayer sheet of stratum corneum lipids is a key component of the functional barrier. Maintenance of the barrier against excessive transepidermal water loss to the environment is important for the survival of all terrestrial animals. Local or systemic disturbances of the epidermal barrier occur in various diseases and conditions of the skin and mucous membranes. These disturbances not only contribute significantly to the morphology of skin lesions but also activate certain skin diseases.

[0004] Active agents are used in the skin treatment of various and diverse dermatological conditions, such as psoriasis, photoaging, age spots, aging appearance of the skin due to exogenous and endogenous causes, skin wrinkles, acne, hyperpigmentation and skin cancer. Active agents are typically prescription active agents and non-prescription active agents. The solvents used in dermatological formulations with skin treatment active agents can be strong solvents, such as acetone, or mild, i.e., weak solvents. However, strong solvents are known to cause effects of skin conditions that require additional treatment, including disruption of the skin barrier, and may prevent patient compliance with skin treatment regimens. On the other hand, mild solvents are known to be ineffective in the delivery of active agents in transdermal and dermal applications. Furthermore, due to the current trend of long-term use of dermatological formulations in skin care, there is a continuing need for topical formulations of active agents for various skin treatments.

[0005] Common moisturizers and emollients also cause a breakdown in barrier function. There has been and remains a need for cosmetically elegant, non-greasy, safe and effective topical compositions that not only protect the skin barrier but also effectively and safely deliver other functional and / or pharmacologic active ingredients to the skin.

[0006] Application of topical products by a user introducing their hands or inanimate applicators (brushes, spatulas, swabs, sponges, puffs) into a container can be unhygienic and have potentially adverse health consequences. Even when "clean" (e.g., free of exogenous contaminants or disease-carrying organisms), hands can contain microorganisms present in the skin microbiome. Applicators are often not cleaned between uses and can become colonized by microorganisms.

[0007] There has been a need for a cosmetically elegant, non-greasy, sprayable composition that applies a safe and effective concentration of at least 30% by weight of petrolatum and other ingredients to not only protect the skin barrier but also effectively and safely deliver other functional and / or pharma- ceutical active ingredients to the skin. These needs are met by the skin barrier protection delivery system of the present disclosure. Summary of the Invention

[0008] 3. Overview One of the objectives of the present disclosure is to provide a cost-effective composition, such as a smooth, non-sticky, sprayable composition, that is easy and hygienic to apply. In one embodiment, the composition increases water retention, improves skin roughness (moisturization), and repairs and protects the skin from harmful conditions.

[0009] Certain skin care formulations disclosed herein provide surprising and unexpected results. In certain embodiments, the disclosed delivery systems include certain ingredients that provide additive or synergistic results.

[0010] The present disclosure provides compositions useful as skin moisturizers, emollients, skin debridement agents, and the like, as well as base compositions for cosmetic formulations, and compositions for therapeutic, e.g., pharmacological, formulations. In cosmetic formulations, the compositions can be used with additional ingredients that are only cosmetic. Alternatively, cosmetic formulations can include ingredients that are both cosmetically and therapeutically active, e.g., "cosmeceutical" ingredients.

[0011] In one embodiment, disclosed herein is a composition that corrects defective epidermal barrier in skin or mucous membrane disease or condition.The disclosed compositions and methods strengthen the barrier to prevent its destruction by environmental insults.The disclosed compositions are useful as moisturizers for softening and hydrating the epidermis, and have a neutral effect on barrier function, and in certain cases improve barrier function or increase its recovery rate.

[0012] Through their effect on epidermal barrier function, the disclosed compositions improve epidermal hyperproliferation and reduce inflammation, resulting in significant long-term or complete remission and preventing recurrence of skin disorders.

[0013] In certain embodiments, the skin barrier protection delivery system comprises a sprayable petrolatum that retains a higher concentration of active ingredient without separation.Unexpectedly, it has been discovered that compositions that comprise at least about 30% by weight of petrolatum can be formulated as a spray.It has further been unexpectedly discovered that formulations with high concentrations of petrolatum as disclosed herein can be easily and efficiently sprayed to a uniform coverage on the skin.In certain embodiments, the sprayable formulation does not contain propellant gas as an additive that may be harmful to the subject.In one embodiment, the composition forms an occlusive film on the skin.

[0014] In some embodiments, there is provided a skin barrier protection delivery system that consists essentially of, and preferably consists of, (a) coconut alkane and / or coconut caprylate, preferably a mixture of the two (more preferably a ratio of coconut alkane to coconut caprylate / caprate of about 3:1 to about 9:1), and (b) petrolatum at a concentration of at least about 30%, wherein 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.

[0015] In some cases, 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 a ceramide, a triglyceride, a phytosterol, a phytosterol ester, a terpene (e.g., squalene), a plant-based ester or wax (e.g., jojoba esters), a tocopherol, and / or a phospholipid.

[0016] Optionally, the skin barrier protection delivery system of the present disclosure contains at least one, at least two, at least three, or at least four of a ceramide, a phytosterol, a squalene, a plant-based ester or wax (e.g., jojoba esters), and / or a phospholipid.

[0017] 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 (Ipomoea Batatas) root extract, Acacia Senegal gum, a buffering agent (e.g., citric acid), and a sugar (e.g., maltodextrin).

[0018] In some embodiments, the skin barrier protection delivery system of the present disclosure comprises: (i) at least 30% by weight petrolatum; (ii) coconut alkanes in the range of 30-70% by weight; (iii) coconut (caprylate / caprate) in the range of 3-7% by weight; (iv) ceramide NP in the range of 0.01-0.1% by weight; (v) ceramide AP in the range of 0.01-0.1% by weight; (vi) jojoba esters in the range of 0.1-1.5% by weight; and (vii) in the range of 0.1-1% by weight. (viii) squalene in the range of 0.01-0.1% by weight; (ix) phytosterols in the range of 0.005-0.1% by weight; (x) tocopherols in the range of 0.001-0.1% by weight; (xi) C18-36 acid triglycerides in the range of 0.5-5% by weight; (xii) C12-18 acid triglycerides in the range of 0.1-1% by weight; (xiii) sweet potato (Ipomoea Batatas) root extract in the range of 0.01-0.1% by weight; (xiv) citric acid in the range of 0.001-0.01% by weight; (xv) Acacia Senegal gum in the range of 0.001-0.1% by weight; and (xvi) maltodextrin in the range of 0.001-0.1% by weight. In some embodiments, the delivery system is a sprayable formulation. In some embodiments, the petrolatum is present in a concentration of 40% by weight. In some embodiments, the petrolatum is present in a concentration of 50% by weight.

[0019] In some embodiments, the skin barrier protection delivery system of the present disclosure comprises: (i) 50% by weight petrolatum; (ii) 42-43% by weight coconut alkane; (iii) 4-5% by weight coconut (caprylate / caprate); (iv) 0.05% by weight ceramide NP; (v) 0.05% by weight ceramide AP; (vi) 0.75% by weight jojoba esters; (vii) 0.3-0.4% by weight squalene. (viii) 0.05-0.06% by weight of phytosteryl macadamiate; (ix) 0.01-0.02% by weight of phytosterol; (x) 0.0045% by weight of tocopherol; (xi) 1-2% by weight of C18-36 acid triglyceride; (xii) 0.4-0.5% by weight of C12-18 acid triglyceride; (xiii) 0.03-0.04% by weight of Ipomoea Batatas root extract; (xiv) 0.003-0.004% by weight of citric acid; (xv) 0.03-0.04% by weight of Acacia Senegal gum; and (xvi) 0.03-0.04% by weight of maltodextrin. In some embodiments, the delivery system is a sprayable formulation.

[0020] In some embodiments, the skin barrier delivery system has a viscosity of about 500 cps to about 10,000 cps.

[0021] In some embodiments, an emulsion is provided comprising the skin barrier protection delivery system described herein.

[0022] In some embodiments, the present disclosure provides a pharmaceutical composition comprising the skin barrier protection delivery system described herein. In some embodiments, the composition is sprayable.

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

[0024] In some embodiments, the present disclosure provides a method of protecting the skin of a subject in need thereof, comprising administering to the skin of the subject a skin barrier protection delivery system described herein, or a pharmaceutical composition comprising a skin barrier protection delivery system.

[0025] In some embodiments, the present disclosure provides a method of making the skin barrier protection delivery system of any one of the preceding claims, comprising: (a) mixing petrolatum, coconut alkane 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. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0026] 4. Detailed Description Stable, non-irritating skin treatment active agent containing formulations and delivery systems for topical application to the skin are disclosed. The disclosed topical formulations and delivery systems provide controlled, gentle release of active agents to the skin for the treatment of applicable skin conditions as well as for the improvement of aesthetic skin properties. Methods for formulating, manufacturing, and using the disclosed formulations and delivery systems are also provided. Petrolatum is not known to have been previously utilized in non-aerosol (non-propellant-based) spray formulations intended to be dispensed via manual spray pump dispensers due to the high viscosity of petrolatum. Furthermore, the percentage of petrolatum required to achieve a skin protection effect is too high, and thus the use of petrolatum can clog the spray pump. This results in liquid or semi-solid (e.g., gel) compositions that either do not spray at all or spray inefficiently by sputtering through the orifice, leaving a very uneven coating on the skin. When the formulation includes petrolatum, the formulation does not include a sufficient amount of petrolatum to provide the necessary skin protection benefit. It has been unexpectedly discovered that formulations containing high concentrations of petrolatum (e.g., 30% by weight or more) as disclosed herein can be easily and efficiently sprayed to a uniform coverage on the skin. In certain embodiments, the sprayable formulations do not contain propellant gases as additives that may be harmful to the subject.

[0027] In certain embodiments, the formulations disclosed herein i) allow for a 10-50 fold reduction in the use of key ingredients, ii) are therefore better for the environment, iii) the formulations leave a smooth, silky feeling on the skin compared to the sticky, greasy, messy feeling obtained with known formulations and pure petrolatum with the same or better therapeutic efficacy, and iv) the formulations are sprayable, providing significantly: 1) improved ease of use (at home as well as hospital and care home environments (e.g., one nurse vs. two nurses), and 2) improved protection against cross-bacteriological contamination (no fingers-spatula in the jar). The sprayable formulations can be applied to the skin surface without the need to touch or rub the skin surface. Thus, the risk of infection or contamination is reduced. In certain embodiments, provided herein is the surprising discovery of a composition comprising a high percentage of petrolatum (e.g., 30% by weight or more) in a sprayable form having improved sprayability compared to existing compositions comprising petrolatum.

[0028] In some embodiments, there is provided a skin barrier protection delivery system comprising coconut alkane and / or coconut (caprylate / caprate), preferably a mixture of the two (more preferably a ratio of coconut alkane to coconut (caprylate / caprate) of about 3:1 to about 9:1), and (b) petrolatum at a concentration of at least about 30%, wherein 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.

[0029] In some embodiments, there is provided a skin barrier protection delivery system consisting essentially of coconut alkane and / or coconut (caprylate / caprate), preferably a mixture of the two (more preferably a ratio of coconut alkane to coconut (caprylate / caprate) of about 3:1 to about 9:1), and (b) petrolatum at a concentration of at least about 30%, wherein 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.

[0030] In some embodiments of the skin barrier protection delivery system of the present disclosure, the ratio of (a) coconut alkane and / or coconut (caprylate / caprate), preferably a mixture of the two, to (b) petrolatum is from about 2:1 to about 1:2.

[0031] In another embodiment of the skin barrier protection delivery system of the present disclosure, the ratio of (a) coconut alkane and / or coconut (caprylate / caprate), preferably a mixture of the two, to (b) petrolatum is from about 3:2 to about 2:3.

[0032] In yet another embodiment of the skin barrier protection delivery system of the present disclosure, the ratio of (a) coconut alkane and / or coconut (caprylate / caprate), preferably a mixture of the two, to (b) petrolatum is from about 5:4 to about 4:5, even more preferably from about 10:9 to about 9:10, and most preferably about 1:1.

[0033] In these embodiments, the ratio of (i) coconut alkane to (ii) coconut alkyl (caprylate / caprate) is from about 3:1 to about 9:1.

[0034] Vaseline Petrolatum is a combination of hydrocarbons obtained as a semi-solid from dewaxed paraffinic residual oils. It consists primarily of saturated crystalline and liquid hydrocarbons with carbon chain lengths of C25 and above.

[0035] Petrolatum has a long history as a safe and effective topical agent suitable for use in 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, lip balms and lipsticks, salves and synthetic rubbers, baby care, and hair care. In medicine, petrolatum is commonly used in the formulation of medicated pain balms, ointments, and creams.

[0036] In 1983, the U.S. Food and Drug Administration approved the inclusion of petrolatum in the Final Monograph on Skin Protectant Drug Products for Over-the-Counter Human Use. In public comments published as part of the rulemaking process, FDA included the following rationale: "The use of petrolatum as an emollient is well accepted for dry skin conditions, particularly peeling and cracking skin such as sunburn." 43 Federal Register (Fed.Reg.) 34628 at 34639. FDA's evaluation of the safety and effectiveness of petrolatum in topical applications was further justified: "Petrolatum is not absorbed through intact or damaged skin and is not sensitizing or irritating.... Clinical and marketing experience confirms that petrolatum is safe in the OTC dose ranges in which it is used as a skin protectant." 43 Fed.Reg.at 33372.

[0037] Under U.S. law, cosmetic, personal care, and dermatological products that contain more than 30% petrolatum may claim a skin protectant "label," i.e., that the product can temporarily protect damaged or exposed skin or mucosal surfaces from harmful or unpleasant irritation and help relieve such surfaces. More specifically, such products may claim as a benefit that they help prevent (or temporarily protect, and possibly help relieve) chafing, chapped, or cracked skin.

[0038] Lip products containing petrolatum in concentrations recognized as safe and effective by the FDA in its final Skin Protectant Monograph can claim as a benefit that they temporarily prevent dryness and help reduce cracking of the exposed surfaces of the lips.

[0039] Both skin and lip products containing more than 30% petrolatum can also claim to help protect the skin / lips from the drying effects of wind and cold weather.

[0040] Despite their long history of safety and effectiveness, petrolatum-based topical formulations are known to have certain limitations: they can be oily and cosmetically inelegant.

[0041] Coconut Alkanes and Coconut Alkyl (Caprylate / Caprate) Palm alkanes are produced by reduction and hydrogenation of a mixture of fatty acids derived from palm oil. Different carbon chain lengths and distributions of different carbon chain lengths ranging from C5 to C14, including C8 to C10, C9 to C12, and C12 to C14, as well as mixtures thereof, are commercially available, including from Biosynthis Ltd. (Saint-Cyr-sous-Dourdan France). Palm alkanes are described in U.S. Pregrant Patent Application Publication Nos. 2012 / 0027702, 2017 / 0143610, 2018 / 0256479, 2019 / 0343753, 2019 / 0343753, and 2021 / 0154110, the disclosures of each of which are incorporated in their entirety in relevant part.

[0042] Coco-caprylate / caprate (CAS number 95912-86-0) is a mixture of coconut alcohol (a mixture of fatty alcohols derived from coconut oil) with caprylic and capric acids. Non-limiting examples of commercially available coco-caprylate / caprate include Cetiol® LC (BASF Corporation, Florham Park, NJ), Dub 810 C (Stearinerie Dubois Fils, Boulogne Billancourt, France), and Lanol™ 2681 (Seppic, Paris, France).

[0043] Mixtures of coconut alkanes and coconut caprylates / caprates are commercially available from specialty ingredient manufacturers (and distributors) including under the trade names Vegelight® 1214 (Biosynthis) and Vegesil™ 345 (Global Ingredient Solutions, Irvine, Calif.). The ratio of coconut alkanes to coconut caprylates / caprates can vary.

[0044] Other excipients In some embodiments, the skin barrier protection delivery system of the present disclosure further comprises at least one of ceramides, triglycerides, phytosterols, phytosterol esters, terpenes (e.g., squalene), plant-based esters or waxes, tocopherols, and / or phospholipids. In some embodiments, the skin barrier protection delivery system of the present disclosure comprises at least two of ceramides, triglycerides, phytosterols, phytosterol esters, terpenes, plant-based esters or waxes, tocopherols, and / or phospholipids. In some embodiments, the skin barrier protection delivery system of the present disclosure comprises at least three of ceramides, triglycerides, phytosterols, phytosterol esters, terpenes, plant-based esters or waxes, tocopherols, and / or phospholipids. In some embodiments, the skin barrier protection delivery system of the present disclosure comprises at least four of ceramides, triglycerides, phytosterols, phytosterol esters, terpenes, plant-based esters or waxes, tocopherols, and / or phospholipids. In some embodiments, the skin barrier protection delivery system of the present disclosure comprises ceramides, triglycerides, phytosterols, phytosterol esters, terpenes, plant-based esters or waxes, tocopherols, and / or phospholipids.

[0045] In some embodiments, the skin barrier protection delivery system of the present disclosure comprises a plant-based ester or wax. Vegetable oils, plant-derived esters and waxes, sterols, and phytosterols and esters of fatty acids (e.g., derived from plant seed oils) can be used in cosmetic, personal care, and dermatological products.

[0046] Vegetable oils, plant-derived esters and waxes, sterols, and phytosterols and esters of fatty acids (e.g., derived from plant seed oils) are widely used in cosmetics, personal care, and dermatology products. In some embodiments, the plant-based oil, ester, or wax comprises jojoba esters.

[0047] Simmondsia Chinensis (Jojoba) Seed Oil is a fixed oil expressed or extracted from the seeds of the desert shrub, jojoba, Simmondsia chinensis.

[0048] Macadamia (Macadamia Integrifolia) seed oil is a fixed oil obtained from the nuts of the macadamia (Macadamia Integrifolia) tree.

[0049] Jojoba Oil / Macadamia Seed Oil Esters (CAS No. 97593-46-9) is a mixture of esters formed by transesterification of jojoba seed oil and Macadamia (Macadamia Integrifolia) seed oil. In some embodiments, the skin barrier protection delivery system of the present disclosure includes at least one ceramide, preferably at least two ceramides. Ceramides are a group of sphingolipids that contain derivatives of sphingosine bases amide-linked to various fatty acids. Ceramides, along with other stratum corneum lipids, play an essential role in building and maintaining the barrier function of the skin. When present, at least one ceramide is included in the skin barrier protection delivery system of the present disclosure, preferably at a concentration ranging from about 0.05% to about 0.5%.

[0050] Preferably, the ceramide is one or both of ceramide AP and / or ceramide NP. Ceramide AP is an N-acylated sphingolipid consisting of phytosphingosine having a D-erythro structure bound to an α-hydroxy saturated or unsaturated fatty acid. Ceramide NP is an N-acylated sphingolipid consisting of phytosphingosine having a D-erythro structure bound to a normal saturated or unsaturated fatty acid.

[0051] Many dermatological conditions and disorders with impaired skin barrier function are characterized by reduced ceramide content. Topical formulations that deliver lipids that are identical to or mimic those in the skin have been reported to improve skin condition.See, for example, Coderch, L., Lopez, O., de la Maza A., Parra J. "Ceramides and skin function" Am.J.Clin.Dermatol.2003;4(2):107-29.

[0052] In some embodiments, the skin barrier protection delivery system of the present disclosure comprises at least one phytosterol. Phytosterol (C 17 H 28 O; CAS number 949109-75-5) is a family of plant-derived alcohols of the gonanes, which are tetracyclic hydrocarbons with no double bonds. More specifically, the hydrogen atom at the 3-position of the gonanes is replaced by a hydroxyl group.

[0053] In some embodiments, the skin barrier protection delivery system of the present disclosure comprises at least one terpene. In some embodiments, the terpene is squalene. Squalene (CAS number 111-02-4) is an unsaturated branched isoprenoid hydrocarbon found in various vegetable oils or derived by fermentation. When present, squalene is preferably included in the skin barrier protection delivery system of the present disclosure at a concentration of up to 5%, for example, at a concentration of less than about 2%, at a concentration of less than about 1%, or at a concentration of less than about 0.5%.

[0054] In some embodiments, the skin barrier protection delivery system comprises vitamin E or any of its forms, such as tocopherol. Vitamin E is a fat-soluble substance derived from plants that is composed of a chromanol ring with a side chain located at the C2 position. Tocopherol (CAS number 10191-41-0) is a form of vitamin E called alpha, beta, gamma, and delta based on the number and position of the methyl groups on the chromanol ring. Some embodiments of the skin barrier protection delivery system of the present disclosure comprise at least one ceramide, at least two ceramides, at least one phytosterol, and / or squalene.

[0055] Some embodiments 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.

[0056] Each of the above embodiments may include one or a mixture of plant-derived esters.

[0057] Exemplary plant-derived esters include jojoba oil / macadamia seed oil esters and / or phytosteryl macadamiate. Phytosteryl macadamiate (CAS number 68990-51-2) is an ester of phytosterol and fatty acids derived from macadamia (Macadamia Integrifolia) seed oil.

[0058] In some embodiments, the skin barrier protection delivery system of the present disclosure comprises jojoba oil / macadamia seed oil esters and phytosteryl macadamiate.

[0059] When present, vegetable-based esters are included in the skin barrier protection delivery system of the present disclosure either alone or in combination with one or more vegetable oils or waxes at a total concentration of up to about 20%, preferably up to about 15%, even more preferably up to about 10%, and even more preferably up to about 5%.

[0060] A variety of functional ingredients can be incorporated into the skin barrier protection delivery system of the present disclosure, including natural, plant and algae derived ingredients, as well as active pharmaceutical ingredients.

[0061] Skin lipid content - particularly 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.

[0062] Designed to mimic the skin lipid distribution of "younger skin," L22® (Flora Technologies, Ltd., Chandler, AZ) is composed of jojoba oil / macadamia seed oil esters, squalene, phytosteryl macadamiate, phytosterols and tocopherols. The main components of L22 are jojoba oil / macadamia seed oil esters (approximately 85%) and squalene (12.5%). Phytosteryl macadamiate and phytosterols are present in L22 at a combined concentration of approximately 2.5%.

[0063] The "active ingredients" may be incorporated (i.e., included) in the skin barrier protection delivery system of the present disclosure at a concentration ranging from about 0.001% to about 20% by weight, preferably from about 0.005% to about 10% by weight, more preferably from about 0.01% to about 5% by weight, and even more preferably from about 0.1% to about 2.0% by weight, and include agents for the treatment of inflammatory skin conditions (including acne, eczema, psoriasis, rosacea, and those due to radiation exposure), both steroidal and non-steroidal; antibacterial and antifungal actives; anti-itch agents; topical anesthetics; sunscreens; emollients and skin soothing agents; humectants and moisturizers, including hyaluronic acid; skin barrier protectors (USFDA OTC Final as defined in Monograph); lipids, including oils and butters of vegetable origin; antioxidants and agents that reduce the appearance of fine lines and wrinkles, including vitamins, proteins and peptides; skin bleaching and lightening agents; agents that contribute to wound healing / wound cosmetology; agents that reduce inflammation (including erythema) and / or edema; active pharmaceutical ingredients (over-the-counter or prescription) that prevent or treat (or aid in the prevention or treatment of) pathophysiological conditions (e.g., diseases), including but not limited to ulcerated skin.

[0064] One non-limiting "active" ingredient included in the skin barrier protection delivery system of the present disclosure is sweet potato (Ipomoea Batatas) root extract, which has been shown to reduce extremity edema when applied in accordance with the present disclosure.

[0065] A novel and essential feature of an embodiment of the present disclosure relates to a skin barrier protection delivery system consisting essentially of (a) coconut alkane and / or coconut (caprylate / caprate), preferably a mixture of the two (more preferably a ratio of coconut alkane to coconut (caprylate / caprate) of about 3:1 to about 9:1), and (b) petrolatum at a concentration of at least about 30%, wherein the ratio of (a) to (b) is about 7:3 to about 1:3, and the skin barrier protection delivery system is sprayable.

[0066] The skin barrier protection delivery system of the present disclosure is preferably applied by spray or mist and preferably has a viscosity (TE@10) of about 500 cps to 10,000 cps. Devices that can be used to spray or mist are known to those skilled in the art and include pump sprays, trigger sprays, atomizers, aerosol containers (pressurized with a propellant, preferably a non-fluorocarbon propellant, including bag-on-valve dispensers).

[0067] The numbers used in describing amounts of ingredients should be understood to be modified in all instances by the term "about."

[0068] Unless otherwise indicated, percentages should be understood to be based on the total weight of the skin barrier protection delivery system.

[0069] Numeric ranges are meant to include the numbers within the recited ranges, as well as combinations of subranges between the given ranges, for example, the range 1 to 5 includes 1, 2, 3, 4, and 5, as well as subranges 2 to 5, 3 to 5, 2 to 3, 2 to 4, 1 to 4, etc.

[0070] "At least one" means one or more and is inclusive of individual components as well as mixtures / combinations.

[0071] The following examples are illustrative. Modifications will be apparent to and can be readily made by those skilled in the art without departing from the spirit and scope of the present disclosure. The scope of the appended claims is not limited to the examples. EXAMPLES

[0072] 5. Working Example Example 1 - Skin Protectant Spray

[0073] [Table 1]

[0074] Example 2 - Skin Protectant Spray

[0075] [Table 2]

[0076] Example 3 - Skin Protectant Spray

[0077] [Table 3]

[0078] Example 4 - Skin Protectant Spray

[0079] [Table 4]

[0080] Example 5 - Skin Protectant Spray

[0081] [Table 5]

[0082] Example 6 - Skin Protectant Spray

[0083] [Table 6]

[0084] Example 7 - Skin Protectant Spray

[0085] [Table 7]

[0086] Example 8 - Method of preparation of formulation Each ingredient was weighed, measured and placed into separate, clean, properly identified and appropriately sized tared containers.

[0087] Step 1: Snow White Petrolatum USP was added to a main reactor vessel equipped with a propeller mixer. The power and temperature of the main reactor vessel were controlled with a variable speed control. The Snow White Petrolatum USP was mixed at high speed and heated to 50°C-55°C and maintained at this temperature.

[0088] Step 2: In a separate vessel, Vegesil and Ceramide were mixed and heated to 85°C-90°C until uniform. After Vegesil and Ceramide were melted and thoroughly combined, the mixture was slowly added to the main reactor vessel from Step 1 and mixed until uniform. The temperature was maintained at 50°C-55°C.

[0089] Step 3: In a separate vessel, L22 and Natpure Xfine Potato were mixed until uniform and maintained at 50° C.-55° C. The mixture was then slowly added to the main reactor vessel from step 1 and mixed until uniform. The mixture in the main reactor vessel was then removed from the heat and homogenized until the Natpure Xfine Potato SP313 was evenly dispersed.

[0090] Step 4: Continue mixing the mixture in the main reactor vessel and cool the mixture to 35° C. A sample of the mixture was then tested and approved.

[0091] Exemplary products, systems, and methods are described in the following sections: 1. A skin barrier protection delivery system comprising (a) a mixture of coconut alkanes and coconut alkyl (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 between 7:3 and 1:3. 2. A skin barrier protection delivery system consisting essentially of (a) a mixture of coconut alkanes and coconut alkyl (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 between 7:3 and 1:3. 3. The skin barrier protection delivery system according to item 1 or 2, wherein the ratio of coconut alkane to coconut alkyl (caprylate / caprate) is from about 7:3 to about 1:3. 4. The skin barrier protection delivery system according to 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. 5. The skin barrier protection delivery system according to any one of items 1 to 4, further comprising at least one of ceramides, phytosterols, squalene, plant-based esters or waxes, and / or phospholipids. 6. The skin barrier protection delivery system according to any one of items 1 to 4, further comprising at least two of ceramides, phytosterols, squalene, plant-based esters or waxes, and / or phospholipids. 7. An emulsion comprising the skin barrier protection delivery system according to any one of items 1 to 6. 8. The skin barrier protection delivery system according to any one of items 1 to 7, which is sprayable. 9. The skin barrier protection delivery system according to any one of items 1 to 8, having a viscosity of about 500 cps to about 10,000 cps. 10. Skin Barrier Protection Delivery System containing a blend of Coco Alkanes and Coco-Caprylate / Caprate, Petrolatum, Ceramide NP, Ceramide AP, Jojoba Esters, Squalene, Phytosterols, Macadamia Nut Phytosteryl Fatty Acid, Tocopherol, C18-C36 Acid Triglycerides, C12-18 Acid Triglycerides, Ipomoea Batatas Root Extract, Acacia Senegal Gum, Citric Acid, and Maltodextrin. 11. (i) at least 30% by weight petrolatum; (i) at least 30% by weight petrolatum; (ii) palm alkanes in the range of 30-70 wt.%; (iii) coco-alkyl (caprylate / caprate) in the range of 3-7% by weight; (iv) ceramide NPs in the range of 0.01–0.1 wt %; (v) ceramide AP in the range of 0.01 to 0.1 wt %; (vi) jojoba esters in the range of 0.1 to 1.5% by weight; (vii) squalene in the range of 0.1 to 1% by weight; (viii) phytosteryl macadamiate in the range of 0.01 to 0.1% by weight; (ix) phytosterols in the range of 0.005 to 0.1% by weight; (x) tocopherol in the range of 0.001 to 0.1% by weight; (xi) C18-36 acid triglycerides in the range of 0.5-5% by weight; (xii) C12-18 acid triglycerides in the range of 0.1-1 wt.%; (xiii) sweet potato (Ipomoea Batatas) root extract in the range of 0.01 to 0.1% by weight; (xiv) citric acid in the range of 0.001 to 0.01% by weight; (xv) Acacia Senegal gum in the range of 0.001 to 0.1% by weight; and (xvi) Maltodextrin in the range of 0.001 to 0.1% by weight A skin barrier protection delivery system comprising: A skin barrier protection delivery system, wherein the delivery system is a sprayable formulation. 12. (i) 50% by weight petrolatum; (ii) 42-43 wt.% palm alkanes; (iii) 4 to 5% by weight of coco-(caprylate / caprate); (iv) 0.05 wt % ceramide NPs; (v) 0.05 wt % ceramide AP; (vi) 0.75% by weight of jojoba esters; (vii) 0.3 to 0.4% by weight of squalene; (viii) 0.05 to 0.06% by weight of phytosteryl macadamiate; (ix) 0.01 to 0.02% by weight of phytosterols; (x) 0.0045% by weight of tocopherol; (xi) 1-2% by weight of C18-36 acid triglyceride; (xii) 0.4 to 0.5% by weight of a C12-18 acid triglyceride; (xiii) 0.03 to 0.04% by weight of sweet potato (Ipomoea Batatas) root extract; (xiv) 0.003 to 0.004% by weight of citric acid; (xv) 0.03 to 0.04 percent by weight of Acacia Senegal gum; and (xvi) 0.03 to 0.04% by weight of maltodextrin 10. The skin barrier protection delivery system according to item 9, comprising: 13. A pharmaceutical composition comprising the skin barrier protection delivery system according to any one of items 1 to 12. 14. A pharmaceutical composition in the form of a sprayable gel, comprising a skin barrier protection delivery system according to any one of items 1 to 13. 15. A method for protecting the skin of a subject in need of skin protection, comprising administering to the skin of the subject a skin barrier protection delivery system according to any one of items 1 to 12 or a pharmaceutical composition according to item 13 or 14. 16. A method for producing the skin barrier protection delivery system according to any one of items 1 to 15, comprising: (a) mixing petrolatum, coconut alkane 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.

Claims

1. A skin barrier protection delivery system comprising (a) a mixture of coconut alkanes and (caprylic / capric acid) coconut alkyls, and (b) petrolatum, wherein petrolatum is present at a concentration of at least 30% and the ratio of (a) to (b) is 7:3 to 1:

3.

2. An emulsion comprising the skin barrier protection delivery system according to claim 1.

3. A sprayable skin barrier protection delivery system according to claim 1 or 2.

4. A skin barrier protection delivery system containing a mixture of coconut alkanes and (caprylic / capric acid) coconut alkyl, petrolatum, ceramide NP, ceramide AP, jojoba esters, squalene, phytosterols, macadamia nut fatty acid phytosteryl, tocopherol, C18-C36 acid triglycerides, C12-18 acid triglycerides, sweet potato (Ipomoea Batatas) root extract, acacia senegal gum, citric acid, and maltodextrin.

5. (i) at least 30% by weight of petrolatum; (i) at least 30% by weight of petrolatum; (ii) Palm alkanes in the range of 30-70% by weight; (iii) 3-7% by weight of (caprylic / capric acid) coconut alkyl; (iv) Ceramide NP in the range of 0.01 to 0.1% by weight; (v) Ceramide AP in the range of 0.01 to 0.1% by weight; (vi) Jojoba esters in the range of 0.1 to 1.5% by weight; (vii) Squalene in the range of 0.1 to 1% by weight; (viiii) Macadamia nut fatty acid phytosteryls in the range of 0.01 to 0.1% by weight; (ix) Phytosterols in the range of 0.005 to 0.1% by weight, (x) Tocopherol in the range of 0.001 to 0.1% by weight; (xi) C18-36 acid triglycerides in the range of 0.5 to 5% by weight; (xi) C12-18 acid triglycerides in the range of 0.1 to 1% by weight; (xiiii) Sweet potato (Ipomoea Batatas) root extract in the range of 0.01 to 0.1% by weight; (xiv) Citric acid in the range of 0.001 to 0.01% by weight; (xv) Acacia Senegal gum in the range of 0.001 to 0.1% by weight; and (xvi) Maltodextrin in the range of 0.001 to 0.1% by weight A skin barrier protection delivery system including, A skin barrier protection delivery system in which the delivery system is a sprayable formulation.

6. (i) 50% by weight of petrolatum; (ii) 42-43% by weight of palm alkanes; (iii) 4-5% by weight of (caprylic / capric acid) coconut alkyl; (iv) 0.05 wt% ceramide NP; (v) 0.05 wt% ceramide AP; (vi) 0.75% by weight of jojoba esters; (vii) 0.3 to 0.4% by weight of squalene; (viiii) 0.05–0.06% by weight of macadamia nut fatty acid phytosteryl; (ix) 0.01–0.02% by weight of phytosterols; (x) 0.0045% by weight of tocopherol; (xi) 1-2% by weight of C18-36 acid triglycerides; (xi) 0.4–0.5% by weight of C12–18 acid triglycerides; (xiiii) 0.03–0.04% by weight of sweet potato (Ipomoea Batatas) root extract; (xiv) 0.003 to 0.004% by weight of citric acid; (xv) 0.03–0.04 wt% acacia senegal gum; and (xvi) 0.03–0.04% by weight of maltodextrin A skin barrier protection delivery system according to claim 1, comprising:

7. A pharmaceutical composition comprising a skin barrier protection delivery system according to any one of claims 1 to 6.

8. A pharmaceutical composition in the form of a sprayable gel, comprising a skin barrier protection delivery system according to any one of claims 1 to 7.

9. A skin barrier protection delivery system according to any one of claims 1 to 6, a pharmaceutical composition according to claim 7 or 8, or a device according to any one of claims 1 to 8, characterized by being for the protection, prevention or treatment of skin barrier damage in a subject requiring it.

10. A method for producing a skin barrier protection delivery system according to any one of claims 1 to 9, comprising: (a) mixing petrolatum, coconut alkane and (caprylic / capric acid) coconut alkyl in a reactor to produce a mixture; (b) heating the mixture until a molten product is obtained; and (c) cooling the mixture.