Rinse-off compositions and uses thereof for delivery of active agents

Abstract

The present application relates to a rinse-off composition comprising an oil phase and an aqueous surfactant matrix, wherein one or more active agents are dissolved in one or more non-polar, water-immiscible solvents, and the oil phase is dispersed in the aqueous surfactant matrix. The present application also relates to methods of delivering the active agent(s) to a subject in need thereof topically, for example to the skin, the hair, and scalp. The present application also relates to use of the rinse-off compositions to treat and/or prevent topical conditions such as dermatitis and psoriasis. In some embodiments, the rinse-off compositions of the present application are shampoo compositions.

1 . A rinse-off composition comprising
 a) an oil phase; and   b) an aqueous surfactant matrix,   
       wherein the oil phase comprises one or more active agents dissolved in one or more non-polar, water-immiscible solvents and the oil phase is dispersed in the aqueous surfactant matrix. 
     
     
         2 . The rinse-off composition of  claim 1 , wherein the aqueous surfactant matrix comprises one or more surfactants and one or more polymers. 
     
     
         3 . The rinse-off composition of  claim 2 , wherein the one or more surfactants are one or more anionic surfactants and the one or more polymers are one or more cationic polymers. 
     
     
         4 . The rinse-off composition of  claim 3 , wherein the one or more anionic surfactants and the one or more cationic polymer form coacervates. 
     
     
         5 . The rinse-off composition of  claim 1 , wherein the aqueous surfactant matrix further comprises water and is substantially free of ethanol and/or other water-miscible solvents. 
     
     
         6 . The rinse-off composition of  claim 3 , wherein the one or more anionic surfactants are selected from sodium laureth sulfate and sodium lauryl sulfate and mixtures thereof. 
     
     
         7 . The rinse-off composition of  claim 3 , wherein the one or more cationic polymers are selected from cationic cellulose derivatives, cationic guar derivatives, acrylamidopropyl trimonium chloride copolymer with acrylamide, homopolymers derived from the monomer diallyldimethylammonium chloride, copolymers derived from diallyldimethylammonium chloride and acrylamide, and homopolymers or copolymers of a cationic monomer selected from:
 (a) a monomer having the Formula I:   
       
         
           
           
               
               
           
         
       
       wherein R 1  is H or CH 3 ; Y is O or NH; Z is C 1-6 alkylene; R 2 , R 3 , and R 4  are each independently C 1-22 alkyl or C 1-22 hydroxyalkyl; and X is a monovalent anion selected from halide and C 1-4 alkyl sulfate; and
 (b) diallyldimethylammonium chloride, 
 (c) and mixtures thereof. 
 
     
     
         8 . The rinse-off composition of  claim 7 , wherein the cationic cellulose derivatives are polymeric quaternary ammonium salts derived from the reaction of hydroxyethyl cellulose with a trimethylammonium-substituted epoxide. 
     
     
         9 . The rinse-off composition of  claim 2 , wherein the one or more surfactants further comprises one or more amphoteric surfactants and/or one or more non-ionic surfactants. 
     
     
         10 . The rinse-off composition of  claim 9 , wherein the one or more amphoteric surfactants are selected from amphocarboxylates, alkyl betaines, amidoalkylbetaines, amidoalkylsultaines, amphophosphates , phosphobetaines , pyrophosphobetaines, c arboxy alkyl alkyl polyamines, cocoamidopropyl betaine, and mixtures thereof. 
     
     
         11 . The rinse-off composition of  claim 9 , wherein the one or more non-ionic surfactants are selected from polysorbate 20, C 8-22 alkyl glucosides, coconut fatty acid monoethanolamides, coconut fatty acid diethanolamides, cocomonoethanolamide, and mixtures thereof. 
     
     
         12 . The rinse-off composition of  claim 1 , wherein the one or more non-polar, water-immiscible solvents are selected from di-isopropyl adipate, peppermint oil, coconut oil, and mixtures thereof. 
     
     
         13 . The rinse-off composition of  claim 12 , wherein the oil phase further comprises one or more water-immiscible or water-insoluble components selected from dimethicone, cyclomethicone, fatty alcohols, and mixtures thereof. 
     
     
         14 . The rinse-off composition of  claim 1 , wherein the one or more active agents are selected from adrenergic agent, adrenocortical steroid, adrenocortical suppressant, aldosterone antagonist, amino acid, anabolic, analeptic, analgesic, anesthetic, anorectic, anti-acne agent, anti-adrenergic, anti-allergic, anti-amebic, anti-anemic, anti-anginal, anti-arthritic, anti-asthmatic, anti-atherosclerotic, antibacterial, anticholinergic, anticoagulant, anticonvulsant, antidepressant, antidiabetic, antidiarrheal, antidiuretic, anti-emetic, anti-epileptic, antifibrinolytic, antifungal, antihemorrhagic, antihistamine, antihyperlipidemia, antihypertensive, antihypotensive, anti-infective, anti-inflammatory, antimicrobial, antimigraine, antimitotic, antimycotic, antinauseant, antineoplastic, antineutropenic, antiparasitic, antiproliferative, antipsychotic, antirheumatic, antiseborrheic, antisecretory, antispasmodic, antithrombotic, antiulcerative, antiviral, appetite suppressant, blood glucose regulator, bone resorption inhibitor, bronchodilator, cardiovascular agent, cholinergic, depressant, diagnostic aid, diuretic, dopaminergic agent, estrogen receptor agonist, fibrinolytic, fluorescent agent, free oxygen radical scavenger, gastric acid suppressant, gastrointestinal motility effector, glucocorticoid, hair growth stimulant, hemostatic, histamine H2 receptor antagonists, hormone, hypocholesterolemic, hypoglycemic, hypolipidemic, hypotensive, imaging agent, immunizing agent, immunomodulator, immunoregulator, immunostimulant, immunosuppressant, keratolytic, LHRH agonist, mood regulator, mucolytic, mydriatic, nasal decongestant, neuromuscular blocking agent, neuroprotective, NMDA antagonist, non-hormonal sterol derivative, plasminogen activator, platelet activating factor antagonist, platelet aggregation inhibitor, psychotropic, radioactive agent, scabicide, sclerosing agent, sedative, sedative-hypnotic, selective adenosine Al antagonist, serotonin antagonist, serotonin inhibitor, serotonin receptor antagonist, steroid, thyroid hormone, thyroid inhibitor, thyromimetic, tranquilizer, amyotrophic lateral sclerosis agent, cerebral ischemia agent, Paget's disease agent, unstable angina agent, vasoconstrictor, vasodilator, wound healing agent, xanthine oxidase inhibitor, growth-promoting agent, hair-strengthening agent, coloring agent, sunblocking agent, hair removal/depilatory agent, anti-perspirant agent, pediculosides, pesticides, retinoids, vitamins, liphophilic vitamins, vitamin derivatives, cannabinoids, corticosteroids, and combinations thereof. 
     
     
         15 . The rinse-off composition of  claim 14 , wherein the active agent is halobetasol propionate. 
     
     
         16 . The rinse-off composition of  claim 1 , wherein the one or more active agents are selected from hydrocortisone, alclometasone, amelometasone, beclometasone, betamethasone, cormetasone, desoximetasone, dexamethasone, flumetasone, halometasone, icometasone, mometasone, paramethasone, amcinonide, budesonide, desonide, fluocinolone acetonide, fluocinonide, halcinonide, triamcinolone acetonide, fluocortolone, alclometasone dipropionate, betamethasone dipropionate, betamethasone valerate, clobetasol propionate, clobetasone butyrate, fluprednidene acetate, mometasone furoate, ciclesonide, cortisone acetate, halobestasol propionate, hydrocortisone aceponate, hydrocortisone acetate, hydrocortisone buteprate, hydrocortisone butyrate, hydrocortisone valerate, prednicarbate, clocortolone pivolate, tixocortol pivalate, progesterone, azole, ketoconazole, econazole, luluconazole, selenium sulfide, pyrithione zinc, terbinafine, sodium sulfacetamide, isotretinoin, tretinoic acid, tar, piroctone olamine, coal tar, sulfur, climbazole, ciclopirox olamine, zinc omadine, salicylic acid, azelaic acid, tranexamic acid, cannabidiol (CBD), tetrahydrocannabiol (THC), vitamin D, vitamin D analogs, calcipotriene, calcipotriol, vitamin A, retinol, resorcinol, lidocaine, minoxidil and mixtures thereof. 
     
     
         17 . The rinse-off composition of  claim 1 , wherein about 25% to about 50% or about 27% to about 45% of the one or more active agents are solubilized in the one or more non-polar water-immiscible solvents. 
     
     
         18 . The rinse-off composition of  claim 1 , wherein the rinse-off composition provides a deposition of the one or more active agents onto an applied surface that is about 5% to about 30% of the total amount of the one or more active agents in the composition, wherein the composition is applied to the surface for less than 15 minutes followed by rinsing. 
     
     
         19 . The rinse-off composition of  claim 1 , wherein the rinse-off composition provides a deposition of the one or more active agents onto the applied surface that is at least 2.1%, 3.4%, or 6.6% or more than 0.6%, 0.7%, 1.1% or 2.5% of the total amount of the one or more active agents in the composition. 
     
     
         20 . The rinse-off composition of  claim 1 , wherein the composition is a facial, hand, or body cleanser or wash, a bath or shower product, or a shampoo composition and/or hair conditioning composition. 
     
     
         21 . A method of topically administering one or more active agents to a subject in need thereof comprising:
 a) topically applying a rinse-off composition of  claim 1  to the subject;   b) adding water and optionally creating a lather; and   c) rinsing the composition.   
     
     
         22 . The method of  claim 21 , wherein steps a) and b) are separated by less than about 15 minutes, less than about 10 minutes, or less than about 5 minutes. 
     
     
         23 . The method of  claim 21 , wherein the rinse-off composition is applied to the skin, the hair, scalp, and or another anatomical surface of the subject. 
     
     
         24 . The method of  claim 21 , wherein an effective amount of the rinse-off composition is applied, wherein the effective amount is an amount effective to treat a disease, disorder, or condition treatable with the one or more active agents and/or to treat symptoms of a disease, disorder, or condition treatable with the one or more active agents. 
     
     
         25 . The method of  claim 24 , wherein the active agent is applied for treatment of a disease, disorder, or condition treatable with the one or more active agents is inflammatory skin diseases, inflammatory scalp disease, fungal skin disease, fungal scalp disease, serborrheic dermatitis, psoriasis, acne, anti-aging, anti-wrinkle, skin lightening, hyperpigmentation, pain relief, skin rejuvenation, dry skin, dry scalp, and/or dandruff. 
     
     
         26 . The method of  claim 21 , wherein the rinse-off composition is applied to the subject for less than 5 minutes to 15 minutes prior to the rinsing. 
     
     
         27 . The method of  claim 21 , wherein the amount of one or more active agents deposited on the skin, the hair, scalp and/or other anatomical surface of the subject step is at least 5%, 10%, 15%, 20%, 25%, 30%, 40%, or 50% of the total concentration of the active agents(s) in the composition, wherein the composition is applied to the skin, the hair, scalp and/or other anatomical surface for less than 15 minutes followed by rinsing. 
     
     
         28 . The method of  claim 21 , wherein the rinse-off composition is a facial, hand, or body cleanser or wash, a bath or shower product, or a shampoo composition and/or hair conditioning composition. 
     
     
         29 . A method of treating and/or preventing a disease, disorder, or condition, or treating and/or preventing symptoms of a disorder, disease, or condition, with one or more active agents comprising:
 a) topically applying the rinse-off composition of  claim 1  to a subject in need thereof;   b) adding water and optionally creating a lather; and   c) rinsing the composition,   
       wherein the disease, disorder or condition is one that is treatable with the one or more active agents. 
     
     
         30 . A method of topically administering a rinse-off composition comprising halobetasol propionate to a subject in need thereof, comprising:
 a) topically applying a rinse-off composition comprising halobetasol propionate to the subject;   b) adding water and optionally creating a lather; and   c) rinsing the composition.