COMPOSITIONS COMPRISING ENCAPSULATED TRETINOIN
The present application is directed to compositions comprising microcapsules comprising encapsulated tretinoin, wherein the microcapsule size is less than 50 μm; and to methods of use thereof.
1 . A composition comprising:
microcapsules comprising tretinoin, wherein:
said microcapsules comprise a core containing tretinoin dispersed in an oil and a phase changing material and a metal oxide shell; and
wherein said tretinoin is in solid form and said microcapsules have a D 90 between 30 μm to 50 μm; and
wherein said tretinoin is in the range of 0.01%-0.1% by weight of the composition; and
microcapsules comprising solid benzoyl peroxide; wherein said benzoyl peroxide is in an amount of 3% by weight of the composition.
2 . The composition according to claim 1 , wherein degradation of said tretinoin is less than 2.5% after two weeks storage at 40° C. and 75% relative humidity.
3 . The composition according to claim 1 , wherein the degradation of said tretinoin is less than 2%.
4 . The composition according to claim 1 , wherein said tretinoin is in the amount of between 0.05% and 0.1% weight of the composition.
5 . The composition according to claim 7 , wherein said tretinoin is in the amount of 0.075% weight of the composition.
6 . The composition according to claim 1 , wherein the composition comprises a carrier, wherein the carrier is in the form of an ointment, a cream, a lotion, an oil, a solution, an emulsion, a gel, a paste, a milk, an aerosol, a powder, or a foam.
7 . The composition according to claim 1 , wherein the concentration of all-trans 5,6-epoxy retinoic acid after two weeks storage at 40° C. and 75% relative humidity is less than 1% by weight of the initial tretinoin amount prior to storage.
8 . The composition according to claim 1 , wherein the degradation of said tretinoin is not more than 5% by weight of the initial tretinoin amount, after 18 or 24 months storage at 2° C.-8° C.
9 . The composition according to claim 1 , wherein the degradation of said tretinoin is not more than 5% by weight of the initial tretinoin amount, after 3 months storage at 25° C. and 60% RH.
10 . The composition according to claim 1 , wherein the amount of said tretinoin is 0.1% weight of the composition and the amount of said benzoyl peroxide is 3% weight of the composition.
11 . The composition of claim 1 , wherein said composition has a tretinoin dissolution rate of less than 60% weight/h as measured in a medium of 30%:70% V/V mixture of water and isopropyl alcohol at ambient temperature.
12 . The composition according to claim 11 , wherein said composition has a tretinoin dissolution rate of less than 40% weight/h.
13 . A method for treating a skin disease, disorder or condition selected from acne, infection, inflammation, pruritus, psoriasis, seborrhea, contact dermatitis, rosacea, melasma, photoaging, photodamage, fine wrinkles, and a combination thereof in a subject in need thereof, said method comprising topically administering to said subject a composition according to claim 1 .