Stabilized topical formulations containing core-shell microcapsules
AssigneeMedicis Pharamaceutical Corporation
InventorsOfer TOLEDANO, Haim BAR-SIMANTOV
Life of this patent
Estimating the term…
Abstract
The present disclosure relates to compositions for topical application, where the compositions comprise microcapsules having a core that comprises benzoyl peroxide and a shell that comprises an inorganic polymer, microcapsules having a core that comprises a retinoid and a shell that comprises an inorganic polymer, and a stabilizing agent. The composition can be in a variety of forms, such as emulsion and gel.
Claims7
A composition for topical application, comprising:
- a plurality of first core-shell microcapsules comprising a first core that comprises benzoyl peroxide and a first shell that comprises a first inorganic polymer;
- and
- a plurality of second core-shell microcapsules comprising a second core that comprises a retinoid and a second shell that comprises a second inorganic polymer;
- wherein said composition is an oil in water emulsion comprising a polyoxylstearate and a glycerylstearate wherein the ratio of said polyoxylstearate to said glycerylstearate is in the range of 0.1:10 to 10:0.1.
A composition for topical application, comprising:
- a plurality of first core-shell microcapsules comprising a first core that comprises benzoyl peroxide and a first shell that comprises a first inorganic polymer;
- and
- a plurality of second core-shell microcapsules comprising a second core that comprises a retinoid and a second shell that comprises a second inorganic polymer;
- wherein said composition is in a gel form comprising at least one non-ionic polymeric dispersant and at least one thickening agent.
A composition for topical application, comprising:
- a plurality of first core-shell microcapsules comprising a first core that comprises benzoyl peroxide and a first shell that comprises a first inorganic polymer;
- a plurality of second core-shell microcapsules comprising a second core that comprises a retinoid and a second shell that comprises a second inorganic polymer;
- and
- an amount of a stabilizing agent that is effective to:
- (i) maintain the amount of benzoyl peroxide and the amount of retinoid in the composition at a level that is at least about 90% of the initial amounts, as measured after storage of the composition at a storage condition of 30° C. for three months;
- and
- (ii) maintain the microbial count of the composition at a level that meets the criteria of USP 51, as measured by Antimicrobial Effectiveness Testing (AET) after storage of the composition at a storage condition of 40° C. for one month.
A composition in a gel form for topical application, comprising:
- a plurality of first core-shell microcapsules comprising a first core that comprises benzoyl peroxide and a first shell that comprises a first silica polymer;
- a plurality of second core-shell microcapsules comprising a second core that comprises all-trans retinoic acid (ATRA) and a second shell that comprises a second silica polymer;
- and
- at least one non-ionic polymer in an amount effective to provide at least one stabilization selected from the group consisting of
- (i) viscosity stabilization whereby the viscosity of said composition is maintained such that the change in viscosity of said composition, as measured after manufacture followed by three months storage at 25° C., is less than about 30%, and
- (ii) degradation stabilization whereby the amount of degradation of said ATRA, as measured after manufacture followed by three months storage at 25° C., is less than about 10%.
A composition in an emulsion form for topical application, comprising:
- a plurality of first core-shell microcapsules comprising a first core that comprises benzoyl peroxide and a first shell that comprises a first silica polymer;
- a plurality of second core-shell microcapsules comprising a second core that comprises all-trans retinoic acid (ATRA) and a second shell that comprises a second silica polymer;
- and
- a stabilizing agent comprising at least one non-ionic surfactant and at least one antimicrobial in amounts effective to:
- (i) maintain the amount of benzoyl peroxide and the amount of retinoid in the composition at a level that is at least about 90% of the initial amounts, as measured after storage of the composition at a storage condition selected from the group consisting of 40° C. for two months, 30° C. for three months, 25° C. for six months and 5° C. for two years;
- and
- (ii) maintain the microbial count of the composition at a level that meets the criteria of USP 51, as measured by Antimicrobial Effectiveness Testing (AET) after storage of the composition at a storage condition of 40° C. for one month.
A composition in an emulsion form for topical application, comprising:
- a plurality of first core-shell microcapsules comprising a first core that comprises benzoyl peroxide and a first shell that comprises a first silica polymer, the benzoyl peroxide being present in the composition in an initial amount of about 6% by weight, based on the total weight of the composition;
- a plurality of second core-shell microcapsules comprising a second core that comprises all-trans retinoic acid (ATRA) and a second shell that comprises a second silica polymer, the ATRA being present in the composition in an initial amount of about 0.1% by weight, based on the total weight of the composition;
- and
- a stabilizing agent comprising (a) at least one non-ionic surfactant selected from the group consisting of polyoxyl 100 stearate and glycerol monostearate;
- and (b) at least one antimicrobial selected from the group consisting of methylparaben and imidazolidinyl urea;
- wherein the stabilizing agent is present in an amount effective to:
- (ia) maintain the amount of benzoyl peroxide at a level of at least about 5.4% by weight based on the total weight of the composition, as measured after storage of the composition at a storage condition selected from the group consisting of 40° C. for two months, 30° C. for three months, 25° C. for six months and 5° C. for two years;
- (ib) maintain the amount of ATRA at a level of at least about 0.09% by weight based on the total weight of the composition, as measured after storage of the composition at a storage condition selected from the group consisting of 40° C. for two months, 30° C. for three months, 25° C. for six months and 5° C. for two years;
- (ii) maintain the microbial count of the composition at a level that meets the criteria of USP 51, as measured by Antimicrobial Effectiveness Testing (AET) after storage of the composition at a storage condition of 40° C. for one month;
- and
- (iii) maintain the bulk viscosity of said composition at about one million cps or less and within a range of about 70% to about 130% of the initial bulk viscosity, as measured after storage of the composition at 25° C. for three months.
A composition in an emulsion form for topical application, comprising:
- a plurality of first core-shell microcapsules comprising a first core that comprises benzoyl peroxide and a first shell that comprises a first silica polymer, the benzoyl peroxide being present in the composition in an initial amount of about 3% by weight, based on the total weight of the composition;
- a plurality of second core-shell microcapsules comprising a second core that comprises all-trans retinoic acid (ATRA) and a second shell that comprises a second silica polymer, the ATRA being present in the composition in an initial amount of about 0.05% by weight, based on the total weight of the composition;
- and
- a stabilizing agent comprising (a) at least one non-ionic surfactant selected from the group consisting of polyoxyl 100 stearate and glycerol monostearate;
- and (b) at least one antimicrobial selected from the group consisting of methylparaben and imidazolidinyl urea;
- wherein the stabilizing agent is present in an amount effective to:
- (ia) maintain the amount of benzoyl peroxide at a level of at least about 2.7% by weight based on the total weight of the composition, as measured after storage of the composition at a storage condition selected from the group consisting of 40° C. for two months, 30° C. for three months, 25° C. for six months and 5° C. for two years;
- (ib) maintain the amount of ATRA at a level of at least about 0.045% by weight based on the total weight of the composition, as measured after storage of the composition at a storage condition selected from the group consisting of 40° C. for two months, 30° C. for three months, 25° C. for six months and 5° C. for two years;
- (ii) maintain the microbial count of the composition at a level that meets the criteria of USP 51, as measured by Antimicrobial Effectiveness Testing (AET) after storage of the composition at a storage condition of 40° C. for one month;
- and
- (iii) maintain the bulk viscosity of said composition at about one million cps or less and within a range of about 70% to about 130% of the initial bulk viscosity, as measured after storage of the composition at 25° C. for three months.
Dependencies are inferred from the claim text.