Compositions and methods for deep dermal drug delivery
Inventors
Osborne, David W. • TOFIG, Babak N.
Assignees
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Publication Number
US-12053481-B2
Publication Date
2024-08-06
Expiration Date
Abstract
Pharmaceutical compositions for the topical administration of a drug to the pilosebaceous unit and methods for administering the same. As disclosed herein, the inventors of the present invention have made the surprising discovery that pharmaceutical compositions comprising small particles of an active pharmaceutical ingredient can be administered to the pilosebaceous unit. The pharmaceutical composition can comprise SHR0302 or spironolactone as an active pharmaceutical ingredient.
Core Innovation
The invention describes topical deep dermal delivery in which a therapeutically effective amount of SHR0302 or a pharmaceutically acceptable salt thereof is administered with silicone dimethicone and/or cyclomethicone. The formulation uses a primary particle size distribution for SHR0302 characterized by a D90 value of less than about 20 μm, with further size distributions described by D50 and D10 thresholds. This particle-size definition supports deep dermal penetration and targeting beyond the stratum corneum.
The disclosed delivery is directed to the pilosebaceous unit, including follicular/hair bulb penetration, with dermal penetration of at least 1 mm. The document emphasizes silicone suspensions or emulsions that include silicones such as dimethicone and cyclomethicone together with small-particle active ingredients. The particle delivery approach enhances deposition targeting in the epidermis and dermis regions associated with the pilosebaceous unit.
The invention further characterizes formulation and performance using in vitro cadaver skin penetration and retention studies, including depth profiling and measurements using Franz cells and IVPT. It also describes support using micronized or roller-milled suspensions and comparative results versus creams and gels, indicating enhanced deposition compared to those topical dosage forms. The document further notes that adding certain preservatives or thickeners can reduce targeting to the pilosebaceous unit.
Claims Coverage
The document includes two independent claims. Both independent claims share the same core formulation and particle-size constraint for SHR0302 and differ mainly in the therapeutic target condition.
Treatment of alopecia areata with silicone and small-particle SHR0302 (D90<20 μm)
A method of treating alopecia areata by topically administering a pharmaceutical composition comprising a therapeutically effective amount of SHR0302 or a pharmaceutically acceptable salt, characterized by a primary particle size distribution having a D90 value of less than about 20 μm, and a silicone selected from dimethicone and cyclomethicone.
Treatment of hair loss condition with silicone and small-particle SHR0302 (D90<20 μm)
A method of treating a hair loss condition by topically administering a pharmaceutical composition comprising a therapeutically effective amount of SHR0302 or a pharmaceutically acceptable salt, characterized by a primary particle size distribution having a D90 value of less than about 20 μm, and a silicone selected from dimethicone and cyclomethicone.
Across both independent claims, the inventive coverage is centered on topical administration of SHR0302 with silicone dimethicone and/or cyclomethicone, where SHR0302 is defined by a primary particle size distribution with D90 less than about 20 μm. Dependent claims further narrow delivery to the pilosebaceous unit and add a dermal penetration threshold of at least 1 mm, while also defining formulation as a suspension and tightening additional particle-size metrics.
Stated Advantages
Enhanced dermal penetration and deposition targeting associated with the pilosebaceous unit compared to creams and gels.
Deeper targeting by achieving follicular/hair bulb penetration and dermal penetration of at least 1 mm.
Documented Applications
Treatment of alopecia areata via topical administration of SHR0302 with dimethicone and/or cyclomethicone and a defined small-particle D90 specification.
Treatment of a hair loss condition, including alopecia, androgenic hair loss, hypotrichosis, and telogen effluvium, via topical administration of SHR0302 with dimethicone and/or cyclomethicone and a defined small-particle D90 specification.
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