Localized delivery of a lipophilic proteasome inhibitor into human skin for treatment of psoriasis.

作者: Meera Gujjar , Jack Arbiser , Rick Coulon , Ajay K. Banga

DOI: 10.3109/1061186X.2015.1087529

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摘要: AbstractPurpose: Pentaerythritol tetrakis (3,5-di-tert-butyl-4-hydroxyhydrocinnamate) (PTTC) is a cinnamate tetraester with proteasome inhibitor activity, which may be used as topical treatment in psoriasis, but has computed log P of 23. The objective this vitro study was to determine the intradermal delivery, skin irritation and potential efficacy PTTC treating psoriasis.Methods: Solubility studies were performed find suitable vehicle for PTTC. Permeation microneedle-treated skin. A cell culture test dosed positive control, negative control An MTT assay evaluate viability irritancy. Psoriatic also IL-6 levels determined by ELISA.Results: greatest dimethyl sulfoxide ethyl pyruvate, delivering greater amount (2343.41 ± 384.26 µg) into stratum corneum. alone well emulsion formulation f...

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