化学
色谱法
体内
渗透
肉豆蔻酸异丙酯
二苯甲酮
体外
生物化学
有机化学
膜
生物
生物技术
作者
Priscila Rosa,Juliana Cardoso dos Santos,Tássia Fontana Lehmen,Julia Weber,Fernanda Cramer Flores,Cristiane de Bona da Silva,Sara Marchesan Oliveira,Indiara Brusco,Gessica Brum Milani,Andréa Inês Horn Adams
标识
DOI:10.3109/03639045.2015.1022554
摘要
Our group previously reported the photoinstability of some desonide topical commercial formulations under direct exposure to UVA radiation.This study aimed to prepare and characterize a gel-cream containing desonide, with greater photostability than the commercial gel-cream (C-GC). Benzophenone-3 (BP-3) was used as a photostabilizing agent.The gel-cream developed (D-GC) containing BP-3 at 0.1% was prepared and characterized regarding its pH, drug content, spreadability, viscosity, in vitro drug release and in vitro permeation. The in vivo anti-inflammatory effect was assessed by ear edema measurement, croton oil-induced acute skin inflammation and myeloperoxidase assay.D-GC presented characteristics compatible with topical application, appropriate drug content and good spreadability, and non-Newtonian behavior with pseudoplastic flow. D-GC showed a good photostability profile, presenting a desonide content of 95.70% after 48 h of exposure to UVA radiation, and stability under room conditions during 60 days. The amount of desonide released from D-GC and C-GC was 57.8 and 51.7 µg/cm2, respectively, measured using the vertical Franz cell. The in vitro skin permeation showed that desonide reached the site of action of the topical corticosteroids, from both formulations; however, the desonide amount retained in the dermis was lower with D-GC. The in vivo evaluation of topical anti-inflammatory activity indicated that D-GC presented the same biological effect as C-GC.D-GC represents a promising approach to treat dermatological disorders, since it presented satisfactory physicochemical characteristics, the same biological activity as C-GC and superior photostability, conferred by the addition of BP-3 at 0.1%.
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