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<i>In vitro</i> and <i>in vivo</i> evaluation of a desonide gel-cream photostabilized with benzophenone-3

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 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
出处
期刊:Drug Development and Industrial Pharmacy [Taylor & Francis]
卷期号:42 (1): 19-27 被引量:3
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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