Development of a topical ointment of betamethasone dipropionate loaded nanostructured lipid carrier

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• 作者：Xin Kong ; Yuan Zhao ; Peng Quan ; Liang Fang ; ^{fangliang2003@yahoo.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Nanostructured lipid carrier (NLC) ; Betamethasone dipropionate (BD) ; Topical ointment ; Atopic dermatitis (AD)
• 刊名：Asian Journal of Pharmaceutical Sciences
• 出版年：2016
• 出版时间：April 2016
• 年：2016
• 卷：11
• 期：2
• 页码：248-254
• 全文大小：1013 K

文摘

The purpose of this study was to design an innovative topical ointment containing betamethasone dipropionate loaded nanostructured lipid carrier (BD-NLC) for the treatment of atopic dermatitis (AD). BD-loaded NLC was produced with precirol ATO 5 and oleic oil (OA) by melt emulsification method. Effects of surfactant concentration, amount of solid lipid and liquid lipid on skin retention and skin penetration were investigated by in vitro percutaneous permeation experiment. The optimized BD-NLC showed a homogeneous particle size of 169.1 nm (with PI = 0.195), negatively charged surface (−23.4 mV) and high encapsulation efficiency (85%). Particle morphology assessed by TEM revealed a spherical shape. In vitro skin permeation study was carried out to investigate the percutaneous behaviors of W/O ointment with BD-NLC and Carbopol emulgel ointment with BD-NLC. W/O ointment with BD-NLC showed high skin retention (35.43 µg/g) and low penetration (0.87 µg/ml). In vitro drug release studies were carried out to demonstrate the drug releasing properties of the two ointments. W/O ointment with BD-NLC showed an advantage for skin retention as it was better for drug release. The tissue distribution test suggested that BD distribution was skin > muscle > blood. Self-made topical ointment in mice showed no skin irritation. The animal experiments indicated that BD-loaded NLC ointment was effective and safe for topical use.