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纳米乳载药凝胶经皮共递送丙酸氯倍他索和卡泊三醇治疗银屑病。

Nanoemulsion loaded gel for topical co-delivery of clobitasol propionate and calcipotriol in psoriasis.

机构信息

Centre for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research, Sector 67, SAS Nagar, Punjab, India.

Centre for Pharmaceutical Nanotechnology, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research, Sector 67, SAS Nagar, Punjab, India.

出版信息

Nanomedicine. 2017 May;13(4):1473-1482. doi: 10.1016/j.nano.2017.02.009. Epub 2017 Mar 1.

Abstract

Current work reports the development and optimization of clobitasol propionate (CP) and calcipotriol (CT) loaded nanoemulsion based gel for topical treatment of psoriasis. Components of nanoemulsion viz., oil and surfactant/co-surfactant were selected depending upon solubility and emulsification potential respectively. The optimized ratio of 5:3:2 of Capmul MCM C8 EP, Cremophor RH 40 and Labrafil 1944 CS was selected. Carbopol 980 was used as gelling agent to achieve final drug concentration of 0.05% w/w and 0.005% w/w respectively for CP and CT. HaCaT cell lines showed higher uptake of drug from nanoemulsion in correlation with the enhancement in penetration of both drugs in stratum corneum (SC) and viable layer from nanoemulsion and gel as compared to free drugs. Imiquimod induced psoriatic BALB/c mice revealed significantly higher anti-psoriatic activity of nanoemulsion gel as compared to free drugs and marketed formulation. The developed formulation showed negligible skin irritation despite increased penetration into the skin.

摘要

目前的工作报道了用于治疗银屑病的丙酸氯倍他索(CP)和卡泊三醇(CT)负载纳米乳凝胶的开发和优化。纳米乳的组成部分,如油和表面活性剂/助表面活性剂,分别根据溶解度和乳化潜力进行选择。选择了 Capmul MCM C8 EP、Cremophor RH 40 和 Labrafil 1944 CS 的优化比例为 5:3:2。Carbopol 980 用作凝胶剂,以实现 CP 和 CT 的最终药物浓度分别为 0.05%w/w 和 0.005%w/w。HaCaT 细胞系显示从纳米乳中摄取药物的能力更高,这与两种药物在角质层(SC)和纳米乳和凝胶的活层中的渗透增强相关,而与游离药物相比。与游离药物和市售制剂相比,咪喹莫特诱导的银屑病 BALB/c 小鼠显示出显著更高的抗银屑病活性。尽管增加了皮肤渗透,但开发的制剂显示出可忽略不计的皮肤刺激性。

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