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用于局部递送罗非昔布的脱水山梨醇酯脂质体

Sorbitan ester niosomes for topical delivery of rofecoxib.

作者信息

Das Malay K, Palei Narahari N

机构信息

Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh 786 004, India.

出版信息

Indian J Exp Biol. 2011 Jun;49(6):438-45.

Abstract

The aim of the present investigation is to encapsulate rofecoxib in niosomes and incorporate the prepared niosomes into dermal gel base for sustained therapeutic action. Niosomes were prepared by lipid film hydration technique and were analyzed for size, entrapment efficiency and drug retention capacity. Niosomal vesicles were then incorporated into blank carbopol gel to form niosomal gel. The in vitro permeation study across pig skin was performed using Keshary-Chien glass diffusion cell. The size and entrapment efficiency of the niosomal vesicles increased with gradual increase in HLB value of nonionic surfactants used. Maximum drug entrapment was observed with Span 20 with HLB value of 8.6 and drug leakage from vesicles was less at refrigerated condition than at the room temperature. Higher proportion of cholesterol made the niosomal formulation more stable with high drug retention properties. The niosomal gel showed a prolong drug release behavior compared to plain drug gel. Differential scanning calorimetric study of drug loaded gel and pig skin after permeation study confirmed inertness of carbopol gel base toward rofecoxib and absence of drug metabolism in the skin during permeation study, respectively. The niosomal formulations were successfully prepared by lipid film hydration technique using cholesterol and Span as nonionic surfactant. Presence of cholesterol made niosomes more stable with high drug entrapment efficiency and retention properties. The lower flux value of niosomal gel as compared to plain drug gel across pig skin assured the prolong drug release behavior with sustained action.

摘要

本研究的目的是将罗非昔布包封于非离子表面活性剂囊泡中,并将制备好的非离子表面活性剂囊泡加入到皮肤凝胶基质中,以实现持续的治疗作用。采用脂质膜水化技术制备非离子表面活性剂囊泡,并对其粒径、包封率和药物保留能力进行分析。然后将非离子表面活性剂囊泡加入空白卡波姆凝胶中制成非离子表面活性剂囊泡凝胶。使用Keshary-Chien玻璃扩散池进行了猪皮体外渗透研究。随着所用非离子表面活性剂HLB值的逐渐增加,非离子表面活性剂囊泡的粒径和包封率增大。观察到用HLB值为8.6的司盘20时药物包封率最高,且在冷藏条件下囊泡中的药物泄漏比室温下少。较高比例的胆固醇使非离子表面活性剂囊泡制剂更稳定,具有较高的药物保留特性。与普通药物凝胶相比,非离子表面活性剂囊泡凝胶表现出药物释放行为延长。渗透研究后对载药凝胶和猪皮进行差示扫描量热分析,分别证实了卡波姆凝胶基质对罗非昔布呈惰性,以及渗透研究过程中皮肤中不存在药物代谢。采用胆固醇和司盘作为非离子表面活性剂,通过脂质膜水化技术成功制备了非离子表面活性剂囊泡制剂。胆固醇的存在使非离子表面活性剂囊泡更稳定,具有较高的药物包封率和保留特性。与普通药物凝胶相比,非离子表面活性剂囊泡凝胶在猪皮上的通量值较低,确保了药物释放行为延长和持续作用。

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