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载有局部麻醉药利多卡因的局部脂质体系统:制备与评价。

Topical liposome system bearing local anaesthetic lignocaine: preparation and evaluation.

作者信息

Sharma B B, Jain S K, Vyas S P

机构信息

Department of Pharmaceutical Sciences, Dr H. S. Gour Vishwavidyalaya, Sagar, India.

出版信息

J Microencapsul. 1994 May-Jun;11(3):279-86. doi: 10.3109/02652049409040457.

DOI:10.3109/02652049409040457
PMID:8064552
Abstract

Topical multiple lamellar vesicular liposomes were formulated by using the method reported by Bangham (1968). The liposomes, composed of different lipid and charge-bearing components such as stearylamine or dicetylphosphate, were characterized for average size, size distribution, charge lamellae and drug loading. The negatively charged liposomes showed high drug loading and were incorporated in different topical vehicles, i.e. gels and ointment. These were evaluated for in vitro drug skin permeation profile. The selected formulations were evaluated for in vivo performance using the pinprick method. The results revealed localized and prolonged activity of local anaesthetic contained in liposomes when compared with equivalent conventional topical application.

摘要

采用班汉姆(1968年)报道的方法制备了局部用多层囊泡脂质体。脂质体由不同的脂质和带电荷成分(如硬脂胺或二鲸蜡基磷酸酯)组成,对其平均大小、大小分布、电荷层和药物负载量进行了表征。带负电荷的脂质体显示出高药物负载量,并被掺入不同的局部给药载体中,即凝胶和软膏。对这些制剂进行了体外药物皮肤渗透曲线评估。使用针刺法对选定的制剂进行了体内性能评估。结果显示,与等效的传统局部应用相比,脂质体中含有的局部麻醉剂具有局部和延长的活性。

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