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阿替洛尔前体脂质体经皮给药系统的研制及体外渗透研究

Development and in vitro permeation studies of proniosomal based transdermal delivery system of Atenolol.

作者信息

Ramkanth Sundarapandian, Chetty Challa Madhusudhana, Sudhakar Yajamans

机构信息

Annamacharya College of Pharmacy, Rajampet, Andhra Pradesh, India.

Government Polytechnic for Women, Kadapa, Andhra Pradesh, India.

出版信息

Pak J Pharm Sci. 2014 Jan;27(1):115-20.

Abstract

Proniosomes refer to a flexible vesicular carrier with the potential for drug administration through the transdermal route. A proniosome gel type transdermal delivery system of Atenolol was prepared and extensively studied both in vitro drug release and ex vivo permeation studies. The prepared formulations were evaluated for vesicle size, entrapment efficiency, in vitro drug loading, and drug release studies. The release of drug had shown considerable improvement in controlled manner from the prepared gel formulation. It was observed that Span 40 & 60 (A 8) based formulations shows vesicles of minimum size and higher entrapment efficiency compared to the other formulations. Proniosomal transdermal therapeutic system (A 8) was found to be the optimized formulation as it possess good drug release and shows permeation in a steady-state manner over a desired period of time. Also the drug diffusion across snake sheded skin, guinea pig abdomen skin, albino rat, porcine ear correlates better with in vitro drug release studies. The formulation was found to be stable when stored at room temperature and at refrigeration temperature (4 ± 2°C) for 90 days.

摘要

前体脂质体是一种具有通过透皮途径给药潜力的柔性囊泡载体。制备了阿替洛尔的前体脂质体凝胶型透皮给药系统,并对其体外药物释放和离体渗透进行了广泛研究。对制备的制剂进行了囊泡大小、包封率、体外载药量和药物释放研究。药物从制备的凝胶制剂中以可控方式释放有了显著改善。观察到,与其他制剂相比,基于司盘40和60(A8)的制剂显示出最小尺寸的囊泡和更高的包封率。前体脂质体透皮治疗系统(A8)被认为是优化制剂,因为它具有良好的药物释放性能,并在所需时间段内以稳态方式显示渗透。此外,药物在蛇蜕皮肤、豚鼠腹部皮肤、白化大鼠、猪耳上的扩散与体外药物释放研究相关性更好。该制剂在室温及冷藏温度(4±2°C)下储存90天时被发现是稳定的。

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