转移体对酮咯酸三聚氰胺皮肤渗透的影响

Anand Krishnan Prakash, K. Pramod
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引用次数: 1

摘要

为了克服其亲脂性、副作用和频繁给药等问题,需要开发一些更新、更安全的药物。酮酸Tromethamine Transferosomes可能有助于增加皮肤渗透深度和药物进入体循环的量(有助于克服亲脂性问题)。同时,它可以提供口服途径(以减少副作用)或肠外途径(防止注射部位疼痛)的选择,也可以提供长时间的作用,以克服频繁给药的问题。以大豆磷脂酰胆碱和边缘活化剂(Span 80和胆酸钠)为原料,采用常规旋转蒸发超声法制备转移体囊泡。通过筛选大豆磷脂酰胆碱-边缘活化剂比的影响、各种边缘活化剂的影响和溶剂的影响等工艺变量,对转移体配方进行了优化。采用Franz扩散池和大鼠皮肤进行皮肤渗透试验。囊泡组成对囊泡系统的形态表征、大小和分布、包封率、可变形程度和体外释放模式有重要影响。本文观察到复合脂质分子转移体可增加透皮通量,延长酮咯酸Tromethamine的释放时间。目前的研究表明,酮咯酸三聚氰胺可能是一种潜在的药物载体,以新型超柔性转移体的形式存在。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
The effect of Transferosomes on skin permeation of Ketorolac tromethamine
To overcome lipophilicity problem, associated side effects and frequent dosing of Tromethamine, it is needed to develop some newer and safer. Ketorolac Tromethamine Transferosomes may help to increase the depth of skin permeation and the amount of drug delivered to systemic circulation (help in overcoming lipophilicity problem). At the same time if may provide the alternative of oral route (to minimize the side effects), or parenteral route (prevent the pain at injection site) and also can provide the long duration of action, to overcome the problem of frequent dosing. The transfersomal vesicles were prepared by conventional rotary evaporation sonication method using Soya phosphatidylcholine and edge activator (Span 80 and Sodium cholate). Optimizations of the transfersomal formulation were done by selecting various process variables such as effect of Soya phosphatidylcholine-edge activator ratio, effect of various edge activator and solvents. The skin permeation was tested using Franz diffusion cell and rat skin. Vesicles composition had a major effect on the morphological characterization, size and size distribution, percent entrapment efficiency, degree of deformability and in vitro release pattern of the vesicular system. Herein, it is observed that complex lipid molecules transfersomes can increase the transdermal flux and prolong the release of Ketorolac Tromethamine. Present investigation showed that Ketorolac tromethamine could be a potential drug carrier in the form of new ultra-flexible transferosomes.
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