胺(铵)离子梯度法载药理论及条件选择的研究进展  

Ammonium ion gradients for loading drugs into liposomes:theories and protocols

作　　者：佘振南[1] 程晓波 邓意辉[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2012年第10期801-811,共11页Journal of Shenyang Pharmaceutical University

基　　金：国家自然科学基金资助项目(81072602)

摘　　要：目的对胺(铵)离子梯度法载药的理论及条件选择进行综述。方法参阅近年来国内外文献共52篇,对胺(铵)离子梯度法的载药机制、理论模型、经验模型、药物性质、胺(铵)离子和反离子的选择等进行归纳、总结和分析。结果胺(铵)离子梯度法载药的动力主要来自于间接pH梯度、铵离子扩散电势以及内水相药物沉淀的生成;理论模型能够帮助研究者深刻理解载药机制,经验模型可直接指导载药参数的选择;药物性质、胺(铵)离子和反离子的种类均能影响药物的装载及释放。结论本文为胺(铵)离子梯度法载药的条件选择及相关制剂的开发提供了参考。Objective To review the theories and protocols of the ammonium ion gradients for loading drugs into liposomes.Methods Drug loading mechanism,theoretical models,empirical models,drug properties,ammonium ion and the counterion of the ammonium ion gradients were summarized and analyzed on the basis of 52 published literatures.Results The driving forces of ammonium ion gradients for drug loading came from the indirect pH gradient,ammonium ion diffusion potential and generation of drug precipitation within the inner water phase of liposomes;the drug loading mechanism could be deeply understood with the help of theoretical model,and the parameters could be chosen guided by the empirical model;drug properties,ammonium ion and counterion could affect drug loading efficiency and release properties.Conclusions This article will provide references for the protocol construction of ammonium ion gradients and development of liposome formulations.

关 键 词：主动载药 胺(铵)离子梯度 反离子 脂质体 

分 类 号：R943[医药卫生—药剂学]