无机盐在提高合成高分子微球包封率的应用与机理

Application and mechanism of inorganic salts in improving encapsulation efficiency of synthetic polymer microspheres

生物可降解微球的研究与应用取得了较大的进展,但其包封率低下以及突释与迟释等问题仍然是研究中面临的重大困扰.针对以常用的乳化-溶剂挥发法制备合成高分子微球的过程,根据已有试验研究及参考文献资料简述了包封率的影响因素,并详述了无机盐在提高包封率时的应用及其机理.其机理主要分为两大方面:一方面是无机盐对渗透压的影响;另一方面是对药物溶解度的影响.按照对溶解度的影响作用机理的不同又可归纳为同离子效应、盐析作用和新盐的生成.最后,对以往研究进行回顾、总结、分析与展望,为今后在微球制剂的研究中解决微球包封率低下的问题提供参考.随着一系列问题的解决,微球制剂将具有广阔的应用前景.

Although remarkable progress had been made in the research and application of biodegradable microspheres,the low encapsulation efficiency,burst release and lag phase were still the major problems in the study.In this paper,we mainly focused on the process of polymer microspheres fabrication using the common emulsification solvent evaporation method.We briefly introduced the factors that influence encapsulation efficiency and described the application and mechanism of inorganic salts in increasing the encapsulation efficiency in detail.The mechanisms could be mainly divided into two aspects.One was the influence of inorganic salts on the osmotic pressure,the other was the effect of inorganic salts on the solubility of drugs.According to the different effects on solubility,it could be concluded as the mechanism of ionic interaction,salting out and formation of new salts.This paper would provide reference for solving the problem of low encapsulation efficiency of microspheres.