固体脂微颗粒载药体系中稳定剂的作用和机理

Mechanism of Stabilizers in Solid Lipid Microparticles

以硬脂精为载体材料,采用熔融-冷却法制备包载布洛芬的固体脂微颗粒(SLM),研究了不同稳定剂对SLM载药体系的稳定效果.实验结果表明聚乙烯醇(PVA)和卵磷脂/牛胆盐是制备硬脂精SLM的较好的稳定剂.进一步研究这两种稳定剂在布洛芬含量增大时对硬脂精SLM的稳定效果,发现当布洛芬含量达7%(质量分数,下同)时,以卵磷脂/牛胆盐为稳定剂的SLM体系开始发生聚集;而对于以PVA为稳定剂的SLM体系,当布洛芬含量增加到25%时,SLM体系仍能保持很好的稳定性.文中还基于对稳定剂分子特征以及载药体系微观结构的分析和介观模拟,从理论上解释了稳定剂的稳定作用和机理.

The emulsion-congealing method was adopted to prepare ibuprofen-loaded solid lipid microparticles （SLM） with tristearin as the carrier. The stabilities of the SLM stabilized with different stabilizers were also investigated, proving that polyvinyl alcohol （PVA） and soy lecithin/bile salt are good stabilizers for the SLM system. The stabilities of the SLM stabilized with these two stabilizers at an increasing ibuprofen content were then investigated. Experimental results show that, at an ibuprofen mass fraction of 7% , the SLM system stabilized with soy lecithin/ bile salt begins to congregate, while the one stabilized with PVA remains stable even when ibuprofen mass fraction is up to 25%. The stabilizing mechanism of the stabilizers was finally interpreted based on the analysis and simulation of the molecular structure of the stabilizer and the microstructure of the drug carrier.