今日药学

2017, v.27(11) 721-724

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载荧光药物聚酯微球释药机制的研究
Characterization of Microsphere's Release Mechanism by the Change of Surface Fluorescence

万斯斯;赵萍;罗永梅;郭喆霏;罗宇燕;张永明;
WAN Sisi;ZHAO Ping;LUO Yongmei;GUO Zhefei;LUO Yuyan;ZHANG Yongming;Department of Pharmacy,the Third Affiliated Hospital,Sun Yat-sen University;School of Pharmaceutical Science,Sun Yat-sen University;

摘要(Abstract):

目的通过一种新的检测方法比较微球释药过程中表面荧光强度的变化,研究聚酯微球的释药机制。方法以异硫氰酸荧光素牛血清白蛋白(FITC-BSA)为模型药物,采用SPG膜乳化法制备聚乳酸-羟基乙酸(PLGA)和m PEG-PLGA微球;以包封率为指标,评价其理化性质;扫描电镜观察微球表面形态;激光共聚焦显微镜(CLSM)观察微球表面荧光强度,并考察微球体外释药行为及降解过程中微球的形态变化。结果 PLGA微球0 d时表面荧光强度较强,微球表面药物分布较多,突释严重,后期微球表面荧光强度均很低,微球表面药物分布少,释放曲线平缓。m PEG-PLGA微球0 d时表面荧光强度较强,微球表面药物分布较多,形成突释,突释后微球表面荧光强度降低,表面药物少,释放进入迟滞期,7 d后微球表面荧光强度增强,表面药物增多,释放加快,30 d时荧光强度降低,药物释放减慢。结论用激光共聚焦显微镜观察微球表面荧光强度的方法可用于研究PLGA微球的释药机制。
OBJECTIVE Elucidating the release mechanism of microspheres by comparing the changes of surface fluorescence during microsphere release. METHODS SPG membrane emulsification method was used to prepare m PEG-PLGA and PLGA microspheres,with FITC-BSA as a model drug. The laser scanning confocal microscope,cold field scanning electron microscope,BCA kit and differential scanning calorimetry were employed to study the in vitro release mechanism of FITC-BSA microspheres. RESULTS Bright fluorescence was observed on the surface of PLGA microspheres at the early stage of the release,and gradually darkened at the later stage of release. m PEG-PLGA microspheres showed typical three-phase release. After the burst release,the fluorescence of the m PEG-PLGA microspheres became darker,and the drug release was accelerated and the fluorescence became bright again when the drug surface was corroded. CONCLUSION The release mechanism of microspheres was successfully characterized by the change of fluorescence intensity of microspheres' surface.

关键词(KeyWords): 微球释药机制;异硫氰酸荧光素牛血清白蛋白;激光共聚焦显微镜;SPG膜乳化法;表面荧光强度
microsphere's release mechanism;FITC-BSA;CLSM;SPG membrane emulsification;surface fluorescence

Abstract:

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基金项目(Foundation): 广东省医院药学研究项目(2015SW12)

作者(Author): 万斯斯;赵萍;罗永梅;郭喆霏;罗宇燕;张永明;
WAN Sisi;ZHAO Ping;LUO Yongmei;GUO Zhefei;LUO Yuyan;ZHANG Yongming;Department of Pharmacy,the Third Affiliated Hospital,Sun Yat-sen University;School of Pharmaceutical Science,Sun Yat-sen University;

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