摘要
用乳化-溶剂挥发法制备尼莫地平(nimodipine,NMP)PLGA微球,在油相中引入石油醚与二氯甲烷作混合溶剂,考察了石油醚对微球性质的影响。石油醚与二氯甲烷的不同体积比(0,1∶10,1∶8,1∶4和1∶2)可调节微球的固化速率,从而得到不同特性的载药微球。混合比为1∶10时,微球突释效应减轻,包封率显著提高。以PLGA浓度、投药比及混合溶剂比为考察因素进行了正交优化设计。结果表明优化后微球包封率提高52.2%,突释率降低58.8%,药物以无定形态存在于微球中,与单一溶剂组相比,微球形态有较大改善,微球缓释效应显著增强。
The effect of petroleum ether,as an organic phase co-solvent,on the characteristics of nimodipine（NMP）-loaded poly（lactide-co-glycolide）（PLGA） microspheres prepared via the emulsion-solvent evaporation/extraction process was studied.Different ratio of petroleum ether to dichloromethane（DCM）（0,1∶10,1∶8,1∶4,and 1∶2,v/v） caused different solidification rate,leading to different properties of microspheres.At the ratio of 1∶10,the initial burst of microspheres was attenuated,and the encapsulation efficiency was improved significantly.To perform the orthogonal design for process optimization,polymer concentration,drug/PLGA ratio and ratio of petroleum ether/DCM were set as the factors for investigation.After optimization,the encapsulation efficiency of microspheres was improved by 52.2%,and the initial burst was declined by 58.8%.Drug was encapsulated in the matrix as amorphous state.Compared with microspheres prepared by single solvent,the morphology of the optimal formulation was modified evidently,therefore NMP was released in a more controlled fashion.
出处
《化学工业与工程》
CAS
2013年第1期1-7,共7页
Chemical Industry and Engineering
基金
国家自然科学基金(20836005
21176173)
关键词
微球
潜溶剂
石油醚
形态
体外释放
microspheres
co-solvent
petroleum ether
morphology
in vitro release
