摘要
目的研制具有肺靶向性的紫杉醇壳聚糖微球,并对处方工艺进行优化。方法以壳聚糖为载体,采用乳化-化学交联法制备紫杉醇壳聚糖微球。单因素试验考察了油/水体积比、紫杉醇浓度、乳化时间、乳化剂量等因素,采用正交设计优化微球制备工艺,以HPLC法测定微球载药量、包封率。结果制得的微球显微观察形态圆整、表面光滑,无黏连;平均粒径为(8.23±0.25)μm,粒径在7～12μm平均占微球总数的84.2%,载药量为16.20%±1.15%,包封率为81.29%±1.62%。结论筛选的最佳处方工艺制备的微球粒径大小适宜,可满足肺靶向微球的要求并免除过敏试剂的加入。
Objective To prepare the paclitaxel-chitosan microspheres with lung targeting, and to screening out the best preparation technology. Methods With chitosan as carrier, paclitaxel-chitosan microspheres were prepared by emulsion-chemical cross-linking method. The formulation and preparation technique was optimized by orthogonal experiment accorded to the results of single-factor selecting experiment. Then HPLC was introduced to determine the drug loading dose and encapsulation efficiency of microspheres. Results The microspheres were round, smooth with no adhesion in microscopy. The average particle size was （8.23 ±0.25） μm, 84.2% of which were in the range of 7 -12 μm, with drug loading dose as 16.20% ±1. 15% and encapsulation efficiency as 81.29% ± 1.62%. Conclusion Selection of the best prescription of preparation process for particle size suitable can meet the requirements of lung targeting microspheres and relieves allergic agent added.
出处
《今日药学》
CAS
2013年第9期565-569,共5页
Pharmacy Today
基金
广东省医院药学研究基金--ABI专项(编号:2010A25)
关键词
紫杉醇
壳聚糖
制备工艺
肺靶向微球
paclitaxel
chitosan
preparation technique
lung targeting microspheres
