摘要
以普朗尼克F127-壳聚糖聚合物(F127-CS)和胆酸钠(NaC)为载体制备载紫杉醇的口服聚电解质复合物胶束,考察其理化性质并对其体外释药特征进行探究。用薄膜超声法制备紫杉醇口服聚电解质复合物胶束,单因素考察和均匀设计实验筛选最优制备工艺,通过高效液相色谱法对载药量进行测定,采用激光散射粒度测定仪测定粒径及Zeta电位,透射电镜观察其外观形态,芘荧光探针法测定其临界胶束浓度,并对其体外释放情况进行动态膜透析法考察。紫杉醇口服聚电解质复合物胶束的平均粒径为62.8 nm,Zeta电位为-0.46 mV,载药量为14.6%,临界胶束浓度约为2.5×10-3mol/L。电镜照片显示胶束圆整完整,罕有粘连。体外释放结果显示,在人工胃肠液中,紫杉醇F127-CS/NaC聚电解质复合物胶束组的释放均明显优于紫杉醇注射液组。F127-CS/NaC口服聚电解质复合物胶束具有较高的载药量,并能延缓药物的释放,是一种较为理想的紫杉醇释药系统。
Paclitaxel（PTX）-loaded polyion micellae was prepared with Pluronic F127-chitosan polymer（F127-CS） to improve the poor solubility of PTX and in vitro evaluation was studied to testify the possibility of enhancing bioavailability via oral medication.Paclitaxel-loaded polyion micellae were prepared by film-ultrasonic method.Preparation technique and optimal formulation were selected via single factor investigation and uniform design.Diameter distribution and Zeta potential of polyion micellae were measured using laser size scattering determinator.Drug loading capacity（DL%） was determined by high performance liquid chromatography（HPLC）.Morphology of polyion micellae was observed under transmission electron microscope.Critical micelle concentration（CMC） was detected via pyrene fluorescence probe method.In vitro release behavior was evaluated by dialysis method.The results showed spherical micellae with an average diameter of 62.8 nm and Zeta potential of-0.46 mV.Drug loading capacity（DL%） was about 14.6% with the optimal formulation.CMC detection confirmed F127-CS/NaC polyion micellae a lower CMC of 2.5 × 10-3mol/L contrasted with NaC micelles.In vitro release study suggested that PTX-loaded F127-CS/NaC micellae was remarkably superior than that of the PTX injection.F127-CS/NaC polyion micellae is a potential drug delivery system for oral administration of PTX.
出处
《药物生物技术》
CAS
2014年第1期31-36,共6页
Pharmaceutical Biotechnology
基金
山东省科技攻关项目(No.2008GG10002028)
