挤出法制备卡巴他赛脂质体的工艺优化

目的 对挤出法制备卡巴他赛脂质体的挤出工艺进行优化。方法 以产品的平均粒径（MD）和多分散指数（PDI）为评价指标，采用正交设计法和部分正交析因法来筛选最优工艺参数。结果 最优挤出工艺参数为：核孔膜组合200 nm + 80 nm（单层或双层），挤出次数组合3 + 3或3 + 2，挤出温度10 ~ 23 ℃，挤出时间控制在18 h内，挤出压力0.5 ~ 1.2 MPa。结论 采用最优挤出工艺参数可以成功制得MD值和PDI值均符合规定标准且储存稳定性良好的卡巴他赛脂质体产品。

Optimization of preparation process of cabazitaxel liposomes by extrusion method

Objective To evaluate the possibility of achieving long-term diffusion-based delivery of proanthocyanidins (PAC) via surface-mediated method.Methods PAC was dissolved in deionized water, and the PAC aqueous solution was mixed with chloroform. The mixture was then emulsified by using the ultrasonic emulsification instrument to make the inverse emulsion with PAC dispersed in the emulsion droplets. The as-prepared inverse emulsion was cast onto the flat film made from polystyrene under the environmental condition of high humidity. After complete solidification, the obtained film was rendered with multi-layered porous structure. Drug release profiling experiments were performed by immersing the PAC-loaded film in phosphate buffer saline (PBS). At the predetermined time-points, the PBS solutions were analyzed by ultraviolet-visible spectrophotometry to calculate the percentage of PAC release. Testing period lasted for 28 days. Results By using the inverse-emulsion casting method, PAC-loaded polymeric film with asymmetric multi-layered micro-porous structures was facilely prepared. Dynamic morphological manipulation on the created porous structures was achieved by tuning the composition of the casting emulsion. By using fluorescent probe combined with confocal laser scanning microscopy, the hydrophilic component was proved to be efficiently dispersed within the porous structures both in the surface and bulk layers. The PAC-loaded film samples with different features of multi-layered porous structures were proved to be able to achieve sustained drug release behavior for more than 28 days, following Fickian diffusion mechanism.Conclusion By the design of porous film or coating as drug carriers, the effective drug loading and long-lasting drug delivery could be achieved. It provides insight for the construction of an efficient and flexible drug delivery platform.