紫杉醇冻干脂质体的制备及含量稳定性

目的制备水化后粒径较小且分布较窄的,具有良好稳定性的紫杉醇冻干脂质体。方法以商品大豆磷脂为膜材,采用薄膜分散-微孔滤膜挤出(或高压均质)-冷冻干燥工艺制备冻干脂质体产品,采用HPLC和微柱离心-HPLC法测定冻干脂质体重建后的含量及包封率。并以加速和长期实验来证实该产品的稳定性。结果薄膜分散-微孔滤膜挤出-冷冻干燥工艺制备的紫杉醇冻干脂质体粒径均一,在130 nm左右,其对药物的包封率较高,可保证在90%以上,储存半年后紫杉醇的含量及包封率均未有降低。结论薄膜分散-微孔滤膜挤出-冷冻干燥工艺是制备紫杉醇脂质体的可工业化生产的方法。

Preparation and content stability of freeze-dried liposomal paclitaxel

Objective To prepare stable freeze-dried liposomal paclitaxel with small and narrow-distributed particle sizes when reconstituted by water. Methods Liposomal paclitaxel with commercial soybean phospholipids as membrane material was prepared by membrane distribution-micromembrane extruding-freeze drying process.HPLC and minicolumn-centrifuge method was employed to determined the content and encapsulation efficiency of the reconstituted liposome.The stability of content and encapsulation efficiency of paclitaxel in liposome was evaluated by accelerated and long term experiment.Results The encapsulation efficiency was high by employing this method which was ensured to be above 90%.The content and encapsulation efficiency showed no decrease after storage for half a year. Conclusions The preparing process is a practical one to produce liposomal paclitaxel in industrial scale.