紫杉醇冻干纳米乳的制备及理化性质

Development and Characterization of Lyophilized Paclitaxel Nanoemulsions

目的:制备紫杉醇冻干纳米乳,研究其体外理化性质。方法:以外观和重分散性为指标,对紫杉醇冻干纳米乳所使用的冻干保护剂进行了筛选,考察了纳米乳滴的形态、粒径和ζ电位以及制剂的含量和有关物质,并对最优处方进行了加速稳定性试验。结果:选用甘露醇作为冻干保护剂较好,甘氨酸可提高冻干纳米乳的外观和重分散性能。60℃加速稳定性考察结果表明,紫杉醇冻干纳米乳各项指标变化不大。结论:冻干纳米乳不仅解决了紫杉醇的水溶性问题,而且解决了其化学不稳定性。

AIM: To develop and characterize lyophilized paclitaxel nanoemulsions. METHOD: The protection reagent of the lyophilized nanoemulsions was screened by observing the appearance and the ability to disperse of the powder. The shape, particle size, zeta potential, content and related substances of the reconstituted nanoemulsions were also examined. The accelerating test of nanoemulsions was carried under 60 ℃ at last. RESULT: Mannose is the proper excipient for the lyophilized paclitaxel nanoemulsions, and glycin can enhance their quality. After accelerating test under 60 ℃, the index of the lyophilized paclitaxel nanoemulsions didn't change much. CONCLUSION: Lyophilized paclitaxel nanoemulsions could not only solved the problem of its solubility, but also enhance its chemical stability.