叶酸介导肿瘤靶向紫杉醇纳米粒冷冻干燥工艺及其表征

Characteristics of Freeze-dried Folate-decorated Paclitaxel-loaded Bovine Serum Albumin Nanoparticles

目的:研究了叶酸介导紫杉醇白蛋白纳米粒的冻干工艺及其表征。方法:选用甘露醇、牛血清白蛋白及海藻糖三种冻干保护剂,以叶酸介导紫杉醇白蛋白纳米粒冻干前与复溶后聚集状态(平均粒径和多分散系数)、表观形态、稳定性系数fc及Zeta电位为指标,筛选冻干保护的合适浓度,并考察在适当浓度下纳米粒微观形态及复溶后8小时连续稳定性。结果:三种冻干保护剂在浓度不小于1%时起到保护作用。与无保护剂样品相比,冻干后紫杉醇纳米粒粒径更小,分布范围更窄,能够在水相中充分溶解,且在复溶后连续8小时内有良好的稳定性。结论:通过对叶酸介导紫杉醇白蛋白纳米粒冻干工艺及表征的研究,证明合适的冻干保护剂浓度条件下可以获得稳定的紫杉醇纳米粒冻干注射剂。

Objective：Aim of this study was to investigate folate - decorated paclltaxel - load bovine serum albumin nano- particles（ PTX - FA - BSANPs） lyophilizing process and its characteristics. Methods： PTX - FA - BSANPs aggregation state （average particle size and polydispersity）, the apparent trait and the Zeta potential as an indicator which screened the protective effect of various types and concentrations of lyoprotectant. Results：The concentration of mannitol, bovine serum albumin and trehalose was not less than 1% playing a protective role. PTX - FA - BSANPs compared with no lyprotectant had a smal- ler particle size and polydispersity. The samples can be sufficienfly dissolved in the aqueous phase, and has a better stability. Conclusion： A stable PTX - FA - BSANPs lyophilization could be obtained with appropriate concentration and lyoph- ilization conditions through screening freeze - drying process and its characteristics.