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目的:对N-三甲基壳聚糖(TMC60)包衣羟喜树碱脂质体(HCPTL)冻干剂的处方及制备工艺进行优化。方法:采用逆向蒸发法制备HCPTL,并用TMC60包衣,经高压乳匀得到纳米级脂质体。以包封率为考察指标,正交试验优选处方及工艺,并筛选最佳的冻干保护剂进行冷冻干燥。对复水化后脂质体的形态、Zeta电位、粒径等进行考察。结果:TMC60包衣HCPTL的最佳处方及工艺为:药脂比为1:30,胆固醇:卵磷脂为1:3,旋蒸温度为35℃,TMC60浓度为0.35%,最佳冻干保护剂为15%(w/v)的海藻糖。复水化后形态圆整,平均包封率为(82.2±2.3)%(n=3),Zeta电位为(53.2±2.0)mV,平均粒径为(92.4±18.5)nm。结论:TMC60包衣HCPTL冻干剂具有包封率高,表面带正电荷等特点,为其进一步研究奠定了基础。
OBJECTIVE: To optimize the formulation and preparation of hydroxyapatite liposome (HCPTL) lyophilized agent of N-trimethyl chitosan (TMC60). Methods: HCPTL was prepared by reverse evaporation method and coated with TMC60. Nanoscale liposomes were obtained by high pressure homogenization. Taking the entrapment efficiency as the index, orthogonal test was conducted to optimize the prescription and process, and the best lyoprotectant was selected for freeze-drying. The morphology, Zeta potential and particle size of the reconstituted liposomes were investigated. Results: The optimum formulation and process of coating HCPTL on TMC60 were as follows: the ratio of lipid to lipid was 1:30, the ratio of cholesterol to lecithin was 1: 3, the temperature was 35 ℃ and the concentration of TMC60 was 0.35%. The best lyoprotectant 15% (w / v) trehalose. The average entrapment efficiency was (82.2 ± 2.3)% (n = 3) and the zeta potential was (53.2 ± 2.0) mV and the average particle diameter was (92.4 ± 18.5) nm. Conclusion: HCPTL freeze-dried TMC60 coated with high encapsulation efficiency, the surface with a positive charge, and laid the foundation for further study.