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目的 制备羟基喜树碱长循环纳米粒并采用星点设计-效应面法筛选制备工艺。方法 以单甲氧基聚乙二醇-聚乳酸-羟基乙酸聚合物作为包封材料,采用改良的乳化-溶剂挥发法制备长循环纳米粒,以包封率与载药量作为评价指标,采用Design-Expert V8.0.6软件进行星点设计,考察了羟基喜树碱的浓度、单甲氧基聚乙二醇-聚乳酸-羟基乙酸聚合物(mPEG_(2000)-PLGA)浓度、水相与有机相的体积比因素对评价指标的影响,并应用效应面法得到最佳制备工艺。结果 羟基喜树碱长循环纳米粒的最佳工艺为:羟基喜树碱浓度为1.41 mg·mL~(-1),mPEG_(2000)-PLGA浓度为3.86 mg·mL~(-1),水相与有机相的体积比为9.90∶1。制备的长循环纳米粒包封率为35.14%,载药量为2.10%,平均粒径为154.10 nm,电位为-38.61 mV。结论 所优化的工艺方法简便、稳定可行,适用于羟基喜树碱长循环纳米粒的制备。
Objective To prepare hydroxycamptothecin long-circulating nanoparticles and use star-spot design-response surface method to screen the preparation process. Methods Monomethoxy polyethylene glycol - polylactic acid - glycolic acid polymer was used as encapsulation material. The modified emulsification - solvent evaporation method was used to prepare long circulating nanoparticles. The entrapment efficiency and drug loading were used as evaluation indexes. Design-Expert V8.0.6 software was used to design the star point. The concentration of hydroxycamptothecin, the concentration of monomethoxy polyethylene glycol-polylactic acid-glycolic acid polymer (mPEG_ (2000) -PLGA) The volume ratio of organic phase factors on the evaluation index, and the effect of surface area method to obtain the best preparation process. Results The optimum conditions of hydroxycamptothecin long-circulating nanoparticles were as follows: the concentration of hydroxycamptothecin was 1.41 mg · mL -1, the concentration of mPEG_ (2000) -PLGA was 3.86 mg · mL -1, The volume ratio of phase to organic phase is 9.90: 1. The entrapment efficiency of long circulating nanoparticles was 35.14% and the drug loading was 2.10%. The average particle size was 154.10 nm and the potential was -38.61 mV. Conclusion The optimized process is simple, stable and feasible, and is suitable for the preparation of long-circulating hydroxycamptothecin nanoparticles.