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目的以聚合物单甲氧基聚乙二醇-聚乳酸聚乙醇酸(Me PEG-PLGA)为载体,羟基喜树碱(hydroxy camptothecin,HCPT)为模型药物,采用改良的透析法优化制备单甲氧基聚乙二醇-聚乳酸聚乙醇酸-羟基喜树碱共聚物纳米粒(Me PEG-PLGA-HCPT-NPs),并进行表征。方法以粒径和载药量为指标,考察各影响因素优化制备工艺。并进行外观、粒径、Zeta电位、载药量和包封率的测定。结果优化制备条件:丙酮作为溶剂,透析温度为25℃,透析初始含水量为1%,透析外水相pH=4.0,聚合物浓度为3 mg·mL~(-1),载体中的PEG含量为15%,载体中的乳酸含量为100%,HCPT与Me PEG-PLGA投料质量比为1∶5。优化制备的Me PEG-PLGA-HCPT-NPs为实心球形壳核结构,表面圆滑,粒径分布均一,分散性好,平均粒径(120.1±2.4)nm,多分散系数为0.057±0.021,Zeta电位为(-31.2±0.98)m V,载药量为7.42%,包封率为44.5%。结论改良透析法适合Me PEG-PLGA-HCPT-NPs的制备,为后续研究奠定了良好的基础。
OBJECTIVE To investigate the protective effect of Meca-PGA on the growth of monopodiacetic acid induced by mono-methoxypolyethylene glycol-polylactic acid polyglycolic acid (Me PEG-PLGA) and hydroxy camptothecin (HCPT) (PEG-PLGA-HCPT-NPs) nanoparticles were synthesized and characterized. Methods Taking the particle size and drug loading as indexes, the influencing factors were investigated to optimize the preparation process. And the appearance, particle size, Zeta potential, drug loading and encapsulation efficiency were measured. Results The optimum preparation conditions were as follows: acetone as solvent, dialysis temperature 25 ℃, dialysis initial water content 1%, dialysis external aqueous phase pH = 4.0, polymer concentration 3 mg · mL -1, carrier PEG content Is 15%, the content of lactic acid in the carrier is 100%, the mass ratio of HCPT to Me PEG-PLGA is 1: 5. The optimized preparation of Me PEG-PLGA-HCPT-NPs was a solid spherical shell structure with smooth surface, uniform particle size distribution, good dispersibility, average particle size (120.1 ± 2.4) nm, polydispersity coefficient of 0.057 ± 0.021, (-31.2 ± 0.98) mV, drug loading was 7.42%, encapsulation efficiency was 44.5%. Conclusion The modified dialysis method is suitable for the preparation of Me PEG-PLGA-HCPT-NPs, which lays a good foundation for the follow-up study.