| 引用本文: | 许浩云,谢黎崖,常迪,侯振清,柯金珍.改良透析法制备MePEG-PLGA-羟基喜树碱共聚物纳米粒[J].中国现代应用药学,2016,33(6):746-751. |
| XU Haoyun,XIE Liya,CHANG Di,HOU Zhenqing,KE Jinzhen.Preparation of MePEG-PLGA Hydroxy Camptothecin Nanoparticles by Improved Dialysis Method[J].Chin J Mod Appl Pharm(中国现代应用药学),2016,33(6):746-751. |
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| 摘要: |
| 目的 以聚合物单甲氧基聚乙二醇-聚乳酸聚乙醇酸(MePEG-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(MePEG-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MePEG-PLGA投料质量比为1∶5。优化制备的MePEG-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)mV，载药量为7.42%，包封率为44.5%。结论 改良透析法适合MePEG-PLGA-HCPT-NPs的制备，为后续研究奠定了良好的基础。 |
| 关键词: 羟基喜树碱 甲氧基封端的聚乙二醇-聚乳酸聚乙醇酸 纳米粒 透析法 |
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| 基金项目:福建省医药卫生科技创新项目(2014-CXB-35) |
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| Preparation of MePEG-PLGA Hydroxy Camptothecin Nanoparticles by Improved Dialysis Method |
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XU Haoyun1, XIE Liya1, CHANG Di2, HOU Zhenqing2, KE Jinzhen1
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1.First Affiliated Hospital of Xiamen University, Xiamen 361003, China;2.Research Center of Biomedical Engineering of Xiamen University, Xiamen 361005, China
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| Abstract: |
| OBJECTIVE To prepare methoxyl poly(ethylene glycol)-poly(lactic-co-glycolic acid)-hydroxy camptothecin nanoparticles(MePEG-PLGA-HCPT-NPs) by an improved dialysis method, and to characterize the nanoparticles. METHODS Using drug-loading and diameter as indexes, each single factor test was used to optimize the preparation technology. The appearance, diameter, Zeta potential, drug-loading and entrapment efficiency were investigated. RESULTS The optimal preparation conditions for MePEG-PLGA-HCPT-NPs were as follows: initial organic solvents was acetone; temperature was 25 ℃; initial water content was 1%; pH of external phase was 4.0; initial copolymer concentration was 3 mg·mL-1; PEG content of copolymer was 15%; lactic acid content of copolymer was 100 %; the ratio of HCPT to MePEG-PLGA was 1∶5. Based on these experimental results, it was proposed that MePEG-PLGA-HCPT-NPs exhibited a solid spherical shape, fairly uniform size, well dispersed, and relatively smooth surface with core-shell structure. The average particle diameter was (120.1±2.4)nm, polydispersity was 0.057±0.021, Zeta potential was (-31.2±0.98)mV, the drug-loading was 7.42% and the entrapment efficiency respectively was 44.5%. CONCLUSION The improved dialysis method is suitable to prepare the MePEG-PLGA-HCPT-NPs, and it can lay a foundation for the future tests. |
| Key words: hydroxyl camptothecin methoxyl poly(ethylene glycol)-poly(lactic-co-glycolic acid) nanoparticles dialysis method |
