Drug delivery by nanocarriers requires characterizations of suitable particle size, high drug loading and safety. In this work, we prepared an amphiphilic dendrimer modified PEG-PLA mixed nanoparticles(NPs) by a dou...Drug delivery by nanocarriers requires characterizations of suitable particle size, high drug loading and safety. In this work, we prepared an amphiphilic dendrimer modified PEG-PLA mixed nanoparticles(NPs) by a double emulsion-solvent evaporation(DESE) method. The particle size and drug encapsulation efficacy(EE) were compared to evaluate and optimize the preparation parameters. The mixed NPs had average size ranging from(102±1) nm to(137±5) nm, and the zeta potential turned to positive with incorporation of the amphiphilic dendrimer. The NPs showed different EE of docetaxel(DTX) and paclitaxel(PTX) with higher affinity to more lipophilic PTX. The blank mixed NPs showed little cytotoxicity, and the DTX-loaded NPs could effectively facilitate the antiproliferation activity on PC-3 cells. The NPs could be used as an effective drug delivery system, and its anti-tumor effect is worthy of further study.展开更多
目的制备苦参碱纳米粒及其麦胚凝集素修饰产物。方法复乳化-溶剂挥发法制备苦参碱纳米粒,以聚乳酸-羟基乙酸共聚物与苦参碱比例、转速和聚乙烯醇浓度为影响因素,粒径、电位、包封率和载药量为评价指标,通过星点设计优化工艺。碳二亚胺...目的制备苦参碱纳米粒及其麦胚凝集素修饰产物。方法复乳化-溶剂挥发法制备苦参碱纳米粒,以聚乳酸-羟基乙酸共聚物与苦参碱比例、转速和聚乙烯醇浓度为影响因素,粒径、电位、包封率和载药量为评价指标,通过星点设计优化工艺。碳二亚胺法制备麦胚凝集素修饰苦参碱纳米粒,以碳二亚胺与N-羟基琥珀酰亚胺比例、麦胚凝集素加入量和孵化时间为影响因素,粒径、电位和修饰率为评价指标,通过均匀设计优化工艺。结果苦参碱纳米粒的最佳条件为聚乳酸-羟基乙酸共聚物与苦参碱比例0.594∶1,转速815 r/min,聚乙烯醇浓度为0.46%,平均粒径、电位、包封率和载药量分别为112.04 nm、-15.38 m V、90.05%和27.14%。其麦胚凝集素修饰产物的最佳条件为碳二亚胺与N-羟基琥珀酰亚胺比例2.8∶0.12,麦胚凝集素加入量3 mg,孵化时间14 h,平均粒径、电位和修饰率分别为474.7 nm、-5.2 m V和69.51%。结论该制备工艺可靠,所得苦参碱纳米粒及其麦胚凝集素修饰产物性质稳定。展开更多
基金National Natural Science Foundation of China(Grant No.81473156,81673365,81273454)Doctoral Foundation of the Ministry of Education(Grant No.20130001110055)National Key Basic Research Program(Grant No.2013CB932501)
文摘Drug delivery by nanocarriers requires characterizations of suitable particle size, high drug loading and safety. In this work, we prepared an amphiphilic dendrimer modified PEG-PLA mixed nanoparticles(NPs) by a double emulsion-solvent evaporation(DESE) method. The particle size and drug encapsulation efficacy(EE) were compared to evaluate and optimize the preparation parameters. The mixed NPs had average size ranging from(102±1) nm to(137±5) nm, and the zeta potential turned to positive with incorporation of the amphiphilic dendrimer. The NPs showed different EE of docetaxel(DTX) and paclitaxel(PTX) with higher affinity to more lipophilic PTX. The blank mixed NPs showed little cytotoxicity, and the DTX-loaded NPs could effectively facilitate the antiproliferation activity on PC-3 cells. The NPs could be used as an effective drug delivery system, and its anti-tumor effect is worthy of further study.
文摘目的制备苦参碱纳米粒及其麦胚凝集素修饰产物。方法复乳化-溶剂挥发法制备苦参碱纳米粒,以聚乳酸-羟基乙酸共聚物与苦参碱比例、转速和聚乙烯醇浓度为影响因素,粒径、电位、包封率和载药量为评价指标,通过星点设计优化工艺。碳二亚胺法制备麦胚凝集素修饰苦参碱纳米粒,以碳二亚胺与N-羟基琥珀酰亚胺比例、麦胚凝集素加入量和孵化时间为影响因素,粒径、电位和修饰率为评价指标,通过均匀设计优化工艺。结果苦参碱纳米粒的最佳条件为聚乳酸-羟基乙酸共聚物与苦参碱比例0.594∶1,转速815 r/min,聚乙烯醇浓度为0.46%,平均粒径、电位、包封率和载药量分别为112.04 nm、-15.38 m V、90.05%和27.14%。其麦胚凝集素修饰产物的最佳条件为碳二亚胺与N-羟基琥珀酰亚胺比例2.8∶0.12,麦胚凝集素加入量3 mg,孵化时间14 h,平均粒径、电位和修饰率分别为474.7 nm、-5.2 m V和69.51%。结论该制备工艺可靠,所得苦参碱纳米粒及其麦胚凝集素修饰产物性质稳定。