Objective To prepare the PEG-PLGA nanoparticles loaded with vincristine sulfate(VCR-loaded PEG-PLGA-NPs) and evaluate their quality.Methods VCR-loaded PEG-PLGA-NPs were prepared by the double emulsion solvent evaporat...Objective To prepare the PEG-PLGA nanoparticles loaded with vincristine sulfate(VCR-loaded PEG-PLGA-NPs) and evaluate their quality.Methods VCR-loaded PEG-PLGA-NPs were prepared by the double emulsion solvent evaporation method.The main experimental factors,which influenced the physical and chemical properties of the nanoparticles,were investigated and optimized.Results Under optimal conditions,the VCR-loaded PEG-PLGA-NPs had an average diameter of 135.9 nm with narrow size distribution.The encapsulation efficiency was 68.2%,while the drug loading capacity was 8.34%.In vitro,VCR was released from the PEG-PLGA-NPs sustainedly for more than 13 days with the total amount of 81%.Moreover,the VCR-loaded PEG-PLGA-NPs were relatively stable,which was confirmed by the stability testing.Conclusion The VCR-loaded PEG-PLGA-NPs are a promising nano drug with controlled release,which can be applied widely.展开更多
基金the National 863 Hi-tech Project for financial support (2007AA021803, 2007AA021901)
文摘Objective To prepare the PEG-PLGA nanoparticles loaded with vincristine sulfate(VCR-loaded PEG-PLGA-NPs) and evaluate their quality.Methods VCR-loaded PEG-PLGA-NPs were prepared by the double emulsion solvent evaporation method.The main experimental factors,which influenced the physical and chemical properties of the nanoparticles,were investigated and optimized.Results Under optimal conditions,the VCR-loaded PEG-PLGA-NPs had an average diameter of 135.9 nm with narrow size distribution.The encapsulation efficiency was 68.2%,while the drug loading capacity was 8.34%.In vitro,VCR was released from the PEG-PLGA-NPs sustainedly for more than 13 days with the total amount of 81%.Moreover,the VCR-loaded PEG-PLGA-NPs were relatively stable,which was confirmed by the stability testing.Conclusion The VCR-loaded PEG-PLGA-NPs are a promising nano drug with controlled release,which can be applied widely.
文摘儿童急性T淋巴细胞白血病(T-cell acute lymphoblastic leukemia,T-ALL)是T系前体细胞发生恶性转化的一种侵袭性肿瘤,化疗药物的毒副作用及耐药性问题仍然是阻碍其治疗成功的难题。长春新碱(vincristine,VCR)是治疗儿童T-ALL疗效显著的传统化疗药物,但其副作用明显。碳酸锂(Li_(2)CO_(3))可增强其它化疗药物的疗效,但其联合VCR的研究未见报道。该研究旨在探讨Li_(2)CO_(3)联合VCR对2种儿童T-ALL细胞系CCRF-CEM和Jurkat细胞增殖、凋亡及细胞周期的作用。噻唑蓝(thiazolyl blue tetrazolium bromide,MTT)比色法结果显示,与对照组比较,单用VCR或Li_(2)CO_(3),随着其浓度的增加,2种细胞存活率均逐渐降低(P<0.05)。2种细胞在相同Li_(2)CO_(3)浓度下存活率不同(P<0.01)。Li_(2)CO_(3)联合VCR处理细胞存活率与单独VCR组处理相比,2种细胞的细胞存活率和VCR的半抑制浓度(half maximal inhibitory concentration,IC_(50))值降低,Li_(2)CO_(3)与VCR的2药相互作用指数(coefficient of drug interaction,CDI)均小于1。流式细胞仪检测结果发现,对照组、Li_(2)CO_(3)组、VCR组和Li_(2)CO_(3)联合VCR组,2种细胞Li_(2)CO_(3)联合VCR组的G_(2)/M期和凋亡细胞占比最高,Li_(2)CO_(3)联合VCR组和VCR组比,均存在显著性差异(P<0.05)。总之,我们的研究结果提示,Li_(2)CO_(3)与VCR联合促进T-ALL细胞增殖抑制,使细胞周期阻滞于G_(2)/M期,且促进细胞凋亡,结果为儿童T-ALL临床治疗及减少VCR毒副作用提供了新的实验依据,也为其药物研发提供新的思路。
