The Shenzhen Key Laboratory of Gene and Antibody Therapy, Center for Biotech and Bio-Medicine and Division of Life Sciences, Graduate School at Shenzhen, Tsinghua University, Shenzhen, People's Republic of China.
Nanomedicine. 2010 Feb;6(1):170-8. doi: 10.1016/j.nano.2009.05.004. Epub 2009 May 15.
The aim of this work was to investigate the effect of triblock copolymer poloxamer 188 on nanoparticle morphology, size, cancer cell uptake, and cytotoxicity. Docetaxel-loaded nanoparticles were prepared by oil-in-water emulsion/solvent evaporation technique using biodegradable poly(lactic-co-glycolic acid) (PLGA) with or without addition of poloxamer 188, respectively. The resulting nanoparticles were found to be spherical with a rough and porous surface. The nanoparticles had an average size of around 200 nm with a narrow size distribution. The in vitro drug-release profile of both nanoparticle formulations showed a biphasic release pattern. An increased level of uptake of PLGA/poloxamer 188 nanoparticles in the docetaxel-resistant MCF-7 TAX30 human breast cancer cell line could be found in comparison with that of PLGA nanoparticles. In addition, the docetaxel-loaded PLGA/poloxamer 188 nanoparticles achieved a significantly higher level of cytotoxicity than that of docetaxel-loaded PLGA nanoparticles and Taxotere (P < .05). In conclusion, the results showed advantages of docetaxel-loaded PLGA nanoparticles incorporated with poloxamer 188 compared with the nanoparticles without incorporation of poloxamer 188 in terms of sustainable release and efficacy in breast cancer chemotherapy.
The effects of poloxamer 188, a triblock copolymer were studied on nanoparticle morphology, size, cancer cell uptake and cytotoxicity. An increased level of uptake of PLGA/poloxamer 188 nanoparticles in resistant human breast cancer cell line was demonstrated, resulting in a significantly higher level of cytotoxicity.
研究三嵌段共聚物泊洛沙姆 188 对纳米粒形态、大小、癌细胞摄取和细胞毒性的影响。方法:采用乳化/溶剂挥发技术,分别使用可生物降解的聚乳酸-共-羟基乙酸(PLGA)和泊洛沙姆 188 制备载多西紫杉醇纳米粒。结果:所得纳米粒呈球形,表面粗糙多孔。纳米粒平均粒径约为 200nm,粒径分布较窄。两种纳米粒制剂的体外药物释放均呈现两相释放模式。与 PLGA 纳米粒相比,耐多西紫杉醇 MCF-7 TAX30 人乳腺癌细胞系对 PLGA/泊洛沙姆 188 纳米粒的摄取水平显著增加。此外,载多西紫杉醇 PLGA/泊洛沙姆 188 纳米粒的细胞毒性明显高于载多西紫杉醇 PLGA 纳米粒和 Taxotere(P<0.05)。结论:与未加入泊洛沙姆 188 的纳米粒相比,载多西紫杉醇 PLGA 纳米粒加入泊洛沙姆 188 具有可持续释放和增强乳腺癌化疗疗效的优势。
研究了三嵌段共聚物泊洛沙姆 188 对纳米粒形态、大小、癌细胞摄取和细胞毒性的影响。在耐药人乳腺癌细胞系中,PLGA/泊洛沙姆 188 纳米粒的摄取水平增加,导致细胞毒性显著升高。