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叶酸修饰的 PLGA-PEG 纳米粒对子宫内膜癌的治疗效果改善。

Improved therapeutic effect of folate-decorated PLGA-PEG nanoparticles for endometrial carcinoma.

机构信息

Department of Obstetrics and Gynecology, Third Affiliated Hospital of Sun Yat-sen University, Guangzhou, China.

出版信息

Bioorg Med Chem. 2011 Jul 1;19(13):4057-66. doi: 10.1016/j.bmc.2011.05.016. Epub 2011 May 18.

Abstract

Folate (FOL) mediated poly-lactide-co-glycolide-polyethylene glycol nanoparticles (FOL-PEG-PLGA NPs) bearing paclitaxel (PTX) were prepared for the effective delivery of drug to endometrial carcinoma. The average size, zeta potential and encapsulation efficiency of FOL-targeted NPs were found to be around 220 nm, -30.43 mV and 95.6%. Cellular uptake was observed. The accumulation of FOL-targeted NPs depends on dual effects of passive and active targeting. The FOL-targeted PTX NPs showed a greater cytotoxicity against HEC-1A cancer cells in vitro and in vivo, which might be induced by apoptosis. H&E staining did not showed apparent tissue damage to liver and kidney of the mice after injecting NPs intravenously. These results suggest that the novel FOL-PEG-PLGA NPs could be a potential delivery system with excellent therapeutic efficacy for targeting the drugs to cancer cells.

摘要

载紫杉醇的叶酸偶联聚乳酸-乙醇酸共聚物-聚乙二醇纳米粒的制备及其用于子宫内膜癌的靶向给药研究。载紫杉醇的叶酸偶联聚乳酸-乙醇酸共聚物-聚乙二醇纳米粒的平均粒径、Zeta 电位和包封率分别约为 220nm、-30.43mV 和 95.6%。观察到细胞摄取。叶酸靶向纳米粒的积累取决于被动和主动靶向的双重作用。叶酸靶向紫杉醇纳米粒在体外和体内对 HEC-1A 癌细胞表现出更强的细胞毒性,这可能是由细胞凋亡引起的。静脉注射纳米粒后,H&E 染色未显示小鼠肝、肾组织明显损伤。这些结果表明,新型叶酸-PEG-PLGA 纳米粒可能是一种具有良好治疗效果的新型给药系统,可将药物靶向递送至癌细胞。

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