文獻:Lipid-Polymer Nanoparticles for Folate-Receptor Targeting Delivery of Doxorubicin
作者:Zheng, Mingbin; Gong, Ping; Zheng, Cuifang; Zhao, Pengfei; Luo, Zhenyu; Ma, Yifan; Cai, Lintao
文獻鏈接:https://www.ingentaconnect.com/contentone/asp/jnn/2015/00000015/00000007/art00004
摘要:
A biocompatible PLGA-lipid hybrid nanoparticles (NPs) was developed for targeted delivery of anticancer drugs with doxorubicin (DOX). The hydrodynamic diameter and zeta potential of DOX-loaded PLGA-lipid NPs (DNPs) were affected by the mass ratio of Lipid/PLGA or DSPE-PEG-COOH/Lecithin. At the 1:20 drug/polymer mass ratio, the mean hydrodynamic diameter of DNPs was the lowest (99.2±1.83 nm) and the NPs presented the encapsulation efficiency of DOX with 42.69±1.30%. Due to the folate-receptor mediated endocytosis, the PLGA-lipid NPs with folic acid (FA) targeting ligand showed significant higher uptake by folate-receptor-positive MCF-7 cells as compared to PLGA-lipid NPs without folate. Confocal microscopic observation and flow cytometry analysis also supported the enhanced cellular uptake of the FA-targeted NPs. The results indicated that the FA-targeted DNPs exhibited higher cytotoxicity in MCF-7 cells compared with non-targeted NPs. The lipid-polymer nanoparticles provide a solution of biocompatible nanocarrier for cancer targeting therapy.
開發(fā)了一種生物相容性PLGA-脂質(zhì)雜化納米粒子(NP),用于與阿霉素(DOX)靶向遞送藥物。
DOX負(fù)載的PLGA脂質(zhì)NP(DNPs)的流體動力學(xué)直徑和ζ電位受到脂質(zhì)/PLGA或DSPE-PEG-COOH/卵磷脂質(zhì)量比的影響。
在1:20的藥物/聚合物質(zhì)量比下,DNP的平均流體動力學(xué)直徑低(99.2±1.83 nm),NP的DOX包封效率為42.69±1.30%。
由于葉酸受體介導(dǎo)的內(nèi)吞作用,與不含葉酸的PLGA脂質(zhì)NP相比,具有葉酸(FA)靶向配體的PLGA脂NP顯示出葉酸受體陽性MCF-7細(xì)胞對葉酸的攝取明顯更高。
共聚焦顯微鏡觀察和流式細(xì)胞術(shù)分析也支持FA靶向NP的細(xì)胞攝取增強。
結(jié)果表明,與非靶向NP相比,F(xiàn)A靶向DNPs在MCF-7細(xì)胞中表現(xiàn)出更高的細(xì)胞毒性。脂質(zhì)聚合物納米顆粒為癌癥靶向治療提供了生物相容性納米載體的解決方案。
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