Paclitaxel loaded folic acid targeted nanoparticles of mixed lipid-shell and polymer-core: In vitro and in vivo evaluation

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• 作者：Peiqi Zhao^a ; ^b ; ¹ ; Hanjie Wang^c ; ¹ ; Man Yu^d ; Zhenyu Liao^c ; Xianhuo Wang^b ; Fei Zhang^a ; Wei Ji^a ; Bing Wu^a ; Jinghua Han^a ; Haichang Zhang^a ; Huaqing Wang^b ; Jin Chang^c ; ^{jinchang@tju.edu.cn} ; Ruifang Niu^a ; ^{niurf1982@yahoo.com.cn}
• 关键词：CLSM ; confocal laser scanning microscopy ; DCM ; dichloromethane ; DLS ; dynamic light scattering ; DMSO ; dimethyl sulfoxide ; EPR ; enhanced permeability and retention ; FA ; folic acid ; FITC ; fluorescein isothiocyanate ; FLPNPs ; folic acid modified lipid-shell an
• 刊名：European Journal of Pharmaceutics and Biopharmaceutics
• 出版年：2012
• 期刊代码：16_09396411
• 类别：pha
• 出版时间：June, 2012
• 卷：81
• 期：2
• 页码：248-256
• 文件大小：1108 K

摘要

A functional drug carrier comprised of folic acid modified lipid-shell and polymer-core nanoparticles (FLPNPs) including poly(d,l-lactide-co-glycolide) (PLGA) core, PEGylated octadecyl-quaternized lysine modified chitosan (PEG-OQLCS) as lipid-shell, folic acid as targeting ligand and cholesterol was prepared and evaluated for targeted delivery of paclitaxel (PTX). Confocal microscopy analysis confirmed the coating of the lipid-shell on the polymer-core. Physicochemical characterizations of FLPNPs, such as particle size, zeta potential, morphology, encapsulation efficiency, and in vitro PTX release, were also evaluated. The internalization efficiency and targeting ability of FLPNPs were demonstrated by flow cytometry and confocal microscopy. PTX loaded FLPNPs showed a significantly higher cytotoxicity than the commercial PTX formulation (Taxol庐). The intravenous administration of PTX encapsulated FLPNPs led to tumor regression and improvement of animal survival in a murine model, compared with that observed with Taxol庐 and biodistribution study showed that PTX concentration in tumor for PTX encapsulated FLPNPs was higher than other PTX formulations. Our data indicate that PTX loaded FLPNPs are a promising nano-sized drug formulation for cancer therapy.