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学科主题: 药学
题名:
Folate-mediated targeted and intracellular delivery of paclitaxel using a novel deoxycholic acid-O-carboxymethylated chitosan-folic acid micelles
作者: Wang, Feihu1; Chen, Yuxuan2; Zhang, Dianrui1; Zhang, Qiang3; Zheng, Dandan1; Hao, Leilei1; Liu, Yue1; Duan, Cunxian1; Jia, Lejiao1; Liu, Guangpu1
关键词: paclitaxel ; folate ; polymeric micelles ; targeted delivery
刊名: INTERNATIONAL JOURNAL OF NANOMEDICINE
发表日期: 2012
DOI: 10.2147/IJN.S27823
卷: 7, 页:325-337
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Nanoscience & Nanotechnology ; Pharmacology & Pharmacy
研究领域[WOS]: Science & Technology - Other Topics ; Pharmacology & Pharmacy
关键词[WOS]: CONJUGATED POLYMER MICELLES ; ANTICANCER DRUGS ; TUMOR PH ; NANOPARTICLES ; COPOLYMER ; CARRIER ; SYSTEM
英文摘要:

Background: A critical disadvantage for successful chemotherapy with paclitaxel (PTX) is its nontargeting nature to cancer cells. Folic acid has been employed as a targeting ligand of various anticancer agents to increase their cellular uptake within target cells since the folate receptor is overexpressed on the surface of such tumor cells. In this study, a novel biodegradable deoxycholic acid-O-carboxymethylated chitosan-folic acid conjugate (DOMC-FA) was used to form micelles for encapsulating the anticancer drug PTX.

Methods and results: The drug-loading efficiency, encapsulation efficiency, in vitro drug release and physicochemical properties of PTX-loaded micelles were investigated in detail. In vitro cell culture studies were carried out in MCF-7 cells, a human breast carcinoma cell line, with folate receptor overexpressed on its surface. An increased level of uptake of folate-conjugated micelles compared to plain micelles in MCF-7 cells was observed, and the enhanced uptake of folate-micelles mainly on account of the effective process of folate receptor-mediated endocytosis. The MTT assay, morphological changes, and apoptosis test implied that the folate-conjugated micelles enhanced the cell death by folate-mediated active internalization, and the cytotoxicity of the FA-micellar PTX (DOMC-FA/PTX) to cancer cells was much higher than micelles without folate (DOMC/PTX) or the commercially available injectable preparation of PTX (Taxol).

Conclusion: Results indicate that the PTX-loaded DOMC-FA micelle is a successful anticancer-targeted drug-delivery system for effective cancer chemotherapy.

语种: 英语
所属项目编号: 2009CB930300
项目资助者: National Basic Research Program of China (973Program)
WOS记录号: WOS:000302705900001
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/67174
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Shandong Univ, Coll Pharm, Dept Pharmaceut, Jinan 250012, Peoples R China
2.Shenzhou Hosp, Dept Pharm, Shenyang, Peoples R China
3.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China

Recommended Citation:
Wang, Feihu,Chen, Yuxuan,Zhang, Dianrui,et al. Folate-mediated targeted and intracellular delivery of paclitaxel using a novel deoxycholic acid-O-carboxymethylated chitosan-folic acid micelles[J]. INTERNATIONAL JOURNAL OF NANOMEDICINE,2012,7:325-337.
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