|Folate-mediated targeted and intracellular delivery of paclitaxel using a novel deoxycholic acid-O-carboxymethylated chitosan-folic acid micelles|
|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|
|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|
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.
|资助机构||National Basic Research Program of China (973Program)|
|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
|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.|
|APA||Wang, Feihu.,Chen, Yuxuan.,Zhang, Dianrui.,Zhang, Qiang.,Zheng, Dandan.,...&Liu, Guangpu.(2012).Folate-mediated targeted and intracellular delivery of paclitaxel using a novel deoxycholic acid-O-carboxymethylated chitosan-folic acid micelles.INTERNATIONAL JOURNAL OF NANOMEDICINE,7,325-337.|
|MLA||Wang, Feihu,et al."Folate-mediated targeted and intracellular delivery of paclitaxel using a novel deoxycholic acid-O-carboxymethylated chitosan-folic acid micelles".INTERNATIONAL JOURNAL OF NANOMEDICINE 7(2012):325-337.|