Histology and antitumor activity study of PTX-loaded micelle,a fluorescent drug delivery system prepared by PEG-TPP |
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Authors: | Huilan Li Jieming Li Xinyi He Bo Zhang Chunxia Liu Qifei Li Ying Zhu Wenlong Huang Wei Zhang Hai Qian Liang Ge |
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Affiliation: | Center of Drug Discovery, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, China; School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China; Jiangsu Key Laboratory of Drug Discovery for Metabolic Disease, China Pharmaceutical University, Nanjing 210009, China; Department of Biochemistry and Molecular Biology, Nanjing Medical University, Nanjing 10029, China |
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Abstract: | We synthesized PEG-TPP as carrier to encapsulate paclitaxel (PTX) in the form of micelles to overcome its water-solubility problem. PTX-loaded micelles possess a-week stability and appropriate particle size (152.1±1.2 nm) which is beneficial for enhanced permeability and retention (EPR) effect. Strong pH dependence of PTX releasing from micelles is verified by in vitro release study. At cellular level, PTXloaded micelles can target mitochondria effectively which may results a better cytotoxicity of micelles (especially IC50=0.123±0.035μmol/L of micelles and 0.298±0.067 μmol/L of PTX alone on MCF-7 cells). The fluorescence distributions of both isolated and sliced organs show that the micelles can effectively target tumors. Moreover, we further prove the enhanced therapeutic effects of micelles in tumor-bearing mice comparing with PTX alone. The results show that the biodegradable drug delivery system prepared by PEG-TPP can overcome the poor solubility of paclitaxel and improve its tumor targeting and antitumor activity. |
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Keywords: | PEG-TPP Anticancer Micelles EPR Mitochondria |
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