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果胶阿霉素大分子前药纳米传递体系的体外抗肿瘤作用评价
引用本文:李志平,陈波,蒋明超,龚娟,杨飒,谭翔文,喻翠云. 果胶阿霉素大分子前药纳米传递体系的体外抗肿瘤作用评价[J]. 南华大学学报(自然科学版), 2018, 32(2): 13-18
作者姓名:李志平  陈波  蒋明超  龚娟  杨飒  谭翔文  喻翠云
作者单位:南华大学湖南省分子靶标新药研究协同创新中心;南华大学药物药理研究所
基金项目:国家自然科学基金资助项目(81471177);湖南省杰出青年基金项目(2017JJ1024);南华大学抗肿瘤药物创新团队项目(NHCXTD05)
摘    要:研究果胶阿霉素大分子前药纳米传递体系(PDC-M)的体外抗肿瘤效果与体内药代动力学.用马尔文纳米粒度仪检测了PDC-M在血清中的稳定性,采用溴化四唑蓝比色法(MTT法)评价PDC-M对SMMC7721人肝癌细胞株的体外抗肿瘤作用,采用倒置荧光显微镜观察细胞对药物的摄取过程,采用细胞划痕法和Transwell法分别检测PDC-M对SMMC7721肝癌细胞迁移能力和侵袭能力的影响.结果表明24 h内PDC-M在血清中有较好的稳定性;PDC-M对SMMC7721肝癌细胞的增殖具有明显抑制作用,呈剂量依赖性和时间依赖性,并有一定缓释效果;果胶上的半乳糖可以通过与去唾液酸糖蛋白受体的特异性相互作用来实现主动靶向的作用;PDC-M能够可以抑制SMMC7721肝癌细胞的迁移和侵袭.

关 键 词:药物传递  果胶阿霉素大分子前药  体外抗肿瘤效果  肝癌
收稿时间:2018-02-07

In Vitro Performance Evaluation of PDC Macromolecular Pro-drug Based Nanoparticles Delivery System
LI Zhi-ping,CHEN Bo,JIANG Ming-chao,GONG Juan,YANG S,TAN Xiang-wen and YU Cui-yun. In Vitro Performance Evaluation of PDC Macromolecular Pro-drug Based Nanoparticles Delivery System[J]. Journal of Nanhua University(Science and Technology), 2018, 32(2): 13-18
Authors:LI Zhi-ping  CHEN Bo  JIANG Ming-chao  GONG Juan  YANG S  TAN Xiang-wen  YU Cui-yun
Affiliation:Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, University of South China,Hengyang,Hunan 421001,China,Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, University of South China,Hengyang,Hunan 421001,China,Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, University of South China,Hengyang,Hunan 421001,China,Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, University of South China,Hengyang,Hunan 421001,China,Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, University of South China,Hengyang,Hunan 421001,China,Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, University of South China,Hengyang,Hunan 421001,China and Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, University of South China,Hengyang,Hunan 421001,China;Institute of Pharmacy and Pharmacology,University of South China,Hengyang,Hunan 421001,China
Abstract:This study reported the evaluation of in vitro anti proliferative effect of PDC macromolecular pro-drug (PDC-M).The physical stability of PDC-M in the serum was monitored by a Zetasizer nanoparticle analyser for 24 h in terms of the mean size.The results have demonstrated that the PDC-M has good stability in serum.Anti proliferative effect of PDC-M in SMMC7721 cells was determined by MTT assay.The results demonstrated that PDC-M have greater properties of delayed and slow release as compared to free doxorubicin (DOX).The cellular uptake of PDC-M into SMMC7721 cells was investigated qualitatively by fluorescence microscopy.It suggested that the cellular uptake of galactosylated nanomedicine was mediated by the asialoglycoprotein receptor (ASGP-R).Cell wound healing test and transwell method were carried out to detect migration and invasion in SMMC7721 cells.The results showed that PDC-M remarkedly inhibited migration and invasion of SMMC7721 cells.The obtained data suggested that PDC-M is a very promising drug delivery system for hepatocellular carcinoma treatment.
Keywords:drug delivery  PDC-M  in vitro performance evaluation  liver cancer
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