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携紫杉醇和Herceptin高分子超声造影剂体外寻靶及体内肿瘤药物含量分析
引用本文:骆杰,王志刚,钟世根,张群霞,宋卫香,张勇.携紫杉醇和Herceptin高分子超声造影剂体外寻靶及体内肿瘤药物含量分析[J].中国介入影像与治疗学,2016,13(2):102-106.
作者姓名:骆杰  王志刚  钟世根  张群霞  宋卫香  张勇
作者单位:重庆医科大学附属第一医院超声科, 重庆 400016,重庆医科大学超声影像学研究所, 重庆 400010,重庆市人民医院超声科, 重庆 400014,重庆医科大学超声影像学研究所, 重庆 400010,重庆医科大学超声影像学研究所, 重庆 400010,重庆医科大学附属第一医院超声科, 重庆 400016
基金项目:国家自然科学基金面上项目(30970752)、国家临床重点专科建设项目(国卫医办函[2013]544号)、重庆市卫计委科研面上项目(2011-2-336)。
摘    要:目的探讨携紫杉醇和Herceptin高分子造影剂(Pac-PLGA-HER)的体外寻靶能力及体内肿瘤药物含量。方法通过双乳化法及碳二亚胺法制备Pac-PLGA-HER,观察其与乳腺癌细胞MCF-7的结合能力。将25只种植有乳腺癌细胞MCF-7的裸鼠分为单纯紫杉醇(PTX)组、单纯载药微球(Pac-PLGA)组、单纯载药微球+超声(Pac-PLGA+US)组、靶向载药微球(Pac-PLGA-HER)组及靶向载药微球+超声(Pac-PLGA-HER+US)组,根据微球载药量调整到相应药物浓度,经尾静脉注入裸鼠体内,观察各组在荷瘤裸鼠肿瘤内药物含量情况。结果Pac-PLGA-HER平均粒径为(777.40±65.90)nm,包封率为(65.84±2.25)%,载药量为(6.58±0.23)%,体外寻靶实验可观察到Pac-PLGA-HER与乳腺癌细胞MCF-7大量结合。体内药物释放实验显示Pac-PLGA-HER+US组在裸鼠肿瘤内药物浓度高于其他各组(P0.01)。结论 Pac-PLGA-HER与乳腺癌细胞MCF-7有较好的结合能力,体内药物释放实验中Pac-PLGA-HER+US组在裸鼠肿瘤内有较高的药物浓度。

关 键 词:紫杉醇  靶向  超声学
收稿时间:2015/11/19 0:00:00
修稿时间:2015/12/23 0:00:00

Targeting analysis of paclitaxel loaded PLGA-COOH-targeted ultrasound contrast agent in vitro and content of paclitaxel in tumor tissue of nude mice
LUO Jie,WANG Zhigang,ZHONG Shigen,ZHANG Qunxi,SONG Weixiang and ZHANG Yong.Targeting analysis of paclitaxel loaded PLGA-COOH-targeted ultrasound contrast agent in vitro and content of paclitaxel in tumor tissue of nude mice[J].Chinese Journal of Interventional Imaging and Therapy,2016,13(2):102-106.
Authors:LUO Jie  WANG Zhigang  ZHONG Shigen  ZHANG Qunxi  SONG Weixiang and ZHANG Yong
Institution:Department of Ultrasound, the First Affiliated Hospital of Chongqing Medical University, Chongqing 400016, China,Institute of Ultrasound Imaging of Chongqing Medical University, Chongqing 400010, China,Department of Ultrasound, Chongqing General Hospital, Chongqing 400014, China,Institute of Ultrasound Imaging of Chongqing Medical University, Chongqing 400010, China,Institute of Ultrasound Imaging of Chongqing Medical University, Chongqing 400010, China and Department of Ultrasound, the First Affiliated Hospital of Chongqing Medical University, Chongqing 400016, China
Abstract:Objective To prepare a kind of paclitaxel(PTX) loaded PLGA-COOH-targeted ultrasound contrast agent,and to investigate its affinity for breast cancer in vitro and content in the tumor tissue of nude mice.Methods The paclitaxel loaded PLGA-COOH-targeted ultrasound contrast agent were produced by the double emulsion technique and carbodiimide technique.The paclitaxel loaded PLGA-COOH-targeted ultrasound contrast agent targeting specifity to breast cancer cells was observed with confocal microscope.Twenty-five xenograft tumor-bearing nude mice were randomly divided into PTX,Pac-PLGA,Pac-PLGA+US,Pac-PLGA-HER and Pac-PLGA-HER+US groups.The distribution of paclitaxel in the tumor tissue of nude mice in each group were observed.Results The average diameter of Pac-PLGA-HER was(777.40±65.90)nm.The drug entrapment efficiency was(65.84±2.25)% and the drug-loading amount was(6.58±0.23)%.In the targeting study in vitro,the conjugation of Pac-PLGA-HER with MCF-7 cells was amount.Stastistical analysis showed that the paclitaxel content in Pac-PLGA-HER+US group increased significantly compared with other groups(P<0.01).Conclusion The Pac-PLGA-HER can bind to breast cancer effectively in vitro,and paclitaxel concentrate in the tumor tissue in Pac-PLGA-HER+US group is more.
Keywords:Paclitaxel  Target  Ultrasonics
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