重庆医学2016，Vol.45Issue(36)：5041-5044,5048,5.DOI:10.3969/j.issn.1671-8348.2016.36.001
人源抗VEGFR-2／As2O3-PEG-PLA隐形纳米粒的构建及质量控制研究
Preparation and quality control of human anti-VEGFR-2/As2 O3-PEG-PLA nanoparticle
摘要
Abstract
Objective To explore the preparation and quality control of As2 O3 nanoparticle .Methods PEG‐PLA was used as the vector material to prepare As2 O3 nanoparticle with ultrasonic emulsification method ,and the VEGFR‐2 was coupled to obtain VEGFR‐2/As2 O3‐PEG‐PLA nanoparticle .The particle size distribution ,Zata potential ,loading efficiency (LE) ,encapsulation effi‐ciency(EE) ,drug release in vitro and stability was determined ,and morphological characteristics was observed by transmission elec‐tron microscope(TEM) .Tweety‐four hepatocellular carcinoma nude mices were randomly divided into VEGFR‐2/As2O3‐PEG‐PLA nanoparticles group and As2 O3‐PEG‐PLA nanoparticles group ,by tail vein injection of nanoparticles .High performance liquid chro‐matography was used to determine content of As2 O3 .After 21 d ,six nude mices in each group were killed ,and the immunohisto‐chemistry and western blot method was used to detect the expression of VEGFR‐2 .Results The particle size of VEGFR‐2/As2 O3‐PEG‐PLA was determined to be (141 .9 ± 13 .2)nm ,Zata potential was (10 .2 ± 1 .1)mV .It was found to spherical or oval shape , with uniform size and dispersibility under TEM .LE and EE was (5 .51 ± 1 .83)% and (62 .12 ± 5 .98)% ,respectively .Drug release in vitro showed that VEGFR‐2/As2 O3‐PEG‐PLA exhibited controlled release effect ,with half of the release time as 10 h .Besides , VEGFR‐2/As2 O3‐PEG‐PLA showed a good stability in 3 days .Compared with As2 O3‐PEG‐PLA nanoparticles group ,the concen‐tration of As2 O3 in tumor and liver tissue was high ,the concentration of As2 O3 in blood ,heart ,kidney tissue was low ,the expression of VEGFR‐2 in tumor tissue was low in VEGFR‐2/As2O3‐PEG‐PLA nanoparticles group(P< 0 .05) .Conclusion The prepared As2 O3 nanoparticle using PEG‐PLA as vector and VEGFR‐2 as target showed uniform size ,high EE and LE ,good stability .And it preliminarily proved that VEGFR‐2 could be targeted in nude mice .关键词
砷剂/聚乙二醇类/聚乳酸/内皮细胞生长因子Key words
arsenicals/polyethylene glycols/polylactide/endothelial grow th factors分类
医药卫生引用本文复制引用
钟志惟,王栋,殷香保,邬林泉,黄长文,黄明文,周凡..人源抗VEGFR-2／As2O3-PEG-PLA隐形纳米粒的构建及质量控制研究[J].重庆医学,2016,45(36):5041-5044,5048,5.基金项目
国家自然科学基金资助项目（81060187）；江西省自然科学基金资助项目（2008GQY0050）；江西省教育厅科技技术研究项目（GJJ11309）。 （）
