肿瘤药学Issue(1)：21-26,6.DOI:10.3969/j.issn.2095-1264.2015.003
PEG-I-dC16酸敏释药胶束的制备与体外评价
Preparation of Acid-sensitive Drug Release PEG-I-dC16 Micelles and in vitroEvaluation
摘要
Abstract
ObjectiveToinvestigatetheadvantagesofacidsensitivemicellesonin vitroanti-tumoractivityandcellu-lar uptake by construction of polyethylene glycol-imine-palmitate and doxorubicin-loaded micelle. Methods Doxorubicin was encapsulated in the micelles by using membrane dialysis method. The determination of micelle drug-loading capacity and encapsulation efficiency were studied by UV. Zeta potential and particle size was measured by a particle size analyzer. Anti-tumoractivityin vitrowasexaminedbyMTTassay,andcelluptakewasmeasuredbyflowcytometry.Thedruginthe nucleus was observed by laser confocal microscopy. Results Drug-loading capacity and encapsulation efficiency of Micelle (PEG molecular weight 2 000) was (12.7±1.1)%and (49.8±2.2)%, respectively. The average particle size was (72.3± 2.5)nm.Thein vitrocytotoxicityandintracellulardruguptakeofacid-sensitivemicelleswerehigherthanthatofnon-acid-sensitive micelles in A549 cells and HepG2 cells. Correspondingly, more drugs was observed in HepG2 nuclear than non-acid-sensitive micelles. Conclusions The acid-sensitive micelles could increase the cell or cell nuclei uptake of drug, and improvetheeffectsofantitumorin vitro.Itprovidesaresearchfoundationforcancertargeteddrugdeliverysystem.关键词
聚乙二醇/酸敏释药胶束/肿瘤靶向治疗/阿霉素Key words
Polyethyleneglycol/Acid-sensitivemicelles/Tumortargeting/Doxorubicin分类
医药卫生引用本文复制引用
申辛,黄榕彬,刘映,邓湘萍,曹轩,唐国涛..PEG-I-dC16酸敏释药胶束的制备与体外评价[J].肿瘤药学,2015,(1):21-26,6.基金项目
湖南省教育厅科学研究项目（13C833），湖南省药学类专业校企合作人才培养基地合作项目。 （）
