Lukyanov Anatoly N, Hartner William C, Torchilin Vladimir P
Department of Pharmaceutical Sciences, Bouve College of Health Sciences, Northeastern University, 360 Huntington Avenue, 312 Mugar Building, Boston, MA 02115, USA.
J Control Release. 2004 Jan 8;94(1):187-93. doi: 10.1016/j.jconrel.2003.10.008.
Micelles prepared from polyethyleneglycol/phosphatidyl-ethanolamine conjugates (PEG-PE) with a size of 7-20 nm and zeta-potential of approximately -18 mV were administered i.v. to rabbits with experimental myocardial infarctions. Micelles demonstrated a prolonged circulation in the blood (half-life of 2 h) and accumulated in the infarction zone with efficiency more than 8-fold higher as compared to a non-damaged part of the heart muscle. Obtained results suggest that the enhanced permeability and retention (EPR) effect is the primary mechanism of accumulation of microparticles in the infarct areas, and that drug carriers such as PEG-PE micelles can be used for the delivery of therapeutic or diagnostic agents to an area of myocardial infarction.
由聚乙二醇/磷脂酰乙醇胺缀合物(PEG-PE)制备的粒径为7-20nm、ζ电位约为-18mV的胶束经静脉注射给予患有实验性心肌梗死的兔子。胶束在血液中的循环时间延长(半衰期为2小时),并且在梗死区域的蓄积效率比心肌未受损部分高8倍以上。所得结果表明,增强的通透性和滞留(EPR)效应是微粒在梗死区域蓄积的主要机制,并且诸如PEG-PE胶束之类的药物载体可用于将治疗剂或诊断剂递送至心肌梗死区域。