【摘要】 目的 研究载药纳米微球在血管组织中的吸收情况，为局部用药防治血管成形术后再狭窄提供理论依据。方法 用超声乳化 /溶剂挥发法制备含抗细胞增生药 2－氨基色酮的聚乳酸聚乙醇酸共聚物（ PLGA）纳米微球，建立纳米微球体内、体外动脉吸收实验模型，评价纳米微球的血管吸收性；分别用环氧化物、氰基丙烯酸异丁酯、纤维蛋白原、粘连蛋白、溴化双十二烷基二甲基铵 (DMAB)、磷脂及 Lipofectin对纳米微球进行表面修饰以增加其血管吸收率。结果 纳米微球的粒径小于 200 nm，含药量为 15％左右，电镜下观察为光滑的球形；用正电性表面活性剂 DMAB表面修饰纳米微球，可极大地提高其血管吸收率；纳米微球在血管中驻留后，可维持局部较高药物浓度达 2 d。 结论 纳米微球有可能作为心血管疾病局部药物治疗的载体。更多还原

【Abstract】 Objective To study the uptake of drug-containing nanoparticles in artery for local therapy of restenosis. Methods Polylactic polyglycolic acid copolymer (PLGA) nanoparticles containing an antiproliferative agent 2-aminochromone were formulated with an oil-in-water sonication emulsion/solvent evaporation technique. Arterial uptake of nanoparticles was assessed both in vitro and in vivo models of dog and rat carotid and femoral arteries . Epoxide, cyanoacrylate, fibrinogen, fibronectin, didodecyldimethylammonium bromide (DMAB), L－α-phosphatidylethanolaine, and lipofectin were selected to modify the surface of nanoparticles to enhance arterial uptake of nanoparticles. Results The nanoparticle size ranged from 100 nm to 200 nm, the drug loading in nanoparticles was about 15％ , the nanoparticle morphology was observed by scanning electron microscopy and showed spherical shape with smooth surface. Arterial uptake of nanoparticles was enhanced greatly by surface modified nanoparticle with positively charged active agent DMAB. Once nanoparticles located in artery, a high drug level could be maintained at local site for 2 days in vivo model. Conclusion The primary results of animal experiments suggested that nanoparticle could be used as drug carrier of local drug delivery for treating cardiovascular diseases.更多还原