载药纳米微球在血管组织中的吸收

目的 研究载药纳米笛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２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

Uptake of drug-containing nanoparticles in dog catotid and femoral arteries

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-amino-chromone 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-alpha-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.