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    • 1. 发明申请
    • POLY(VINYL BENZOATE) NANOPARTICLES FOR MOLECULAR DELIVERY
    • 用于分子递送的POLY(乙烯基苯甲酸酯)纳米粒子
    • WO2012068476A3
    • 2012-08-30
    • PCT/US2011061429
    • 2011-11-18
    • UNIV SOUTH FLORIDATUROS EDWARDLABRUERE RAPHAELCORMIER RYAN SCOTTSICARD RENAUD
    • TUROS EDWARDLABRUERE RAPHAELCORMIER RYAN SCOTTSICARD RENAUD
    • A61K47/34A61K9/14A61K9/16A61K47/30A61K49/06A61K49/12C08F18/04
    • A61K9/146A61K9/0019A61K9/10A61K9/5138A61K47/10A61K47/489A61K47/6933A61K49/0039A61K49/0043A61K49/0093
    • The present invention comprises poly(vinyl benzoate) nanoparticle suspensions as molecular carriers. These nanoparticles can be formed by nanoprecipitation of poly(vinyl benzoate) in water using Pluronic F68 as surfactant, to create spherical nanostructures measuring about 200-250 nm in diameter which are stable in phosphate buffer and blood serum, and only slowly degrade in the presence of esterases. Kinetics experiments in phosphate buffer indicate that 78% of the coumarin-6 was encapsulated within the polymer matrix of the nanoparticle, and the residual 22% of coumarin-6 was surface-bound and quickly released. The nanoparticles are non-toxic in vitro towards human epithelial cells (IC50 >1000 µg/mL) and primary bovine primary aortic endothelial cells (IC50 >500 µg/mL), and exert non-observable bactericidal activity against a selection of representative test microbes (MIC >250 µg/mL). Poly(vinyl benzoate) nanoparticles are suitable carriers for molecular delivery of lipophilic small molecules such as drugs pharmaceutical and imaging agents.
    • 本发明包含聚(苯甲酸乙烯酯)纳米颗粒悬浮液作为分子载体。 这些纳米颗粒可以通过使用Pluronic F68作为表面活性剂在水中纳米沉淀聚(苯甲酸乙烯酯)以形成直径为约200-250nm的球形纳米结构,其在磷酸盐缓冲液和血清中稳定并且在存在时仅缓慢降解 的酯酶。 磷酸盐缓冲液中的动力学实验表明,香豆素-6的78%被包封在纳米粒子的聚合物基质内,并且剩余22%的香豆素-6被表面结合并且快速释放。 纳米颗粒在体外对人上皮细胞(IC50>1000μg/ mL)和原代牛主动脉内皮细胞(IC50>500μg/ mL)无毒性,并对选择的代表性测试微生物发挥不可观察的杀菌活性 (MIC>250μg/ mL)。 聚(苯甲酸乙烯酯)纳米粒子是用于分子递送亲脂性小分子的合适载体,例如药物药物和成像剂。