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1. 发明申请

WO2012068476A3 POLY(VINYL BENZOATE) NANOPARTICLES FOR MOLECULAR DELIVERY 审中-公开
标题翻译：用于分子递送的POLY（乙烯基苯甲酸酯）纳米粒子
公开(公告)号：WO2012068476A3
公开(公告)日：2012-08-30
申请号：PCT/US2011061429
申请日：2011-11-18
申请人： UNIV SOUTH FLORIDA , TUROS EDWARD , LABRUERE RAPHAEL , CORMIER RYAN SCOTT , SICARD RENAUD
发明人： TUROS EDWARD , LABRUERE RAPHAEL , CORMIER RYAN SCOTT , SICARD RENAUD
IPC分类号： A61K47/34 , A61K9/14 , A61K9/16 , A61K47/30 , A61K49/06 , A61K49/12 , C08F18/04
CPC分类号： A61K9/146 , A61K9/0019 , A61K9/10 , A61K9/5138 , A61K47/10 , A61K47/489 , A61K47/6933 , A61K49/0039 , A61K49/0043 , A61K49/0093
摘要： 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.
摘要翻译：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。

2. 发明申请

WO2012068476A2 POLY(VINYL BENZOATE) NANOPARTICLES FOR MOLECULAR DELIVERY 审中-公开
标题翻译： POLY（VINYL BENZOATE）NANOPARTICLES FOR MOLECULAR DELIVERY
公开(公告)号：WO2012068476A2
公开(公告)日：2012-05-24
申请号：PCT/US2011/061429
申请日：2011-11-18
申请人： UNIVERSITY OF SOUTH FLORIDA , TUROS, Edward , LABRUERE, Raphael , CORMIER, Ryan Scott , SICARD, Renaud
发明人： TUROS, Edward , LABRUERE, Raphael , CORMIER, Ryan Scott , SICARD, Renaud
IPC分类号： A61K47/34 , A61K47/30 , A61K9/16 , A61K9/14 , A61K49/06 , A61K49/12 , C08F18/04
CPC分类号： A61K9/146 , A61K9/0019 , A61K9/10 , A61K9/5138 , A61K47/10 , A61K47/489 , A61K47/6933 , A61K49/0039 , A61K49/0043 , A61K49/0093
摘要： 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 (IC 50 >1000 µg/mL) and primary bovine primary aortic endothelial cells (IC 50 >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.
摘要翻译：本发明包括作为分子载体的聚（苯甲酸乙烯酯）纳米颗粒悬浮液。这些纳米颗粒可以通过使用Pluronic F68作为表面活性剂在水中的聚（乙烯基苯甲酸酯）的纳米沉淀形成，以产生直径约200-250nm的球形纳米结构，其在磷酸盐缓冲液和血清中是稳定的，并且在存在下仅缓慢降解的酯酶。在磷酸盐缓冲液中的动力学实验表明，78％的香豆素-6被包封在纳米颗粒的聚合物基质内，剩余的22％的香豆素-6被表面结合并迅速释放。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，并且对代表性测试微生物的选择施加不可观察的杀菌活性（MIC>250μg/ mL）。聚（苯甲酸乙烯酯）纳米颗粒是分子递送亲脂性小分子如药物药物和成像剂的合适的载体。

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