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Development and in vitro characterization of a particulate oral peptide drug delivery system based on thiolated poly(acrylic acid)

机译:基于硫醇聚(丙烯酸)的颗粒状口腔肽药物输送系统的开发和体外表征

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The aim of the present study was to develop a particulate carrier system for the oral application of the peptide drug leuprolide acetate. Therefore, the drug was incorporated into a carrier based on a thiolated polymer, namely a poly(acrylic acid)-cysteine conjugate, synthesised via a carbodiimide method. The resulting thiomer was characterized by Ellman’s, TNBS and disulphide test regarding the amount of attached free thiol groups. Microparticles formed upon the addition of acetonitrile to an aqueous solution of the thiomer containing leuprolide acetate were characterized regarding size distribution, drug load and drug release profile in vitro.
机译:本研究的目的是开发一种颗粒载体系统,用于口服肽药物甘醇乙酸酯。因此,将该药物基于硫醇化聚合物掺入载体中,即聚(丙烯酸) - 琥珀酰胺缀合物,通过碳二亚胺方法合成。得到的巯基特征在于Ellman,TNB和关于无附着的游离硫醇基的二硫化物测试。在将乙腈加入含有甘醇乙酸核苷酸水溶液的微粒上形成的微粒,表征在体外尺寸分布,药物载荷和药物释放曲线。

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