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载有非甾体抗炎药物的聚(己二酸甘油酯)纳米粒的研制。

Development of poly(glycerol adipate) nanoparticles loaded with non-steroidal anti-inflammatory drugs.

机构信息

Medway School of Pharmacy, Universities of Kent/Greenwich, Central Avenue, Chatham Maritime, ME4 4TB Kent, UK.

出版信息

J Microencapsul. 2012;29(5):497-504. doi: 10.3109/02652048.2012.665087. Epub 2012 Jul 6.

Abstract

The aim of this study was to assess acylated and non-acylated poly(glycerol adipate) polymers (PGA) as suitable nanoparticulate systems for encapsulation and release of ibuprofen, ibuprofen sodium salt (IBU-Na) and ketoprofen as model drugs. Drug encapsulated nanoparticles were prepared using the interfacial deposition method in the absence of surfactants. Physicochemical characterisation studies of the produced loaded nanoparticles showed that drug-polymer interactions depend on the characteristics of the actual active substance. IBU-Na showed strong interactions with the polymers and it was found to be molecularly dispersed within the polymer matrix while ibuprofen and ketoprofen retained their crystalline state. The drug release profiles showed stepwise patterns which involve an initial burst release effect, diffusion of the drug from the polymer matrix and eventually drug release possibly via a combined mechanism. PGA polymers can be effectively used as drug delivery carriers for various active substances.

摘要

本研究旨在评估酰化和非酰化聚(甘油己二酸酯)聚合物(PGA)作为合适的纳米颗粒系统,用于封装和释放布洛芬、布洛芬钠盐(IBU-Na)和酮洛芬作为模型药物。使用界面沉积方法在没有表面活性剂的情况下制备包封药物的纳米颗粒。对所制备的负载纳米颗粒的理化特性研究表明,药物-聚合物相互作用取决于实际活性物质的特性。IBU-Na 与聚合物表现出强烈的相互作用,发现其在聚合物基质中呈分子分散状态,而布洛芬和酮洛芬保持其结晶状态。药物释放曲线显示出阶跃式模式,其中包括初始突释效应、药物从聚合物基质中的扩散,最终可能通过联合机制释放药物。PGA 聚合物可有效用作各种活性物质的药物递送载体。

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