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聚合物纳米颗粒——玻璃化转变温度对药物释放的影响。

Polymeric nanoparticles - Influence of the glass transition temperature on drug release.

作者信息

Lappe Svenja, Mulac Dennis, Langer Klaus

机构信息

Institute of Pharmaceutical Technology and Biopharmacy, University of Muenster, Corrensstraße 48, 48149 Münster, Germany.

Institute of Pharmaceutical Technology and Biopharmacy, University of Muenster, Corrensstraße 48, 48149 Münster, Germany.

出版信息

Int J Pharm. 2017 Jan 30;517(1-2):338-347. doi: 10.1016/j.ijpharm.2016.12.025. Epub 2016 Dec 13.

Abstract

The physico-chemical characterisation of nanoparticles is often lacking the determination of the glass transition temperature, a well-known parameter for the pure polymer carrier. In the present study the influence of water on the glass transition temperature of poly (DL-lactic-co-glycolic acid) nanoparticles was assessed. In addition, flurbiprofen and mTHPP as model drugs were incorporated in poly (DL-lactic-co-glycolic acid), poly (DL-lactic acid), and poly (L-lactic acid) nanoparticles. For flurbiprofen-loaded nanoparticles a decrease in the glass transition temperature was observed while mTHPP exerted no influence on this parameter. Based on this observation, the release behaviour of the drug-loaded nanoparticles was investigated at different temperatures. For all preparations an initial burst release was measured that could be attributed to the drug adsorbed to the large nanoparticle surface. At temperatures above the glass transition temperature an instant drug release of the nanoparticles was observed, while at lower temperatures less drug was released. It could be shown that the glass transition temperature of drug loaded nanoparticles in suspension more than the corresponding temperature of the pure polymer is the pivotal parameter when characterising a nanostructured drug delivery system.

摘要

纳米颗粒的物理化学表征往往缺少玻璃化转变温度的测定,而玻璃化转变温度是纯聚合物载体的一个众所周知的参数。在本研究中,评估了水对聚(DL-乳酸-共-乙醇酸)纳米颗粒玻璃化转变温度的影响。此外,将氟比洛芬和mTHPP作为模型药物载入聚(DL-乳酸-共-乙醇酸)、聚(DL-乳酸)和聚(L-乳酸)纳米颗粒中。对于载有氟比洛芬的纳米颗粒,观察到玻璃化转变温度降低,而mTHPP对该参数没有影响。基于这一观察结果,研究了载药纳米颗粒在不同温度下的释放行为。对于所有制剂,均测定到初始突释,这可归因于吸附在大纳米颗粒表面的药物。在高于玻璃化转变温度时,观察到纳米颗粒的药物瞬间释放,而在较低温度下释放的药物较少。可以可以表明,在表征纳米结构药物递送系统时,悬浮液中载药纳米颗粒的玻璃化转变温度比纯聚合物的相应温度更关键。

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