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制备和萘普生-PLGA 纳米粒的物理化学特性。

Preparation and physicochemical characterization of naproxen-PLGA nanoparticles.

机构信息

Faculty of Pharmacy, Biotechnology Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.

出版信息

Colloids Surf B Biointerfaces. 2010 Dec 1;81(2):498-502. doi: 10.1016/j.colsurfb.2010.07.047. Epub 2010 Jul 30.

Abstract

Naproxen is a non-steroidal anti-inflammatory drug which can be used for the treatment of inflammatory disorders like uveitis and arthirit rheumatoid. The aim of the present study was to investigate the physicochemical characteristics of naproxen-PLGA nanoparticles. The nanoparticles of naproxen with PLGA were formulated using the solvent evaporation/extraction technique (the single emulsion technique). Several process parameters i.e., drug/polymer ratio, aqueous phase volume and speed of homogenization were considered with the aim of achieve optimal preparation conditions. The physicochemical characteristics of nanoparticles were studied applying particle size analysis, differential scanning calorimetry, X-ray crystallography, Fourier transform infrared spectroscopy and scanning electron microscopy. The release rate of naproxen from various drug/polymer nanoparticles was investigated as well. All the prepared formulations using PLGA resulted in nano-range size particles (352-571 nm) with spherical smooth morphology. The nanoparticles of naproxen-PLGA displayed lower crystallinity with no chemical interactions between the drug and polymer molecules. The nanoparticles exhibited the slower release of drug in comparison with the intact drug and the physical mixtures. According of these findings, formulation of the naproxen-PLGA nanoparticles was able to improve the physicochemical characteristics of the drug and possibly will increase the anti-inflammatory effects of drug following its ocular or intra-joint administration.

摘要

萘普生是一种非甾体抗炎药,可用于治疗葡萄膜炎和类风湿性关节炎等炎症性疾病。本研究旨在研究萘普生-PLGA 纳米粒的理化特性。采用溶剂蒸发/萃取技术(单乳液技术)制备了萘普生-PLGA 纳米粒。考虑了几种工艺参数,如药物/聚合物比、水相体积和均质速度,以达到最佳的制备条件。通过粒径分析、差示扫描量热法、X 射线结晶学、傅里叶变换红外光谱和扫描电子显微镜研究了纳米粒的理化特性。还研究了不同药物/聚合物纳米粒中萘普生的释放速率。所有使用 PLGA 制备的制剂均得到纳米级大小的颗粒(352-571nm),呈球形光滑形态。萘普生-PLGA 纳米粒的结晶度较低,药物与聚合物分子之间没有化学相互作用。与完整药物和物理混合物相比,纳米粒显示出较慢的药物释放。根据这些发现,萘普生-PLGA 纳米粒的制剂能够改善药物的理化特性,并可能会增加药物经眼部或关节内给药后的抗炎效果。

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