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Encapsulation of Naproxen in Lipid-Based Matrix Microspheres: Characterization and Release Kinetics

机译:萘普生在基于脂质的基质微球中的包封:表征和释放动力学。

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摘要

The objective of this study was to microencapsulate the anti-inflammatory drug (naproxen) to provide controlled release and minimizing or eliminating local side effect by avoiding the drug release in the upper gastrointestinal track. Naproxen was microencapsulated with lipid-like carnauba wax, hydrogenated castor oil using modified melt dispersion (modified congealable disperse phase encapsulation) technique. Effect of various formulation and process variables such as drug-lipid ratio, concentration of modifier, concentration of dispersant, stirring speed, stirring time, temperature of external phase, on evaluatory parameters such as size, entrapment efficiency, and in vitro release of naproxen were studied. The microspheres were characterized for particle size, scanning electron microscopy (SEM), FT-IR spectroscopy, drug entrapment efficiency, in vitro release studies, for in vitro release kinetics. The shape of microspheres was found to be spherical by SEM. The drug entrapment efficiency of various batches of microspheres was found to be ranging from 60 to 90 %w/w. In vitro drug release studies were carried out up to 24 h in pH 7.4 phosphate buffer showing 50-65% drug release. In vitro drug release from all the batches showed better fitting with the Korsmeyer-Peppas model, indicating the possible mechanism of drug release to be by diffusion and erosion of the lipid matrix.
机译:这项研究的目的是将抗炎药(萘普生)微囊化,以通过避免在上消化道内释放药物来提供控释并最大程度减少或消除局部副作用。将萘普生用脂质状巴西棕榈蜡,氢化蓖麻油微囊化,方法是使用改进的熔体分散液(改进的可凝结的分散相包封)技术。各种制剂和工艺变量(如药物脂质比,改性剂的浓度,分散剂的浓度,搅拌速度,搅拌时间,外相温度)对评估参数(如大小,包封效率和萘普生的体外释放)的影响研究。表征微球的粒径,扫描电子显微镜(SEM),FT-IR光谱,药物截留效率,体外释放研究以及体外释放动力学。通过SEM发现微球的形状为球形。发现不同批次的微球的药物截留效率为60至90%w / w。在pH 7.4磷酸盐缓冲液中进行了长达24小时的体外药物释放研究,显示出50-65%的药物释放。所有批次的体外药物释放均显示出与Korsmeyer-Peppas模型更好的拟合,表明药物释放的可能机制是通过脂质基质的扩散和侵蚀。

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