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载盐酸左西替利嗪的壳聚糖纳米粒:制剂与评价

Levocetirizine Dihydrochloride-Loaded Chitosan Nanoparticles: Formulation and Evaluation.

作者信息

Yurtdaş Kirimlioğlu Gülsel, Öztürk A Alper

机构信息

Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Technology, Eskişehir, Turkey.

出版信息

Turk J Pharm Sci. 2020 Feb;17(1):27-35. doi: 10.4274/tjps.galenos.2018.34392. Epub 2020 Feb 19.

Abstract

OBJECTIVES

The aim of the present study was to formulate levocetirizine hydrochloride (LCD)-loaded chitosan nanoparticles at submicron level with high entrapment efficiency and prolonged effect for optimizing the plasma drug concentration enhancing bioavailability.

MATERIALS AND METHODS

LCD was successfully incorporated into chitosan nanoparticles by spray drying for the purpose of oral application. characteristics were evaluated in detail.

RESULTS

LCD was successfully loaded into the polymeric matrices by spray drying. Characterization of the nanoparticles including encapsulation efficiency, particle size, zeta potential, morphology, polydispersity index, solid-state characterizations, and LCD quantification by high performance liquid chromatography was performed. The release pattern of LCD from the nanoparticles was determined using a dialysis tube in simulated intestinal fluid (pH 6.8). release profiles indicated prolonged release of LCD from the nanoparticles that followed the Korsmeyer-Peppas kinetic model.

CONCLUSION

Chitosan-based LCD-loaded polymeric nanoparticles appear to be a promising drug delivery system for the active agent.

摘要

目的

本研究旨在制备亚微米级的载盐酸左西替利嗪(LCD)壳聚糖纳米粒,使其具有高包封率和长效作用,以优化血浆药物浓度并提高生物利用度。

材料与方法

为实现口服给药,通过喷雾干燥法成功将LCD载入壳聚糖纳米粒,并对其特性进行了详细评估。

结果

通过喷雾干燥法成功将LCD载入聚合物基质中。对纳米粒进行了表征,包括包封率、粒径、ζ电位、形态、多分散指数、固态表征以及通过高效液相色谱法定量分析LCD。使用透析管在模拟肠液(pH 6.8)中测定了LCD从纳米粒中的释放模式。释放曲线表明LCD从纳米粒中呈长效释放,符合Korsmeyer-Peppas动力学模型。

结论

基于壳聚糖的载LCD聚合物纳米粒似乎是该活性剂的一种有前景的药物递送系统。

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