Levocetirizine Dihydrochloride-Loaded Chitosan Nanoparticles: Formulation and In Vitro Evaluation

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. In vitro 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). In vitro 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.

Keywords: Levocetirizine dihydrochloride; chitosan; polymeric nanoparticle; spray drying.