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Molecules 2017, 22(1), 182; doi:10.3390/molecules22010182

The Influence of Chitosan Cross-linking on the Properties of Alginate Microparticles with Metformin Hydrochloride—In Vitro and In Vivo Evaluation

1
Department of Pharmaceutical Technology, Medical University of Białystok, Mickiewicza 2c, Białystok 15-222, Poland
2
Department of Biopharmacy, Medical University of Białystok, Mickiewicza 2c, Białystok 15-222, Poland
3
Department of Histology and Cytophysiology, Medical University of Białystok, Mickiewicza 2c, Białystok 15-222, Poland
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 20 December 2016 / Revised: 10 January 2017 / Accepted: 18 January 2017 / Published: 22 January 2017
(This article belongs to the Special Issue Natural Products and Chronic Diseases)
View Full-Text   |   Download PDF [6023 KB, uploaded 22 January 2017]   |  

Abstract

Sodium alginate is a polymer with unique ability to gel with different cross-linking agents in result of ionic and electrostatic interactions. Chitosan cross-linked alginate provides improvement of swelling and mucoadhesive properties and might be used to design sustained release dosage forms. Therefore, the aim of this research was to develop and evaluate possibility of preparing chitosan cross-linked alginate microparticles containing metformin hydrochloride by the spray-drying method. In addition, influence of cross-linking agent on the properties of microparticles was evaluated. Formulation of microparticles prepared by the spray drying of 2% alginate solution cross-linked by 0.1% chitosan was characterized by good mucoadhesive properties, high drug loading and prolonged metformin hydrochloride release. It was shown that designed microparticles reduced rat glucose blood level, delayed absorption of metformin hydrochloride and provided stable plasma drug concentration. Additionally, histopathological studies of pancreas, liver and kidneys indicated that all prepared microparticles improved degenerative changes in organs of diabetic rats. Moreover, no toxicity effect and no changes in rats behavior after oral administration of chitosan cross-linked alginate microparticles were noted. View Full-Text
Keywords: alginate; chitosan; cross-linking; microparticles; spray drying; hypoglycemic activity; metformin hydrochloride; toxicity alginate; chitosan; cross-linking; microparticles; spray drying; hypoglycemic activity; metformin hydrochloride; toxicity
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MDPI and ACS Style

Szekalska, M.; Sosnowska, K.; Zakrzeska, A.; Kasacka, I.; Lewandowska, A.; Winnicka, K. The Influence of Chitosan Cross-linking on the Properties of Alginate Microparticles with Metformin Hydrochloride—In Vitro and In Vivo Evaluation. Molecules 2017, 22, 182.

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