Calcium Chloride Modified Alginate Microparticles Formulated by the Spray Drying Process: A Strategy to Prolong the Release of Freely Soluble Drugs.

Marta Szekalska,Katarzyna Sosnowska,Katarzyna Winnicka,Anna Czajkowska-Kośnik

doi:10.3390/ma11091522

Marta Szekalska, Katarzyna Sosnowska + Show 2 more

Open Access

https://doi.org/10.3390/ma11091522

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Journal: Materials	Publication Date: Aug 24, 2018
Citations: 47	License type: CC BY 4.0

Affiliation: Medical University of Białystok

Abstract

Alginate (ALG) cross-linking by CaCl2 is a promising strategy to obtain modified-release drug delivery systems with mucoadhesive properties. However, current technologies to produce CaCl2 cross-linked alginate microparticles possess major disadvantages, such as a poor encapsulation efficiency of water-soluble drugs and a difficulty in controlling the process. Hence, this study presents a novel method that streamlines microparticle production by spray drying; a rapid, continuous, reproducible, and scalable technique enabling obtainment of a product with low moisture content, high drug loading, and a high production yield. To model a freely water-soluble drug, metformin hydrochloride (MF) was selected. It was observed that MF was successfully encapsulated in alginate microparticles cross-linked by CaCl2 using a one-step drying process. Modification of ALG provided drug release prolongation—particles obtained from 2% ALG cross-linked by 0.1% CaCl2 with a prolonged MF rate of dissolution of up to 12 h. Cross-linking of the ALG microparticles structure by CaCl2 decreased the swelling ratio and improved the mucoadhesive properties which were evaluated using porcine stomach mucosa.

Highlights

Polysaccharides are polymeric carbohydrate molecules commonly exploited in the design of pharmaceutical formulations with prolonged drug release
Drug solubility exerts an evident impact on the mechanism and release kinetics
The rapid dissolution of active compounds characterized by being freely soluble in water is one of the main dissolution of active compounds characterized by being freely soluble in water is one of the main drawbacks when designing pharmaceutical formulations

Summary

Introduction

Polysaccharides are polymeric carbohydrate molecules commonly exploited in the design of pharmaceutical formulations with prolonged drug release. These polymers possess many advantages such as non-toxicity, wide availability, simplicity to receive, and gelling ability using different cross-linking agents [1]. Dosage forms with mucoadhesive properties provide continuous contact with the mucosal membrane and as a consequence, a prolonged drug residence time and improved drug absorption and bioavailability can be achieved [4,5]. Microparticles are characterized by a high surface area of drug release and short diffusion pathway, which enables the improvement of the therapeutic efficacy and a reduction of the drug toxicity [6,7]

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