Influence of zinc ions as the cross-linking agent on the properties of alginate microcapsules with posaconazole
Author | Affiliation | |
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Szekalska, M. | ||
Date | Start Page | End Page |
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2024-09-16 | 91 | 92 |
INTRODUCTION Microcapsules as an example of multiple unit dosage forms are defined as spherical particles consisting of polymer shell and core substance [1]. Sodium alginate (ALG) is a natural polysaccharide polymer which possesses many advantages such as non-toxicity, biodegradability, gelling and mucoadhesive properties [2]. Posaconazole (POS) is a triazole antifungal substance with an extended spectrum of antifungal activity against commonly encountered fungal species [3]. The purpose of this study was to prepare ALG microcapsules cross-linked by zinc ions to ensure modified POS release. MATERIALS AND METHODS Microcapsules preparation. In the first step, POS was solubilized in 1% solution of polysorbate 80 and suspended in 2% ALG solution. The prepared mixture was extruded using microcapsule pump (Landgraf Laborsysteme, Langenhagen, Germany) into the solution of zinc acetate applied as crosslinker solution (Tab. 1). The microcapsules were filtered, washed with purified water and dried at room temperature (22 ± 2 °C) for 24 h. Prepared microcapsules were evaluated for weight uniformity, diameter, morphology and POS content. The firmness was evaluated by using TA.XT.Plus Texture Analyzer (Stable Micro Systems, Godalming, UK) [4]. POS in vitro release was tested in paddle apparatus (Erweka Dissolution Tester Type DT 600 HH, Heusenstamm, Germany) [5]. Antifungal activity was performed by plate diffusion method [4]. RESULTS AND DISCUSSION The study proved that ALG microcapsules cross-linked by zinc ions obtained by extrusion technique were characterized by uniformity of weight, size and drug loading (data not shown). All formulations provided enteric POS release (Fig. 1). Interestingly, firmness and antifungal activity of prepared microcapsules were zinc ions concentration dependent (Tab. 2). CONCLUSIONS Developed microcapsules were characterized by satisfactory firmness, exhibited zinc ions concentration dependent antifungal activity, and ensured enteric POS release.