Zinc Acetate as a Cross-Linking Agent in the Development of Enteric Microcapsules for Posaconazole

<b>Background/Objectives:</b> Posaconazole is an antifungal agent from triazoles with variable bioavailability. To avoid its irregular absorption caused by gastric conditions and ensure more repeatable pharmacokinetic enabling the maximization of its absorption regardless of food intake without the need to administer multiple doses, can be provided by the technology of enteric drug preparations. The cross-linking of polysaccharide polymers with divalent and trivalent cations enables multi-unit formulations to be obtained that prevent drug absorption in the stomach. Microcapsules, as an example of multi-unit drug dosage forms, provide more predictable gastric emptying, depending on nutritional status, and spread extensively throughout the gastrointestinal tract. <b>Methods:</b> Therefore, the utilization of zinc acetate for the cross-linking of the alginate and pectin mixture was evaluated. The obtained formulations were evaluated for the impact of cross-linking process and pectin's presence on their pharmaceutical, mucoadhesive, physicochemical and antifungal properties. <b>Results:</b> It was shown that cross-linked microcapsules by zinc acetate provided delayed posaconazole release. Additionally, the cross-linking process with Zn<sup>2+</sup> ions significantly enhanced antifungal activity against the analyzed <i>Candida</i> strains. It was observed that pectin content in the formulation enhanced the swelling ability in an intestinal condition and increased the mucoadhesive properties of drug-loaded formulations to the intestinal mucosa.

Authors

Institutions

Publication Details

Journal
Pharmaceutics
Published
2025-02-22
DOI
https://doi.org/10.3390/pharmaceutics17030291
Citations
4
Primary Topic
Advanced Drug Delivery Systems
Type
article
Field-Weighted Citation Impact
3.16
Controls
|||
ALL TIME
JAN
FEB
MAR
APR
MAY
JUN
JUL
AUG
SEP
OCT
article

Zinc Acetate as a Cross-Linking Agent in the Development of Enteric Microcapsules for Posaconazole

Paweł Misiak, Anna Czajkowska-Kośnik, Katarzyna Winnicka, Marta Szekalska et al.
4 citations
Pharmaceutics
Advanced Drug Delivery Systems
3.16
article

Zinc Acetate as a Cross-Linking Agent in the Development of Enteric Microcapsules for Posaconazole

Paweł Misiak, Anna Czajkowska-Kośnik, Katarzyna Winnicka, Marta Szekalska, Jurga Bernatonienė, Giedrė Kasparavičienė, Agnieszka Zofia Wilczewska, Karolina H. Markiewicz, Eliza Wolska
article en
4 citations

Abstract

<b>Background/Objectives:</b> Posaconazole is an antifungal agent from triazoles with variable bioavailability. To avoid its irregular absorption caused by gastric conditions and ensure more repeatable pharmacokinetic enabling the maximization of its absorption regardless of food intake without the need to administer multiple doses, can be provided by the technology of enteric drug preparations. The cross-linking of polysaccharide polymers with divalent and trivalent cations enables multi-unit formulations to be obtained that prevent drug absorption in the stomach. Microcapsules, as an example of multi-unit drug dosage forms, provide more predictable gastric emptying, depending on nutritional status, and spread extensively throughout the gastrointestinal tract. <b>Methods:</b> Therefore, the utilization of zinc acetate for the cross-linking of the alginate and pectin mixture was evaluated. The obtained formulations were evaluated for the impact of cross-linking process and pectin's presence on their pharmaceutical, mucoadhesive, physicochemical and antifungal properties. <b>Results:</b> It was shown that cross-linked microcapsules by zinc acetate provided delayed posaconazole release. Additionally, the cross-linking process with Zn<sup>2+</sup> ions significantly enhanced antifungal activity against the analyzed <i>Candida</i> strains. It was observed that pectin content in the formulation enhanced the swelling ability in an intestinal condition and increased the mucoadhesive properties of drug-loaded formulations to the intestinal mucosa.

PharmaceuticsVol. 17(3)
Lithuanian University of Health Sciences (LT), Medical University of Białystok (PL), University of Białystok (PL), Gdańsk Medical University (PL)
Zero hunger
Openalex Percentile: Top 10%
Advanced Drug Delivery Systems
3.16
AI Navigator

Ask Laika to Summarize, Analyze, and Connect papers live on the map.

Summarize Papers & Methodologies

Extract key findings, datasets, and comparative methods across publications.

Benchmark Rankings & Visual Analytics

Rank top research institutions, authors, funders, topics, and journals by Field-Weighted Citation Impact (FWCI) and paper volume with instant charts.

Connect Distant Disciplines

Bridge topological clusters on the map to find hidden collaborative intersections.