Development and optimization of an innovative raft-forming antiemetic gastro-retentive system

Gastro-retentive drug delivery systems are vital for enhancing bioavailability and prolonging gastric residence time, especially for drugs with a short half-life like Ondansetron HCl. This study developed a raft-forming gastroretentive drug delivery system using a polyelectrolyte complex (PEC) of Chitosan and anionic polymers to improve stomach retention, regulate drug release, and enhance therapeutic efficacy. Various formulations were optimized based on polymer type, ratio, cross-linking agent concentration, and hydroxypropyl methylcellulose (HPMC K100M). The best formulation (F12: Chitosan: Carbopol 934) showed high entrapment efficiency (98%), drug loading (11.5%), buoyancy (>12 hours), extended drug release (over 12 hours), and a swelling ratio of 1584% at 8 hours. FTIR and DSC confirmed PEC formation and stability, while FE-SEM demonstrated homogeneity. Drug release followed non-Fickian kinetics, indicating that both diffusion and matrix relaxation contributed to the drug release. This PEC-based system shows promise for sustained stomach delivery of Ondansetron HCl, improving therapeutic efficacy and patient adherence.

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Publication Details

Journal
Pharmacia
Published
2025-04-16
DOI
https://doi.org/10.3897/pharmacia.72.e147836
Citations
2
Primary Topic
Nausea and vomiting management
Type
article
Field-Weighted Citation Impact
4.01

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article

Development and optimization of an innovative raft-forming antiemetic gastro-retentive system

Mina Safa Aziz, Methaq Hamad Sabar
2 citations
Pharmacia
Nausea and vomiting management
4.01
article

Development and optimization of an innovative raft-forming antiemetic gastro-retentive system

Mina Safa Aziz, Methaq Hamad Sabar
article en
2 citations

Abstract

Gastro-retentive drug delivery systems are vital for enhancing bioavailability and prolonging gastric residence time, especially for drugs with a short half-life like Ondansetron HCl. This study developed a raft-forming gastroretentive drug delivery system using a polyelectrolyte complex (PEC) of Chitosan and anionic polymers to improve stomach retention, regulate drug release, and enhance therapeutic efficacy. Various formulations were optimized based on polymer type, ratio, cross-linking agent concentration, and hydroxypropyl methylcellulose (HPMC K100M). The best formulation (F12: Chitosan: Carbopol 934) showed high entrapment efficiency (98%), drug loading (11.5%), buoyancy (>12 hours), extended drug release (over 12 hours), and a swelling ratio of 1584% at 8 hours. FTIR and DSC confirmed PEC formation and stability, while FE-SEM demonstrated homogeneity. Drug release followed non-Fickian kinetics, indicating that both diffusion and matrix relaxation contributed to the drug release. This PEC-based system shows promise for sustained stomach delivery of Ondansetron HCl, improving therapeutic efficacy and patient adherence.

PharmaciaVol. 72
Mustansiriyah University (IQ)
Mustansiriyah University
Openalex Percentile: Top 8%
Nausea and vomiting management
4.01
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Development and optimization of an innovative raft-forming antiemetic gastro-retentive system — Mina Safa Aziz, Methaq Hamad Sabar · Pharmacia (2025) | TGRS Research Map | TGRS