Eluxadoline-Loaded Eudragit Nanoparticles for Irritable Bowel Syndrome with Diarrhea: Formulation, Optimization Using Box-Behnken Design, and Anti-Diarrheal Activity

Eluxadoline (ELD), a recently approved drug, exhibits potential therapeutic effects in the management and treatment of IBS-D. However, its applications have been limited due to poor aqueous solubility, leading to a low dissolution rate and oral bioavailability. The current study's goals are to...

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Bibliographic Details
Published in:Pharmaceutics 2023-05, Vol.15 (5), p.1460
Main Authors: Anwer, Md Khalid, Ahmed, Mohammed Muqtader, Aldawsari, Mohammed F, Iqbal, Muzaffar, Soliman, Gamal A, Aljuffali, Ibrahim A
Format: Article
Language:English
Subjects:
Bioavailability
Constipation
defecation frequency
Diarrhea
disease activity index
dissolution
Drug approval
Drug dosages
eluxadoline
eudragit
Gastrointestinal agents
Health aspects
Irritable bowel syndrome
Motility
Nanoparticles
Narcotics
Optimization
Particle size
Polymers
Technology application
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Summary:Eluxadoline (ELD), a recently approved drug, exhibits potential therapeutic effects in the management and treatment of IBS-D. However, its applications have been limited due to poor aqueous solubility, leading to a low dissolution rate and oral bioavailability. The current study's goals are to prepare ELD-loaded eudragit (EG) nanoparticles (ENPs) and to investigate the anti-diarrheal activity on rats. The prepared ELD-loaded EG-NPs (ENP1-ENP14) were optimized with the help of Box-Behnken Design Expert software. The developed formulation (ENP2) was optimized based on the particle size (286 ± 3.67 nm), PDI (0.263 ± 0.01), and zeta potential (31.8 ± 3.18 mV). The optimized formulation (ENP2) exhibited a sustained release behavior with maximum drug release and followed the Higuchi model. The chronic restraint stress (CRS) was successfully used to develop the IBS-D rat model, which led to increased defecation frequency. The in vivo studies revealed a significant reduction in defecation frequency and disease activity index by ENP2 compared with pure ELD. Thus, the results demonstrated that the developed eudragit-based polymeric nanoparticles can act as a potential approach for the effective delivery of eluxadoline through oral administration for irritable bowel syndrome diarrhea treatment.
ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics15051460