Title:Enhancing Oral Bioavailability of Domperidone Maleate: Formulation,
In vitro Permeability Evaluation In-caco-2 Cell Monolayers and In situ Rat
Intestinal Permeability Studies
Volume: 21
Issue: 7
Author(s): Neslihan Üstündağ Okur*, Emre Şefik Çağlar, Mustafa Sinan Kaynak*, Mine Diril, Saniye Özcan and Hatice Yeşim Karasulu
Affiliation:
- Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Health Sciences, Istanbul, Turkey
- Department of Pharmaceutical Technology, Faculty of Pharmacy, Anadolu University, Eskişehir, Turke
Keywords:
Domperidone, SEDDS, oral drug delivery, in situ intestinal permeability, Caco-2 cell, microbial colonization.
Abstract:
Background: The domperidone maleate, a lipophilic agent classified as a Biopharmaceutical
Classification System Class II substance with weak water solubility. Self- Emulsifying Drug Delivery
System is a novel approach to improve water solubility and, ultimately bioavailability of drugs.
Objective: This study aimed to develop and characterize new domperidone-loaded self-emulsifying drug
delivery systems as an alternative formulation and to evaluate the permeability of domperidone-loaded
self-emulsifying drug delivery systems by using Caco-2 cells and via single-pass intestinal perfusion
method.
Methods: Three self-emulsifying drug delivery systems were prepared and characterized in terms of pH,
viscosity, droplet size, zeta potential, polydispersity index, conductivity, etc. Each formulation underwent
10, 100, 200, and 500 times dilution in intestinal buffer pH 6.8 and stomach buffer pH 1.2, respectively.
Female Sprague Dawley rats were employed for in situ single-pass intestinal perfusion investigations.
Results: Results of the study revealed that the ideal self-emulsifying drug delivery systems formulation
showed narrow droplet size, ideal zeta potential, and no conductivity. Additionally, as compared to the
control groups, the optimum formulation had better apparent permeability (12.74 ± 0.02×10-4) from
Caco-2 cell monolayer permeability experiments. The study also revealed greater Peff values (2.122 ±
0.892×10-4 cm/s) for the optimal formulation from in situ intestinal perfusion analyses in comparison to
control groups (Domperidone; 0.802 ± 0.418×10-4 cm/s).
Conclusion: To conclude, prepared formulations can be a promising way of oral administration of Biopharmaceutical
Classification System Class II drugs.
