Enhancing Oral Bioavailability of Domperidone Maleate: Formulation, <i>In vitro</i> Permeability Evaluation In-caco-2 Cell Monolayers and <i>In situ</i> Rat Intestinal Permeability Studies

Okur N. U., Caglar E. S., KAYNAK M. S., Diril M., ÖZCAN S., KARASULU H. Y.

CURRENT DRUG DELIVERY, vol.21, no.7, pp.1010-1023, 2024 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 21 Issue: 7
  • Publication Date: 2024
  • Doi Number: 10.2174/1567201820666230214091509
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, BIOSIS, Biotechnology Research Abstracts, Chemical Abstracts Core, EMBASE, MEDLINE
  • Page Numbers: pp.1010-1023
  • Anadolu University Affiliated: Yes


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 +/- 0.02x10-4) from Caco-2 cell monolayer permeability experiments. The study also revealed greater Peff values (2.122 +/- 0.892x10-4 cm/s) for the optimal formulation from in situ intestinal perfusion analyses in comparison to control groups (Domperidone; 0.802 +/- 0.418x10-4 cm/s). Conclusion To conclude, prepared formulations can be a promising way of oral administration of Biopharmaceutical Classification System Class II drugs.