Development of fexofenadine self-microemulsifying delivery systems: an efficient way to improve intestinal permeability

Ther Deliv. 2024;15(8):593-604. doi: 10.1080/20415990.2024.2363635. Epub 2024 Jun 28.

Abstract

Aim: The present study aimed to prepare and evaluate fexofenadine self-microemulsifying drug-delivery systems (SMEDDS) formulation and to determine and compare its intestinal permeability using in situ single-pass intestinal perfusion (SPIP) technique.Methods: Fexofenadine-loaded SMEDDS were prepared and optimized. Droplet size, polydispersity index, zeta potential, drug release and intestinal permeability were evaluated.Results: Optimized formulation consisted of 15% oil, 80% surfactant and 5% cosolvent. Droplet size and drug loading of optimized formulation was 13.77 nm and 60 mg/g and it has released 90% of its drug content. Intestinal permeability of fexofenadine was threefold enhanced in SMEDDS compared with free fexofenadine.Conclusion: The results of our study revealed that SMEDDS could be a promising tool for oral delivery of fexofenadine with enhanced dissolution rate and intestinal permeability.

Keywords: SPIP; dissolution; fexofenadine; permeability; self-microemulsifying.

Plain language summary

[Box: see text].

MeSH terms

  • Administration, Oral
  • Animals
  • Chemistry, Pharmaceutical / methods
  • Drug Delivery Systems* / methods
  • Drug Liberation
  • Emulsions*
  • Intestinal Absorption*
  • Intestinal Barrier Function
  • Intestinal Mucosa / metabolism
  • Male
  • Particle Size
  • Permeability*
  • Rats
  • Solubility
  • Surface-Active Agents / chemistry
  • Terfenadine* / administration & dosage
  • Terfenadine* / analogs & derivatives
  • Terfenadine* / chemistry
  • Terfenadine* / pharmacokinetics

Substances

  • fexofenadine
  • Terfenadine
  • Emulsions
  • Surface-Active Agents