Solubility enhancement of fexofenadine using self-nano emulsifying drug delivery system for improved biomimetic attributes

Ann Pharm Fr. 2024 May;82(3):433-445. doi: 10.1016/j.pharma.2023.10.003. Epub 2023 Oct 11.

Abstract

Background: Fexofenadine is a poorly water-soluble drug, which limit its bioavailability and ultimately therapeutic efficacy. Liquid self-nano emulsifying drug delivery system (L-SNEDDs) is an approach that can enhance the solubility of fexofenadine by increasing its surface area and reducing the particle size, which increases the rate and extent of drug dissolution.

Method: In this investigation, L-SNEDDs of fexofenadine was made up using surfactants and co-surfactant. The SNEDDS formulation was optimized using a pseudo-ternary phase diagram and characterized.

Results: The optimized L-SNEDDS incorporated fexofenadine were thermodynamically stable and showed mean droplet size and zeta potential of 155nm and -18mV, respectively unaffected by the media pH. In addition, the viscosity, and refractive index were observed 18.4 and 1.49 cps, respectively for optimized L-SNEDDS fortified fexofenadine. The results of Fourier transform infrared spectroscopy revealed an insignificant interaction between the fexofenadine and excipients. A drug loading efficiency of 94.20% resulted with a complete in vitro drug release in 2h, compared with the pure drug, which demonstrate significant improvement in the efficacy. Moreover, these results signify that on further in vivo assessment L-SNEDDS fortified fexofenadine can indicate improvement in pharmacokinetic and clinical outcome.

Conclusion: Thus, the investigation revealed that, the L-SNEDDs incorporated fexofenadine was most effective with a mixture of surfactant and co-surfactant with improved solubility intend to relieve pain associated with inflammation with single-dose oral administration.

Keywords: Co-surfactant; Fexofenadine; Self-nano emulsifying system; Solubility; Solubilité; Surfactant; Système auto-nano-émulsionnant; Tensioactif.

MeSH terms

  • Administration, Oral
  • Biomimetics
  • Drug Delivery Systems* / methods
  • Emulsions
  • Nanoparticle Drug Delivery System
  • Nanoparticles* / chemistry
  • Particle Size
  • Solubility
  • Surface-Active Agents / chemistry
  • Terfenadine / analogs & derivatives*

Substances

  • Nanoparticle Drug Delivery System
  • fexofenadine
  • Emulsions
  • Surface-Active Agents
  • Terfenadine