Preparation and characterisation of self-emulsifying drug delivery system (SEDDS) for enhancing oral bioavailability of metformin hydrochloride using hydrophobic ion pairing complexation

J Microencapsul. 2023 Jan;40(1):53-66. doi: 10.1080/02652048.2023.2170488. Epub 2023 Jan 28.

Abstract

Aim: The aim of this study was preparation of a self-emulsifying drug delivery system (SEEDS) containing metformin hydrochloride.

Methods: Hydrophobic ion paired complexes were prepared by electrostatic interaction between metformin and sodium lauryl sulphate (SLS). The nanodroplets were optimised using two-level full factorial methodology and their morphology were examined. In vitro release of metformin from SEDDS was evaluated in simulated gastric and intestinal fluids. Finally, the ex-vivo efficacy of the optimised formulation in enhancing the intestinal permeability of metformin was evaluated using non-everted intestinal sac.

Results: The data revealed that in weight ratio 1:4(metformin: SLS), the highest recovery was achieved. The physico-chemical properties of the optimised nano-droplets including size, polydispersity index (PdI), zeta potential, and loading efficiency (%) were 192.33 ± 9.9 nm, 0.275 ± 0.051; -1.52 mV, and 93.75 ± 0.77% (w/w), respectively.

Conclusions: The data obtained from the intestinal transport study demonstrated that SEDDS can significantly enhance the oral permeability of the compound.

Keywords: Metformin hydrochloride; hydrophobic ion pairing; oral bioavailability; self-emulsifying drug delivery system (SEDDS).

MeSH terms

  • Administration, Oral
  • Biological Availability
  • Drug Delivery Systems / methods
  • Emulsifying Agents / chemistry
  • Emulsions / chemistry
  • Metformin*
  • Sodium Dodecyl Sulfate
  • Solubility

Substances

  • Emulsions
  • Metformin
  • Sodium Dodecyl Sulfate
  • Emulsifying Agents