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

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
• self-emulsifying drug delivery system (SEDDS)
• oral bioavailability
• hydrophobic ion pairing

Acknowledgement

The authors would like to thank to Mrs. Mousavi (Lab technician).

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

This study was made possible by financial supports from Deputy of Research and Technology, Hamadan University of Medical Sciences (Grant No. 9809196966).