Improving the Intestinal Permeability of Aprepitant via Self-Microemulsifying Delivery System: In Vitro Development and in Situ Permeation Assessment

Abstract

Background

The present study aimed to design and develop aprepitant-loaded self-microemulsifying drug delivery systems (SMEDDS) and to characterize and assess their intestinal permeability.

Methods

D-optimal design has been used to design and optimize the ratio of formulation components. Prepared aprepitant-loaded SMEDDS formulations were subjected to in vitro characterization studies. Single pass intestinal perfusion method (SPIP) was applied to evaluate the intestinal permeation of aprepitant-loaded SMEDDS and compare it with free aprepitant.

Results

The optimum level of formulation components was determined as oleic acid 10%, Tween 80 60%, and Transcutol P 30%. The particle size of aprepitant-loaded SMEDDS was 152 nm and its PDI (polydispersity index) was 0.35. The optimized aprepitant-loaded SMEDDS showed a zeta potential of -21 ± 8. Effective intestinal permeability (P_eff) of free aprepitant was 1.27 ± 0.44 × 10^− 4 cm/s, whereas for the optimized aprepitant-loaded SMEDDS formulation, it was 2.61 ± 0.79 × 10^− 4 cm/s.

Conclusion

SMEDDS could be considered a promising delivery system for increasing oral bioavailability of aprepitant as the optimized aprepitant-loaded SMEDDS formulation revealed appropriate physicochemical properties and significantly enhanced intestinal permeability.