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Background <p>The present study aimed to design and develop aprepitant-loaded self-microemulsifying drug delivery systems (SMEDDS) and to characterize and assess their intestinal permeability.</p> Methods <p>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.</p> Results <p>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&#xa0;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<sub>eff</sub>) of free aprepitant was 1.27 ± 0.44 × 10<sup>− 4</sup> cm/s, whereas for the optimized aprepitant-loaded SMEDDS formulation, it was 2.61 ± 0.79 × 10<sup>− 4</sup> cm/s.</p> Conclusion <p>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.</p>

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

  • 期刊论文

  • 发表日期：

    2025年1月24日

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  • Ziba Islambulchilar,
  • Giso Akbarian,
  • Mohammad Mahmoudian,
  • Hadi Valizadeh,
  • Parvin Zakeri-Milani

摘要

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 (Peff) 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.