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Purpose <p>The aim of this present study is to develop and optimise a self-nano emulsifying drug delivery system (SNEDDS) for the enhanced oral delivery of dolutegravir (DTG), a poorly water-soluble antiretroviral drug.</p> Methods <p>The SNEDDS formulation was developed using Capmul MCM (oil), Kolliphor RH40 (surfactant), and PEG 400 (co-surfactant). Box Behnken design was employed to optimize the composition of the SNEDDS formulation. The prepared formulations were evaluated for droplet size, polydispersity index (PDI), zeta potential, self-emulsification time, and in vitro drug release.</p> Results <p>The optimized SNEDDS formulation (F2) exhibited a droplet size of 79.2 ± 0.9 nm, PDI of 0.105 ± 0.012, zeta potential of -32.1 ± 1.5 mV, and self-emulsification time of 22 ± 2&#xa0;s. In vitro drug release studies demonstrated a significantly higher cumulative drug release from the optimised SNEDDS formulation (98.9 ± 0.9% in 60&#xa0;min) than pure DTG (42.5 ± 2.1%). The optimized formulation exhibited excellent thermodynamic stability and robustness under various stress conditions. Ex vivo drug release studies using rat stomach tissue confirmed the enhanced drug release potential of the optimized SNEDDS formulation in the gastric environment.</p> Conclusion <p>The developed SNEDDS formulation offers a promising approach for the enhanced oral delivery of DTG, potentially improving its bioavailability and therapeutic efficacy.</p>

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Development and Optimization of a Self-Nanoemulsifying Drug Delivery System (SNEDDS) for Enhanced Oral Delivery of Dolutegravir

  • 期刊论文

  • 发表日期：

    2025年3月7日

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  • Raghuveer Pathuri,
  • Lakshmi Devi Gottemukkula

摘要

Purpose

The aim of this present study is to develop and optimise a self-nano emulsifying drug delivery system (SNEDDS) for the enhanced oral delivery of dolutegravir (DTG), a poorly water-soluble antiretroviral drug.

Methods

The SNEDDS formulation was developed using Capmul MCM (oil), Kolliphor RH40 (surfactant), and PEG 400 (co-surfactant). Box Behnken design was employed to optimize the composition of the SNEDDS formulation. The prepared formulations were evaluated for droplet size, polydispersity index (PDI), zeta potential, self-emulsification time, and in vitro drug release.

Results

The optimized SNEDDS formulation (F2) exhibited a droplet size of 79.2 ± 0.9 nm, PDI of 0.105 ± 0.012, zeta potential of -32.1 ± 1.5 mV, and self-emulsification time of 22 ± 2 s. In vitro drug release studies demonstrated a significantly higher cumulative drug release from the optimised SNEDDS formulation (98.9 ± 0.9% in 60 min) than pure DTG (42.5 ± 2.1%). The optimized formulation exhibited excellent thermodynamic stability and robustness under various stress conditions. Ex vivo drug release studies using rat stomach tissue confirmed the enhanced drug release potential of the optimized SNEDDS formulation in the gastric environment.

Conclusion

The developed SNEDDS formulation offers a promising approach for the enhanced oral delivery of DTG, potentially improving its bioavailability and therapeutic efficacy.