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<p>Stiripentol (STP), an antiepileptic drug, is administered orally in the form of capsule and dry suspension. However, it is extremely unstable in acidic environment. Hence, to find the feasibility of alternate route of administration and to enhance the bioavailability of drug, STP loaded intranasal <i>in-situ</i> nanolipoidal gel formulation was formulated. The nanostructured lipid carriers (NLC) of the drug were systematically optimized using QbD tool. Melt emulsification &amp; homogenization method was adopted to avoid the degradation of drug. The developed formulation was characterized w.r.t particle size, Polydispersity index (PDI), zeta potential (ZP) along with entrapment efficiency. The developed STP-NLC formulation was further loaded into thermosensitive polymeric solution to form <i>in-situ</i> STP-NLC-gel formulation and evaluated for the <i>in vitro</i> drug release, <i>ex vivo</i> permeation, pharmacokinetic behavior and pharmacodynamic efficacy. The developed formulation was found to possess a particle size of around 196&#xa0;nm, PDI around 0.174 and entrapment efficiency of around 86%. Further, the <i>in-situ</i> STP-NLC-gel formulation demonstrated drug release of ~ 80% in 12&#xa0;h and <i>ex vivo</i> permeation of around ~ 70% in 12&#xa0;h. Intranasal administration of STP-NLC-gel resulted in higher drug distribution in brain, with much lower dose as compared to oral STP formulation. From these experimental outcomes, it can be concluded that the developed <i>in-situ</i> STP-NLC-gel may be beneficial and innovative system considered as a promising formulation for Epilepsy.</p> Graphical Abstract <p></p>

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In-situ Nanolipoidal Gel of Stiripentol for Intranasal Administration: Preclinical Evidence of Enhanced Biopharmaceutical and Therapeutic Outcomes

  • 期刊论文

  • 发表日期：

    2025年8月25日

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  • Harshada Mahajan,
  • Pradip Nirbhavane,
  • Shailesh Chalikwar,
  • Kailas K Moravkar

摘要

Stiripentol (STP), an antiepileptic drug, is administered orally in the form of capsule and dry suspension. However, it is extremely unstable in acidic environment. Hence, to find the feasibility of alternate route of administration and to enhance the bioavailability of drug, STP loaded intranasal in-situ nanolipoidal gel formulation was formulated. The nanostructured lipid carriers (NLC) of the drug were systematically optimized using QbD tool. Melt emulsification & homogenization method was adopted to avoid the degradation of drug. The developed formulation was characterized w.r.t particle size, Polydispersity index (PDI), zeta potential (ZP) along with entrapment efficiency. The developed STP-NLC formulation was further loaded into thermosensitive polymeric solution to form in-situ STP-NLC-gel formulation and evaluated for the in vitro drug release, ex vivo permeation, pharmacokinetic behavior and pharmacodynamic efficacy. The developed formulation was found to possess a particle size of around 196 nm, PDI around 0.174 and entrapment efficiency of around 86%. Further, the in-situ STP-NLC-gel formulation demonstrated drug release of ~ 80% in 12 h and ex vivo permeation of around ~ 70% in 12 h. Intranasal administration of STP-NLC-gel resulted in higher drug distribution in brain, with much lower dose as compared to oral STP formulation. From these experimental outcomes, it can be concluded that the developed in-situ STP-NLC-gel may be beneficial and innovative system considered as a promising formulation for Epilepsy.

Graphical Abstract