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<p>Trifluoperazine hydrochloride (TFP), a typical antipsychotic drug used in schizophrenia management, exhibits poor oral bioavailability due to extensive first-pass metabolism, necessitating frequent dosing and leading to poor patient compliance. This study aimed to develop and optimize a novel transferosomal nanogel formulation for the sustained transdermal delivery of TFP. Transferosomes were prepared using the thin-film hydration technique and optimized through a central composite design to achieve minimal particle size and maximum entrapment efficiency. The optimized vesicles were incorporated into a carbopol-based gel matrix to enhance skin retention and prolong drug release. Physicochemical characterization confirmed nanoscale vesicle size (142.9&#xa0;nm), high entrapment efficiency (91.61%), and suitable colloidal stability. In vitro and ex vivo studies demonstrated enhanced drug release and skin permeation, with a 77.36% cumulative release at 24&#xa0;h and a 1.28-fold increase in transdermal flux compared to TFP suspension. Pharmacokinetic analysis in Wistar rats revealed a significantly prolonged half-life (48.52&#xa0;h) and higher systemic exposure (AUC<sub>0–∞</sub>: 8705.98&#xa0;ng&#xa0;h/mL), confirming sustained absorption. Pharmacodynamic studies using an MK-801-induced schizophrenia model showed improved therapeutic efficacy, with reduced locomotor activity compared to oral treatment. The developed transferosomal nanogel presents a promising alternative to conventional delivery routes by offering improved bioavailability, sustained release, and enhanced therapeutic outcomes in schizophrenia treatment.</p>

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Engineering a Transferosomal Nanogel for Sustained Transdermal Delivery of Trifluoperazine: A Strategy for Improved Schizophrenia Management

  • 期刊论文

  • 发表日期：

    2025年12月17日

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  • Jay Gadge,
  • Pramod.S. Salve,
  • Mohammad Qutub,
  • Ujban Md Hussain,
  • Ram Satpute,
  • Amol A. Tatode,
  • Samiksha Tammewar,
  • Tanvi Premchandani

摘要

Trifluoperazine hydrochloride (TFP), a typical antipsychotic drug used in schizophrenia management, exhibits poor oral bioavailability due to extensive first-pass metabolism, necessitating frequent dosing and leading to poor patient compliance. This study aimed to develop and optimize a novel transferosomal nanogel formulation for the sustained transdermal delivery of TFP. Transferosomes were prepared using the thin-film hydration technique and optimized through a central composite design to achieve minimal particle size and maximum entrapment efficiency. The optimized vesicles were incorporated into a carbopol-based gel matrix to enhance skin retention and prolong drug release. Physicochemical characterization confirmed nanoscale vesicle size (142.9 nm), high entrapment efficiency (91.61%), and suitable colloidal stability. In vitro and ex vivo studies demonstrated enhanced drug release and skin permeation, with a 77.36% cumulative release at 24 h and a 1.28-fold increase in transdermal flux compared to TFP suspension. Pharmacokinetic analysis in Wistar rats revealed a significantly prolonged half-life (48.52 h) and higher systemic exposure (AUC0–∞: 8705.98 ng h/mL), confirming sustained absorption. Pharmacodynamic studies using an MK-801-induced schizophrenia model showed improved therapeutic efficacy, with reduced locomotor activity compared to oral treatment. The developed transferosomal nanogel presents a promising alternative to conventional delivery routes by offering improved bioavailability, sustained release, and enhanced therapeutic outcomes in schizophrenia treatment.