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Background <p>Levodopa remains the gold standard for Parkinson’s disease (PD) therapy, but oral administration is limited by poor bioavailability, rapid metabolism, and short half-life, leading to fluctuating therapeutic effects. This study aimed to overcome these limitations by developing a liposome-based intranasal spray for direct nose-to-brain delivery using a Quality by Design (QbD) approach.</p> Methods <p> Levodopa-loaded liposomes were prepared via the thin-film hydration method using soya lecithin and cholesterol, and optimized using a 3² full factorial design (Design Expert® 13) with entrapment efficiency and drug release as responses. The optimized liposomes were characterized for particle size, Polydispersibility index (PDI), zeta potential, morphology, drug content, and Fourier transform infra-red (FTIR) compatibility. The selected formulation was incorporated into a nasal spray and evaluated for pH, viscosity, ex vivo permeation, drug release, and stability.</p> Results <p> The optimized formulation (LL3) exhibited high entrapment efficiency (97.2%), drug release (94.8%), nanosized particles (220.7 nm), and good stability (zeta potential –45.4 mV). The nasal spray (NS2) demonstrated suitable pH (6.09), viscosity (26 CP), sustained release (91.5% over 24 h), and enhanced ex vivo drug permeability (82.5%). Stability studies confirmed formulation integrity and reproducibility.</p> Conclusion <p> The QbD-driven Levodopa liposomal nasal spray showed promising potential for brain targeting, particle size 220.7 nm, EE 97.2%, drug release 94.8%., and improved nasal absorption, offering a superior alternative to oral therapy by reducing peripheral side effects and improving patient compliance. Future in vivo pharmacokinetic and pharmacodynamic studies are warranted to confirm its clinical applicability in PD management.</p>

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QbD-Based Development and Optimization of Intranasal Levodopa Liposomal Spray for Improved Brain Targeting in Parkinson’s Disease

  • 期刊论文

  • 发表日期：

    2025年10月30日

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  • Sayali Devdikar,
  • Balaji Shetkar,
  • Rajshree Badagu,
  • Kranti Satpute,
  • Shoaeb Mohammad Syed

摘要

Background

Levodopa remains the gold standard for Parkinson’s disease (PD) therapy, but oral administration is limited by poor bioavailability, rapid metabolism, and short half-life, leading to fluctuating therapeutic effects. This study aimed to overcome these limitations by developing a liposome-based intranasal spray for direct nose-to-brain delivery using a Quality by Design (QbD) approach.

Methods

Levodopa-loaded liposomes were prepared via the thin-film hydration method using soya lecithin and cholesterol, and optimized using a 3² full factorial design (Design Expert® 13) with entrapment efficiency and drug release as responses. The optimized liposomes were characterized for particle size, Polydispersibility index (PDI), zeta potential, morphology, drug content, and Fourier transform infra-red (FTIR) compatibility. The selected formulation was incorporated into a nasal spray and evaluated for pH, viscosity, ex vivo permeation, drug release, and stability.

Results

The optimized formulation (LL3) exhibited high entrapment efficiency (97.2%), drug release (94.8%), nanosized particles (220.7 nm), and good stability (zeta potential –45.4 mV). The nasal spray (NS2) demonstrated suitable pH (6.09), viscosity (26 CP), sustained release (91.5% over 24 h), and enhanced ex vivo drug permeability (82.5%). Stability studies confirmed formulation integrity and reproducibility.

Conclusion

The QbD-driven Levodopa liposomal nasal spray showed promising potential for brain targeting, particle size 220.7 nm, EE 97.2%, drug release 94.8%., and improved nasal absorption, offering a superior alternative to oral therapy by reducing peripheral side effects and improving patient compliance. Future in vivo pharmacokinetic and pharmacodynamic studies are warranted to confirm its clinical applicability in PD management.