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Purpose <p>The present study aimed to develop and optimize an intranasal liposomal formulation of quetiapine fumarate to enhance nose-to-brain delivery and address limitations associated with oral administration.</p> Methods <p>Quetiapine-loaded liposomes developed using film hydration technique and optimized employing a Box–Behnken factorial design. The influence of formulation independent variables such as lipid composition (X1), hydration time (X2), and sonication time (X3) on size of the liposomes (Y1), polydispersity index (Y2), and %encapsulation efficiency (Y3) was observed. The optimized formulation was characterized for physicochemical properties, compatibility study using FTIR and DSC, morphology by SEM, and in-vitro drug release behavior. In-vivo brain distribution and kinetic studies were conducted on Wistar rats following intranasal administration, and the results were compared with quetiapine dispersion.</p> Results <p>The optimized quetiapine-loaded liposomal formulation exhibited nanosized vesicles with approximately 70% of drug encapsulation in the lipid bilayer. SEM analysis confirmed the formation of spherical and uniformly distributed vesicles. In vitro drug diffusion studies showed a sustained release quetiapine from liposomes, a complete drug release achieved within 6&#xa0;h, compared to rapid release from the quetiapine dispersion. In vivo brain distribution studies following intranasal administration revealed enhanced and prolonged brain exposure of quetiapine from the liposomal formulation, with higher peak brain concentration and 1.5-fold increase in brain compared to the drug dispersion, confirming effective intranasal delivery.</p> Conclusion <p>These findings suggest that intranasal liposomal delivery may represent a potential approach for improving nose-to-brain transport of quetiapine. Further pharmacodynamic and long-term safety studies are warranted to establish its clinical applicability.</p>

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Formulation and Optimization of Novel Liposomal Formulation of Quetiapine Fumarate Intranasal Drug Delivery Using Box Behnken Design Approach

  • 期刊论文

  • 发表日期：

    2026年3月19日

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  • Bhargav Chandegra,
  • Rajnikant Suthar,
  • Jigar Raval,
  • Prajesh Prajapati

摘要

Purpose

The present study aimed to develop and optimize an intranasal liposomal formulation of quetiapine fumarate to enhance nose-to-brain delivery and address limitations associated with oral administration.

Methods

Quetiapine-loaded liposomes developed using film hydration technique and optimized employing a Box–Behnken factorial design. The influence of formulation independent variables such as lipid composition (X1), hydration time (X2), and sonication time (X3) on size of the liposomes (Y1), polydispersity index (Y2), and %encapsulation efficiency (Y3) was observed. The optimized formulation was characterized for physicochemical properties, compatibility study using FTIR and DSC, morphology by SEM, and in-vitro drug release behavior. In-vivo brain distribution and kinetic studies were conducted on Wistar rats following intranasal administration, and the results were compared with quetiapine dispersion.

Results

The optimized quetiapine-loaded liposomal formulation exhibited nanosized vesicles with approximately 70% of drug encapsulation in the lipid bilayer. SEM analysis confirmed the formation of spherical and uniformly distributed vesicles. In vitro drug diffusion studies showed a sustained release quetiapine from liposomes, a complete drug release achieved within 6 h, compared to rapid release from the quetiapine dispersion. In vivo brain distribution studies following intranasal administration revealed enhanced and prolonged brain exposure of quetiapine from the liposomal formulation, with higher peak brain concentration and 1.5-fold increase in brain compared to the drug dispersion, confirming effective intranasal delivery.

Conclusion

These findings suggest that intranasal liposomal delivery may represent a potential approach for improving nose-to-brain transport of quetiapine. Further pharmacodynamic and long-term safety studies are warranted to establish its clinical applicability.