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Objective <p>Ropinirole hydrochloride (RH) is widely used in the management of Parkinson’s disease but suffers from low oral bioavailability and limited brain targeting due to extensive hepatic first-pass metabolism and restricted blood–brain barrier permeability. The present study reports a novel intranasal nanostructured lipid carrier (NLC) system incorporating anise oil as a bioactive liquid lipid, designed to enhance nose-to-brain delivery while providing synergistic neuroprotective effects.</p> Methods <p>RH-loaded NLCs were prepared using high-pressure homogenization and optimized through a Box–Behnken design to achieve desirable physicochemical characteristics. The optimized batch formulation was evaluated for particle size, PDI, entrapment efficiency, in vitro release, ex vivo nasal permeation, pharmacodynamic, pharmacokinetics, nasal histology, and stability testing.</p> Results <p>The optimized formulation exhibited a particle size of 152 ± 0.47&#xa0;nm, low polydispersity index (0.206 ± 0.03), and high entrapment efficiency (85.21 ± 0.43%). The system demonstrated sustained, near-zero-order drug release and significantly improved nasal permeation. Pharmacodynamic and pharmacokinetic evaluations were conducted in a haloperidol-induced Parkinsonian rat model, revealing enhanced motor function, reduced cataleptic behavior, increased brain drug concentration, and decreased systemic exposure compared to conventional formulations. Histopathological analysis confirmed the safety of the nasal mucosa, and the formulation remained stable over six months.</p> Conclusion <p>This study demonstrates the potential of a bioactive intranasal NLC platform for efficient nose-to-brain drug delivery in Parkinson’s disease. The incorporation of anise oil as a functional excipient differentiates the system from conventional NLCs, enabling sustained drug release and enhanced therapeutic efficacy. The developed formulation offers a promising strategy to improve brain targeting while minimizing systemic exposure and associated side effects.</p> Graphical Abstract <p></p>

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Nanostructured Lipid Carriers for Synergistic Nose-to-Brain Delivery of Ropinirole Hydrochloride with Anise Oil for Parkinson’s Disease: Formulation and Preclinical Assessment

  • 期刊论文

  • 发表日期：

    2026年6月25日

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  • Mukesh P. Ratnaparkhi,
  • Prachi D. Jadhav,
  • Aditya P. Kakad,
  • Rahul H. Khiste,
  • Sampada D. Dalvi

摘要

Objective

Ropinirole hydrochloride (RH) is widely used in the management of Parkinson’s disease but suffers from low oral bioavailability and limited brain targeting due to extensive hepatic first-pass metabolism and restricted blood–brain barrier permeability. The present study reports a novel intranasal nanostructured lipid carrier (NLC) system incorporating anise oil as a bioactive liquid lipid, designed to enhance nose-to-brain delivery while providing synergistic neuroprotective effects.

Methods

RH-loaded NLCs were prepared using high-pressure homogenization and optimized through a Box–Behnken design to achieve desirable physicochemical characteristics. The optimized batch formulation was evaluated for particle size, PDI, entrapment efficiency, in vitro release, ex vivo nasal permeation, pharmacodynamic, pharmacokinetics, nasal histology, and stability testing.

Results

The optimized formulation exhibited a particle size of 152 ± 0.47 nm, low polydispersity index (0.206 ± 0.03), and high entrapment efficiency (85.21 ± 0.43%). The system demonstrated sustained, near-zero-order drug release and significantly improved nasal permeation. Pharmacodynamic and pharmacokinetic evaluations were conducted in a haloperidol-induced Parkinsonian rat model, revealing enhanced motor function, reduced cataleptic behavior, increased brain drug concentration, and decreased systemic exposure compared to conventional formulations. Histopathological analysis confirmed the safety of the nasal mucosa, and the formulation remained stable over six months.

Conclusion

This study demonstrates the potential of a bioactive intranasal NLC platform for efficient nose-to-brain drug delivery in Parkinson’s disease. The incorporation of anise oil as a functional excipient differentiates the system from conventional NLCs, enabling sustained drug release and enhanced therapeutic efficacy. The developed formulation offers a promising strategy to improve brain targeting while minimizing systemic exposure and associated side effects.

Graphical Abstract