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Purpose <p>This study was aimed to develop and optimize Pramipexole-loaded nanostructured lipid carriers (NLCs) incorporating <i>Caesalpinia crista</i> seed extract as a natural mucoadhesive agent as a novel approach for enhanced intranasal delivery and effective brain targeting in the management of Parkinson’s disease (PD), while bypassing the blood–brain barrier.</p> Methods <p>Pramipexole-loaded NLCs were prepared using the solvent diffusion method. Glycerol monostearate and triacetins were used as solid and liquid lipid matrices, respectively, while Tween 40 and Poloxamer 188 served as surfactant and co-surfactant. A Box–Behnken Design was employed to optimize formulation variables, including particle size, polydispersity index, zeta potential, drug content, entrapment efficiency, and in vitro drug release. The optimized formulation (NF10) was further evaluated through in vitro release studies, ex vivo nasal permeation and mucoadhesion studies, and in vivo pharmacokinetic studies in rats.</p> Results <p>The NF10 batch exhibited high drug content (98.84 ± 0.82%) and entrapment efficiency (96.02 ± 1.38%). The mean particle size was 215.6 ± 1.9&#xa0;nm with PDI of 0.271 ± 0.92 and zeta potential of − 28 ± 1.25&#xa0;mV, indicating good stability. Sustained drug release was observed in vitro, with 94.71 ± 0.065% release over 6&#xa0;h. Ex vivo studies demonstrated high nasal mucosal permeation (91.51 ± 1.08%) and strong mucoadhesive strength (7357.5 dyne/cm<sup>2</sup>). In vivo pharmacokinetic studies revealed higher Pramipexole concentration in the brain (C<sub>max</sub> 1.27289&#xa0;µg/mL) compared to plasma (1.05289&#xa0;µg/mL).</p> Conclusion <p>The developed mucoadhesive Pramipexole-loaded NLCs significantly enhanced brain targeting via the intranasal route and represent a promising therapeutic approach for effective management of PD.</p>

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Design, Optimization, and In Vivo Evaluation of Mucoadhesive Nanostructured Lipid Carriers for Nose-to-Brain Delivery of Pramipexole in Parkinson’s Disease

  • 期刊论文

  • 发表日期：

    2026年3月26日

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  • Vidhya Thorat,
  • Avinash Tekade

摘要

Purpose

This study was aimed to develop and optimize Pramipexole-loaded nanostructured lipid carriers (NLCs) incorporating Caesalpinia crista seed extract as a natural mucoadhesive agent as a novel approach for enhanced intranasal delivery and effective brain targeting in the management of Parkinson’s disease (PD), while bypassing the blood–brain barrier.

Methods

Pramipexole-loaded NLCs were prepared using the solvent diffusion method. Glycerol monostearate and triacetins were used as solid and liquid lipid matrices, respectively, while Tween 40 and Poloxamer 188 served as surfactant and co-surfactant. A Box–Behnken Design was employed to optimize formulation variables, including particle size, polydispersity index, zeta potential, drug content, entrapment efficiency, and in vitro drug release. The optimized formulation (NF10) was further evaluated through in vitro release studies, ex vivo nasal permeation and mucoadhesion studies, and in vivo pharmacokinetic studies in rats.

Results

The NF10 batch exhibited high drug content (98.84 ± 0.82%) and entrapment efficiency (96.02 ± 1.38%). The mean particle size was 215.6 ± 1.9 nm with PDI of 0.271 ± 0.92 and zeta potential of − 28 ± 1.25 mV, indicating good stability. Sustained drug release was observed in vitro, with 94.71 ± 0.065% release over 6 h. Ex vivo studies demonstrated high nasal mucosal permeation (91.51 ± 1.08%) and strong mucoadhesive strength (7357.5 dyne/cm2). In vivo pharmacokinetic studies revealed higher Pramipexole concentration in the brain (Cmax 1.27289 µg/mL) compared to plasma (1.05289 µg/mL).

Conclusion

The developed mucoadhesive Pramipexole-loaded NLCs significantly enhanced brain targeting via the intranasal route and represent a promising therapeutic approach for effective management of PD.