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<p>This study focuses on the development of lyophilized nasal powders of ropinirole hydrochloride (RH), composed of Poloxamer 407 triblock copolymer (P407), surfactant Tween 80 (Tw80) and derivatives of βCD [methyl-β-CD (MβCD) or hydroxy-propyl-β-CD (HPβCD)] for managing Parkinson's disease. The lyophilized compositions were produced by freeze-drying of the corresponding colloidal dispersions. The innovative aspect of this research lies in the integration of these diverse biomaterials to develop advanced drug delivery systems for nasal administration. The optimal lyophilized formulations were blended with spray-dried microparticles of mannitol and lecithin (MLMPs) in various ratios. The blending process resulted in powders with improved morphological characteristics, as evidenced by Scanning Electron Microscopy analysis. Nasal powders were characterized&#xa0;through <i>in vitro</i>&#xa0;diffusion and&#xa0;<i>ex vivo</i> permeation studies. Finally, a comparison between the nasal powders and the corresponding colloidal dispersions was held. Results showed that the lyophilized powders had a superior release profile compared to colloidal dispersions, and blending with MPMPs further enhanced this effect. <i>Ex vivo</i> powders' permeation across rabbit nasal mucosa was found to be more efficient compared to pure RH solution.&#xa0;In particular, the lyophilized formulation of (P407/Tw80/HPβCD)/RH 10:5 blended with MLMPs (25:75) achieved 54.40 ± 3.30% permeation of the loading dose and a mass balance of 98.15 ± 1.61%. This study demonstrates the potential of these formulations for effective nose-to-brain drug delivery. Ongoing <i>in vivo</i> pharmacokinetic studies are being conducted to assess the performance of the optimal formulations in an appropriate animal model.</p> Graphical Abstract <p></p>

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Advanced P407/Tw80/βCD based Nasal Powders of Ropinirole Hydrochloride for Nose-to-Brain Delivery in Parkinson’s Disease: Preparation and Comprehensive In Vitro and Ex Vivo Evaluation

  • 期刊论文

  • 发表日期：

    2025年9月18日

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  • Elmina-Marina Saitani,
  • Paraskevi Papakyriakopoulou,
  • Stefanos Kikionis,
  • Natassa Pippa,
  • Stergios Pispas,
  • Georgia Valsami

摘要

This study focuses on the development of lyophilized nasal powders of ropinirole hydrochloride (RH), composed of Poloxamer 407 triblock copolymer (P407), surfactant Tween 80 (Tw80) and derivatives of βCD [methyl-β-CD (MβCD) or hydroxy-propyl-β-CD (HPβCD)] for managing Parkinson's disease. The lyophilized compositions were produced by freeze-drying of the corresponding colloidal dispersions. The innovative aspect of this research lies in the integration of these diverse biomaterials to develop advanced drug delivery systems for nasal administration. The optimal lyophilized formulations were blended with spray-dried microparticles of mannitol and lecithin (MLMPs) in various ratios. The blending process resulted in powders with improved morphological characteristics, as evidenced by Scanning Electron Microscopy analysis. Nasal powders were characterized through in vitro diffusion and ex vivo permeation studies. Finally, a comparison between the nasal powders and the corresponding colloidal dispersions was held. Results showed that the lyophilized powders had a superior release profile compared to colloidal dispersions, and blending with MPMPs further enhanced this effect. Ex vivo powders' permeation across rabbit nasal mucosa was found to be more efficient compared to pure RH solution. In particular, the lyophilized formulation of (P407/Tw80/HPβCD)/RH 10:5 blended with MLMPs (25:75) achieved 54.40 ± 3.30% permeation of the loading dose and a mass balance of 98.15 ± 1.61%. This study demonstrates the potential of these formulations for effective nose-to-brain drug delivery. Ongoing in vivo pharmacokinetic studies are being conducted to assess the performance of the optimal formulations in an appropriate animal model.

Graphical Abstract