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<p>Parkinson's disease (PD) is a major neurodegenerative disorder associated with the loss of dopaminergic neurons, particularly in older adults. The effectiveness of orally administered anti-PD drugs is often limited by low plasma levels and drug efflux mechanisms in neural tissues. Baicalin (BA), a flavone with neuroprotective properties, faces challenges due to its poor water solubility and difficulty in crossing the blood–brain barrier. To overcome these issues, BA nanocrystals (BA-NC) were developed, which show potential as a treatment for PD. These cubic nanocrystals, approximately 126.8&#xa0;nm with a surface charge of -12.4 and 86.03% drug content, demonstrated rapid dissolution in vitro. Biosafety was confirmed through morphological studies of goat nasal tissue, and permeation studies indicated enhanced flux for BA-NCs compared to BA suspension. In vitro assays using the SH-SY5Y cell line, treated with rotenone, indicated that both BA-NCs and BA solution could alleviate oxidative stress and maintain mitochondrial function. Furthermore, in vivo studies revealed that intranasal administration of BA-NCs provided a longer mean residence time and greater systemic exposure than oral administration of either BA-NCs or BA solution. These findings suggest that BA-NCs offer a promising strategy for improving PD therapy.</p>

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Neuroprotective Potential of Baicalin Nanocrystals: Optimisation, Comprehensive In Vitro SH-SY5Y Cell Studies and In Vivo Pharmacokinetics

  • 期刊论文

  • 发表日期：

    2025年2月8日

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  • Akshay Fadnis,
  • Akshada Mhaske,
  • Rahul Shukla

摘要

Parkinson's disease (PD) is a major neurodegenerative disorder associated with the loss of dopaminergic neurons, particularly in older adults. The effectiveness of orally administered anti-PD drugs is often limited by low plasma levels and drug efflux mechanisms in neural tissues. Baicalin (BA), a flavone with neuroprotective properties, faces challenges due to its poor water solubility and difficulty in crossing the blood–brain barrier. To overcome these issues, BA nanocrystals (BA-NC) were developed, which show potential as a treatment for PD. These cubic nanocrystals, approximately 126.8 nm with a surface charge of -12.4 and 86.03% drug content, demonstrated rapid dissolution in vitro. Biosafety was confirmed through morphological studies of goat nasal tissue, and permeation studies indicated enhanced flux for BA-NCs compared to BA suspension. In vitro assays using the SH-SY5Y cell line, treated with rotenone, indicated that both BA-NCs and BA solution could alleviate oxidative stress and maintain mitochondrial function. Furthermore, in vivo studies revealed that intranasal administration of BA-NCs provided a longer mean residence time and greater systemic exposure than oral administration of either BA-NCs or BA solution. These findings suggest that BA-NCs offer a promising strategy for improving PD therapy.