Background <p>Tremors and rigid muscles are symptoms of Parkinson’s disease (PD), which affects about 1% of the global population.</p> Purpose <p>To investigate the integrated therapeutic benefits of the phytopharmaceutical berberine and mucoadhesive nanoliposomes, administered via the nose-to-brain route, to enhance bioavailability, facilitate blood-brain barrier penetration, and augment efficacy against neurodegenerative progression in Parkinson’s disease (PD).</p> Study design <p>This study aimed to develop and characterize chitosan-decorated liposomes (chitosomes) loaded with berberine (BER) for targeted brain delivery via the intranasal route.</p> Methods <p>In vitro characterization of BER loaded chitosomes was conducted including measurement of particle size, zeta potential, EE % and in vitro drug release. The optimized formulation was intranasally administered in rats with rotenone-induced PD animal model, motor function and coordination were investigated besides testing the levels of different biomarkers and histopathological examination.</p> Results <p>The prepared chitosomes had a particle size of 312&#xa0;nm, zeta potential of 34 mV, and high encapsulation efficiency (89.3%) and sustained drug release. In vivo assessments conducted in a rotenone-induced PD animal model revealed notable improvements in motor function and coordination. Biochemical evaluations showed that BER chitosomes reduced α-synuclein by 49% and raised dopamine levels by 55% as compared to the model group. Additionally, BER chitosomes significantly decreased oxidative stress markers by a 67% decrease in NF-κB levels and a one-fold increase in Nrf2. Histological examination showed a noticeable reduction in neuronal degeneration and Lewy body formation.</p> Conclusion <p>Our findings imply that BER chitosomes are a viable intranasal delivery tool for the efficient treatment of PD due to their enhanced bioavailability. and greater nasal mucosa penetration.</p> Graphical Abstract <p></p>

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Innovative approach in Parkinson’s targeting via berberine-loaded mucoadhesive surface-modified liposomes: a multi-faceted study

  • Hisham A. Nematalla,
  • Mona Elharoun,
  • Mohammad M. Abd-Alhaseeb,
  • Hend A. Sharafeldin,
  • Manal A Elsheikh,
  • Haidy Abbas,
  • Amr Elkelish,
  • Komla Mawunyo Dossouvi,
  • Amir E. Mehana,
  • Fathy Elsayed Abdelgawad,
  • Mariam Zewail

摘要

Background

Tremors and rigid muscles are symptoms of Parkinson’s disease (PD), which affects about 1% of the global population.

Purpose

To investigate the integrated therapeutic benefits of the phytopharmaceutical berberine and mucoadhesive nanoliposomes, administered via the nose-to-brain route, to enhance bioavailability, facilitate blood-brain barrier penetration, and augment efficacy against neurodegenerative progression in Parkinson’s disease (PD).

Study design

This study aimed to develop and characterize chitosan-decorated liposomes (chitosomes) loaded with berberine (BER) for targeted brain delivery via the intranasal route.

Methods

In vitro characterization of BER loaded chitosomes was conducted including measurement of particle size, zeta potential, EE % and in vitro drug release. The optimized formulation was intranasally administered in rats with rotenone-induced PD animal model, motor function and coordination were investigated besides testing the levels of different biomarkers and histopathological examination.

Results

The prepared chitosomes had a particle size of 312 nm, zeta potential of 34 mV, and high encapsulation efficiency (89.3%) and sustained drug release. In vivo assessments conducted in a rotenone-induced PD animal model revealed notable improvements in motor function and coordination. Biochemical evaluations showed that BER chitosomes reduced α-synuclein by 49% and raised dopamine levels by 55% as compared to the model group. Additionally, BER chitosomes significantly decreased oxidative stress markers by a 67% decrease in NF-κB levels and a one-fold increase in Nrf2. Histological examination showed a noticeable reduction in neuronal degeneration and Lewy body formation.

Conclusion

Our findings imply that BER chitosomes are a viable intranasal delivery tool for the efficient treatment of PD due to their enhanced bioavailability. and greater nasal mucosa penetration.

Graphical Abstract