Objective: To develop, optimize, and evaluate diosgenin-loaded solid lipid nanoparticles (DG-SLNs) and nanostructured lipid carriers (DG-NLCs) incorporated into hydrogel formulations (DG-SLN-C and DG-NLC-C) for improved oral and topical delivery in PD management.

Background: Parkinson’s disease (PD) is a progressive neurodegenerative disorder primarily affecting dopaminergic neurons. Existing treatments manage symptoms but fail to halt disease progression. Diosgenin, a naturally occurring steroidal sapogenin found in plants like wild yam and fenugreek, exhibits neuroprotective potential. This study explores lipid-based diosgenin delivery systems to enhance therapeutic efficacy.

Method: DG-SLNs and DG-NLCs were prepared and integrated into a hydrogel using carbopol 934. Formulations were characterized for particle size, zeta potential, entrapment efficiency, and in vitro release kinetics. A haloperidol-induced PD rat model was used to assess pharmacokinetic (PK) and pharmacodynamic (PD) parameters, including bioavailability and neuroprotective effects.

Results: Characterization revealed an average particle size of 132.3 ± 20 nm, a polydispersity index of 0.893, zeta potential of −11.9 mV, and entrapment efficiency of 88.87% ± 0.15%. The in vitro release profile followed the Higuchi model (R² = 0.9821), indicating sustained drug release. Ex vivo permeation studies demonstrated enhanced absorption compared to control formulations. PK studies showed 2.2- and 2.9-fold increases in bioavailability for DG-SLN and DG-NLC (oral), and 3.0- and 3.3-fold increases for DG-SLN-C and DG-NLC-C (topical), respectively. Topical formulations exhibited 1.5- and 1.3-fold higher bioavailability than oral routes. PD studies showed increased dopamine, glutathione, and catalase levels, with reduced lipid peroxidation, supporting neuroprotection. Behavioral assessments confirmed motor function improvement.

Conclusion: Diosgenin-loaded lipid nanoparticles exhibit potential as a neuroprotective strategy for PD. The hydrogel-based formulations provide an alternative approach for enhanced drug delivery, supporting further clinical investigations and large-scale production for improved PD management.

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MDS Abstracts - https://www.mdsabstracts.org/abstract/neuroprotective-role-of-diosgenin-loaded-lipid-nanoparticles-for-parkinsons-disease-pharmacokinetic-and-pharmacodynamic-insights/