*Corresponding Author: Virashri Dhumal, Department of Pharmaceutical Sciences, Jayoti Vidyapeeth Women's University, Jaipur-303122, Rajasthan, India.
Objectives: To develop and optimize Syzygium aromaticum extract-loaded microspheres using Box-Behnken design and evaluate their neuroprotective efficacy in rotenone-induced Parkinson's disease model for potential clinical translation in neurodegenerative disorder management.
Methods: Syzygium aromaticum ethanolic extract was prepared by Soxhlet extraction and characterized for physicochemical properties. Microspheres were formulated using oil-in-water emulsion-solvent evaporation method and optimized through Box-Behnken design with sodium alginate concentration, Tween 80 concentration, and stirring speed as independent variables. Seventeen formulations were prepared and evaluated for particle size, entrapment efficiency, drug release, and stability. The optimized batch (F14) was selected based on desirability function demonstrating optimal particle size and maximum entrapment efficiency. Neuroprotective efficacy was assessed in Swiss albino mice using rotenone-induced Parkinson's model through behavioral tests (rotarod, catalepsy, open field, actophotometer) and biochemical estimations (CAT, GSH, SOD, MDA).
Results: The optimized formulation F14 exhibited particle size of 378.64±16.15 μm, entrapment efficiency of 83.66±3.35%, and sustained release of 89.92±4.68% over 12 hours. In vivo studies demonstrated superior neuroprotection with microsphere formulation significantly improving motor coordination (144.3±13.9 sec), reducing catalepsy (33.8±5.9 sec), enhancing locomotor activity (146.5±12.8 counts), and restoring antioxidant enzymes (catalase: 11.25±1.3 µM/mg protein/min; GSH: 10.95±1.3 nM/mg protein) compared to pure extract (p < 0.05-0.001).
Conclusion: The developed microsphere formulation demonstrated enhanced neuroprotective efficacy through improved bioavailability and sustained release, offering significant clinical potential for neurodegenerative disease management. These findings provide strong rationale for advancing this formulation toward preclinical toxicity studies and clinical trials.
Keywords: Syzygium aromaticum, Microspheres, Box-Behnken design, Neuroprotection, Parkinson's disease, Rotenone, Antioxidant activity.
How to cite this article: Dhumal V, Kaura S. Formulation development and in vivo evaluation of Syzygium aromaticum extract-loaded microspheres for neuroprotective activity. Int J Drug Deliv Technol. 2026;16(6s): 30-50; DOI: 10.25258/ijddt.16.6s.4
Source of support: Nil.
Conflict of interest: None