FORMULATION AND EVALUATION OF LORAZEPAM LOADED TRANSFEROSOMES FOR THE MANAGE NEURODEGENERATIVE DISORDERS
Amit Kr Yadav, Reena Shende, Satkar Prasad
ABSTRACT
The present study was undertaken to develop and evaluate a Lorazepam-loaded transfersomal formulation for enhanced topical/transdermal drug delivery with the objective of improving skin permeation, providing sustained drug release, and enhancing therapeutic efficacy. Transfersomes were prepared by varying the concentrations of soya phosphatidylcholine, ethanol, drug, and processing conditions to obtain an optimized vesicular system. Nine formulations (F1–F9) were developed and evaluated for vesicle size and entrapment efficiency. The optimized formulation (F9) exhibited an average vesicle size of 165.58 nm, entrapment efficiency of 73.49%, and a zeta potential of ?40.36 mV, indicating excellent colloidal stability. Transmission Electron Microscopy confirmed the formation of spherical, uniformly distributed vesicles with smooth surfaces. The in-vitro drug release study demonstrated a sustained release profile, with 98.12% cumulative drug release over 12 hours, suggesting efficient controlled drug delivery. Release kinetic analysis revealed that the formulation best fitted the Higuchi model (R² = 0.9902), indicating diffusion-controlled drug release, while the Korsmeyer–Peppas model (R² = 0.9899) suggested the contribution of both diffusion and matrix relaxation mechanisms. Stability studies performed for three months under refrigerated and room temperature conditions demonstrated superior stability under refrigerated storage (4.0 ± 0.2°C), with minimal reduction in drug assay and no significant changes in physical appearance, whereas formulations stored at room temperature exhibited slight turbidity and marginal drug degradation. The overall findings indicate that the optimized Lorazepam-loaded transfersomal formulation possesses desirable physicochemical characteristics, sustained drug release behavior, and satisfactory stability, making it a promising carrier system for topical/transdermal delivery of Lorazepam with the potential to improve therapeutic efficacy and patient compliance.
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