FORMULATION, DEVELOPMENT AND EVALUATION OF LIPOSPHERES OF TOLBUTAMIDE
Uditanshu Singh Rajput, Janki Prasad Rai, Kehar Singh Dhakad, Akhlesh Kumar Singhai
ABSTRACT
This study aims to formulate, develop and evaluate lipospheres of tolbutamide to enhance its solubility, stability, and therapeutic efficacy. Lipospheres were prepared using various lipids and surfactants through the melt-emulsification technique. The prepared lipospheres were characterized for percentage yield, drug entrapment efficiency, particle size distribution, zeta potential, and flow properties. In vitro drug release studies were conducted, and the release kinetics were analyzed using various models. The percentage yield of the formulations ranged from 74.45% to 85.45%, with formulation F2 showing the highest yield (85.45% ± 0.32). The drug entrapment efficiency ranged from 71.12% to 82.25%, with formulation F2 exhibiting the highest efficiency (82.25% ± 0.25). Particle size analysis of the optimized formulation F2 showed a uniform distribution, and the zeta potential indicated good stability. Flow properties of the formulations were satisfactory, with Carr’s Index values below 16% and Hausner’s Ratio close to 1.1. The in vitro drug release profile of formulation F2 demonstrated a controlled release pattern, with 98.74% of the drug released over 12 hours. Release kinetics analysis suggested that the first-order model best described the drug release, indicating a concentration-dependent release mechanism.The formulation and evaluation of tolbutamide lipospheres were successful, with formulation F2 showing optimal characteristics. The lipospheres provided a sustained release of tolbutamide, potentially enhancing its therapeutic efficacy and patient compliance. This study highlights the potential of lipospheres as an effective drug delivery system for tolbutamide, addressing its solubility and stability challenges.
[Full Text Article]