Formulation and Characterization of Bromocriptine Mesylate as Liquid Self-Nano Emulsifying Drug Delivery System

[摘要] Bromocriptine mesylate is a semisynthetic ergot alkaloid derivative with a potent dopaminergic activity, used in the treatment of pituitary tumors, Parkinson's disease (PD), hyperprolactinemia, neuroleptic malignant syndrome, and type 2 diabetes, the oral bioavailability is approximately 6%.Therefore, the aim is the preparation and evaluation of bromocriptine mesylate as a liquid self-nano emulsifying drug delivery system to enhance its solubility, dissolution and thermodynamic stability of the formulation. Solubility study was made in different vehicles to select the best one for dissolving bromocriptine mesylate. Pseudo-ternary phase diagrams were constructed at 1:1, 2:1, 3:1 and 4:1ratios of surfactant and co-surfactant. Four formulations were prepared, using various concentrations of castor oil, tween 80 and ethanol. All the prepared formulations were evaluated for particle size distribution, polydispersity index, drug content, thermodynamic stability, dispersibility and emulsification time, robustness to dilution and in vitro drug dissolution. It was found that, the rate and extent of release for all prepared formulations were significantly higher (p ≤ 0.05) than that in crude drug powder. From the study, it was concluded that self-Nano emulsifying drug delivery system is a promising approach to improve solubility, dissolution and stability of the formulation.

[学科分类] 计算机网络和通讯

[关键词] Bromocriptine Mesylate;Pseudo-ternary phase diagram;Dissolution rate;SNEDDS.