The aim of the present study was to formulate and evaluate Budesonide proniosomes for enhancement of solubility and bioavailability. To develop and evaluate budesonide proniosomes was the main objective of this research work. For the preparation of proniosomes slurry, a method was used using different ratios of (cholesterol: surfactant) (1:1.5) with the help of carriers. For optimization of formulation Box-Behnken Design was used in that concentration of span 60, cholesterol, and maltodextrin. The prepared proniosomes were evaluated for particle size, entrapment efficiency, and in-vitro drug release (up to 6 h). Particle size, entrapment efficiency, and drug release of optimized batch (F14) were found to be 220.3 nm, 81.42%, and 30.71%, respectively. The data were fitted into a zero order model, and the correlation value found to be 0.952, indicating controlled release. Transformation of niosomes from proniosomes and morphology study of the optimized batch was studied by Inverted Microscopy and Transmission Electron Microscopy, etc. Statistical analysis of ex-vivo permeation enhancement assessed from the flux, permeability coefficient, and enhancement ratio was significantly higher for proniosomes as compared to control. During the stability study of 30 days, it was found that no signs of instability like agglomeration, crystallization, and variation in vesicle size and entrapment efficiency. The preparation method of Budesonide proniosomes was more efficient and more effective. The optimized Budesonide proniosomes did improve the solubility and bioavailability of budesonide and offer a new approach to enhance the targeted drug delivery system of poorly water-soluble drugs.
INTRODUCTION:Budesonide is a locally acting glucocorticosteroid with an extensive, primarily hepatic, metabolism after oral administration. It is rapidly absorbed and biotransformed by cytochrome P450 (CYP) 3A to metabolites with negligible glucocorticoid activity 1.