FORMULATION AND EVALUATION OF BARICITINIB TRANSFERSOMES

ABSTRACT

Transferosomes' are specially optimized particles or vesicles, which can respond to an external stress by rapid and energetically inexpensive, shape transformations. The present study was carried out to use statistical techniques of quality by design to develop and optimize Methotrexate Transfersomes by conventional rotary evaporation sonication techniques. A32 full factorial design was used to understand the main effects and interaction of formulation variables. The relationship between the dependent and independent variables was further elucidated using contour plots. Then, experimental design combined with desirability functions to predict the desired quality.

A conventional rotary evaporation sonication technique was developed to prepare Baricitinib transfersomes using Phopholipon 90 G as a lipid (SPC) and SPAN 80 as an edge activator (EA).Preformulationstudiesprovedthepurityofdrugandcompatibilityof drug and excipients was evaluated by DSC study. BCT loaded transfersomes was successfully formulated using 32 full factorial design and desirability function. The %entrapment efficiency, deformability index and particle size were highly dependent on the SPC: EA ratio, and BCT concentration for the preparation of BCT loaded Transfersomes. SPC: EA ratio and BCT concentration had a positive effect on % Entrapment efficiency and negative effect on deformability. But particle size was not much affected. Using contour plots, response surface plots and % Bias, formulation was optimized. Batch M5 (1:1PC: EA, 2%w/v BCT) is best batch among nine combinations. Surface morphology of transfersomes was evaluated by TEM study. A good interaction between drug and excipients were found with FTIR study of transferosomes. It was advisable to store BCT-TFS at refrigerated conditions (4±2 0C).Optimum drug: lipidratiois0.1-0.4.BCT-TFS was successfully optimized with experimental design and desirability function.                                                                                

KEYWORDS: Baricitinib, transferosomes, BCT-TFS.