Preparation and optimization of microemulsions of posaconazole

Posaconazole (PSC), a triazole antifungal drug, in light of the need for stronger and broad-spectrum therapeutic options is a white powder with a poor aqueous solubility. The purpose of this study was to develop and optimiz stable mikroemulsions formulations which enhance oral bioavailability of Posaconazol BCS Class II compound by examining the impact of some of the major factors influencing their formation and stability: oil type and composition; surfactant type and concentration, kosurfaktan type and S/KoS ratio). Optimization is directed to achieving an optimum in the function using microemulsions. The other objective of this study was to develop Posaconazole loading ME and to evaluate its physicochemical characteristics and drug release profile. The properties of microemulsions depend not only on the composition variables, but also on the preparation variables such as emulsification path, agitation or emulsification time. These variables can have a significant impact on the final properties of the micro emulsion. The selection of surfactant, co-surfactant and oil to surfactant/co-surfactant ratio is an important determining factor in formation of mikroemulsion. The type of mikroemulsion formed depends on properties of oil, surfactant and co-surfactant. Appropriate oil phase, surfactants and cosurfactants were chosen, considering the solubility of posaconazole in various oils, surfactants and cosurfactants. Microemulsions (MEs) were prepared as thermodynamically stable colloidal dispersions, which were formed by self-emulsification by mixing oil, surfactants and cosurfactants with water titration. This resulted in optically transparent dispersions. The developed formulation was processed through several processes to optimize the formulation, mean particle size, poli dispersite ındix (PDI), zeta potential, pH, stability formulation and dosage forms and in vitro release of the formulations. Droplet size of the ME's is critical for the release of the drug from it post systemic absorption . It was well known that the increase in droplet size was associated with increased oil concentration in the formulation. The (PDI) measurement gives information about the homogeneity of the droplet distribution in formulated microemulsions. Measurements were made three times. The impact of surfactant type on emulsion formation and stability was determined by measuring particle size, PDI, microstructure and stability. The in vitro drug release of the MEs, was carried out using a dialysis membrane. The formulation (1 ml) was placed on the dialysis membrane and suspended in the beaker containing phosphate buffer medium (100 ml). The purpose of optimizing microemulsions is to reduce particle size and PDI, increase stability. optimization is also aimed at achieving an optimum in the function in which microemulsions are used (eg. drug delivery). The results show that MEs have better in vitro release in thermodynamically stable, low viscosity, nanometer size, low PDI simulated fluids. By increasing the water solubility of the antifungal drug (PSC), increasing its antifungal effectiveness and bioavailability, It reduces side effects, increasing stability and targeting infected tissues. With the expansion of the formulations in which this study was conducted, Solubility, stability and control release tests showed that microemulsion systems significantly improve Posaconazole stability and solubility, and that in vitro release of Posaconazole improved significantly compared to the PSC suspension (Noxafil). The results of antifungal tests have been shown that PSC loaded microemulsions are much stronger and more effective than Noxafil. Therefore, in this study, an attempt was made to design, develop, evaluate and characterize the physicochemical properties and drug release profile of PSC's new, thermodynamically stable O / W ME's by spontaneous method for oral use. Quantification of PSC in microemulsions was determined by UV Spectrophotometer and UV detection in HPLC system. With the optimization and development of self-emulsifying systems, the effectiveness of the drug is increased, it allows to reduce the total dose, thereby minimizing its side effects. Less energy requirement in the preparation of self-emulsifying systems.