DEVELOPMENT AND CHARACTERIZATION OF BAICALEIN-LOADED ASPASOMES AND EVALUATION OF CYTOTOXICITY ON RAW 264.7 CELL LINE

Baicalein is a flavonoid obtained from the Scuteellaria baicalensis plant. It is known to have a wide variety of effects such as antibacterial, antitumoral, antioxidant and anti-inflammatory. Since Baicalein has low bioavailability and stability, its sufficient effect in treatment cannot be seen. It is possible to increase its effectiveness with an appropriate formulation that will increase its stability, protect its chemical structure and demonstrate its effectiveness.Micro and nanoparticulate drug forms are a group that has been studied intensively in order to increase the treatment effectiveness provided by conventional drug forms and to reduce the therapeutic dose and side effects used in treatment. Aspasomal drug carrier systems discovered in recent years are defined as a vesicular system formed by a double layer of ascorbyl palmitate. In our study, aspasomes were prepared by the film hydration method using ascorbyl palmitate, cholesterol and dicethyl phosphate. Following development of aspasomes, characterization parameters (particle size and distribution, zeta potential, polydispersity index, encapsulation efficiency, in vitro release) were examined. In addition, cytotoxicity tests were carried out on RAW 264.7 cells in order to determine the maximum amounts of active and excipients to be used during formulation development that can be used safely while preserving the viability of the cells. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide (MTT) test, which is widely used to evaluate the viability of cells, was applied. As results, Baicalein-loaded aspasomes were successfully obtained. The particle size of Baicalein-loaded aspasomes was 425±0.258 nm, the polydispersity index was 0.207±0.035, the zeta potential was -38.1±2.31 mV, the loading efficiency was 40±1.02%, and the in vitro release rate at the end of 24 hours was 85±0.95%. In formulation development, the initial dose of Baicalein (20 μg/mL) and the viability rate of aspasomes on RAW 264.7 cells were determined as 74.1% and 80.0%, respectively.<br>