Design and Characterization of Ceritinib Self-nanoemulsifying Drug Delivery Systems

Abstract

Objective: The main objective of the current study was to develop ceritinib SNEDDS for the improvement of solubility, permeability, and drug release. Methods: Solubility of ceritinib was studied in various oils, surfactants, and co-surfactants, and based on its maximum solubility, an oil, surfactant, and co-surfactant were chosen (captex355, tergitol, and propylene glycol) and mixed in varying ratios, the ratios with no phase separation, maximum transmittance and clear in appearance were identified and used for plotting pseudo tertiary phase diagram. Fifteen selfnanoemulsifying drug delivery systems (SNEDDS) formulations were selected from miscible regions of the pseudo ternary phase diagram subjected to thermodynamic stability testing. Formulations that passed stability testing were evaluated for % transmission, drug content, and in vitro drug release analysis. The final optimized formulation was analyzed for particle size, Z average, and zeta potential, followed by fourier transform infrared spectroscopy (FTIR) and SEM analysis. Results: Formulation F13 with maximum drug release of 98.9% in 60 minutes higher than 48 % of the pure drug is considered the optimized formulation. The particle size, Z average, and zeta potential of the ceritinib SNEDDS formulation F13 were 144 nm, 132 nm, and -7.2 mV, respectively. The FTIR and SEM studies do not indicate any drug excipient interaction and confirm uniform drug distribution. The formulation subjected to accelerated stability study is proved to be stable over six months. Conclusion: The results indicate that ceritinib SNEDDS formulations can be designed to enhance the solubility of ceritinib and increase its absorption rate and drug release.