%0 Journal Article %T Optimization and characterization of self-nanoemulsifying drug delivery system of iloperidone using box-behnken design and desirability function. %A Earle RR %A Gadela VR %J Ann Pharm Fr %V 81 %N 1 %D Jan 2023 %M 36037934 暂无%R 10.1016/j.pharma.2022.08.008 %X OBJECTIVE: Iloperidone (IP) is an antipsychotic drug which belongs to Biopharmaceutical Classification System (BCS) II exhibiting poor aqueous solubility. The current investigation explores the possibility of enhancement of solubility and dissolution characteristics of IP by formulation of liquid self-nano emulsifying drug delivery system (L-SNEDDS) utilizing Box-Behnken Design (BBD) and desirability function.
METHODS: The oils, surfactants and co-surfactants used in the study were selected based on solubility of the drug and their emulsification ability. Optimization of the formulation was performed using BBD by employing four response variables such as globule size (nm), percentage transmittance (%), self-emulsification time (sec) and percent drug released in 15min. 2D contour plots and 3D response surface plots were constructed using Design Expert software.
RESULTS: The developed optimal L-SNEDDS of IP through BBD approach resulted in improvement of solubility and dissolution rate as compared with the pure drug. Based on desirability function, optimized formulation was prepared and was assessed for response variables (globule size, percentage transmittance, self-emulsification time and percent drug dissolved in 15min). The characterization studies revealed droplet size to be 21.80±2.41nm, 99.584±0.65% transmittance, 24.43±2.12sec emulsification time and 95.31±1.57% cumulative drug release in 15min.
CONCLUSIONS: The results conclude the potentiality of prepared L-SNEDDS in improving solubility and dissolution rate of IP.