Abstract：
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.
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.
摘要：
目的：伊洛哌酮（IP）是一种抗精神病药物，属于生物药物分类系统（BCS）II，水溶性差。当前的研究探索了通过利用Box-Behnken设计（BBD）和合意功能配制液体自纳米乳化药物递送系统（L-SNEDDS）来增强IP的溶解度和溶出特性的可能性。
方法：油，研究中使用的表面活性剂和助表面活性剂是基于药物的溶解度和它们的乳化能力来选择的。使用BBD通过采用四个响应变量，例如小球大小（nm），透光率(%),自乳化时间(秒)和15min内药物释放百分比。使用DesignExpert软件构建2D等高线图和3D响应面图。
结果：与纯药物相比，通过BBD方法开发的IP最佳L-SNEDDS导致溶解度和溶出速率的提高。基于可取性函数，制备了优化的配方，并评估了响应变量(小球大小，透光率百分比,自乳化时间和15min内药物溶解百分比)。表征研究显示液滴尺寸为21.80±2.41nm，99.584±0.65%透光率，乳化时间24.43±2.12秒,15min内累积药物释放95.31±1.57%。
结论：结果得出结论，所制备的L-SNEDDS在改善IP的溶解度和溶出度方面的潜力。
方法：油，研究中使用的表面活性剂和助表面活性剂是基于药物的溶解度和它们的乳化能力来选择的。使用BBD通过采用四个响应变量，例如小球大小（nm），透光率(%),自乳化时间(秒)和15min内药物释放百分比。使用DesignExpert软件构建2D等高线图和3D响应面图。
结果：与纯药物相比，通过BBD方法开发的IP最佳L-SNEDDS导致溶解度和溶出速率的提高。基于可取性函数，制备了优化的配方，并评估了响应变量(小球大小，透光率百分比,自乳化时间和15min内药物溶解百分比)。表征研究显示液滴尺寸为21.80±2.41nm，99.584±0.65%透光率，乳化时间24.43±2.12秒,15min内累积药物释放95.31±1.57%。
结论：结果得出结论，所制备的L-SNEDDS在改善IP的溶解度和溶出度方面的潜力。
