Shehata Tamer M, Almostafa Mervt M, Elsewedy Heba S
Food and Security in Saudi Arabia, Scientific Research, Graduate Studies and Scientific Research, King Faisal University, Alhofuf 36362, Al-Ahsa, Saudi Arabia.
Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Alhofuf 31982, Al-Ahsa, Saudi Arabia.
Polymers (Basel). 2022 Jul 26;14(15):3021. doi: 10.3390/polym14153021.
Diabetes mellitus (DM) is a metabolic disorder associated with an increased blood glucose level. The world health burden of DM has increased as a result of numerous causes that necessitates suitable treatment. Pioglitazone (PGZ) is a generally prescribed medication for managing type II diabetes. However, its low solubility creates complications for its formulation. Therefore, the aim of the current study was to incorporate PGZ into a nanoemulsion (NE) formulation prepared with oil (NSO) to boost the action of PGZ. To our knowledge, no previous study has addressed the combination and synergistic effect of PGZ and NSO as a hypoglycemic NE formulation intended for oral administration. An experiment was designed to test several PGZ-loaded NE formulations, varying factors such as NSO, surfactant and co-surfactant concentrations. These factors were investigated for their influence on responses including particle size and release. An optimized PGZ-loaded NE was selected and examined for its morphology, kinetic activity and stability. Further, the anti-diabetic effect of the optimized formulation was evaluated using diabetically induced rats. The optimized formula exhibited a good particle size of 167.1 nm and release of 89.5%. A kinetic study revealed that the drug release followed the Korsmeyer-Peppas mechanism. Additionally, the PGZ-loaded NE formulation was found to be stable, showing non-significant variation in the evaluated parameters when stored at 4 and 25 °C for a period of 3 months. In vivo investigation of the PGZ-loaded NE formulation showed a significant reduction in blood glucose level, which appeared to be enhanced by the presence of NSO. In conclusion, NS-NE could be a promising nanocarrier for enhancing the hypoglycemic effect of PGZ.
糖尿病（DM）是一种与血糖水平升高相关的代谢紊乱疾病。由于多种原因，DM的全球健康负担有所增加，这就需要合适的治疗方法。吡格列酮（PGZ）是一种常用于治疗II型糖尿病的药物。然而，其低溶解度给制剂带来了并发症。因此，本研究的目的是将PGZ纳入用纳米结构油（NSO）制备的纳米乳剂（NE）制剂中，以增强PGZ的作用。据我们所知，以前没有研究探讨过PGZ和NSO作为口服降糖NE制剂的组合及协同作用。设计了一项实验来测试几种载PGZ的NE制剂，改变诸如NSO、表面活性剂和助表面活性剂浓度等因素。研究了这些因素对包括粒径和释放等响应的影响。选择了一种优化的载PGZ的NE并对其形态、动力学活性和稳定性进行了研究。此外，使用糖尿病诱导大鼠评估了优化制剂的抗糖尿病作用。优化后的配方显示出良好的粒径为167.1nm，释放率为89.5%。动力学研究表明药物释放遵循Korsmeyer-Peppas机制。此外，发现载PGZ的NE制剂是稳定的，在4℃和25℃下储存3个月时，评估参数没有显著变化。载PGZ的NE制剂的体内研究表明血糖水平显著降低，NSO的存在似乎增强了这种降低效果。总之，NS-NE可能是一种有前途的纳米载体，可增强PGZ的降糖作用。
