Kumar Vipan, Poonia Neelam, Kumar Pradeep, Kumar Verma Prabhakar, Alshammari Abdulrahman, Albekairi Norah A, Kabra Atul, Yadav Neera
Department of Pharmaceutical Chemistry, JCDM College of Pharmacy, Sirsa 125055, India.
Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak 124001, India.
Saudi Pharm J. 2024 May;32(5):102046. doi: 10.1016/j.jsps.2024.102046. Epub 2024 Mar 21.
Glipizide; an insulin secretagogue belonging to the sulfonylurea class, is a widely used antidiabetic drug for managing type 2 diabetes. However, the need for life-long administration and repeated doses poses challenges in maintaining optimal blood glucose levels. In this regard, orally active sustained-release nano-formulations can be a better alternative to traditional antidiabetic formulations. The present study explored an innovative approach by formulating orally active sustained-release nano-micelles using the amphiphilic lauric acid-conjugated-F127 (LAF127) block copolymer. LAF127 block copolymer was synthesized through esterification and thoroughly characterized before being employed to develop glipizide-loaded nano-micelles (GNM) the thin-film hydration technique. The optimized formulation exhibited mean particle size of 341.40 ± 3.21 nm and depicted homogeneous particle size distribution with a polydispersity index (PDI) < 0.2. The formulation revealed a surface charge of -17.11 ± 6.23 mV. The release studies of glipizide from developed formulation depicted a sustained release profile. Drug loaded micelles exhibited a substantial reduction in blood glucose levels in diabetic rats for a duration of up to 24 h. Notably, neither the blank nano-micelles of LAF127 nor the drug loaded micelles manifested any indications of toxicity in healthy rats. This study provides an insight on suitability of synthesized LAF127 block copolymer for development of effective oral drug delivery systems for anti-diabetic activity without any significant adverse effects.
格列吡嗪是一种属于磺酰脲类的胰岛素促泌剂,是一种广泛用于治疗2型糖尿病的抗糖尿病药物。然而,终身给药和重复给药的需求给维持最佳血糖水平带来了挑战。在这方面,口服活性缓释纳米制剂可能是传统抗糖尿病制剂的更好替代品。本研究探索了一种创新方法,即使用两亲性月桂酸共轭F127(LAF127)嵌段共聚物制备口服活性缓释纳米胶束。LAF127嵌段共聚物通过酯化反应合成,并在用于通过薄膜水化技术制备载格列吡嗪纳米胶束(GNM)之前进行了全面表征。优化后的制剂平均粒径为341.40±3.21nm,粒径分布均匀,多分散指数(PDI)<0.2。该制剂的表面电荷为-17.11±6.23mV。格列吡嗪从所开发制剂中的释放研究显示出缓释特性。载药胶束在长达24小时的时间内使糖尿病大鼠的血糖水平大幅降低。值得注意的是,LAF127的空白纳米胶束和载药胶束在健康大鼠中均未表现出任何毒性迹象。本研究为合成的LAF127嵌段共聚物用于开发有效的口服抗糖尿病药物递送系统的适用性提供了见解,且无任何明显不良反应。