School of Pharmacy & Biomedical Sciences, Curtin University, Bentley 6102, Australia.
Biotechnology & Drug Development Research Laboratory, The School of Pharmacy & Biomedical Sciences, Curtin Health Innovation Research Institute, Curtin University, Bentley 6102, Australia.
Ther Deliv. 2020 Nov;11(11):733-753. doi: 10.4155/tde-2020-0102. Epub 2020 Sep 23.
Metformin was originally derived from a botanical ancestry and became the most prescribed, first-line therapy for Type 2 diabetes in most countries. In the last century, metformin was discovered twice for its antiglycemic properties in addition to its antimalarial and anti-influenza effects. Metformin exhibits flip-flop pharmacokinetics with limited oral bioavailability. This review outlines metformin pharmacokinetics, pharmacodynamics and recent advances in polymeric particulate delivery systems as a potential tool to target metformin delivery to specific tissues/organs. This interesting biguanide is being rediscovered this century for multiple clinical indications as anticancer, anti-aging, anti-inflammatory, anti-Alzheimer's and much more. Microparticulate delivery systems of metformin may improve its oral bioavailability and optimize the therapeutic goals expected.
二甲双胍最初源自植物起源,成为大多数国家治疗 2 型糖尿病的最常用、一线治疗药物。在上个世纪,二甲双胍除了具有抗疟疾和抗流感作用外,还因其降血糖特性而被发现了两次。二甲双胍表现出翻转的药代动力学特征,口服生物利用度有限。本综述概述了二甲双胍的药代动力学、药效学以及聚合物颗粒传递系统的最新进展,作为将二甲双胍递送到特定组织/器官的潜在工具。本世纪,这种有趣的双胍类药物因其在抗癌、抗衰老、抗炎、抗老年痴呆症等多种临床适应症中的应用而被重新发现。二甲双胍的微粒传递系统可能会提高其口服生物利用度,并优化预期的治疗目标。