Long-acting Antidiabetic Carrier

While Diabetes is a serious chronic disease and corresponding carriers of a sustained release of antidiabetic drugs are much desired, one is faced with a dilemma of a hyperglycemic symptom after meal and a hypoglycemic symptom during limosis. Such a dilemma is hopefully resolved upon the emergence of a new peptide drug as an agonist of glucagon-like peptide-1 (GLP-1) and a polymeric thermogel.

A biodegradable block copolymer was used to encapsulate drugs at room or lower temperatures. The mixture is injectable and exhibits a physical gelation at body temperature. Besides the thermogelling, the key of the material techniques comes also from some additives to reduce initial burst release and enhance late relate, another dilemma in the sustained release of peptide drugs.

Due to the novel techniques developed by Ding group in Fudan University and Chen group in State Institute of Pharmaceutical Industry, a long-acting formulation of exenatide (EXT) was invented and one-week drug efficacy after a single injection has been achieved in a mice model. The cooperation article with Dr. Lin YU as the co-first author has been published in Biomaterials.

Kun Li, Lin Yu (equal contribution), Xiaojun Liu, Chang Chen, Qinghua Chen*, and Jiandong Ding*, A long-acting formulation of a polypeptide drug exenatide in treatment of diabetes using an injectable block copolymer hydrogel, Biomaterials, 34(11), 2834–2842 (2013)

(a) Amino acid sequence of EXT with acidic residues in red, alkaline residues in blue, and neutral residues in black. (b) Schematic presentation of a mixing approach to achieve a thermogel system; (c) Schematic presentation of the initial burst and incomplete release and a possible facile strategy to partially improve them simply by addition of some appropriate combination of excipients.