Son, Sohee Lim, Sung Mook Chae, Su Young Kim, Kwangmeyung Park, Eun Ji Lee, Kang Choon Na, Dong Hee 2024-01-20T05:33:58Z 2024-01-20T05:33:58Z 2022-01-25 2015-11 0378-5173 https://pubs.kist.re.kr/handle/201004/124780 Hydrophobically modified glycol chitosan (HGC) nanoparticles loaded with mono-lithocholic acid-conjugated exendin-4 at the Lys(27) residue (LAM1-Ex4) were prepared and characterized by particle size measurement, proteolytic stability, in vitro drug-release profile, and in vivo antidiabetic effects in a db/db diabetic mouse model. Compared with Ex-4-loaded HGC nanoparticles (Ex4/HGC NPs) prepared as a control, LAM1-Ex4-loaded HGC nanoparticles (LAM1-Ex4/HGC NPs) showed improved drug-loading efficiency, small particle size, enhanced resistance against proteolytic digestion, and an extended in vitro drug release profile. These findings may be attributable to the strong hydrophobic interaction between LAM1-Ex4 and the inner core of HGC. Furthermore, LAM1-Ex4/HGC NPs showed prolonged hypoglycemic efficacy in db/db mice, lasting 1 week after a single subcutaneous administration. The present study demonstrated that LAM1-Ex4/HGC NPs have considerable potential as a long-acting sustained-release antidiabetic system for type 2 diabetes. (C) 2015 Elsevier B.V. All rights reserved. English ELSEVIER Mono-lithocholated exendin-4-loaded glycol chitosan nanoparticles with prolonged antidiabetic effects Article 10.1016/j.ijpharm.2015.08.084 1 INTERNATIONAL JOURNAL OF PHARMACEUTICS, v.495, no.1, pp.81 - 86 INTERNATIONAL JOURNAL OF PHARMACEUTICS 495 1 81 86 N scie scopus 000362970000010 2-s2.0-84940727466 Pharmacology & Pharmacy Pharmacology & Pharmacy Article PEGYLATED EXENDIN-4 TYPE-2 EXENATIDE STABILITY DELIVERY RECEPTOR RELEASE WEIGHT ANALOG Exendin-4 Glycol chitosan Nanoparticles Lithocholic acid Antidiabetic effects