期刊
INTERNATIONAL JOURNAL OF PHARMACEUTICS
卷 495, 期 1, 页码 81-86出版社
ELSEVIER
DOI: 10.1016/j.ijpharm.2015.08.084
关键词
Exendin-4; Glycol chitosan; Nanoparticles; Lithocholic acid; Antidiabetic effects
资金
- National Research Foundation of Korea (NRF) grants - Ministry of Education [NRF-2013R1A1A2064165]
- Ministry of Science, ICT and Future Planning [NRF-2013R1A1A2062043, NRF-2013R1A2A2A01068858]
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.
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