Mono-lithocholated exendin-4-loaded glycol chitosan nanoparticles with prolonged antidiabetic effects

International Journal of Pharmaceutics
Sohee SonDong Hee Na

Abstract

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.

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Citations

Feb 26, 2016·Biomacromolecules·Wonhwa LeeJong-Sup Bae
Mar 15, 2016·International Journal of Pharmaceutics·George Dan MogoşanuLudovic Everard Bejenaru
Feb 17, 2018·Archives of Pharmacal Research·Yejin KimDong Hee Na
Sep 14, 2017·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Hongxia WangFuyuan Ding
Jul 4, 2017·International Journal of Pharmaceutics·Maryam Sadat SafaviDong Hee Na

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