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

Sohee Son, Sung Mook Lim, Su Young Chae, Kwangmeyung Kim, Eun Ji Park, Kang Choon Lee, Dong Hee Na

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13 Scopus citations


Hydrophobically modified glycol chitosan (HGC) nanoparticles loaded with mono-lithocholic acid-conjugated exendin-4 at the Lys27 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.

Original languageEnglish
Pages (from-to)81-86
Number of pages6
JournalInternational Journal of Pharmaceutics
Issue number1
StatePublished - 10 Nov 2015

Bibliographical note

Publisher Copyright:
© 2015 Elsevier B.V. All rights reserved.


  • Antidiabetic effects
  • Exendin-4
  • Glycol chitosan
  • Lithocholic acid
  • Nanoparticles


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