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

Int J Pharm · 2015

Last updated 2026-05-28

In a study on diabetic mice, a new form of the diabetes drug exendin-4, delivered via specially designed nanoparticles, maintained blood sugar control for a full week after a single injection. The modified drug, called LAM1-Ex4, was more stable and released slowly compared to the standard version, likely due to its strong interaction with the nanoparticle carrier. The nanoparticles were also smaller and better at protecting the drug from breaking down in the body.

AI summary of the abstract below.

Journal	Int J Pharm, 2015
Citations	10
Relative citation ratio	0.45
NIH percentile	27
Molecules	—
Conditions studied	Type 2 Diabetes

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.

Verbatim abstract via PubMed 26325318 ↗