Pharmacological Signatures of the Exenatide Nanoparticles Against Hepatic Ischemia/Reperfusion-induced Pancreatic Injury

Transplant Proc. 2019 Apr;51(3):960-965. doi: 10.1016/j.transproceed.2019.01.031. Epub 2019 Jan 9.

Abstract

Background: Hepatic ischemia/reperfusion-induced pancreatic injury (HI/RPI) is an important pathophysiological phenomenon in clinics. Exenatide is found to have hepatopancreatic protection; however, the half-life of exenatide is extremely short, which limits its clinical application. In the present study, we described an exenatide nanocarrier based on poly(L-lysine)-poly(ethylene glycol)-poly(L-lysine) (PLL-PEG-PLL) and aimed to investigate the protective effects of exenatide/PLL-PEG-PLL on HI/RPI.

Methods: PLL-PEG-PLL was synthesized and estimated by being applied as a nanocarrier for lengthening delivery of exenatide. Exenatide was loaded into PLL-PEG-PLL by electrostatic interactions at pH 7.4. The loading and release of exenatide from PLL-PEG-PLL were characterized in vitro. The pancreatic protection of exenatide/PLL-PEG-PLL was assessed using the animal model, histopathological examination, blood biochemical indices detection, antioxidant activity, and anti-inflammatory evaluation in vivo.

Results: Exenatide/PLL-PEG-PLL displayed efficient loading and sustained release. Exenatide/PLL-PEG-PLL complex moderated HI/RPI and enlarged islet functionality compared to free exenatide.

Conclusion: We propose that the nanocarrier PLL-PEG-PLL may function as a potent exenatide nanocarrier for augmenting anti-HI/RPI pharmacotherapy with unprecedented clinical benefits.

MeSH terms

  • Animals
  • Disease Models, Animal
  • Exenatide / pharmacology*
  • Hypoglycemic Agents / pharmacology
  • Liver / blood supply*
  • Male
  • Nanoparticles*
  • Pancreatic Diseases / drug therapy*
  • Pancreatic Diseases / etiology
  • Pancreatic Diseases / pathology
  • Rats
  • Rats, Sprague-Dawley
  • Reperfusion Injury / complications
  • Reperfusion Injury / drug therapy*
  • Reperfusion Injury / pathology

Substances

  • Hypoglycemic Agents
  • Exenatide