PEGylation of interleukin-10 for the mitigation of enhanced pain states

J Biomed Mater Res A. 2010 Jun 1;93(3):1169-79. doi: 10.1002/jbm.a.32611.

Abstract

The anti-inflammatory cytokine interleukin-10 (IL-10) shows promise for the treatment of neuropathic pain, but for IL-10 to be clinically useful as a short-term therapeutic its duration needs to be improved. In this study, IL-10 was covalently modified with polyethylene glycol (PEG) with the goal of stabilizing and increasing protein levels in the CSF to improve the efficacy of IL-10 for treating neuropathic pain. Two different PEGylation methods were explored in vitro to identify suitable PEGylated IL-10 products for subsequent in vivo testing. PEGylation of IL-10 by acylation yielded a highly PEGylated product with a 35-fold in vitro biological activity reduction. PEGylation of IL-10 by reductive amination yielded products with a minimal number of PEG molecules attached and in vitro biological activity reductions of approximately 3-fold. In vivo collections of cerebrospinal fluid after intrathecal administration demonstrated that 20 kDa PEG attachment to IL-10 increased the concentration of IL-10 in the cerebrospinal fluid over time. Relative to unmodified IL-10, the 20 kDa PEG-IL-10 product exhibited an increased therapeutic duration and magnitude in an animal model of neuropathic pain. This suggests that PEGylation is a viable strategy for the short-term treatment or, in conjunction with other approaches, the long-term treatment of enhanced pain states.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Behavior, Animal / drug effects
  • Cell Line
  • Dose-Response Relationship, Drug
  • Electrophoresis, Polyacrylamide Gel
  • Humans
  • Injections, Spinal
  • Interleukin-10 / administration & dosage
  • Interleukin-10 / cerebrospinal fluid
  • Interleukin-10 / chemistry
  • Interleukin-10 / pharmacology
  • Interleukin-10 / therapeutic use*
  • Mice
  • Pain / chemically induced
  • Pain / drug therapy*
  • Polyethylene Glycols / chemistry
  • Polyethylene Glycols / metabolism*
  • Rats
  • Rats, Sprague-Dawley
  • Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
  • Time Factors

Substances

  • Interleukin-10
  • Polyethylene Glycols