Controlled Delivery of a Focal Adhesion Kinase Inhibitor Results in Accelerated Wound Closure with Decreased Scar Formation

J Invest Dermatol. 2018 Nov;138(11):2452-2460. doi: 10.1016/j.jid.2018.04.034. Epub 2018 Jul 12.

Abstract

Formation of scars after wounding or trauma represents a significant health care burden costing the economy billions of dollars every year. Activation of focal adhesion kinase (FAK) has been shown to play a pivotal role in transducing mechanical signals to elicit fibrotic responses and scar formation during wound repair. We have previously shown that inhibition of FAK using local injections of a small molecule FAK inhibitor (FAKI) can attenuate scar development in a hypertrophic scar model. Clinical translation of FAKI therapy has been challenging, however, because of the lack of an effective drug delivery system for extensive burn injuries, blast injuries, and large excisional injuries. To address this issue, we have developed a pullulan collagen-based hydrogel to deliver FAKI to excisional and burn wounds in mice. Specifically, two distinct drug-laden hydrogels were developed for rapid or sustained release of FAKI for treatment of burn wounds and excisional wounds, respectively. Controlled delivery of FAKI via pullulan collagen hydrogels accelerated wound healing and reduced collagen deposition and activation of scar-forming myofibroblasts in both wound healing models. Our study highlights a biomaterial-based drug delivery approach for wound and scar management that has significant translational implications.

Keywords: FAK; FAKI; HTS; focal adhesion kinase; focal adhesion kinase inhibitor; hypertrophic scar; p-; phosphorylated.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Burns / drug therapy*
  • Cells, Cultured
  • Cicatrix / drug therapy*
  • Collagen / chemistry
  • Disease Models, Animal
  • Drug Delivery Systems
  • Female
  • Focal Adhesion Protein-Tyrosine Kinases / antagonists & inhibitors
  • Glucans / chemistry
  • Humans
  • Hydrogel, Polyethylene Glycol Dimethacrylate / chemistry
  • Hydrogel, Polyethylene Glycol Dimethacrylate / therapeutic use*
  • Indoles / pharmacology
  • Indoles / therapeutic use*
  • Mice
  • Mice, Inbred C57BL
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use*
  • Skin / drug effects*
  • Skin / pathology
  • Sulfonamides / pharmacology
  • Sulfonamides / therapeutic use*
  • Wound Healing / drug effects*

Substances

  • Glucans
  • Indoles
  • N-methyl-N-(3-((2-(2-oxo-2,3-dihydro-1H-indol-5-ylamino)-5-trifluoromethyl-pyrimidin-4-ylamino)-methyl)-pyridin-2-yl)-methanesulfonamide
  • Protein Kinase Inhibitors
  • Sulfonamides
  • Hydrogel, Polyethylene Glycol Dimethacrylate
  • pullulan
  • Collagen
  • Focal Adhesion Protein-Tyrosine Kinases