Non-ionic amphiphilic biodegradable PEG-PLGA-PEG copolymer enhances gene delivery efficiency in rat skeletal muscle

J Control Release. 2007 Apr 2;118(2):245-53. doi: 10.1016/j.jconrel.2006.11.025. Epub 2006 Dec 1.

Abstract

Naked plasmid DNA (pDNA)-based gene therapy has low delivery efficiency, and consequently, low therapeutic effect. We present a biodegradable nonionic triblock copolymer, PEG(13)-PLGA(10)-PEG(13), to enhance gene delivery efficiency in skeletal muscle. Effects of PEG(13)-PLGA(10)-PEG(13) on physicochemical properties of pDNA were evaluated by atomic force microscopy (AFM) imaging, gel electrophoresis and zeta-potential analysis. AFM imaging suggested a slightly compacted structure of pDNA when it was mixed with the polymer, while zeta-potential measurement indicated an increased surface potential of negatively charged pDNA. PEG(13)-PLGA(10)-PEG(13) showed a relatively lower toxicity compared to Pluronic P85 in a skeletal muscle cell line. The luciferase expression of pDNA delivered in 0.25% polymer solution was up to three orders of magnitude more than branched polyethylenimine (bPEI(25 k))/pDNA and three times more than that of naked pDNA five days after intramuscular administration. This in vivo gene delivery enhancement was also observed displaying a two-fold higher expression of human vascular endothelial growth factor (VEGF). Based on fluorescence labeled pDNA distribution, it is speculated that the greater diffusivity of PEG(13)-PLGA(10)-PEG(13)/pDNA compared to bPEI(25 k)/pDNA accounts for better transfection efficiency in vivo. To summarize, combining PEG(13)-PLGA(10)-PEG(13) with pDNA possesses the potential to improve gene delivery efficiency in skeletal muscle.

Publication types

  • Comparative Study
  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Cell Line
  • Cell Survival / drug effects
  • Electrophoresis, Agar Gel
  • Genes, Reporter
  • Humans
  • Luciferases
  • Male
  • Mice
  • Microscopy, Atomic Force
  • Muscle, Skeletal / drug effects
  • Muscle, Skeletal / metabolism*
  • Nucleic Acid Conformation
  • Plasmids / chemistry
  • Plasmids / metabolism*
  • Poloxalene / toxicity
  • Polyethylene Glycols / chemistry*
  • Polyethylene Glycols / toxicity
  • Polyethyleneimine / chemistry
  • Polyglactin 910 / chemistry*
  • Polyglactin 910 / toxicity
  • Rats
  • Rats, Sprague-Dawley
  • Surface Properties
  • Time Factors
  • Transfection / methods*
  • Vascular Endothelial Growth Factor A / biosynthesis
  • Vascular Endothelial Growth Factor A / genetics

Substances

  • VEGFA protein, human
  • Vascular Endothelial Growth Factor A
  • pluronic block copolymer p85
  • polyethylene glycol-poly(lactic-co-glycolic acid)-polyethylene glycol
  • Polyglactin 910
  • Polyethylene Glycols
  • Polyethyleneimine
  • Poloxalene
  • Luciferases