title: Promoted transfection efficiency of pDNA polyplexes-loaded biodegradable microparticles containing acid-labile segments and galactose grafts.
abstract: OBJECTIVE
  Targeting to antigen-presenting cells and efficient intracellular delivery of pDNA are essential for development of microsphere formulations of DNA vaccine.
  
  
  METHODS
  Biodegradable polymers containing acid-labile segments and galactose grafts were developed to entrap pDNA polyplexes into microspheres, which were proposed to promote transfection efficiency of pDNA.
  
  
  RESULTS
  Acid-labile characteristics were approved by the hemolysis capabilities of red blood cells and degradation behaviors of matrix polymers; release of pDNA polyplexes from microspheres was significantly accelerated after incubation in acid buffers. Presence of galactose moieties enhanced cellular uptake of microspheres and increased acid-lability due to hydrophilic grafts on acid-labile segments. There was no apparent cytotoxicity of blank microspheres; cytotoxicity of pDNA polyplexes was significantly decreased after encapsulation into and sustained release from microspheres. High transfection efficiency and a dose-dependent transfection were indicated for pDNA polyplex-loaded acid-labile microspheres when balancing with cytotoxicity.
  
  
  CONCLUSIONS
  Integration of acid-lability, targeting effect into full biodegradable backbone represents an exciting approach to promote transfection efficiency through modulating release of pDNA polyplexes, targeting to antigen-presenting cells and intracellular delivery of pDNA.
authors: Key Laboratory of Advanced Technologies of Materials Ministry of Education of China, School of Materials Science & Engineering, Southwest Jiaotong University, Chengdu, 610031, People's Republic of China.
authors: Zhu
authors: Z
authors: Chen
authors: Xiaojun
authors: X
authors: Cai
authors: Ye
authors: Y
authors: Yang
authors: Guannan
authors: G
authors: Wu
authors: Yaowen
authors: Y
authors: Liu
authors: Fang
authors: F
authors: Chen
authors: Xiaohong
authors: X
authors: Li
mesh_terms: D000818:Animals; D002470:Cell Survival; D002478:Cells, Cultured; D004247:DNA / Q000008:administration & dosage* / Q000235:genetics; D005690:Galactose / Q000737:chemistry* / Q000378:metabolism; D006461:Hemolysis; D006801:Humans; D008099:Liver / Q000166:cytology; D008264:Macrophages / Q000166:cytology / Q000378:metabolism; D008863:Microspheres; D010957:Plasmids / Q000008:administration & dosage* / Q000235:genetics; D051381:Rats; D014162:Transfection
chemical_list: D004247:DNA; D005690:Galactose