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Glycol chitosan as a stabilizer for protein encapsulated into poly(lactide-co-glycolide) microparticle.

Abstract
Glycol chitosan (GC), a chitosan derivative conjugated with ethylene glycol, is soluble in water at a neutral/acidic pH and is viscous. This GC was incorporated into poly(lactide-co-glycolide) (PLGA) microparticles (prepared by the multi-emulsion W(1)/O/W(2) (water-in-oil-in-water) method) to stabilize lysozyme (Lys) used as a model protein. Herein, GC's viscous property helped to improve Lys encapsulation efficacy and reduce Lys denaturaton at the water/organic solvent interface. When the GC concentration in the W(1) phase increased, the formation of non-covalent Lys aggregates decreased. This may be because the aqueous microdroplets surrounded by the firm viscous interface protect Lys from the degrading environment formed by the water/organic solvent interface. In an in vitro Lys release test, 40mg incorporation of GC led to continuous Lys release of up to 78wt.% for 1 month and presented bioactivity of more than 95% for Lys released from microparticles. In addition, there was negligible immune response in the tissue treated with the GC-incorporated PLGA microparticles, whereas there was a moderate foreign body reaction in the muscle layer and many configurations of neutrophils in the tissue treated with the PLGA microparticles without GC. It is expected that GC facilitates a decrease in immune responses exacerbated as a consequence of PLGA degradation.
AuthorsEun Seong Lee, Keun-Hong Park, In Suh Park, Kun Na
JournalInternational journal of pharmaceutics (Int J Pharm) Vol. 338 Issue 1-2 Pg. 310-6 (Jun 29 2007) ISSN: 0378-5173 [Print] Netherlands
PMID17363202 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Polymers
  • Proteins
  • glycol-chitosan
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid
  • Chitosan
  • Muramidase
Topics
  • Animals
  • Chitosan (administration & dosage)
  • Foreign-Body Reaction
  • Lactic Acid (administration & dosage, toxicity)
  • Male
  • Materials Testing
  • Microspheres
  • Muramidase (administration & dosage, chemistry)
  • Polyglycolic Acid (administration & dosage, toxicity)
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polymers (administration & dosage, toxicity)
  • Proteins (administration & dosage, chemistry)
  • Rats
  • Rats, Sprague-Dawley
  • Solubility

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