Characterisation and stability studies of a hydrophilic decapeptide in different adjuvant drug delivery systems: a comparative study of PLGA nanoparticles versus chitosan-dextran sulphate microparticles versus DOTAP-liposomes

Int J Pharm. 2011 Dec 12;421(1):151-9. doi: 10.1016/j.ijpharm.2011.09.011. Epub 2011 Sep 17.

Abstract

Poly[lactic-co-glycolide] (PLGA) nanoparticles, chitosan-dextran sulphate microparticles, and DOTAP-liposomes were prepared as vaccine adjuvants and drug carriers for a small hydrophilic model peptide, and their different physico-chemical properties (size, PDI, zeta-potential, pH-value and peptide loading) were investigated. The model peptide's encapsulation efficiency (EE) in PLGA particles amounted to 15%, for DOTAP-liposomes to 20% and for chitosan particles up to 90%. The structural appearance of the particles was visualized by SEM and TEM. The stability of the aqueous formulations and the corresponding lyophilisates was monitored for 12 weeks (stored at T=2-8°C). The freeze-drying process and the addition of an appropriate cryoprotective agent (sucrose) proved to be essential for all carrier systems. As a result of this study, three different peptide-loaded drug delivery systems with different properties were successfully manufactured and showed sufficient product stability of their freeze-dried formulations over 12 weeks of storage.

Publication types

  • Comparative Study

MeSH terms

  • Adjuvants, Pharmaceutic / chemistry
  • Chitosan / chemistry*
  • Dextran Sulfate / chemistry*
  • Drug Stability
  • Fatty Acids, Monounsaturated / chemistry*
  • Freeze Drying
  • Hydrophobic and Hydrophilic Interactions
  • Lactic Acid / chemistry*
  • Liposomes
  • Nanoparticles / chemistry*
  • Oligopeptides / chemistry*
  • Particle Size
  • Polyglycolic Acid / chemistry*
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Quaternary Ammonium Compounds / chemistry*

Substances

  • Adjuvants, Pharmaceutic
  • Fatty Acids, Monounsaturated
  • Liposomes
  • Oligopeptides
  • Quaternary Ammonium Compounds
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid
  • Chitosan
  • Dextran Sulfate
  • 1,2-dioleoyloxy-3-(trimethylammonium)propane