title: 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.
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.
authors.affiliation: Merck Serono, Formulation and Process Development, Frankfurter Straße 250, D-64293 Darmstadt, Germany.
authors.forename: Alena
authors.initials: A
authors.lastname: Wieber
authors.forename: Torsten
authors.initials: T
authors.lastname: Selzer
authors.forename: Jörg
authors.initials: J
authors.lastname: Kreuter
mesh_terms: D000277:Adjuvants, Pharmaceutic / Q000737:chemistry; D048271:Chitosan / Q000737:chemistry*; D016264:Dextran Sulfate / Q000737:chemistry*; D004355:Drug Stability; D005229:Fatty Acids, Monounsaturated / Q000737:chemistry*; D005612:Freeze Drying; D057927:Hydrophobic and Hydrophilic Interactions; D019344:Lactic Acid / Q000737:chemistry*; D008081:Liposomes; D053758:Nanoparticles / Q000737:chemistry*; D009842:Oligopeptides / Q000737:chemistry*; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D000644:Quaternary Ammonium Compounds / Q000737:chemistry*
chemical_list: D000277:Adjuvants, Pharmaceutic; D005229:Fatty Acids, Monounsaturated; D008081:Liposomes; D009842:Oligopeptides; D000644:Quaternary Ammonium Compounds; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D048271:Chitosan; D016264:Dextran Sulfate; C070046:1,2-dioleoyloxy-3-(trimethylammonium)propane