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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
Authors:Wieber Alena  Selzer Torsten  Kreuter Jörg
Affiliation:a Merck Serono, Formulation and Process Development, Frankfurter Straße 250, D-64293 Darmstadt, Germany
b Institute of Pharmaceutical Technology, Biocenter of Johann Wolfgang Goethe-University, D-60438 Frankfurt am Main, Germany
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.
Keywords:PLGA   DOTAP-liposomes   Chitosan   Particles   Micro-flow-imaging   Adjuvant
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