Preparation and in vitro evaluation of chitosan nanoparticles containing a caspase inhibitor

The aim of this work was to develop a formulation for Z-DEVD-FMK, a peptide which is a caspase inhibitor and has been used in experimental animal studies for a decade. Peptide loaded chitosan nanoparticles were obtained by ionotropic gelation process and Z-DEVD-FMK was quantified by an HPLC method....

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Veröffentlicht in:International journal of pharmaceutics 2005-07, Vol.298 (2), p.378-383
Hauptverfasser: Aktaş, Yeşim, Andrieux, Karine, Alonso, Maria Jose, Calvo, Pilar, Gürsoy, R. Neslihan, Couvreur, Patrick, Çapan, Yılmaz
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Sprache:eng
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Zusammenfassung:The aim of this work was to develop a formulation for Z-DEVD-FMK, a peptide which is a caspase inhibitor and has been used in experimental animal studies for a decade. Peptide loaded chitosan nanoparticles were obtained by ionotropic gelation process and Z-DEVD-FMK was quantified by an HPLC method. The influence of the initial peptide concentration on the nanoparticle characteristics and release behavior was evaluated. The CS nanoparticles have a particle diameter (Z-average) ranging from approximately 313–412 nm and a positive zeta potential (20–28 mV). The formulation with the initial peptide concentration of 400 ng/ml provided the highest loading capacity (0.46%) and the highest extent of release (65% at 24 h) suggesting the possibility to achieve a therapeutic dose. According to the data obtained, this chitosan-based nanotechnology opens new and interesting perspectives for anticaspase activity.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2005.03.027