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

被引:116
作者
Aktas, Y
Andrieux, K [1 ]
Alonso, MJ
Calvo, P
Gürsoy, RN
Couvreur, P
Çapan, Y
机构
[1] Univ Paris Sud, Fac Pharm, CNRS, UMR 8612, F-92296 Chatenay Malabry, France
[2] Hacettepe Univ, Fac Pharm, Dept Pharmaceut Technol, TR-06100 Ankara, Turkey
[3] Univ Santiago de Compostela, Dept Pharmaceut Technol, Sch Pharm, Santiago De Compostela 15782, Spain
关键词
chitosan; nanoparticles; Z-DEVD-FMK; HPLC;
D O I
10.1016/j.ijpharm.2005.03.027
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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. (c) 2005 Elsevier B.V. All rights reserved.
引用
收藏
页码:378 / 383
页数:6
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