期刊
JOURNAL OF PEPTIDE SCIENCE
卷 12, 期 1, 页码 43-50出版社
WILEY
DOI: 10.1002/psc.681
关键词
leuprolide; synthesis; liposomes; differential scanning calorimetry; solid state NMR
A novel liposomal formulation was developed for the encapsulation of the oligopeptide leuprolide (GlpHisTrpSerTyr-D-LeuLeuArglProNHEt), a potent analogue of gonadotropin releasing hormone used in the treatment of advanced prostate cancer, endometriosis and precocious puberty. Leuprolide was synthesized using solid phase methodology on a [3-1(ethyl-Fmoc-amino)methyl]-1-indol-1-yl)-acetyl AM resin and Fmoc/tBu chemistry. The new liposomal formulation. called liposomes in liposomes, is composed of egg phosphatidyleholine:dipallmitoylphosphatidylglycerol in a molar ratio of 98.91:1.09 (internal liposomes) and egg phosphatidylcholine: dipalmitoylphosphatidylglycerol: cholesterol in a molar ratio of 68.71:0.76:30.53 (external liposomes). It offers high encapsulation efficiency (73.8% for leuprolide): it can provide new delivery characteristics and it may have possible advantages in future applications regarding the encapsulation and delivery of bioactive peptides to target tissues. Furthermore, the physicochemical characteristics (size distribution and zeta-potential) of the liposomal formatations and the thermal effects on leuprolide in model lipidic bilayers composed of dipalmitoylphosphatidylcholine were studied using differential scanning calorimetry. Finally, the dynamic effects of leuprolide in an egg phosphatidylcholine/cholesterol system were examined using solid state C-13 MAS NMR spectroscopy. Copyright (c) 2005 European Peptide Society and John Wiley & Sons. Ltd.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据