[EN] CORONA-LIKE (GUANIDYL)-OLIGOSACCHARIDIC DERIVATIVES AS CELL-PENETRATING ENHANCERS FOR INTRACELLULAR DELIVERY OF COLLOIDAL THERAPEUTIC SYSTEMS<br/>[FR] DÉRIVÉS (GUANIDYL)-OLIGOSACCHARIDIQUES DE TYPE COURONNE EN TANT QU'AMÉLIORATEURS DE LA PÉNÉTRATION CELLULAIRE POUR L'ADMINISTRATION INTRACELLULAIRE DE SYSTÈMES THÉRAPEUTIQUES COLLOÏDAUX
申请人:UNIV PADOVA
公开号:WO2012097876A1
公开(公告)日:2012-07-26
A novel class of cell-penetrating enhancers with unusual chemical structure is herein disclosed. Said cell-penetrating enhancers are non-linear and non peptidic (guanidyl)-oligosaccharidic derivatives, which can be easily obtained according to simple and reproducible synthetic steps. A wide array of cell penetration enhancers can be obtained by slight modification of the main structure oligosaccharidic backbone and in order to provide for their conjugation or physical combination with a variety of therapeutic systems. These molecules can be designed for conjugation to proteins or polymer therapeutics or for surface decoration of liposomes or nanoparticles. Finally, the cationic features and the penetration enhancer properties of the corona-like (guanidyl)-oligosaccharidic derivatives can be exploited for oligonucleotide, namely siRNA, or gene delivery.
本文披露了一种新型的细胞穿透增强剂,其化学结构不同寻常。这些细胞穿透增强剂是非线性和非肽的(鸟氨酸)-寡糖衍生物,可以通过简单可重复的合成步骤轻松获得。通过略微修改主要结构寡糖骨架,可以获得各种细胞穿透增强剂,以便与各种治疗系统进行结合或物理组合。这些分子可以设计用于与蛋白质或聚合物治疗系统结合,或用于脂质体或纳米粒子的表面装饰。最后,这种类似冠状的(鸟氨酸)-寡糖衍生物的阳离子特性和穿透增强剂特性可以用于寡核苷酸,即siRNA或基因传递。