Institut Galien Paris-Sud, Univ. Paris-Sud, CNRS, Université Paris-Saclay, Châtenay-Malabry, France; Molecular Biology Research Laboratory, Faculty of Medicine, The University of Jordan, Amman, Jordan; Cell therapy center, The University of Jordan, Amman, Jordan.
Institut Galien Paris-Sud, Univ. Paris-Sud, CNRS, Université Paris-Saclay, Châtenay-Malabry, France.
J Control Release. 2018 Feb 10;271:98-106. doi: 10.1016/j.jconrel.2017.12.022. Epub 2017 Dec 23.
In this study, we describe a liposome-based siRNA delivery system with a core composed of siRNA:protamine complex and a shell designed for the active targeting of CD44-expressing cells using for the first time the anti-CD44 aptamer (named Apt1) as targeting ligand. Among all functions, CD44 is the most common cancer stem cell surface biomarker and is found overexpressed in many tumors making this an attractive receptor for therapeutic targeting. This unique non-cationic system was evaluated for the silencing of the reporter gene of luciferase (luc2) in a triple-negative breast cancer model in vitro and in vivo. We show the possibility of conjugating an aptamer to siRNA-containing liposomes for an efficient gene silencing in CD44-expressing tumor cells in vivo, in the perspective of silencing disease-related genes in tumors.
在这项研究中，我们描述了一种基于脂质体的 siRNA 递药系统，其核心由 siRNA：鱼精蛋白复合物组成，外壳设计用于通过首次使用抗 CD44 适体（命名为 Apt1）作为靶向配体主动靶向表达 CD44 的细胞。在所有功能中，CD44 是最常见的癌症干细胞表面生物标志物，在许多肿瘤中过度表达，使其成为治疗靶向的有吸引力的受体。我们评估了这种独特的非阳离子系统在体外和体内三阴性乳腺癌模型中对报告基因荧光素酶（luc2）的沉默作用。我们展示了将适体与含 siRNA 的脂质体缀合以在体内有效沉默表达 CD44 的肿瘤细胞中基因的可能性，以期在肿瘤中沉默与疾病相关的基因。
