Siosomal formulation for intracellular delivery and targeting of therapeutic agents
申请人:Salama, Zoser B.
公开号:EP2384743A1
公开(公告)日:2011-11-09
The invention relates to a carrier and targeting system for the intracellular delivery and triggered release of a siosome- and/or siosome-liposome-entrapped or encapsulated active substance or therapeutic agent. The invention further relates to the targeted release and delivery of doxorubicin, cis-platin, carbo-platin and/or oxali-platin, characterized in that one or more anionic lipids, such as cholesteryl hemisuccinate residues, cardiolipin and/or their derivatives and/or other anionic groups, are covalently linked to the silicone central atom of the silanes, sugar silanes and/or amino-sugar silanes. The invention further relates to the use of cationic lipids that are covalently attached to the silicone central atom of the silanes. The invention also relates to a method for preparing such carrier and targeting systems and methods for their administration.
该发明涉及一种用于细胞内递送和触发释放siosome和/或siosome-脂质体包埋或封装活性物质或治疗剂的载体和靶向系统。该发明还涉及对阿霉素、顺铂、卡铂和/或奥沙利铂的靶向释放和递送,其特征在于将一个或多个阴离子脂质,如胆固醇半琥珀酸酯残基、心磷脂和/或它们的衍生物和/或其他阴离子基团,共价连接到硅烷、糖硅烷和/或氨基糖硅烷的硅中心原子上。该发明还涉及将阳离子脂质共价连接到硅烷的中心原子的使用。该发明还涉及一种制备这种载体和靶向系统的方法以及它们的给药方法。