【作者】 邱利焱；

【Author】 Liyan Qiu;College of Pharmaceutical Sciences, Zhejiang University;

【机构】 浙江大学药学院；

【摘要】 聚合物囊泡是装载和递送水溶性药物的适宜载体,但是常常存在载药不稳定药物过早释放的问题。在本研究中,我们以PEG为亲水链、4-氨基苯甲酸(2-二乙氨基)乙酯(DEAB)或(1H-苯并咪唑-2-亚甲基)胺(BIMA)为疏水基分别构建了聚膦腈自组装囊泡PNP和PEBP。该聚合物囊泡能高效装载水溶性化疗药物盐酸阿霉素;借助添加的氯金酸原位生成纳米金与DEAB形成配位作用或添加的胆固醇琥珀酸单酯与BIMA形成氢键作用,提高囊泡疏水膜的致密度,有效抑制药物在正常生理条件下的渗漏,从而显著提高动物体内的抑瘤效果。更多还原

【Abstract】 Polymeric vesicle is one kind of vehicles for loading and delivering water soluble drugs. However, for those polymersomes encapsulating water-soluble drugs, the problem of drug leakage always occurs. Herein, two self-assembled polyphosphazene vesicles PNP and PEBP containing hydrophobic 2-diethylaminoethyl 4-aminobenzoate(DEAB) or(1 H-benzo-[d] imidazol-2-yl) methanamine(BIMA) were separately constructed. Then hydrated chloroauric acid or cholesteryl hemisuccinate was introduced into the polymersomes, respectively, and by taking advantage of the coordination interaction between in situ generated gold nanoparticles and PNP or the hydrogen bonding interaction between cholesteryl hemisuccinate and PEBP, the drug leakage was effectively inhibited, leading to the improved in vivo antitumor efficiency.更多还原