专利内容由知识产权出版社提供
专利名称：DYE-STABILIZED NANOPARTICLES AND
METHODS OF THEIR MANUFACTURE ANDTHERAPEUTIC USE
发明人：Daniel A. HELLER,Yosef SHAMAY申请号：US15549985申请日：20160209
公开号：US20180021259A1公开日：20180125
专利附图：
摘要：Described herein are nanoparticles which are largely made of (e.g., 90 wt. %)hydrophobic drugs and are stabilized by water soluble dyes. The nanoparticles can range
in size from 30 nm to 150 nm and have highly negative surface charge (e.g., −55 mV).These nanoparticles are highly soluble in water, stable for days in PBS buffer and can beeasily lyophilzed and reconstituted in water. Using quantitative self-assembly predictioncalculations, topochemical molecular descriptors were identified and validated as highlypredictive indicators of nano-assembly, nanoparticle size, and drug loading. The resultingnanoparticles selectively targeted kinase inhibitors to caveolin-1-expressing human coloncancer and autochthonous liver cancer models to yield striking therapeutic effects whileavoiding pERK inhibition in healthy skin. The nanoparticles exhibited remarkable anti-tumor efficacy in vitro and in vivo in models of hepatocellular carcinoma.
申请人：Memorial Sloan Kettering Cancer Center
地址：New York NY US
国籍：US
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