2010 Annual Meeting

(480g) A New Charge Reversal PCL-Block-Polyhistidine Nanoprticles for Nuclear Targeting Drug Delivery

Authors

Erlei Jin - Presenter, University of Wyoming
Bo Zhang - Presenter, University of Wyoming
Jianbin Tang - Presenter, Zhejiang University
Maohong Fan - Presenter, University of Wyoming
Huadong Tang - Presenter, Department of Chemical and Petroleum Engineering, University of Wyoming
Maciej Radosz - Presenter, Department of Chemical and Petroleum Engineering, University of Wyoming
Edward A. Van Kirk - Presenter, Department of Animal Science, University of Wyoming
William J. Murdoch - Presenter, Department of Animal Science, University of Wyoming
Youqing Shen - Presenter, Zhejiang University


Poly (L-histidine) (polyhis) has an endosomal membrane disruption activity due to its imidazole groups. It would be useful for cytosolic delivery of anticancer drug. However, its low aqueous solubility limits its application. We amidized its imidazole groups and thus substantially enhanced its water solubility. Its block copolymer with PCL could form nanoparticles with a size of around 130 nm. The nanoparticles are negatively charged at pH 7.4 but become positively charged at pH 5.0 due to the hydrolysis of the amides. The nanoparticles can go into nuclei within five hours for effective nuclear drug delivery. CPT and DOX loaded in the nanopartricles had higher cytotoxicity than the free drug.