This work presents a highly efficient, broad spectrum and self-delivery anticancer agent, which is the hyperbranched polydiselenide (HPSe) consisting of alternative hydrophobic diselenide groups and hydrophilic phosphate segments in the backbone framework. The data of systematic evaluations demonstrate that HPSe is very potent to inhibit the proliferation of many forms of cancer cell. The dose of HPSe required for growth inhibition of 50% (IC50) in all of the tested cancer cell lines is within the concentration range between 1 and 2.5 ug mL-1 with the incubation time of 72 h. Furthermore, the amphiphilic HPSe can self-assembly into nanomicelles with an average diameter of 50 nm and spontaneously enter into tumor cells by the enhanced permeability and retention (EPR) effect. Besides, other hydrophobic anticancer drugs such as doxorubicin (DOX) can be encapsulated into HPSe micelles for combining therapy.

This paper was originally published in Biomaterials (2012) 33, 7765-7774.

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