Internalization of Ineffective Platinum Complex in Nanocapsules Renders It Cytotoxic

journal article in Web of Science

English

Anticancer therapy by platinum complexes, based on nanocarrier-based delivery, may offer a new approach to improve the efficacy and tolerability of the platinum family of anticancer drugs. The original rules for the design of new anticancer platinum drugs were affected by the fact that, although cisplatin (cis-[PtCl2(NH3)2) was an anticancer drug, its isomer transplatin was not cytotoxic. For the first time, it is demonstrated that simple encapsulation of an inactive platinum compound in phospholipid bilayers transforms it into an efficient cytotoxic agent. Notably, the encapsulation of transplatin makes it possible to overcome the resistence mechanisms operating in cancer cells treated with cisplatin and prevents inactivation of transplatin in the extracellular environment. It is also shown that transplatin delivered to the cells in nanocapsules, in contrast to free (nonencapsulated) complex, forms cytotoxic cross-links on DNA.

Cancer; DNA; liposomes; phospholipids; platinum

VRÁNA, O.; NOVOHRADSKÝ, V.; MEDŘÍKOVÁ, Z.; BURDÍKOVÁ, J.; STUCHLÍKOVÁ, O.; KAŠPÁRKOVÁ, J.; BRABEC, V.

20. 1. 2016

Wiley-VCH Verlag GmbH & Co. KGaA

Weinheim

0947-6539

CHEMISTRY-A EUROPEAN JOURNAL

22

1

Federal Republic of Germany

2728

2735

8