Internalization of Ineffective Platinum Complex in Nanocapsules Renders It Cytotoxic

0471974 - BFÚ 2017 RIV DE eng J - Journal Article
Vrána, Oldřich - Novohradský, Vojtěch - Medrikova, Z. - Burdikova, J. - Stuchlíková, O. - Kašpárková, Jana - Brabec, Viktor
Internalization of Ineffective Platinum Complex in Nanocapsules Renders It Cytotoxic.
Chemistry - A European Journal. Roč. 22, č. 8 (2016), s. 2728-2735. ISSN 0947-6539. E-ISSN 1521-3765
R&D Projects: GA ČR(CZ) GA14-21053S
Institutional support: RVO:68081707
Keywords : interstrand cross-links * dna-adducts * cisplatin nanocapsules
Subject RIV: BO - Biophysics
Impact factor: 5.317, year: 2016

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 resistance 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.
Permanent Link: http://hdl.handle.net/11104/0269333