Internalization of Ineffective Platinum Complex in Nanocapsules Renders It Cytotoxic
Language English Country Germany Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
- Keywords
- DNA, cancer, liposomes, phospholipids, platinum,
- MeSH
- DNA Adducts MeSH
- Cisplatin chemistry pharmacology MeSH
- DNA chemistry drug effects metabolism MeSH
- Phospholipids chemistry MeSH
- Humans MeSH
- Liposomes chemistry MeSH
- Nanocapsules chemistry MeSH
- Platinum chemistry MeSH
- Antineoplastic Agents chemistry metabolism pharmacology MeSH
- Platinum Compounds chemistry pharmacology MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- DNA Adducts MeSH
- Cisplatin MeSH
- DNA MeSH
- Phospholipids MeSH
- Liposomes MeSH
- Nanocapsules MeSH
- Platinum MeSH
- Antineoplastic Agents MeSH
- Platinum Compounds MeSH
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.
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