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A carrier-free nanostructure based on platinum(IV) prodrug enhances cellular uptake and cytotoxicity.

07:00 EST 9th March 2018 | BioPortfolio

Summary of "A carrier-free nanostructure based on platinum(IV) prodrug enhances cellular uptake and cytotoxicity."

Flurbiprofen, a hydrophobic COX inhibitor, was coordinated axially with oxoplatin to form a new conjugate cis, cis, trans-[Pt(IV)(NH3)2Cl2(flurbiprofen)2]. The successful synthsis of this new conjugate was confirmed by 1H, 13C and 195Pt NMR. The potential of this conjugate being reduced to cisplatin and subsequently exerting its DNA cross-linking ability was verified using cyclic voltammetry (CV), HPLC and mass spectrum (MS). This conjugate showed markedly higher cytotoxicity on many cancer cell lines than cisplatin, flurbiprofen and physical mixture (mol ratio, cisplatin: flurbiprofen=1:2) of them. This is consistent with the result of apoptosis-inducing assay. This conjugate spontaneously assembles carrier-free nanoparticles in aqueous solution, which is confirmed by DLS, TEM, SEM and AFM, thus facilitates cellular uptake, markedly improves its cytotoxicity and apoptosis-inducing ability in vitro.

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Name: Molecular pharmaceutics
ISSN: 1543-8392
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