Background: Considering the limitations of cisplatin in clinical application, there is
ongoing research to fabricate new platinum-containing prodrug which are highly effective to tumor
cells and have low toxicity to normal cells.
Methods: In this study, a cyclodextrin-based supramolecular platinum prodrug that is 6,6’-ophenylenediseleno-
bridged bis (β-cyclodextrin)s (CD) and its potassium tetrachloroplatinate(II)
complex was reported. The cytotoxicity experiments were performed to evaluate the anticancer
activities of supramolecular prodrug in vitro by means of MTT assay. The practical application of
supramolecular prodrug in tumor treatment in vivo were evaluated using BALB/c nude mice model
bearing Hela cancer cells.
Results: Compared with commercial anticancer drug cisplatin, the resultant cyclodextrin-based
platinum prodrug exhibited comparative anticancer effect but with much lower toxicity side effects
in vitro and in vivo.
Conclusion: The cyclodextrin-based supramolecular platinum prodrug displayed antitumor activity
comparable to the commercial antitumor drug cisplatin but with lower side effects both in vitro and
in vivo, implying that the two adjacent cyclodextrin cavities not merely act as desired solubilizer,
but also endowed the prodrug with cell permeability through the interaction of cyclodextrin with
phospholipids and cholesterol on cell membrane.