This work is aimed to introduce a new kind of water-soluble polymer which bears cucurbit[7]uril (CB[7]) in the main-chain for supramolecular polymeric chemotherapy. To this end, we synthesized a bis-alkynyl functionalized CB[7] and polymerized it with α,ω-diazide-PEG through click reaction to form the desired CB[7] based main-chain polymer (poly-CB[7]). Anticancer drugs, such as oxaliplatin, could encapsulate into the cavity of poly-CB[7] to form a supramolecular polymeric complex, which displayed low cytotoxicity to normal cells. In addition, the anticancer activity of the oxaliplatin was recovered when it met cancer cells that could overexpress spermine, e.g. colorectal cancer cell, through competitive release of the anticancer drugs from CB[7] cavity by spermine. Interestingly, the antitumor activity of the supramolecular polymeric complex is higher than oxaliplatin itself. The enhanced antitumor activity results from a cooperative effect by combining the release of oxaliplatin from the supramolecular polymeric complex and decrease of spermine in the micro-environment of the cancer cells. One more advantage of the supramolecular polymeric complex is its long circulation performance in vivo compared with the supramolecular complex between oxaliplatin and CB[7]. In addition to oxaliplatin, poly-CB[7] could encapsulate other kind of antitumor drugs with decreased toxicity to normal cells and increased antitumor activity to cancer cells. Therefore, this line of research may open new horizons for supramolecular polymeric chemotherapy.

Cucurbit[7]uril based main-chain polymer as drug carrier for supramolecular polymeric chemotherapy

255th National Meeting (2018)

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