Triptolide (TPL) has been employed to treat hepatocellular carcinoma (HCC). However, the poor water solubility of TPL restricts its applications. Therefore, we prepared TPL-loaded cyclodextrin-based metal-organic framework (TPL@CD-MOF) to improve the solubility and bioavailability of TPL, thus enhancing the anti-tumor effect on HCC. The BET surface and the pore size of TPL@CD-MOF were 10.4 m·g and 1.1 nm, respectively. The results of XRD indicated that TPL in TPL@CD-MOF was encapsuled. TPL@CD-MOF showed a slower release than free TPL in vitro. Moreover, the CD-MOF improved the bioavailability of TPL. TPL@CD-MOF showed slightly higher, but statistically significant, anti-tumor efficacy in vitro and in vivo compared to free TPL. In addition, TPL@CD-MOF exhibited a modest improvement of the anti-tumor effects, which may be associated to the enhanced in vivo absorption. Overall, these findings suggested the potential CD-MOF as oral drug delivery carriers for anti-tumor drugs. The process of TPL loading into CD-MOF and its enhanced oral bioavailability and anti-tumor activity.
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