Department of Pharmacy, Shanghai 9Th People's Hospital, Shanghai Jiao Tong University School of Medicine, No. 280 Mohe Road, Shanghai, 201999, China.
Drug Deliv Transl Res. 2022 May;12(5):1096-1104. doi: 10.1007/s13346-021-00978-7. Epub 2021 Apr 15.
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.
雷公藤红素(TPL)已被用于治疗肝细胞癌(HCC)。然而,TPL 的水溶性差限制了其应用。因此,我们制备了载雷公藤红素的环糊精基金属有机骨架(TPL@CD-MOF),以提高 TPL 的溶解度和生物利用度,从而增强对 HCC 的抗肿瘤作用。TPL@CD-MOF 的 BET 表面积和孔径分别为 10.4 m·g 和 1.1 nm。XRD 结果表明 TPL 被包封在 TPL@CD-MOF 中。TPL@CD-MOF 在体外的释放速度比游离 TPL 慢。此外,CD-MOF 提高了 TPL 的生物利用度。与游离 TPL 相比,TPL@CD-MOF 在体外和体内显示出稍高但具有统计学意义的抗肿瘤疗效。此外,TPL@CD-MOF 显示出抗肿瘤作用的适度改善,这可能与体内吸收的增强有关。总的来说,这些发现表明 CD-MOF 有潜力作为抗肿瘤药物的口服药物递送载体。TPL 加载到 CD-MOF 中的过程及其增强的口服生物利用度和抗肿瘤活性。