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Investigation of Metal-Organic Framework-5 (MOF-5) as an Antitumor Drug Oridonin Sustained Release Carrier

School of Chinese materia medica, Beijing University of Chinese Medicine, Beijing 102488, China
Beijing Research Institute of Chinese Medicine, Beijing University of Chinese Medicine, Beijing 100029, China
Authors to whom correspondence should be addressed.
Molecules 2019, 24(18), 3369;
Received: 16 August 2019 / Revised: 9 September 2019 / Accepted: 13 September 2019 / Published: 16 September 2019
Oridonin (ORI) is a natural active ingredient with strong anticancer activity. But its clinical use is restricted due to its poor water solubility, short half-life, and low bioavailability. The aim of this study is to utilize the metal organic framework material MOF-5 to load ORI in order to improve its release characteristics and bioavailability. Herein, MOF-5 was synthesized by the solvothermal method and direct addition method, and characterized by Scanning Electron Microscopy (SEM), X-Ray Diffraction (XRD), Fourier Transform Infrared Spectrometer (FTIR), Thermogravimetric Analysis (TG), Brunauer–Emmett–Teller (BET), and Dynamic Light Scattering (DLS), respectively. MOF-5 prepared by the optimal synthesis method was selected for drug-loading and in vitro release experiments. HepG2 cells were model cells. MTT assay, 4′,6-diamidino-2-phenylindole (DAPI) staining and Annexin V/PI assay were used to detect the biological safety of blank carriers and the anticancer activity of drug-loaded materials. The results showed that nano-MOF-5 prepared by the direct addition method had complete structure, uniform size and good biocompatibility, and was suitable as an ORI carrier. The drug loading of [email protected] was 52.86% ± 0.59%. The sustained release effect was reliable, and the cumulative release rate was about 87% in 60 h. [email protected] had significant cytotoxicity (IC50:22.99 μg/mL) and apoptosis effect on HepG2 cells. [email protected] is hopeful to become a new anticancer sustained release preparation. MOF-5 has significant potential as a drug carrier material. View Full-Text
Keywords: MOF-5; Oridonin; Antitumor; HepG2 cells; sustained release MOF-5; Oridonin; Antitumor; HepG2 cells; sustained release
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Chen, G.; Luo, J.; Cai, M.; Qin, L.; Wang, Y.; Gao, L.; Huang, P.; Yu, Y.; Ding, Y.; Dong, X.; Yin, X.; Ni, J. Investigation of Metal-Organic Framework-5 (MOF-5) as an Antitumor Drug Oridonin Sustained Release Carrier. Molecules 2019, 24, 3369.

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