Delivery of Oridonin and Methotrexate via PEGylated Graphene Oxide

Chai, Dongdong; Hao, Bingjie; Hu, Rong; Zhang, Fang; Yan, Jia; Sun, Yu; Huang, Xiaoyu; Zhang, Qingxiao; Jiang, Hong

doi:10.1021/acsami.9b03983

Cited by 54 publications

(35 citation statements)

References 57 publications

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“…However, the great potential for clinical application of ORI is severely limited by its poor aqueous solubility and low bioavailability [10][11][12]. A variety of strategies such as graphene oxide or nanosuspensions have been attempted to deliver ORI [13][14][15], but drug loading is generally low, which limits clinical use. And less attention is paid to the effects of release characteristics.…”

Section: Introductionmentioning

confidence: 99%

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

et al. 2019

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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 ORI@MOF-5 was 52.86% ± 0.59%. The sustained release effect was reliable, and the cumulative release rate was about 87% in 60 h. ORI@MOF-5 had significant cytotoxicity (IC50:22.99 μg/mL) and apoptosis effect on HepG2 cells. ORI@MOF-5 is hopeful to become a new anticancer sustained release preparation. MOF-5 has significant potential as a drug carrier material.

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Section: Introductionmentioning

confidence: 99%

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

et al. 2019

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“…The nanocomplexes (ORI@GO-PEG 10K−6arm ) obtained by combining ORI with PEG 10k−6arm have good thermostability and the DL is 10%. The cytotoxicity to cancer cells CAL 27, MG 63, HepG2 is approximately 10-times that of free ORI [142].…”

Section: Combination Of Formulationsmentioning

confidence: 95%

Solubility and Bioavailability Enhancement of Oridonin: A Review

et al. 2020

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Oridonin (ORI), an ent-kaurene tetracyclic diterpenoid compound, is isolated from Chinese herb Rabdosia rubescens with various biological and pharmacological activities including anti-tumor, anti-microbial and anti-inflammatory effects. However, the clinical application of ORI is limited due to its low solubility and poor bioavailability. In order to overcome these shortcomings, many strategies have been explored such as structural modification, new dosage form, etc. This review provides a detailed discussion on the research progress to increase the solubility and bioavailability of ORI.

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“…Methotrexate (MTX) and doxorubicin (DOX) are well-known anti-cancer drugs, which are routinely used by research groups as effective anti-cancer drugs against human bone tissue cancer Methotrexate (MTX) and doxorubicin (DOX) are well-known anti-cancer drugs, which are routinely used by research groups as effective anti-cancer drugs against human bone tissue cancer cell lines [54][55][56][57]. Herein, we used both of these anti-cancer drugs (with serial dilution from 20 to 0.612 µg/mL) as a well-studied criterion to compare our synthesized compound's cytotoxicity with their anti-cancer activities.…”

Section: Cytotoxicity Assaymentioning

confidence: 99%

Synthesis, Crystal Structure, and Biological Activity of a Multidentate Calix[4]arene Ligand Doubly Functionalized by 2-Hydroxybenzeledene-Thiosemicarbazone

et al. 2020

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The design and synthesis of a novel tert-butyl-calix[4]arene functionalized at 1, 3 positions of the lower rim with two terminal 2-hydroxybenzeledene-thiosemicarbazone moieties is reported. The new ligand with multi-dentate chelating properties was fully characterized by several techniques: ESI-Mass spectroscopy, FT-IR, 1H-NMR, and single crystal X-ray diffraction. The solid state structure confirms that the calix[4]arene macrocycle has the expected open cone conformation, with two opposite phenyl rings inclined outwards with large angles. The conformation of the two alkoxythiosemicarbazone arms produces a molecule with a C2 point group symmetry. An interesting chiral helicity is observed, with the two thiosemicarbazone groups oriented in opposite directions like a two-blade propeller. A water molecule is encapsulated in the center of the two-blade propeller through multiple H-bond coordinations. The antibacterial, antifungal, anticancer, and cytotoxic activities of the calix[4]arene-thiosemicarbazone ligand and its metal derivatives (Co2+, Ni2+, Cu2+, and Zn2+) were investigated. A considerable antibacterial activity (in particular against E. coli, MIC, and MBC = 31.25 μg/mL) was observed for the ligand and its metal derivatives. Significant antifungal activities against yeast (C. albicans) were also observed for the ligand (MIC = 31.25 μg/mL and MBC = 125 μg/mL) and for its Co2+ derivative (MIC = 62.5 μg/mL). All compounds show cytotoxicity against the tested cancerous cells. For the Saos-2 cell line, the promising anticancer activity of ligand L (IC50 < 25 μg/mL) is higher than its metal derivatives. The microscopic analysis of DAPI-stained cells shows that the treated cells change in morphology, with deformation and fragmentation of the nuclei. The hemo-compatibility study demonstrated that this class of compounds are suitable candidates for further in vivo investigations.

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Delivery of Oridonin and Methotrexate via PEGylated Graphene Oxide

Cited by 54 publications

References 57 publications

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

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

Solubility and Bioavailability Enhancement of Oridonin: A Review

Synthesis, Crystal Structure, and Biological Activity of a Multidentate Calix[4]arene Ligand Doubly Functionalized by 2-Hydroxybenzeledene-Thiosemicarbazone

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