Preparation, Characterization, and In Vitro and Vivo Antitumor Activity of Oridonin-Conjugated Multiwalled Carbon Nanotubes Functionalized with Carboxylic Group

Abstract EN

Carbon nanotubes have shown great potential in tumor therapy.

Oridonin (ORI) is a poorly water-soluble diterpenoid compound (C20H28O6) used in the treatment of esophageal and hepatic carcinoma for decades.

For the purpose of enhancing the antitumor potency and reducing cytotoxicity of ORI, multiwalled carbon nanotubes functionalized with carboxylic group (MWCNTs-COOH) were used as ORI carrier.

ORI was noncovalently encapsulated into (or onto) the functionalized carbon nanotubes (MWCNTs-ORI).

The obtained MWCNTs-ORI has been characterized.

The ORI loading efficiency in MWCNTs-COOH carrier was studied to be about 82.6% (w/w).

In vitro cytotoxicity assay on MWCNTs-ORI gave IC50 of 7.29 ± 0.5 μg/mL and ORI-F gave IC50 of 14.5 ± 1.4 μg/mL.

The antitumor effect studies in vivo showed that MWCNTs-ORI improved antitumor activity of ORI in comparison with ORI-F.

The tumor inhibition ratio for MWCNTs-ORI ( 1 .

68 × 1 0 - 2 g·Kg−1·d−1) was 86.4%, higher than that of ORI-F ( 1 .

68 × 1 0 - 2 g·Kg−1·d−1) which was 39.2%.

This can greatly improve the pharmaceutical efficiency and reduce potential side effects.