Objective:

To determine and characterize the antitumor activity of a hydrogel loaded with octenidine hydrochloride (OCTH) and its action mechanism on human tumor cells.

Material and methods:

The antibiofilm property of OCTH against a clinical methicillin-resistant Staphylococcus aureus isolate (MRSA-CI) was evaluated by disk diffusion assays and a human bone-biofilm model in combination with the BacLight™ staining. The antitumor activity of soluble OCTH and OCTH-loaded biodegradable hydrogels was assessed in human tumor cell lines (MCF-7, CAL-27, FaDu, and A549) under different experimental conditions. Cell viability was measured with the MTT assay, and membrane permeability after OCTH-loaded hydrogel exposure was evaluated with the Calcein AM assay. Genotoxicity was evaluated with comet assay and fluorescence microscopy.

Results:

A stable, transparent, and biodegradable OCTH hydrogel with a pH of 7.2 was successfully developed. Biofilms exposed to 50 μm OCTH for 24 h exhibited only dead bacteria (red fluorescence), comparable to the effect of 100 μm vancomycin. Soluble OCTH demonstrated dose-dependent inhibition of tumor cell growth in all tested cell lines, with significant effects observed from 1 μm. The LD₅₀ values for soluble OCTH across the tumor cell lines ranged from 2.32 to 5.1 µm. Notably, hydrogel loaded with 50 μm OCTH significantly reduced cell growth by 44% after a 15-min exposure and by 97% after 120 min. The Calcein AM assay revealed that OCTH’s antitumor mechanism involves the disruption of tumor cell plasma membrane permeability.

Conclusion:

This study is the first that describes the antitumor activity of octenidine hydrochloride on different human tumor cell lines. A biodegradable hydrogel loaded with octenidine hydrochloride constitutes an innovative, low-cost alternative for the topical treatment of cancer.

Search results

Antitumor and antibiofilm effect of a hydrogel loaded with octenidine hydrochloride (OCTH) for topical treatment of cancer