Formulation, optimization, and characterization of naringenin-loaded halloysite nanotube to achieve enhanced antioxidant and anticancer properties

Objective(s): Poor solubility and stability of naringenin result in its low bioavailability. Halloysite nanotubes (HNTs) were investigated as a potential carrier for the controlled delivery of naringenin to HT-29 (human colon adenocarcinoma) and MCF-7 (human breast cancer) cell lines. Materials and Methods: Naringenin was loaded in HNTs at different HNTs: drug ratios (w/w) of 30, 24, 16, 8, and 4, then characterized by SEM (Scanning electron microscope), FTIR (Fourier transform infrared spectroscopy), DSC (Differential scanning calorimetry), and XRD (X-ray diffraction). The effect of naringenin loaded in HNTs on its solubility was investigated by an innovative change in the DPPH (2, 2-diphenyl-1-picrylhydrazyl) assay. Cytotoxicity of naringenin and naringenin-loaded HNTs was investigated by MTT assay. Results: At a ratio of 30, the highest encapsulation efficiency (87.7± 5%), and at a ratio of 4, the highest loading capacity was obtained (12± 0.6%). The drug release study indicated prolonged drug release from naringenin-loaded HNTs (67±5% after 24h). Naringenin showed antioxidant activity by scavenging DPPH radical with an IC50 value of 400 ±4 µg/mL. Naringenin solubility after loading was considerably increased and subsequently, showed 2.2-fold higher antioxidant activity than the free drug. Cytotoxicity assay indicated the anticancer activity of naringenin was significantly improved after loading. Conclusion: HNTs can be a promising carrier for the delivery of naringenin.