A novel cationic arginine-modified Self-Nanoemulsifying drug delivery system (SNEDDS) for improved anticancer and antioxidant activities of Naringin

Abstract

Naringin (NRG) is a flavonoid derived from citrus fruits. Despite its pharmacological significance, NRG's therapeutic effectiveness is constrained by its unusual physicochemical characteristics, such as its lower aqueous solubility. This study was intended to develop an alkylated arginine (AL-ARG) containing self-nanoemulsifying drug delivery system (SNEDDS) serving as a positively charged amphiphile for enhanced anticancer and antioxidant activities of NRG. The drug solubility along with emulsification investigations resulted in the development of a ternary phase diagram for selected suitable formulation components. Lipid (cinnamon oil), surfactant (labrasol), and co-surfactant (Transcutol) were selected as the main components of the formulation. FTIR, zetasizer, and atomic force microscope were employed to characterize optimized formulations, which were then tested for dilution and thermodynamic stability. It was found that the average droplet size and zeta potential of NRG-SNEDDS were 118.47 ± 21.16 nm and −21 ± 2.10 mV, respectively, while those of AL-ARG-incorporated NRG-SNEDDS were 162.17 ± 19.11 nm and −17 ± 1.83 mV. The developed SNEDDS were extremely stable and did not change the chemical nature of the drug. The developed SNEDDS were tested for their antioxidant activity, and the findings showed that the antioxidant potential of NRG was greatly improved by its incorporation into the AL-ARG-modified SNEDDS. When AL-ARG was incorporated into NRG-SNEDDS, its anticancer potential was greatly increased against the human chronic myeloid leukemia cell. It can be concluded that novel cationic arginine-modified SNEDDS have the potential to substantially enhance the antioxidant and anticancer properties of NRG.