β-Cyclodextrin nanosponges for enhanced anti-melanoma potential of silymarin with functions of anti-oxidant, anti-inflammatory and anti-tyrosinase

Abstract

Overproduction of inflammatory and oxidative species has been identified as key contributors for skin cancer progression. Silymarin (SLY), a natural flavonoid has demonstrated potential anti-inflammatory, anti-oxidant, anti-tyrosinase and anti-cancer activities. Nonetheless, its inherent physicochemical properties such as low solubility, low bioavailability and instability restrict its utility. Hence, current research was planned to address these challenges via encasing silymarin in nanosponges (NS) and exploring for application against skin cancer. Aiming this, silymarin was encased into NS batches prepared by melt technique and pre-eminent batch was selected on the basis of solubility, encapsulation and release. The selected batch (SLY-NS6) was suitably characterized and assessed for in-vitro DPPH scavenging, anti-inflammatory and anti-tyrosinase activities. Cell viability and apoptosis potential against B16F10 cells were performed. Further, evaluation of photostabiility was also conducted. Particle size and zeta potential of SLY-NS6 was found as 334.73 ± 79.63 nm and −29 ± 3.87 mV, respectively. The solubility and encapsulation efficiency of SLY-NS6 was 208.60 ± 13.63 µg/ml and 70.37 ± 1.04, respectively. All batches of SLY-NS has demonstrated delayed release pattern and found to follow Korsmeyer-Peppas model and Fickian diffusion mechanism. The anti-inflammatory activity of SLY and SLY-NS6 were noted 97.02% and 95.19%, respectively, at maximum concentration. The DPPH scavengingand anti-tyrosinase potential of bioactive was also found preserved after its encasement into NS. In-vitro cell viability assay of both SLY and SLY-NS6 showed concentration dependent cytotoxicity with IC50 values 118.75 µg/ml and 87.73 µg/ml, respectively. Further, it was observed that apoptosis effect of SLY-NS6 was remarkably enhanced in comparison to SLY. Photostability study revealed better protection of bioactive after its encasement. In conclusion, SLY-NS is able to address the inherent solubility and stability issues, thereby, enhancing efficacy of bioactive. Promising findings of anti-inflammatory, anti-oxidant, anti-tyrosinase and anti-cancer activities of SLY-NS advocated its potential for management skin cancer.