Quercetin-loaded transliposomal gel for effective management of skin cancer: In vitro and cell line efficacy studies

Abstract

In this research work, Quercetin-loaded transliposomes (QUR-TL) were developed for dermal application against skin cancers. The utilization of nano-formulation for dermal application presents several notable advantages. Using an ethanol injection method followed by sonication, the QUR-loaded TL was developed and optimized by Box-Behnken Design (BBD). The optimized QUR-TL exhibited the vesicle size of 200.1 nm, polydispersity-index of 0.181, zeta potential of −31.89 mV and an entrapment efficiency of 82.1 %. The morphology of the optimized QUR-TL assessed by Transmission Electron Microscopy has revealed the spherical shape of the vesicles. In vitro release of QUR from QUR-TL was higher as compared to QUR-Suspn. Ex vivo skin permeation has shown ≈2-fold increased permeation of QUR from QUR-TL gel (QUR-TLG) as compared to QUR-conventional gel (QUR-CFG). This demonstrated a prolonged release pattern and an increased permeability of QUR from QUR-TLG. The QUR-TL has shown 1.3-fold higher antioxidant activity as compared to pure-QUR (QUR-SOL). The CLSM demonstrated an enhanced penetration of QUR-TLG, which was substantiated by the quantification of QUR during the dermatokinetics investigation. The QUR-TLG was evaluated for its cytotoxic potential against the B16F10 melanoma cells, which has shown lowest IC50 value (9.3 μM) as compared to QUR-CFG (16.8 μM) and QUR-SOL (23 μM). This suggested strong evidence of QUR indication for skin cancers. Conclusively, QUR-TLG has significantly (p < 0.05) targeted the deeper layers of skin and can be regarded as a promising carrier for topical application of QUR or other lipophilic drugs for the management of skin cancers.