Glucospanlastics: innovative antioxidant and anticancer ascorbyl-2-glucoside vesicles for striking topical performance of repurposed itraconazole†

Abstract

Presently, the development of functional derivatives exploiting biocompatible pharmaceutical materials has become a pressing demand. Among them, ascorbyl-2-glucoside (AA-2G), an ascorbic acid derivative, has significant potential owing to its stability, solubilization and antioxidant prospects. Herein, AA-2G was utilized for the fabrication of itraconazole (ITZ) spanlastics, which were denoted as “glucospanlastics”. Subsequently, the newly designed glucospanlastics were characterized to determine their dimensions, charge, entrapment, solubilization efficiency, morphology, stability and antioxidant activity. Further, their cytotoxicity towards A431 cells and their ex vivo skin deposition were investigated. Subsequently, the competence of the formulated cream containing glucospanlastics to suppress Ehrlich carcinoma and modulate the antioxidant profile was evaluated in vivo. The results revealed that the proposed nano-sized glucospanlastics performed better than conventional spanlastics (without AA-2G) with respect to optimal solubilization efficiency and ITZ entrapment (>95%) together with antioxidant, cytotoxic and skin permeation potentials. More importantly, glucospanlastics containing 10 and 20 mg AA-2G demonstrated considerable tumor suppression and necrosis, improvement in glutathione (GSH) content by 1.68- and 2.26-fold, elevation of total antioxidant capacity (TAC) levels by 1.67- and 2.84-fold and 1.78- and 2.03-fold reduction in malondialdehyde (MDA) levels, respectively, compared to a conventional ITZ cream. These innovative antioxidant vesicles show future potential for the dermal delivery of cancer-directed therapies.

Abstract

Ascorbyl glucoside utilization in the preparation of innovative glucospanlastics loaded itraconazole for topical delivery.