Progress in the design of ascorbic acid derivative-mediated drug delivery

Antioxidant-based pharmaceutical products are currently experiencing a surge in popularity and satisfaction, demonstrating promising preclinical and clinical prospects. These products exert their beneficial effects by displaying protection against mischievous free radicals. One potent antioxidant is ascorbic acid (AA), which plays numerous crucial biochemical roles and is typically distinguished as a primary hydrophilic, non-enzymatic antioxidant in tissues. AA is a water-soluble essential antioxidant vitamin that can only be obtained from the diet. However, AA's instability, coupled with challenges related to its delivery, has presented formulation challenges for chemists. As a result, various stable hydrophilic and lipophilic derivatizations of AA have been devised. Capitalizing on their potential, delivery platforms, particularly nano-sized ones utilizing ascorbic acid derivatives, have been extensively investigated in recent years. Two such derivatives, namely, ascorbyl-6-palmitate (AP; a lipophilic derivative) and ascorbyl-2-glucoside (AA-2G; a hydrophilic derivative), have been extensively studied in previous works. Herein, the scientific data related to their utilization, either as a drug or as an integral component in delivery vehicles, and their pharmaceutical applications are evaluated.