Maltodextrin-α-tocopherol conjugates of vitamin E: Influence of degree of derivatization on physicochemical properties and biological evaluation

Vitamin E is one of the essential antioxidants whose limited aqueous solubility retracted its various applications. Herein, we report the synthesis of tailored bio-conjugates composed of maltodextrin and vitamin E succinate at different degree of derivatization to address the poor solubility of vitamin E. The identity of bioconjugates was characterized by FTIR and H-1 NMR besides evaluation of antioxidant activity and in-vitro/in-vivo toxicological studies. Our findings displayed formation of new chemical entities with 4 folds increase in aqueous solubility compared to parent vitamin E succinate. Evaluation of the antioxidant activity using ABTS/DPPH scavenging assay was found to be dependent on degree of derivatization (DD) and revealed superior enhancement in antioxidant activity (similar to 80%) of the bioconjugates. In vitro/in vivo bio-evaluations e.g. hemolysis, MTT assay and subacute toxicity study demonstrated the biological compatibility of bio-conjugates at specific ratios. Moreover, histopathological inspection of liver and kidney showed no clear signs of cellular toxicity or inflammatory reaction. Overall, Maltodextrin-alpha-tocopherol bioconjugates represent new candidates of vitamin E with enhanced aqueous solubility and antioxidant activity and offer amphiphilic molecules to be employed as biocompatible carriers for different pharmaceutical applications.