Synthesis, characterization, and biological activities of folic acid conjugates with polyvinyl alcohol, chitosan, and cellulose

Abstract

AbstractPolyvinyl alcohol (PVA), chitosan (CS), and cellulose (CL) are promising polymers for chemical functionalization and biomedical applications. This study aimed to synthesize folic acid (FA) conjugates with PVA, CS, and CL via chloroacetyl chloride, 2‐bromopropionyl bromide, and epichlorohydrin to enhance it biomedical applications. The functionalized polymer conjugates were characterized by FT‐IR, 1H‐NMR, GPC, and TGA techniques. FT‐IR and 1H‐NMR revealed the main functional groups (OH, NH, C═O, C═N), the aromatic CH and NH protons of FA moieties. TGA illustrated two stages of decompositions of all‐polymer conjugates. FA showed no antifungal activity, while two of the newly grafted polymer conjugates (chitosan bromopropionate‐grafted FA and cellulose chloroacetate‐grafted FA) illustrated antifungal activity against both Aspergillus fumigatus and Candida albicans. Polymer conjugates; poly(vinyl chloroacetate)‐grafted FA and chitosan‐EPCH‐grafted FA revealed good antifungal effect on C. albicans and A. fumigatus, respectively. Most FA polymer conjugates showed significant antitumor activity against EAC‐bearing mice. Among these conjugates, chitosan chloroacetate‐grafted FA (P‐2A) showed the highest antitumor effect against EAC‐bearing mice via reduction in total tumor volume. Thus, these conjugates provided enhanced antifungal and antitumor activities as compared with FA itself. These conjugates may act as promising biologically active carrier systems for other applications such as drug delivery.