To design a novel preactived carboxymethyl cellulose derivative. Methods: First, carboxymethyl cellulose (CMC) was chemically modified by amide bond formation between primary amino group of cysteine (CYS) and carboxylic moiety of CMC mediated by carbodiimide. Second, obtained CMCCYS was preactivated with 2,2′-dithiodinicotinic acid. Designed CMC-S-S-MNA was characterized by FT-IR. Furthermore, cytotoxicity was conducted on Caco-2 cell line. Swelling behavior, erosion and release of novel CMC-S-S-MNA were performed compared with thiolated and unmodified cellulose, respectively. Results: CMC-S-S-MNA showed no harmful effect on cells. CMC-S-S-MNA exhibited 2.13-fold higher stability in comparison to unmodified cellulose. Furthermore, preactivated carboxymethyl cellulose-cysteine revealed 1.9-fold controlled released compared with respective unmodified carboxymethyl cellulose. Conclusion: Novel preactivated carboxymethyl cellulose represents a versatile excipient for drug delivery.

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