In-vitro cytotoxic studies of 1-hexylcarbamoyl-5-fluorouracil encapsulated nanogels in BMG-1 cells

Abstract

5-Fluorouracil (5-FU) has become one of the most widely employed antimetabolite chemotherapeutic agents in the treatment of several cancers including brain, colorectal, breast, head and neck, pancreas and stomach cancers. The variability in 5-FU pharmacokinetics makes oral dosing impractical due to low and unpredictable bioavailability. Carmofur or HCFU (1-hexylcarbamoyl-5fluorouracil) is a lypophilic-masked analogue of 5-FU. We present studies on encapsulation of HCFU into the nanogels synthesized through copolymerization of N-isopropylacrylamide (NIPAAM) and N-vinylpyrrolidone (VP) having hydrophobic core and hydrophilic shell by crosslinking with N, N'methylenebisacrylamide. This enables easy entrapment and retention of HCFU inside the hydrophobic core of the nanoparticles. A comparison of the therapeutic efficacies and cell sustainability of 5-fluorouracil, HCFU, HCFU loaded nanogels and unencapsulated nanogels as studied in BMG-1 Cells, is reported.