Heparin-appended polycaprolactone core/corona nanoparticles for site specific delivery of 5-fluorouracil

Abstract

The aim of the present work is to formulate heparin-modified-polycaprolactone (HEP) core shell nanoparticles (NPs) of 5-fluorouracil (5-FU). These NPs were characterized for various in vitro parameters like particle size, zeta potential, etc. HEP NPs were found to maintain comparatively slower drug release pattern (98.9% in 96 h) than PCL NPs. Cytotoxicity studies demonstrated a massive cytotoxic potential of 5-FU-loaded HEP NPs in A549, MDA-MD-435, and SK-OV-3 cancer cell lines. Pharmacokinetic parameters were also determined in blood after IV administration of HEP NPs: AUC, Cmax, MRT, and Tmax values are 6096.075 ± 5.90 μg h/mL, 144.38 ± 1.52 μg/L, 58.71 ± 0.25 h, 96 ± 0.50 h, respectively and 117.92 ± 1.78, 45.35 ± 3.00, 1.2 ± 0.25, 0.5 ± 0.02 in plain 5-FU solution.