Novel 5-flurouracil-Embedded non-woven PVA - PVP electrospun nanofibers with enhanced anti-cancer efficacy: Formulation, evaluation and in vitro anti-cancer activity

Abstract

In this study we describe the development of an effective nanofiber (NF) formulation that uses two low-cost and easily available polymers, PVA and PVP, to embed and release a well-known anticancer drug, 5-flurouracil (5FU), which is intended to treat colon cancer. PVA:PVP polymers in a variety of ratios (10:2, 8:4, 6:6, 4:8, 2:10) were used for NF fabrication to find the optimum composition. The selected NF composition (10:2 PVA:PVP) was then characterized by UV–Visible spectroscopy, Fourier-Transform InfraRed spectroscopy (FTIR), Scanning Electron Microscopy (SEM), and Powder X-Ray Diffraction (PXRD). The FTIR results demonstrate effective loading of the drug into the polymer matrices, this is further supported by a decrease in the intensity of the 5-FU crystallinity peak shown in the PXRD results. Drug loading experiments showed that approximately 95.97, 94.48 and 93.22% of 5–FU was successfully loaded to the selected NFs when 10, 20 and 30% initial proportions of the drug, respectively, were added. Entrapment efficiencies of 91.2, 93.85 and 96.06% by the PVA-PVP NF were achieved from initial 5-FU proportions of 10, 20 and 30%, respectively. Drug release experiments show that all of the drug-loaded NFs exhibit an initial burst of elevated drug release followed by slow sustained release over a period of more than 20 h that follows a Fickian diffusion mechanism (n > 0.5), we believe this mechanism controls release of the drug by a combination of diffusion and erosion. An in vitro cyctotoxicity evaluation of the nanofibers against a human colorectal adenocarcinoma cell line (HT29) showed enhanced anti-cancer performance, suggesting additional advantages of these fluorouracil nanofibers.