pH-dependent, extended release and enhanced in vitro efficiency against colon cancer of Tegafur formulated using chitosan-coated poly (ε-caprolactone) nanoparticles Medina Moreno, Ana El-Hammadi, Mazen M. Arias Mediano, José Luis Poly(ε-caprolactone) Chitosan Tegafur Nanoparticles Colorectal cancer Drug delivery Tegafur is used to treat various malignant lesions, including advanced gastric and colorectal cancers. However, its efficacy is limited by its low oral bioavailability, short half-life and serious toxicity. To address these drawbacks, a nanoformulation of poly(ε-caprolactone) nanoparticles coated with chitosan was developed for the delivery of Tegafur. Poly(ε-caprolactone) particles were prepared by an interfacial polymer disposition method, while surface functionalization with chitosan followed a coacervation procedure. Transmission electron microscopy and elemental analyses, and electrokinetics of the particles demonstrated that such core/shell nanostructure was obtained. Compared to unmodified particles, chitosan-coated nanoparticles demonstrated a substantially increased stability at both 4 and 25 ◦C over 30 days. Particles showed an encapsulation efficiency of ≈64% and a pH-dependent behavior in which complete Tegafur release was extended over 168, 48 or 24 h at pH 7.4 (blood), 6.5 (extracellular microenvironment of tumors) or 5.5 (endosomes/lysosomes of tumor cells), respectively. Based on hemocompatibility and cell viability tests, chitosan-coated nanoparticles exhibited satisfactory biocompatibility and safety for drug delivery. Furthermore, Tegafur-loaded chitosan-decorated particles demonstrated enhanced anticancer efficiency, with half maximal inhibitory concentration values in HT- 29 and T-84 cells of ≈ 4-fold and ≈3.5-fold less than that of the free drug and drug-loaded unmodified nanoparticles, respectively. In vivo studies are needed to fully assess their efficacy and safety 2023-07-21T08:57:48Z 2023-07-21T08:57:48Z 2023-05-26 info:eu-repo/semantics/article A. Medina-Moreno et al. pH-dependent, extended release and enhanced in vitro efficiency against colon cancer of Tegafur formulated using chitosan-coated poly (ε-caprolactone) nanoparticles. Journal of Drug Delivery Science and Technology 86 (2023) 104594[https://doi.org/10.1016/j.jddst.2023.104594] https://hdl.handle.net/10481/83905 10.1016/j.jddst.2023.104594 eng http://creativecommons.org/licenses/by-nc-nd/4.0/ info:eu-repo/semantics/openAccess Attribution-NonCommercial-NoDerivatives 4.0 Internacional Elsevier