@misc{10481/83905,
year = {2023},
month = {5},
url = {https://hdl.handle.net/10481/83905},
abstract = {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},
organization = {FEDER/Junta de Andalucía – Consejería
de Transformaci´on Econ´omica, Industria, Conocimiento y Universidades,
Spain (Grant P20_00346).},
publisher = {Elsevier},
keywords = {Poly(ε-caprolactone)},
keywords = {Chitosan},
keywords = {Tegafur},
keywords = {Nanoparticles},
keywords = {Colorectal cancer},
keywords = {Drug delivery},
title = {pH-dependent, extended release and enhanced in vitro efficiency against colon cancer of Tegafur formulated using chitosan-coated poly (ε-caprolactone) nanoparticles},
doi = {10.1016/j.jddst.2023.104594},
author = {Medina Moreno, Ana and El-Hammadi, Mazen M. and Arias Mediano, José Luis},
}