pH-dependent, extended release and enhanced in vitro efficiency against colon cancer of Tegafur formulated using chitosan-coated poly (ε-caprolactone) nanoparticles
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Elsevier
Materia
Poly(ε-caprolactone) Chitosan Tegafur Nanoparticles Colorectal cancer Drug delivery
Date
2023-05-26Referencia bibliográfica
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]
Sponsorship
FEDER/Junta de Andalucía – Consejería de Transformaci´on Econ´omica, Industria, Conocimiento y Universidades, Spain (Grant P20_00346).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