Paclitaxel-Loaded Folate-Targeted Albumin-Alginate Nanoparticles Crosslinked with Ethylenediamine. Synthesis and In Vitro Characterization.
Autor: Martínez Relimpio, Ana María; Benito, Marta; Pérez Izquierdo, Elena; Teijón, César; Olmo, Rosa María; Blanco, María Dolores
Resumen: Among the different ways to reduce the secondary effects of antineoplastic drugs in cancer
treatment, the use of nanoparticles has demonstrated good results due to the protection of the
drug and the possibility of releasing compounds to a specific therapeutic target. The -isoform
of the folate receptor (FR) is overexpressed on a significant number of human cancers; therefore,
folate-targeted crosslinked nanoparticles based on BSA and alginate mixtures and loaded with
paclitaxel (PTX) have been prepared to maximize the proven antineoplastic activity of the drug
against solid tumors. Nanometric-range-sized particles (169 28 nm–296 57 nm), with negative
Z-potential values (between �����0.12 0.04 and �����94.1 0.4), were synthesized, and the loaded PTX
(2.63 0.19–3.56 0.13 g PTX/mg Np) was sustainably released for 23 and 27 h. Three cell lines
(MCF-7, MDA-MB-231 and HeLa) were selected to test the efficacy of the folate-targeted PTX-loaded
BSA/ALG nanocarriers. The presence of FR on the cell membrane led to a significantly larger uptake
of BSA/ALG–Fol nanoparticles compared with the equivalent nanoparticles without folic acid on
their surface. The cell viability results demonstrated a cytocompatibility of unloaded nanoparticle–
Fol and a gradual decrease in cell viability after treatment with PTX-loaded nanoparticle–Fol due to
the sustainable PTX release.
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