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Poly(ε-caprolactone)-poly(ethylene glycol) Tri-Block Copolymer as Quercetin Delivery System for Human Colorectal Carcinoma Cells: Synthesis, Characterization and In Vitro Study

by Ferrentino, Nancy , Zappavigna, Silvia , Romano, Dario , Grifa, Celestino , Filosa, Rosanna , Pappalardo, Daniela , Germinario, Chiara , Romano, Maria Preziosa , Abate, Marianna , Del Vecchio, Vitale

in Bioavailability / Biodegradability / Block copolymers / Blood circulation / Breast cancer / Cancer therapies / Cell cycle / Chromatography / Colorectal cancer / Copolymers / Drug delivery systems / Drugs / Flow cytometry / Hydrophobicity / Liquid chromatography / Micelles / Molecular weight / Nanoparticles / NMR / NMR spectroscopy / Nuclear magnetic resonance / Pharmacokinetics / Photon correlation spectroscopy / Polycaprolactone / Polyethylene glycol / Polymerization / Ring opening polymerization / Self-assembly / Software / Spectrum analysis / Toxicity

2023

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Poly(ε-caprolactone)-poly(ethylene glycol) Tri-Block Copolymer as Quercetin Delivery System for Human Colorectal Carcinoma Cells: Synthesis, Characterization and In Vitro Study

2023

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Poly(ε-caprolactone)-poly(ethylene glycol) Tri-Block Copolymer as Quercetin Delivery System for Human Colorectal Carcinoma Cells: Synthesis, Characterization and In Vitro Study

2023

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Journal Article

Poly(ε-caprolactone)-poly(ethylene glycol) Tri-Block Copolymer as Quercetin Delivery System for Human Colorectal Carcinoma Cells: Synthesis, Characterization and In Vitro Study

Ferrentino, Nancy,

Zappavigna, Silvia,

Romano, Dario,

Grifa, Celestino,

Filosa, Rosanna,

Pappalardo, Daniela,

Germinario, Chiara,

Romano, Maria Preziosa,

Abate, Marianna,

Del Vecchio, Vitale

2023

Overview

Quercetin is a hydrophobic molecule with short blood circulation times and instability. The development of a nano-delivery system formulation of quercetin may increase its bioavailability, resulting in greater tumor suppressing effects. Triblock ABA type polycaprolactone-polyethylenglycol- polycaprolactone (PCL-PEG-PCL) copolymers have been synthetized using ring-opening polymerization of caprolactone from PEG diol. The copolymers were characterized by nuclear magnetic resonance (NMR), diffusion-ordered NMR spectroscopy (DOSY), and gel permeation chromatography (GPC). The triblock copolymers self-assembled in water forming micelles consisting of a core of biodegradable polycaprolactone (PCL) and a corona of polyethylenglycol (PEG). The core-shell PCL-PEG-PCL nanoparticles were able to incorporate quercetin into the core. They were characterized by dynamic light scattering (DLS) and NMR. The cellular uptake efficiency of human colorectal carcinoma cells was quantitatively determined by flow cytometry using nanoparticles loaded with Nile Red as hydrophobic model drug. The cytotoxic effect of quercetin-loaded nanoparticles was evaluated on HCT 116 cells, showing promising results.

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