Poly(ε-caprolactone)-poly(ethylene glycol) Tri-Block Copolymer as Quercetin Delivery System for Human Colorectal Carcinoma Cells: Synthesis, Characterization and In Vitro Study
Nancy Ferrentino,
Maria Preziosa Romano,
Silvia Zappavigna,
Marianna Abate,
Vitale Del Vecchio,
Dario Romano,
Chiara Germinario,
Celestino Grifa,
Rosanna Filosa,
Daniela Pappalardo
Affiliations
Nancy Ferrentino
Dipartimento di Scienze e Tecnologie, Università del Sannio, Via de Sanctis snc, 82100 Benevento, Italy
Maria Preziosa Romano
Dipartimento di Scienze e Tecnologie, Università del Sannio, Via de Sanctis snc, 82100 Benevento, Italy
Silvia Zappavigna
Department of Precision Medicine, University of Campania “Luigi Vanvitelli”, Via Santa Maria di Costantinopoli, 16, 80138 Naples, Italy
Marianna Abate
Department of Precision Medicine, University of Campania “Luigi Vanvitelli”, Via Santa Maria di Costantinopoli, 16, 80138 Naples, Italy
Vitale Del Vecchio
Department of Experimental Medicine, University of Campania “Luigi Vanvitelli”, Via Santa Maria di Costantinopoli, 16, 80138 Naples, Italy
Dario Romano
Physical Science and Engineering Division, King Abdullah University of Science and Technology (KAUST), Thuwal 23955-6900, Saudi Arabia
Chiara Germinario
Dipartimento di Scienze e Tecnologie, Università del Sannio, Via de Sanctis snc, 82100 Benevento, Italy
Celestino Grifa
Dipartimento di Scienze e Tecnologie, Università del Sannio, Via de Sanctis snc, 82100 Benevento, Italy
Rosanna Filosa
Dipartimento di Scienze e Tecnologie, Università del Sannio, Via de Sanctis snc, 82100 Benevento, Italy
Daniela Pappalardo
Dipartimento di Scienze e Tecnologie, Università del Sannio, Via de Sanctis snc, 82100 Benevento, Italy
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.
