In the present work, quercetin and resveratrol, natural polyphenols with strong antioxidant and anti-inflammatory properties, were co-loaded in polymer-associated liposomes conceived for oral delivery,by exploiting the potential of pH-sensitive succinyl-chitosan. Chitosan was succinylated, character-ized by Nuclear Magnetic Resonance spectroscopy and Gel Permeation Chromatography, and used toform a protective shell on the surface of liposomes. The physico-chemical properties of the succinyl-chitosan liposomes were assessed by light scattering, zeta potential, cryogenic transmission electronmicroscopy, and small angle X-ray scattering. Small, spherical, uni- and bilamellar vesicles were produced. The succinyl-chitosan shell increased not only the physical stability of the vesicular system, asdemonstrated by accelerated stability tests, but also the release of the polyphenols to a greater extent at pH 7.0, mimicking the intestinal environment.The proposed approach based on polyphenol vesicular formulations may be of value in the treatmentof pre-cancerous/cancerous intestinal conditions associated with inflammation and oxidative stress.
PHYSICO-CHEMICAL CHARACTERIZATION OF SUCCINYL CHITOSAN-STABILIZED LIPOSOMES FOR THE ORAL CO-DELIVERY OF QUERCETIN AND RESVERATROL
CARBONE, CLAUDIA;
2017-01-01
Abstract
In the present work, quercetin and resveratrol, natural polyphenols with strong antioxidant and anti-inflammatory properties, were co-loaded in polymer-associated liposomes conceived for oral delivery,by exploiting the potential of pH-sensitive succinyl-chitosan. Chitosan was succinylated, character-ized by Nuclear Magnetic Resonance spectroscopy and Gel Permeation Chromatography, and used toform a protective shell on the surface of liposomes. The physico-chemical properties of the succinyl-chitosan liposomes were assessed by light scattering, zeta potential, cryogenic transmission electronmicroscopy, and small angle X-ray scattering. Small, spherical, uni- and bilamellar vesicles were produced. The succinyl-chitosan shell increased not only the physical stability of the vesicular system, asdemonstrated by accelerated stability tests, but also the release of the polyphenols to a greater extent at pH 7.0, mimicking the intestinal environment.The proposed approach based on polyphenol vesicular formulations may be of value in the treatmentof pre-cancerous/cancerous intestinal conditions associated with inflammation and oxidative stress.File | Dimensione | Formato | |
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