Effect of quercetin and resveratrol co-incorporated in liposomes against inflammatory/oxidative response associated with skin cancer

• Published in: International journal of pharmaceutics Vol. 513; no. 1-2; pp. 153 - 163
• Main Authors: Caddeo, Carla, Nacher, Amparo, Vassallo, Antonio, Armentano, Maria Francesca, Pons, Ramon, Fernàndez-Busquets, Xavier, Carbone, Claudia, Valenti, Donatella, Fadda, Anna Maria, Manconi, Maria
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 20-11-2016
• Subjects: Administration, Topical; Animals; Antioxidant; Antioxidants - administration & dosage; Disease Models, Animal; Drug Combinations; Drug Delivery Systems; Dynamic Light Scattering; Female; Fibroblast; Fibroblasts - drug effects; Fibroblasts - metabolism; Humans; Inflammation - drug therapy; Inflammation - pathology; Liposome; Liposomes; Mice; Oxidative Stress - drug effects; Quercetin; Quercetin - administration & dosage; Quercetin - pharmacology; Reactive Oxygen Species - metabolism; Resveratrol; Skin lesion; Skin Neoplasms - drug therapy; Skin Neoplasms - pathology; Stilbenes - administration & dosage; Stilbenes - pharmacology; Liposome; Skin lesion; Antioxidant; Fibroblast; Quercetin; Resveratrol
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2016.09.014

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The present investigation reports the development of liposomes for the co-delivery of naturally occurring polyphenols, namely quercetin and resveratrol. Small, spherical, uni/bilamellar vesicles were produced, as demonstrated by light scattering, cryo-TEM, SAXS. The incorporation of quercetin and resveratrol in liposomes did not affect their intrinsic antioxidant activity, as DPPH radical was almost completely inhibited. The cellular uptake of the polyphenols was higher when they were formulated in liposomes, and especially when co-loaded rather than as single agents, which resulted in a superior ability to scavenge ROS in fibroblasts. The in vivo efficacy of the polyphenols in liposomes was assessed in a mouse model of skin lesion. The topical administration of liposomes led to a remarkable amelioration of the tissue damage, with a significant reduction of oedema and leukocyte infiltration. Therefore, the proposed approach based on polyphenol vesicular formulation may be of value in the treatment of inflammation/oxidative stress associated with pre-cancerous/cancerous skin lesions.