Cross-linked chitosan/liposome hybrid system for the intestinal delivery of quercetin

被引:109
作者
Caddeo, Carla [1 ]
Diez-Sales, Octavio [2 ,3 ]
Pons, Ramon [4 ]
Carbone, Claudia [5 ]
Ennas, Guido [6 ,7 ]
Puglisi, Giovanni [5 ]
Fadda, Anna Maria [1 ]
Manconi, Maria [1 ]
机构
[1] Univ Cagliari, Dept Sci Vita & Ambiente, Sez Sci Farmaco, I-09124 Cagliari, Italy
[2] Univ Valencia, Dept Pharm & Pharmaceut Technol, E-46100 Valencia, Spain
[3] Univ Cagliari, Univ Politecn Valencia, Ctr Mixto, Inst Reconocimiento Mol & Desarrollo Tecnol, I-09124 Cagliari, Italy
[4] CSIC, IQAC, Dept Tecnol Quim & Tensioactius, ES-08034 Barcelona, Spain
[5] Univ Catania, Dept Sci Farmaco, I-95125 Catania, Italy
[6] Univ Cagliari, Dept Sci Chim & Geol, I-09042 Monserrato, CA, Italy
[7] Consorzio Nazl Sci & Tecnol Mat INSTM, Unita Ric, I-09042 Monserrato, CA, Italy
关键词
Quercetin; Chitosan; Liposomes; Intestinal delivery; IN-VITRO EVALUATION; ORAL BIOAVAILABILITY; CHITOSAN; LIPOSOMES; DRUG; NANOPARTICLES; ENHANCEMENT; ABSORPTION; MICELLES;
D O I
10.1016/j.jcis.2015.09.013
中图分类号
O64 [物理化学(理论化学)、化学物理学];
学科分类号
070304 ; 081704 ;
摘要
Quercetin is a flavonoid with antioxidant/anti-inflammatory properties, poorly absorbed when administered orally. To increase its bioavailability and optimize its release in the intestine, a hybrid system made of liposomes coated with cross-linked chitosan, named TPP-chitosomes, was developed and characterized by light scattering, transmission electron microscopy, differential scanning calorimetry, X-ray powder diffraction and Turbiscan (R) technology. The TPP-chitosomes were nanosized (similar to 180 nm), fairly spherical in shape and unilamellar. The actual coating of the surface of liposomes with the cross-linked chitosan was demonstrated by Small-Angle X-ray Scattering. The release of quercetin in simulated gastric and intestinal pH was investigated, the results showing that the system provided resistance to acidic conditions, and promoted the release in alkaline pH, mimicking the intestinal environment. The proposed hybrid system represents a promising combination of nanovesicles and chitosan for the delivery of quercetin to the intestine in the therapy of oxidative stress/inflammation related disorders. (C) 2015 Elsevier Inc. All rights reserved.
引用
收藏
页码:69 / 78
页数:10
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