Characterization of trans-Resveratrol-Loaded Lipid-Core Nanocapsules and Tissue Distribution Studies in Rats

被引：152
作者：
Frozza, Rudimar L. [1 ]
Bernardi, Andressa [2 ]
Paese, Karina [2 ]
Hoppe, Juliana B. [1 ]
da Silva, Thaline [1 ]
Battastini, Ana M. O. [1 ]
Pohlmann, Adriana R. [2 ,3 ]
Guterres, Silvia S. [2 ]
Salbego, Christianne [1 ]
机构：
[1] Univ Fed Rio Grande do Sul, Dept Bioquim, Inst Ciencias Basicas Saude, BR-90035003 Porto Alegre, RS, Brazil
[2] Univ Fed Rio Grande do Sul, Programa Posgrad Ciencias Farmaceut, Fac Farm, BR-90610000 Porto Alegre, RS, Brazil
[3] Univ Fed Rio Grande do Sul, Programa Posgrad Quim, Inst Quim, BR-91501970 Porto Alegre, RS, Brazil
来源：
JOURNAL OF BIOMEDICAL NANOTECHNOLOGY | 2010年 / 6卷 / 06期
关键词：
trans-Resveratrol; Nanocapsule; Drug Delivery; Physical Stability; Biodistribution; BLOOD-BRAIN-BARRIER; TARGETED DELIVERY; SMALL-INTESTINE; NANOPARTICLES; BIOAVAILABILITY; INSTABILITY; METABOLISM; ABSORPTION; PARTICLES; PEPTIDES;
D O I：
10.1166/jbn.2010.1161
中图分类号：
TB3 [工程材料学];
学科分类号：
0805 ; 080502 ;
摘要：
Several studies have reported that orally ingested trans-resveratrol is extensively metabolized in the enterocyte before it enters the blood and target organs. Additionally, trans-resveratrol is photosensitive, easily oxidized and presents unfavorable pharmacokinetics. Therefore, it is of great interest to stabilize trans-resveratrol in order to preserve its biological activities and to improve its bioavailability in the brain. Here, trans-resveratrol was loaded into lipid-core nanocapsules and analyzed for particle size, polydispersity and zeta potential. The nanocapsule distribution in brain tissue was evaluated by intraperitoneal (i.p.) and gavage routes in healthy rats. The lipid-core nanocapsules had a mean diameter of 241 nm, a polydispersity index of 0.2, and a zeta potential of -15 mV. No physical changes were observed after 1, 2 and 3 months of storage at 25 degrees C. Lipid-core nanocapsules showed high entrapment of trans-resveratrol and displayed a higher trans-resveratrol concentration in the brain, the liver and the kidney after daily i.p. or gavage administration than that observed for the free trans-resveratrol. Because trans-resveratrol is a potent cyclooxygenase-1 inhibitor, gastrointestinal damage was evaluated. The animals that were administered with trans-resveratrol-loaded lipid-core nanocapsules showed significantly less damage when compared to those administered with free trans-resveratrol. In summary, lipid-core nanocapsules exhibited great trans-resveratrol encapsulation efficiency. trans-Resveratrol-loaded lipid-core nanocapsules increased the concentration of trans-resveratrol in the brain tissue. Gastrointestinal safety was improved when compared with free trans-resveratrol. Thus, trans-resveratrol-loaded lipid-core nanocapsules may be used as an alternative potential therapeutic for several diseases including Alzheimer's disease.
引用
收藏
页码：694 / 703
页数：10
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