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

页码：694 / 703

页数：10

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