Zein nanoparticles for oral delivery of quercetin: Pharmacokinetic studies and preventive anti-inflammatory effects in a mouse model of endotoxemia.
Zein nanoparticles were evaluated as nanocarriers to promote the oral bioavailability of quercetin and, thus, improve its anti-inflammatory effect on a mouse model of induced endotoxemia. For this purpose, the flavonoid and 2-hydroxypropyl-β-cyclodextrin were encapsulated in zein nanoparticles. The resulting nanoparticles displayed a mean size of about 300nm and the payload was calculated to be close to 70μg/mg nanoparticle. The release of quercetin from zein nanoparticles followed a zero-order kinetic. After oral administration, nanoparticles provided high and sustained levels of quercetin in plasma and the relative oral bioavailability was calculated to be approx. 60%. Animals treated with quercetin-loaded nanoparticles (1 dose every two days; 1week) presented endotoxic symptoms less severe than those observed in animals treated with the oral solution of the flavonoid (1 dose every day; 1week). This was further corroborated by the significantly low circulating TNF-alpha in the quercetin-loaded nanoparticles treated mice.
Department of Pharmacy and Pharmaceutical Technology, University of Navarra, Pamplona, Spain.
Rebeca
R
Penalva
Centre for Nutrition Research, University of Navarra, Pamplona, Spain.
Carlos J
CJ
González-Navarro
Department of Microbiology, University of Navarra, Pamplona, Spain.
Carlos
C
Gamazo
Department of Pharmacy and Pharmaceutical Technology, University of Navarra, Pamplona, Spain.
Irene
I
Esparza
Department of Pharmacy and Pharmaceutical Technology, University of Navarra, Pamplona, Spain. Electronic address: jmirache@unav.es.
Juan M
JM
Irache
D000284:Administration, Oral; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage*; D004337:Drug Carriers / Q000737:chemistry*; D019446:Endotoxemia / Q000188:drug therapy*; D051379:Mice; D008810:Mice, Inbred C57BL; D053758:Nanoparticles / Q000737:chemistry*; D011794:Quercetin / Q000008:administration & dosage* / Q000493:pharmacokinetics; D017208:Rats, Wistar; D014409:Tumor Necrosis Factor-alpha / Q000097:blood; D015028:Zein / Q000737:chemistry*
D000893:Anti-Inflammatory Agents; D004337:Drug Carriers; D014409:Tumor Necrosis Factor-alpha; D015028:Zein; D011794:Quercetin
Cyclodextrin; Nanoparticles; Oral delivery; Quercetin; Sepsis