title: Bioavailability of curcumin and curcumin glucuronide in the central nervous system of mice after oral delivery of nano-curcumin.
abstract: Curcumin is a bioactive molecule extracted from Turmeric roots that has been recognized to possess a wide variety of important biological activities. Despite its great pharmacological activities, curcumin is highly hydrophobic, which results in poor bioavailability. We have formulated this hydrophobic compound into stable polymeric nanoparticles (nano-curcumin) to enhance its oral absorption. Pharmacokinetic analysis after oral delivery of nano-curcumin in mice demonstrated approximately 20-fold reduction in dose requirement when compared to unformulated curcumin to achieve comparable plasma and central nervous system (CNS) tissue concentrations. This investigation corroborated our previous study of curcumin functionality of attenuating opioid tolerance and dependence, which shows equivalent efficacy of low-dose (20mg/kg) nano-curcumin and high-dose (400mg/kg) pure curcumin in mice. Furthermore, the highly selective and validated liquid chromatography-mass spectrometry (LC-MS) method was developed to quantify curcumin glucuronide, the major metabolite of curcumin. The results suggest that the presence of curcumin in the CNS is essential for prevention and reversal of opioid tolerance and dependence.
authors.affiliation: Department of Chemical Engineering, University of Illinois at Chicago, Chicago, IL 60607, United States.
authors.forename: Magdalena
authors.initials: M
authors.lastname: Szymusiak
authors.affiliation: Department of Biopharmaceutical Sciences, University of Illinois at Chicago, Chicago, IL 60612, United States.
authors.forename: Xiaoyu
authors.initials: X
authors.lastname: Hu
authors.affiliation: Department of Chemical Engineering, University of Illinois at Chicago, Chicago, IL 60607, United States.
authors.forename: Paola A
authors.initials: PA
authors.lastname: Leon Plata
authors.affiliation: Department of Chemical Engineering, University of Illinois at Chicago, Chicago, IL 60607, United States.
authors.forename: Paulina
authors.initials: P
authors.lastname: Ciupinski
authors.affiliation: Department of Biopharmaceutical Sciences, University of Illinois at Chicago, Chicago, IL 60612, United States.
authors.forename: Zaijie Jim
authors.initials: ZJ
authors.lastname: Wang
authors.affiliation: Department of Chemical Engineering, University of Illinois at Chicago, Chicago, IL 60607, United States; Department of Biopharmaceutical Sciences, University of Illinois at Chicago, Chicago, IL 60612, United States. Electronic address: liuying@uic.edu.
authors.forename: Ying
authors.initials: Y
authors.lastname: Liu
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D001921:Brain / Q000187:drug effects / Q000378:metabolism*; D003474:Curcumin / Q000008:administration & dosage* / Q000031:analogs & derivatives / Q000378:metabolism*; D016503:Drug Delivery Systems / Q000379:methods; D020719:Glucuronides / Q000008:administration & dosage / Q000378:metabolism; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D053758:Nanoparticles / Q000008:administration & dosage* / Q000378:metabolism*; D013116:Spinal Cord / Q000187:drug effects / Q000378:metabolism*
chemical_list: D020719:Glucuronides; C000591193:curcumin glucuronide; D003474:Curcumin
keywords: Bioavailability; Central nervous system (CNS); Liquid chromatography–mass spectrometry (LC–MS); Nano-curcumin; Oral delivery