Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 511, Issue 1, Pages 415-423Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2016.07.027
Keywords
Nano-curcumin; Oral delivery; Bioavailability; Central nervous system (CNS); Liquid chromatography-mass spectrometry (LC-MS)
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Funding
- National Science Foundation Nanomanufacturing Program [NSF-CMMI-1350731]
- University of Illinois at Chicago Proof-of-Concept Award
- Div Of Civil, Mechanical, & Manufact Inn
- Directorate For Engineering [1350731] Funding Source: National Science Foundation
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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 (20 mg/kg) nano-curcumin and high-dose (400 mg/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. (C) 2016 Elsevier B.V. All rights reserved.
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