Document Detail

Polymeric curcumin nanoparticle pharmacokinetics and metabolism in bile duct cannulated rats.
MedLine Citation:
PMID:  23534919     Owner:  NLM     Status:  MEDLINE    
The objective of this study was to compare the pharmacokinetics and metabolism of polymeric nanoparticle-encapsulated (nanocurcumin) and solvent-solubilized curcumin formulations in Sprague-Dawley (SD) rats. Nanocurcumin is currently under development for cancer therapy. Since free, unencapsulated curcumin is rapidly metabolized and excreted in rats, upon intravenous (i.v.) administration of nanocurcumin only nanoparticle-encapsulated curcumin can be detected in plasma samples. Hence, the second objective of this study was to utilize the metabolic instability of curcumin to assess in vivo drug release from nanocurcumin. Nanocurcumin and solvent-solubilized curcumin were administered at 10 mg curcumin/kg by jugular vein to bile duct-cannulated male SD rats (n = 5). Nanocurcumin increased the plasma Cmax of curcumin 1749 fold relative to the solvent-solubilized curcumin. Nanocurcumin also increased the relative abundance of curcumin and glucuronides in bile but did not dramatically alter urine and tissue metabolite profiles. The observed increase in biliary and urinary excretion of both curcumin and metabolites for the nanocurcumin formulation suggested a rapid "burst" release of curcumin. Although the burst release observed in this study is a limitation for targeted tumor delivery, nanocurcumin still exhibits major advantages over solvent-solubilized curcumin, as the nanoformulation does not result in the lung accumulation observed for the solvent-solubilized curcumin and increases overall systemic curcumin exposure. Additionally, the remaining encapsulated curcumin fraction following burst release is available for tumor delivery via the enhanced permeation and retention effect commonly observed for nanoparticle formulations.
Peng Zou; Lawrence Helson; Anirban Maitra; Stephan T Stern; Scott E McNeil
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural     Date:  2013-04-22
Journal Detail:
Title:  Molecular pharmaceutics     Volume:  10     ISSN:  1543-8392     ISO Abbreviation:  Mol. Pharm.     Publication Date:  2013 May 
Date Detail:
Created Date:  2013-05-06     Completed Date:  2013-12-16     Revised Date:  2014-05-08    
Medline Journal Info:
Nlm Unique ID:  101197791     Medline TA:  Mol Pharm     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1977-87     Citation Subset:  IM    
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MeSH Terms
Antineoplastic Agents / administration & dosage,  chemistry,  pharmacokinetics
Bile / metabolism
Bile Ducts
Chemistry, Pharmaceutical
Curcumin / administration & dosage,  chemistry,  pharmacokinetics*
Delayed-Action Preparations
Drug Delivery Systems
Drug Stability
Injections, Intravenous
Nanocapsules / chemistry
Polymers / administration & dosage,  chemistry,  pharmacokinetics
Rats, Sprague-Dawley
Grant Support
261200800001E//PHS HHS; Z99 CA999999/CA/NCI NIH HHS
Reg. No./Substance:
0/Antineoplastic Agents; 0/Delayed-Action Preparations; 0/Nanocapsules; 0/Polymers; IT942ZTH98/Curcumin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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