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In vitro characterization and in vivo evaluation of nanostructured lipid curcumin carriers for intragastric administration
Journal article   Open access   Peer reviewed

In vitro characterization and in vivo evaluation of nanostructured lipid curcumin carriers for intragastric administration

Min Fang, Yilin Jin, Wei Bao, Hui Gao, Mengjin Xu, Di Wang, Xia Wang, Ping Yao and Liegang Liu
International journal of nanomedicine, Vol.7, pp.5395-5404
2012
DOI: 10.2147/IJN.S36257
PMCID: PMC3471604
PMID: 23091382
url
https://doi.org/10.2147/IJN.S36257View
Published (Version of record) Open Access

Abstract

Curcumin has a variety of pharmacological effects. However, poor water solubility and low oral bioavailability limit its clinical utility. A delivery system for nanostructured lipid carriers has been reported to be a promising approach to enhancing the oral absorption of curcumin. The aim of the present study was to investigate the pharmacokinetics, tissue distribution, and relative bioavailability of curcumin in rats after a single intragastric dose of a nanostructured lipid curcumin carrier formulation. Nanostructured lipid curcumin carriers were prepared using the ethanol dripping method and characterized in terms of the particle size, polydispersity index, zeta potential, differential scanning calorimetry, drug-loading capacity, encapsulation efficiency, and in vitro release. The pharmacokinetics and tissue distribution of nanostructured lipid curcumin carriers and curcumin suspension were compared after intragastric administration. Nanostructured lipid curcumin carriers showed a significantly higher peak plasma concentration (564.94 ± 14.98 ng/mL versus 279.43 ± 7.21 ng/mL, P < 0.01), a shorter time taken to reach peak plasma concentration (0.5 ± 0.01 hour versus 1.0 ± 0.12 hour, P < 0.01), and a greater AUC(0-∞) (820.36 ± 25.11 mg × hour/L versus 344.11 ± 10.01 mg × hour/L, P < 0.05) compared with curcumin suspension. In the tissue distribution studies, curcumin could be detected in the spleen, heart, liver, kidneys, lungs, and brain. Following intragastric administration of the nanostructured lipid curcumin carrier formulation, tissue concentrations of curcumin also increased, especially in the brain. The nanostructured lipid curcumin carrier formulation improved the ability of curcumin to cross the blood-brain barrier, with an 11.93-fold increase in the area under the curve achieved in the brain when compared with curcumin suspension. The nanostructured lipid carrier formulation significantly improved the oral bioavailability of curcumin and represents a promising method for its oral delivery.
Administration, Oral Curcumin - chemistry Curcumin - pharmacokinetics Rats Metabolic Clearance Rate Curcumin - administration & dosage Organ Specificity Nanocapsules - chemistry Rats, Sprague-Dawley Nanocapsules - ultrastructure Tissue Distribution Lipids - chemistry Animals Diffusion

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