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Preparation and characterization of water-soluble albumin-bound curcumin nanoparticles with improved antitumor activity.

Abstract：

:Curcumin (CCM), a yellow natural polyphenol extracted from turmeric (Curcuma longa), has potent anti-cancer properties as has been demonstrated in various human cancer cells. However, the widespread clinical application of this efficient agent in cancer and other diseases has been limited by its poor aqueous solubility and bioavailability. In this study, we prepared novel CCM-loaded human serum albumin (HSA) nanoparticles (CCM-HSA-NPs) for intravenous administration using albumin bound technology. Field emission scanning electron microscopy (FE-SEM) and dynamic light scattering (DLS) investigation confirmed a narrow size distribution in the 130-150nm range. Furthermore, CCM-HSA-NPs showed much greater water solubility (300-fold) than free CCM, and on storage, the biological activity of CCM-HSA-NPs was preserved with negligible activity loss. In vivo distributions and vascular endothelial cells transport studies demonstrated the superiority of CCM-HSA-NPs over CCM. Amounts of CCM in tumors after treatment with CCM-HSA-NPs were about 14 times higher at 1h after injection than that achieved by CCM. Furthermore, vascular endothelial cell binding of CCM increased 5.5-fold, and transport of CCM across a vascular endothelial cell monolayer by Transwell testing was 7.7-fold greater for CCM-HSA-NPs than CCM. Finally, in vivo antitumor tests revealed that CCM-HSA-NPs (10 or 20mg/kg) had a greater therapeutic effect (50% or 66% tumor growth inhibition vs. PBS-treated controls) than CCM (18% inhibition vs. controls) in tumor xenograft HCT116 models without inducing toxicity. We attribute this potent antitumor activity of CCM-HSA-NPs to enhanced water solubility, increased accumulation in tumors, and an ability to traverse vascular endothelial cell.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Kim TH,Jiang HH,Youn YS,Park CW,Tak KK,Lee S,Kim H,Jon S,Chen X,Lee KC

doi

10.1016/j.ijpharm.2010.10.041

subject

Has Abstract

pub_date

2011-01-17 00:00:00

pages

285-91

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(10)00816-1

journal_volume

403

pub_type

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Preparation and characterization of water-soluble albumin-bound curcumin nanoparticles with improved antitumor activity.