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

Tae Hyung Kim, Hai Hua Jiang, Yu Seok Youn, Chan Woong Park, Kyung Kook Tak, Seulki Lee, Hyungjun Kim, Sangyong Jon, Xiaoyuan Chen, Kang Choon Lee

Research output: Contribution to journalArticle

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 130-150 nm 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 1 h 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 20 mg/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.

Original languageEnglish (US)
Pages (from-to)285-291
Number of pages7
JournalInternational Journal of Pharmaceutics
Volume403
Issue number1-2
DOIs
StatePublished - Jan 17 2011
Externally publishedYes

Fingerprint

Curcumin
Nanoparticles
Albumins
Water
Serum Albumin
Endothelial Cells
Neoplasms
Solubility
Curcuma
Human Activities
Polyphenols
Therapeutic Uses

Keywords

  • Antitumor
  • Curcumin
  • Human serum albumin
  • Nanoparticle
  • Solubility

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Preparation and characterization of water-soluble albumin-bound curcumin nanoparticles with improved antitumor activity. / Kim, Tae Hyung; Jiang, Hai Hua; Youn, Yu Seok; Park, Chan Woong; Tak, Kyung Kook; Lee, Seulki; Kim, Hyungjun; Jon, Sangyong; Chen, Xiaoyuan; Lee, Kang Choon.

In: International Journal of Pharmaceutics, Vol. 403, No. 1-2, 17.01.2011, p. 285-291.

Research output: Contribution to journalArticle

Kim, Tae Hyung ; Jiang, Hai Hua ; Youn, Yu Seok ; Park, Chan Woong ; Tak, Kyung Kook ; Lee, Seulki ; Kim, Hyungjun ; Jon, Sangyong ; Chen, Xiaoyuan ; Lee, Kang Choon. / Preparation and characterization of water-soluble albumin-bound curcumin nanoparticles with improved antitumor activity. In: International Journal of Pharmaceutics. 2011 ; Vol. 403, No. 1-2. pp. 285-291.
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AU - Jiang, Hai Hua

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AU - Tak, Kyung Kook

AU - Lee, Seulki

AU - Kim, Hyungjun

AU - Jon, Sangyong

AU - Chen, Xiaoyuan

AU - Lee, Kang Choon

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AB - 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 130-150 nm 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 1 h 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 20 mg/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.

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