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Issue 4, 2011
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Curcumin-loaded biodegradable polymeric micelles for colon cancer therapy in vitro and in vivo

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Abstract

Curcumin is an effective and safe anticancer agent, but its hydrophobicity inhibits its clinical application. Nanotechnology provides an effective method to improve the water solubility of hydrophobic drug. In this work, curcumin was encapsulated into monomethoxy poly(ethylene glycol)-poly(ε-caprolactone) (MPEG-PCL) micelles through a single-step nano-precipitation method, creating curcumin-loaded MPEG-PCL (Cur/MPEG-PCL) micelles. These Cur/MPEG-PCL micelles were monodisperse (PDI = 0.097 ± 0.011) with a mean particle size of 27.3 ± 1.3 nm, good re-solubility after freeze-drying, an encapsulation efficiency of 99.16 ± 1.02%, and drug loading of 12.95 ± 0.15%. Moreover, these micelles were prepared by a simple and reproducible procedure, making them potentially suitable for scale-up. Curcumin was molecularly dispersed in the PCL core of MPEG-PCL micelles, and could be slow-released in vitro. Encapsulation of curcumin in MPEG-PCL micelles improved the t1/2 and AUC of curcuminin vivo. As well as free curcumin, Cur/MPEG-PCL micelles efficiently inhibited the angiogenesis on transgenic zebrafish model. In an alginate-encapsulated cancer cell assay, intravenous application of Cur/MPEG-PCL micelles more efficiently inhibited the tumor cell-induced angiogenesisin vivo than that of free curcumin. MPEG-PCL micelle-encapsulated curcumin maintained the cytotoxicity of curcumin on C-26 colon carcinoma cellsin vitro. Intravenous application of Cur/MPEG-PCL micelle (25 mg kg−1curcumin) inhibited the growth of subcutaneous C-26 colon carcinoma in vivo (p < 0.01), and induced a stronger anticancer effect than that of free curcumin (p < 0.05). In conclusion, Cur/MPEG-PCL micelles are an excellent intravenously injectable aqueous formulation of curcumin; this formulation can inhibit the growth of colon carcinoma through inhibiting angiogenesis and directly killing cancer cells.

Graphical abstract: Curcumin-loaded biodegradable polymeric micelles for colon cancer therapy in vitro and in vivo

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Publication details

The article was received on 12 Oct 2010, accepted on 28 Nov 2010 and first published on 31 Jan 2011


Article type: Paper
DOI: 10.1039/C0NR00758G
Citation: Nanoscale, 2011,3, 1558-1567
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    Curcumin-loaded biodegradable polymeric micelles for colon cancer therapy in vitro and in vivo

    M. Gou, K. Men, H. Shi, M. Xiang, J. Zhang, J. Song, J. Long, Y. Wan, F. Luo, X. Zhao and Z. Qian, Nanoscale, 2011, 3, 1558
    DOI: 10.1039/C0NR00758G

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