In Vivo Anticancer Activity of Methotrexate-loaded Layered Double Hydroxide Nanoparticles

Author(s): Soo-Jin Choi, Jae-Min Oh, Hae-Eun Chung, Seung-Hee Hong, In-Hoo Kim, Jin-Ho Choy

Journal Name: Current Pharmaceutical Design

Volume 19 , Issue 41 , 2013

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A methotrexate (MTX)-loaded layered double hydroxide (LDH) nanoparticle system was synthesized by intercalating MTX into the interlayer spaces of LDH. In vivo pharmacokinetic study demonstrated that the MTX-LDH hybrid had similar kinetic behaviors as free MTX, showing a rapid decline in the plasma MTX level, with characteristics of a biexponential function. However, the hybrid system remarkably suppressed tumor growth in human osteosarcoma-bearing mice compared to an equivalent amount of free MTX. Using MTX-LDH nanoparticles, a significantly high amount of MTX was delivered to target tumor tissue, whereas a low level was found in normal tissues. Moreover, LDH nanocarriers did not accumulate in any specific tissue nor cause acute toxicity up to the applied dose for the hybrid system. These results suggest that the MTX-LDH nanohybrid system has great potential as an anti-cancer drug with enhanced in vivo anti-tumor activity and bioavailability in target tumor tissue along with reduced side effects.

Keywords: layered double hydroxide, methotrexate, anti-tumor activity, pharmacokinetics, toxicity.

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Article Details

Year: 2013
Page: [7196 - 7202]
Pages: 7
DOI: 10.2174/138161281941131219123718
Price: $65

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