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.
Rights & PermissionsPrintExport