Biodegradable conjugate of TPGS–FOL was successfully synthesized by click reaction.
The MTX-conjugated nanoparticles could be decorated by TPGS–FOL.
10% MTX-conjugated nanoparticles possessed better carrier properties than 20% MTX.
The nanoparticles could potentiate the toxicity of MTX to cancer cells.
TPGS–FOL decorated nanoparticles enhanced toxicity and cellular uptake efficiency.