The invention discloses mesoporous carbon nanoparticles modified by macromolecules and the application thereof in preparation of drug carriers. The macromolecules refer to PVP (Polyvinyl Pyrrolidone)or DSPE-mPEG2000. According to the invention, the well aligned mesoporous carbon nanoparticles are synthetized through a low-concentration hydrothermal method, the macromolecule with biocompatibilityis used for modification through strong absorption of the mesoporous carbon nanoparticles, so that the hydrophilia and the dispersibility of the mesoporous carbon nanoparticles are improved. Through aseries of representations and cellular uptake experiments, the following conclusions are drawn: the synthetic well aligned mesoporous carbon nanoparticles are about 90 nm in diameter, uniform in nanoparticles and well aligned in mesoporous passages. PVP (Polyvinyl Pyrrolidone) and DSPE-mPEG2000 are successfully used for modification onto the surfaces of mesoporous carbon nanoparticles, so that the hydrophilia and the dispersibility of the mesoporous carbon nanoparticles are improved, the mesoporous carbon nanoparticles can be taken in by normal cells and cancer cells within 2 hours, to assemble on cytoplasm. The mesoporous carbon nanoparticles provided by the invention can be used as excellent drug carriers, and can be targeted at tumor tissues through an EPR (enhanced permeability and retention) effect.