This article mainly introduced novel carrier-modified methods for active targeting antitumor preparation as well as their evaluation methodology in recent years.By reviewing related domestic and overseas literatures,the up-to-date scientific researches concerning active targeting antitumor preparation were elaborated and the problems existing in present studies were discussed.Numerous valid vectorembellished methods had been discovered with excellent targeting effects,and the significant progress was acquired for the evaluation tools in vitro and in vivo.The active targeting agent would be a major direction in prospective tumor or cancer therapeutic regimen. This article was originally introduced novel carrier-modified methods for active targeting antitumor preparation as well as their evaluation methodology in recent years. By reviewing related domestic and overseas literatures, the up-to-date scientific researches concerning active targeting antitumor preparation were elaborated and the problems existing in present studies were discussed. Numerous valid vectorembellished methods had been discovered with excellent targeting effects, and the significant progress was acquired for the evaluation tools in vitro and in vivo. The active targeting agent would be major direction in prospective tumor or cancer therapeutic regimen.