Background: The use of chemotherapeutic drugs is restricted in the
tumor-
therapy because of the severely toxic and side effects among most important factors. The active herbal extracts are always used as a high dose while in the tumortherapy to achieve good anti-
tumor effects. Hydrous
icaritin has a high activity while there are few existing
dosage forms as a result of low solubility in water and poor bioavailability. Results: The prepared hydrous
icaritin nanorods (DP-HICT NRs) using mPEG2000-DSPE as a stabilizer, presented a narrow distribution of particle size with of 217 nm and a properly high
drug-loading content of approximately 65.3±1.5%. A low dose of hydrous
icaritin nano-formulation shows remarkable efficacy in
cancer therapy (
tumor inhibition rate: 61.36±10.80%) compared with the same dose of
Paclitaxel injection (
tumor inhibition rate: 66.80±4.43%), which approved as medicaments. Not only that, DP-HICT NRs can escape the clearance of the immune system and enhance targeting ability to the
tumor site with only one
excipient and such a low dose. Conclusions: This kind of nanoparticles contain a low dose of HICT used mPEG2000-DSPE as a stabilizer, while can achieve good
tumor targeting as some active targeting agents and an anti-
tumor effect as the PTX injection. There are broad prospects in
drug safety, anti-
tumor efficacy and even prognosis.