A saponin nano micelle, preparing method, application and pharmaceutical composition thereof is disclosed in the present invention. The saponin nano micelle comprises one or more of saponins represented by formula 1, in which, R1 and R2 are independently —H or a hydrophilic group, R3 is —H or —OH, R4 is a lipophilic group. The preparing method of the saponin nano micelle is that mixing the saponin with an organic solvent which can dissolve saponin, and then removing the organic solvent. The saponin micelle acts as a convey medium of the drug ingredients, and can replace conventional drug carriers such as pharmaceutical solubilizers or polymeric micelle, which has high safety and great significance. The pharmaceutical ingredients can prolong circulation time and biological half-life of drug in the blood, and increase the accumulation of drug in lesions, and reduce adverse reactions.
