Disclosed is a water-soluble vitamin E derivative modified fat-soluble anti-cancer drug compound, having a structure as represented by formula I or II. The active ingredients of the anti-cancer drug, camptothecin or a camptothecin derivative, are covalently bound with lipophilic partially water-soluble vitamin E ester or amide by a linking group to form the fat-soluble anti-cancer drug compound. Also disclosed are a formulation, preparation method and use of the drug compound.
