The application of chitosan-based surfactants in biomedicine and daily chemicals are progressively increasing for their feature of non-toxic and biodegradable. The micelles formed by amphiphilic modified chitosan can solubilize water-insoluble drugs, slow the drug release, reduce the cytotoxicity and improve the bioavailability of drugs. This paper reviews the researches on the surface activity of chitosan derivatives and their application in drug solubilization and drug carrier. The recent studies on coupling, alkylation, acylation, carboxymethyl-based, quaternary ammonium derivatives of chitosan, and on the drug solubilization of paclitaxel, camptothecin, doxorubicin and methyl-amino folic acid by chitosan-based surfactants are introduced in detail. In the new method of modified chitosan, two ways are worth to notice. The first is to use hydrophobic interactions to constitute the self-assembly system, the second is to introduce the functional groups to form the intelligent drug-loaded micelles.