In vitro evaluation on novel modified chitosan for targeted antitumor drug delivery

► Synthesis and characterization of novel amphiphilic chitosan derivates as drug delivery system. ► Introduction of phthalyl groups could lower CMC and improve solubility in aqueous and organic system. ► Drug-loaded micelles with small particle size, narrow distribution and high drug loading efficiency. ► Enhancement on cellular uptake by active tumor targeting. ► Mechanism of cellular uptake varied from different surface properties.