Lipophilic starch derivatives offer several advantages, such as low costs, biocompatibility, and biodegradability, compared to synthetic polymers. We are especially interested in the design of polymeric excipients for the controlled delivery of drugs sparingly soluble in water. Lipophilic propyl-, butyl- and hexyl-starches were synthesized by reaction of native starches with alkylbromides in DMSO solution. The degrees of substitution (1 - 2.75) could be controlled by the reaction conditions. Products were purified by eco-friendly nanofiltration processes. Stable nanoparticles with high loads of various drugs (flufenamic acid, testosterone, caffeine) were obtained by the emulsion-evaporation technique. Particle sizes ranged between 150 and 250 nm. Since these particles showed release profiles without burst effect, they are very interesting candidates for the targeted administration of cytostatic drugs (e.g. idarubicine) for the treatment of cancer. Ex vivo and in vivo tests are in progress. Targeting is aimed by cellspecific ligands as it is pyrofolic acid and derivatives thereof.