Self-assembled nanoparticles have reached a growing interest for the improvement ofcancer diseases and associated inflammation processes. This article describes the mostrepresentative types of self-assembling nanosystems, including a detailed review ofdifferent methodologies for their preparation. Nanoparticles are commonly formed by self-assembling of amphiphilic polymers in aqueous environment. For that reason, the mainstrategies for the design of amphiphilic polymeric systems are also reviewed, with anemphasis on the different polymerization techniques of synthetic monomers and severalstrategies of chemical modification of polysaccharides and proteins. Additionally, mostadvanced applications of self-assembled nanocarriers for the improvement of treatmentof cancer and inflammation diseases are also discussed, focusing on the description ofdrug-loaded and drug-conjugated systems, active targeted strategies and most recentlypossibilities for the multimodality treatment of cancer diseases. ; Financial support from CIBER-BBN/ECO (NANOVIT) is appreciated. ; Peer reviewed