Nanoformulations　with　advantages　in　drug　delivery,　safety　and　pharmacodynamics　have　been　booming　as　a　promising　strategy　for　cancer　therapy.　However,　the　traditional　nanocarrier　still　suffers　from　the　low　drug　loading　capacity,　potential　systematic　toxicity,　unclear　metabolism,　and　other　uncertainties.　To　overcome　these　issues,　carrier-free　nanodrugs　with　desirable　bioactivity　were　developed　rapidly　and　drawn　considerable　attention.　Meanwhile,　the　multifunctional　self-delivery　nanoarcheticture　fabricated　by　a　simple　and　＂green＂　method,　has　significant　advantages　in　synergistic　cancer　therapy　and　inhibition　of　multidrug　resistant　(MDR).　Till　now,　carrier-free　nanoparticles　for　tumor　theranostics,　phototherapy,　chemotherapy,　diagnose　and　synergistic　therapy,　have　made　outstanding　progress.　In　this　review,　we　make　an　integrated　and　exhaustive　overview　of　lately　reports　on　carrier-free　nanodrug　delivery　systems　formed　by　several　active　agents.　We　summarize　the　self-assembly　and　modified　strategies,　with　emphasis　on　application　superiority　of　carrier-free　nanocrystal,　and　give　new　insight　into　the　establishment　of　ideal　nanosystems　for　cancer　treatment.