The　in-depth　intersection　between　nanoscience　and　oncology　comes　from　the　fact　that　nanomaterials　are　in　a　similar　dimension　to　basic　biomolecules.　Drug　delivery　systems　(DDSs),　which　are　either　targeted　to　a　particular　site　or　intended　for　the　controlled　release　in　a　particular　position,　have　been　studied　extensively　at　the　nanoscale　and　are,　by　far,　the　most　advanced　technology　in　the　area　of　nanoparticle　applications.　This,　consequently　lead　to　the　improvement　and　development　of　convenient　administration　routes,　lower　toxicity,　fewer　side　effects,　and　extended　drug　life　cycle.　Carbon　nanomaterials　(CNMs)　with　favorable　size　and　unique　fluorescence　properties,　which　was　considered　an　ideal　candidate　to　transport　or　deliver　therapeutic　drugs　to　specific　targets　in　a　controlled　manner.　The　development　of　DDSs　based　on　them　constitutes　an　interesting　topic　in　highly　effective　and　universal　therapies　to　achieve　better　therapeutic　outcomes　and　reduce　the　side　effects　of　malignancies.　In　this　review,　the　cutting-edge　progress　of　CNMs　in　DDSs　was　comprehensively　summarized.　Additionally,　the　emphasis　was　placed　on　the　applications　of　CNMs　including　fullerene,　graphene,　carbon　nanotubes　(CNTs),　carbon　dots　(CDs),　and　nano-diamonds　(NDs)　in　drug　delivering.　Further,　we　gave　some　insights　into　the　future　direction　and　foreseeable　challenges　of　DDSs　based　on　CNMs　used　in　cancer　therapy,　which　we　hope　these　inspirations　in　DDSs　associated　with　anti-cancer　therapy　will　provide　perspectives　in　designing　new　drugs　for　further　tumor　treatment.