The　purpose　of　the　current　study　was　to　construct　a　β-cyclodextrin　drug　carrier　for　rubropunctatin　to　improve　its　water　solubility　and　light　stability　for　future　cytotoxicity　studies.　The　inclusion　complexation　behavior　of　rubropunctatin　with　β-cyclodextrin　was　investigated　using　FESEM,　FT-IR　and　XRD.　A　molecular　docking　study　was　performed　to　elucidate　the　most　probable　inclusion　structure.　The　inclusion　complex　could　be　completely　dispersed　in　water　and　had　a　small　size　of　121.87　±　2.13　nm　(n　=　3),　a　good　PDI　(0.320　±　0.017),　and　an　acceptable　potential　value　of　−27.7　±　0.32　mV　(n　=　3).　Furthermore,　the　stability　of　the　rubropunctatin　in　water　under　light　irradiation　was　found　to　be　greatly　enhanced　after　being　encapsulated　in　cyclodextrin,　and　it　exhibited　a　retention　rate　of　over　70%　vs.　10.17%.　In　addition,　the　cytotoxicity　of　the　inclusion　complex　was　evaluated　by　MTT　assay　and　Annexin　V-FITC/PI　detection　using　cervical　adenocarcinoma　HeLa　cells.　The　results　showed　that　the　inclusion　complex　had　comparable　toxicity　compared　to　rubropunctatin　solubilized　with　0.4%　DMSO.　More　importantly,　the　formation　of　the　inclusion　complex　contributed　greatly　to　the　intensification　of　the　bioavailability　of　rubropunctatin　because　the　use　of　organic　solvent　was　avoided.　©　The　Royal　Society　of　Chemistry.