Ursolic　acid　(UA),　a　natural　triterpene　acid,　is　a　promising　anti-cancer　drug　due　to　its　inhibitory　effect　on　tumor　growth　and　metastasis.　However,　clinical　translation　of　UA　is　limited　by　its　poor　water　solubility　and　low　bioavailability.　To　overcome　these　problems,　herein　an　amphiphilic　self-assembly　nanodrug　composed　of　UA,　lactobionic　acid　(LA)　and　low-polyamidoamine　(low-PAMAM)　dendrimers　is　developed.　This　near-spherical　nanodrug　with　a　uniform　size　(~180　nm)　demonstrated　to　have　an　enhanced　cytotoxicity　against　liver　cancer　SMMC7721　cells,　and　could　attenuate　the　migration　and　adhesion　of　SMMC7721　cells　at　non-toxic　concentrations　by　suppressing　metastasis-related　protein　MMP-9　expression.　Furthermore,　in　vivo　study　indicates　that　the　nanodrug　exhibited　prolonged　circulation　time　in　blood　as　well　as　increased　AUC,　MRT　and　Cmax,　and　could　effectively　inhibit　the　tumor　growth　in　H22　mice　model.　Overall,　the　UA-based　nanodrug　delivery　system　reported　in　the　present　work　represents　a　novel　strategy　for　targeted　tumor　therapy.　©　2017　Elsevier　Inc.