Rubropunctatin,　a　metabolite　isolated　from　the　fungi　of　the　genus　Monascus,　is　a　natural　lead　compound　applied　for　the　suppression　of　tumors　with　good　anti-cancer　activity.　However,　its　poor　aqueous　solubility　has　limited　its　further　clinical　development　and　utilization.　Lecithin　and　chitosan　are　excellently　biocompatible　and　biodegradable　natural　materials,　which　have　been　approved　by　the　FDA　as　drug　carrier.　Here,　we　report　for　the　first　time　the　construction　of　a　lecithin/chitosan　nanoparticle　drug　carrier　of　the　Monascus　pigment　rubropunctatin　by　electrostatic　self-assembly　between　lecithin　and　chitosan.　The　nanoparticles　are　near-spherical　with　a　size　110–120　nm.　They　are　soluble　in　water　and　possess　excellent　homogenization　capacity　and　dispersibility.　Our　in　vitro　drug　release　assay　showed　a　sustained　release　of　rubropunctatin.　CCK-8　assays　revealed　that　lecithin/chitosan　nanoparticles　loaded　with　rubropunctatin　(RCP-NPs)　had　significantly　enhanced　cytotoxicity　against　mouse　mammary　cancer　4T1　cells.　The　flow　cytometry　results　revealed　that　RCP-NPs　significantly　boosted　cellular　uptake　and　apoptosis.　The　tumor-bearing　mice　models　we　developed　indicated　that　RCP-NPs　effectively　inhibited　tumor　growth.　Our　present　findings　suggest　that　lecithin/chitosan　nanoparticle　drug　carriers　improve　the　anti-tumor　effect　of　the　Monascus　pigment　rubropunctatin.　©　2023　Elsevier　B.V.