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The present application relates to the field of pharmaceutical preparation and nanomedicine, and particularly relates to a kind of nano-drug composition, its combined drug delivery system and application.The nano-drug composition comprises alpha 1-AR blocker and amphiphilic nano-carrier;The alpha 1-AR blocker is loaded in the hydrophobic core formed by amphiphilic nano-carrier;The alpha 1-AR blocker is selected from one or more of prazosin, terazosin, doxazosin;The average particle size of the nano-drug composition is 220-260 nm, the polydispersity index is less than 0.3, and the encapsulation efficiency is greater than 50%.The nano-drug composition of the present application has dual functions of anti-tumor proliferation and immune microenvironment remodeling, improves the dispersion stability of the drug in physiological medium, effectively reduces the in vivo clearance rate, prolongs the circulation time, and realizes the efficient in vivo delivery of the drug.The preparation process of the nano-preparation is stable and can be produced on a large scale.