The invention belongs to the technical fields of preparation and applications of nano-carriers, and in particular discloses a preparation method and an application of a multifunctional membrane-controlled targeting nano-carrier integrating tracing and targeted drug delivery effects. With nano mesoporous silica (MSN) as a drug 'warehouse', a positively charged high molecular material and a negatively charged high molecular material as preparation materials of a gating membrane, and adriamycin (DOX), cis-platinum, imatinib, taxol and the like as model anti-cancer drugs, research contents mainlyinclude optimization and improvement of natural materials, construction and process optimization of the gating membrane, structural characterization of a nano complex, drug release kinetic characteristics of drug molecules under the control of the gating membrane, and the like. Meanwhile, in the combination with the tracing imaging function of a fluorescent quantum dot, drug delivery behaviors andanti-tumor effectiveness of the membrane-controlled nano drug delivery system undergo preliminary evaluation through in-vitro experiments. Based upon research results, references are provided for thedesign and preparation of the novel membrane-controlled nano drug delivery system.