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&NA; Theranostic polymeric NPs developed for both cancer diagnosis and cancer therapy. This multifunctional polymeric vehicle was prepared by a single emulsion evaporation method, using carboxyl‐terminated PLGA. LHRH as a targeting moiety, was conjugated to the surface of polymeric carrier by applying polyethylene glycol. The results indicated that the diameter of NPs was ˜ 185.4 ± 4.6 nm as defined by DLS. The entrapment efficacy of docetaxel, silibinin, and SPIONs was 84.6 ± 4.1%, 80.6 ± 2.7%, and 77.9 ± 4.3%, respectively. The NPs showed a triphasic in‐vitro drug release pattern. MTT assay was done on two cell lines, MCF‐7 and SKOV‐3. Enhanced cellular uptake ability of the targeted NPs to MCF‐7 was evaluated in‐vitro by confocal laser scanning microscopy. The results indicated that compared to non‐targeted NPs, the LHRH targeted NPs had significant efficacy at IC50 concentration. The effect of the NPs on VEGF expression in MCF‐7 and SKOV‐3 cells was investigated by Real‐Time PCR method. VEGF mRNA level expression in MCF‐7 cell line reduced by 83% in comparison to control cell line. The designed NPs can be used as promising multifunctional platform for detection and targeted drug delivery in breast cancer. Graphical abstract Figure. No caption available.