摘要： Boron neutron capture therapy (BNCT) induces high-energy radiation within cancer cells while avoiding damage to normal cells that without uptake of BNCT drugs, which is holding great promise to provide excellent control over locally invasive malignant tumors. However, lack of quantitative imaging technique to determine local boron concentration has been a great challenge for nuclear physicians to apply accurate neutron irradiation during the treatment, which is a key factor that has limited BNCT’s application in clinics. To meet this challenge, this study describes coating boronated porphyrins with a biocompatible Poly(lactide–co-glycolide)–monomethoxy-poly(polyethylene-glycol) (PLGA-mPEG) micelle for selective tumor accumulation and reduced toxicity comparing with previously reported boronated porphyrin drugs. Fluorescence imaging and PET imaging were performed, unveiling the potential imaging properties of this boronated porphyrin nanocomplex (BPN) to locate tumor region and to determine tissue-localized boron concentration which facilitates treatment planning. By studying the pharmacokinetics of BPN with Cu-64 PET imaging, the treatment plan was adjusted from single bolus injection to multiple times of injections of smaller doses. As expected, high tumor uptake of boron (125.17±13.54 ppm) was achieved with an extraordinarily high tumor to normal tissue ratio: tumor to liver, muscle, fat and blood were 3.24±0.22, 61.46±20.26, 31.55±10.30 and 33.85±5.73, respectively. At last, neutron irradiation with BPN showed almost complete tumor suppression, demonstrating that BPN holds a great potential for being an efficient boron delivery agent for imaging-guided BNCT.