Emerging tumor treatment demands high sensitivity and high-spatial resolution diagnosis in combination with targeted therapy. Here, we report that iodine-rich polymersomes (I-PS) enable versatile single-photon emission computed tomography (SPECT)/computed tomography (CT) dual-modal imaging and potent radioisotope therapy for breast cancer in vivo. Interestingly, I-PS could be easily and stably labeled with radioiodine, 125I and 131I. Dynamic light scattering and transmission electron microscopy showed that 125I-PS had a size of 106 nm and vesicular morphology, similar to those of the parent I-PS. Methyl thiazolyl tetrazolium assays displayed that I-PS and 125I-PS were noncytotoxic, whereas 131I-PS caused significant death of 4T1 cells at 5 mg PS/mL with a radioactivity of 12 μCi. Pharmacokinetic and biodistribution studies showed that 125I-PS has a prolonged circulation and distributes mainly in tumor and the reticuloendothelial system. The intravenous injection of 125I-PS to 4T1 murine breast tumor-bearing mice allowed simultaneous high sensitivity and high-spatial resolution imaging of tumor by SPECT and CT, respectively. The therapeutic studies revealed that 131I-PS could effectively retard the growth of 4T1 breast tumor and significantly prolong mice survival time. The hematoxylin and eosin staining assay proved that 131I-PS induced tumor cell death. I-PS emerges as a robust and versatile platform for dual-modal imaging and targeted radioisotope therapy.
Keywords: SPECT/CT; contrast agents; polymersomes; radioisotope; theranostics.