¹³¹I‐Labeled Multifunctional Polyphosphazene Nanospheres for SPECT Imaging‐Guided Radiotherapy of Tumors

Abstract

Design of theranostic nanoplatforms represents a major topic for current nanomedicine. Here, the preparation of multifunctional poly(cyclotriphosphazene‐co‐polyethylenimine) nanospheres (PNSs) labeled with radionuclide 131I for single photon emission computed tomography (SPECT) imaging‐guided radiotherapy of tumors is reported. In this work, PNSs are prepared using hexachlorocyclotriphosphazene as a crosslinker to crosslink branched polyethylenimine (PEI) via a nucleophilic substitution reaction, modified with 3‐(4′‐hydroxyphenyl) propionic acid‐OSu (HPAO) for 131I labeling, and reacted with 1,3‐propane sulfonate (1,3‐PS) to render the particles with antifouling property, followed by acetylation of the remaining surface amines and labeling with 131I. The acquired PNS.NHAc‐HPAO(131I)‐PS particles are well characterized. It is shown that the multifunctional PNSs with an average size of 184 ± 29.3 nm exhibit favorable antifouling properties, high 131I labeling efficiency (76.05 ± 3.75%), and excellent radiostability and colloidal stability. With these properties owned, the developed PNS.NHAc‐HPAO(131I)‐PS spheres enable much more efficient SPECT imaging and radiotherapy of a xenografted tumor model in vivo than the PEI counterpart material (PEI.NHAc‐HPAO(131I)‐PS). The developed PNSs may be used as a versatile platform for further development of different forms of nanomedicine for various biomedical applications.

Antifouling Strategies of Nanoparticles for Diagnostic and Therapeutic Application: A Systematic Review of the Literature

“…These nanoplatforms, further modified with RGD peptide, displayed a high relaxivity, cytocompatibility, targeting specificity to cancer cells, and allowed dual-mode imaging of metastatic lung cancer in vivo model. 1,3-PS was also used to provide antifouling property to multifunctional poly(cyclotriphosphazene-co-polyethylenimine) nanospheres (PNSs), labelled with radionuclide 131 I, and realized for single-photon emission computed tomography (SPECT) imaging-guided radiotherapy of tumors [ 29 ]. Multifunctional PNSs with an average diameter of 184 nm exhibited cell viability above 81.7 ± 2.21% in the assessed range of concentration (0–100 µM/mL), colloidal stability, and high 131 I labelling efficiency (76.05 ± 3.75%).…”

Polyethyleneimine-Based Drug Delivery Systems for Cancer Theranostics

“…To overcome these disadvantages, labeling radionuclides on a PEI-based nanoplatform can effectively enhance their imaging performance. As an example, Zhu et al constructed multifunctional poly (cyclotriphosphazene-co-PEI) nanospheres (PNSs) labeled with radionuclide 131 I through 3-(4′-hydroxyphenyl) propionic acid-OSu for SPECT imaging of tumors [ 196 ]. The PNSs displayed a high 131 I label efficiency of up to 76.05 % and a favorable colloidal/radio stability.…”

Preparation of Single, Heteromorphic Microspheres, and Their Progress for Medical Applications

“…Compared with the traditional way of injection, microsphere has the advantages of poor invasiveness and good repeatability. [ 83 ] The treatment of diabetes often uses subcutaneous injection of insulin, as a result, frequent injection causes serious damage to the skin and blood vessels of patients. [ 84 ] For this question, Lin et al.…”