Phenylboronic acid conjugated multifunctional nanogels with 131I-labeling for targeted SPECT imaging and radiotherapy of breast adenocarcinoma

Abstract

We report a new 131I-labeling functional platform for targeted single-photon emission computed tomography (SPECT) imaging and radiotherapy of breast adenocarcinoma. In this study, polyethyleneimine (PEI) based nanogels (P.NH2 NGs) were prepared by water/oil polymerization, modified with targeted agent phenylboronic acid (PBA), and labeled with radionuclide 131I. The NGs without 131I-labeling own a spherical structure, uniform size distribution, and good cell viability. After 131I-labeling, the obtained 131I-PBA-PHP NGs displayed much higher cellular uptake than the non-targeted NGs due to the good softness and fluidity of NGs and the PBA targeting. The in vivo results demonstrated that 131I-PBA-PHP NGs could specifically target breast cancer cells and efficiently aggregate into xenograft breast adenocarcinoma for tumor SPECT imaging and specific radiotherapy. The developed 131I-labeling NGs may be used as a promising platform for efficient radioactive theranostic nanoplatform of tumor.

Theranostic nanogels: multifunctional agents for simultaneous therapeutic delivery and diagnostic imaging

“…140 Despite the myriad nanogel systems in conjunction with PET/SPECT imaging, 141–143 studies involving theranostic nanogels remain scarce (Table 3). 144,145 A noteworthy example of radiolabeling nanogels was reported by Soni et al 146 In their study, N , N -methylene bisacrylamide (MBA) was employed to crosslink N -isopropyl acrylamide (NIPAAM) and N -vinylpyrrolidone, yielding a nanogel platform designed for delivering N -hexylcarbamoyl-5-fluorouracil (HCFU) to brain tissue (Fig. 9a).…”

Exploring the Potential of Nanogels: From Drug Carriers to Radiopharmaceutical Agents

“…The biodistribution of these 64 Culabeled nanogels in mice was visualized by PET imaging. The [231] Copyright 2022, Frontiers.…”

“…Recently, a theranostic nanogel platform has been developed by Kong et al. [ 231 ] They synthesized polyethyleneimine (PEI)‐based nanogels crosslinked with 3‐(4′hydroxyphenyl)propionic acid N‐hydroxysuccinimide (HPAO). Additionally, the PEI‐based nanogels were equipped with phenylboronic acid (PBA) ensuring active targeting to sialylated epitopes which are overexpressed on the surface of many tumors, e.g., breast cancer cells ( Figure ).…”

“…B) Biodistribution data (% ID) of [ 131 I]-PHP and [ 131 I]I-PBA-PHP nanogels at 16 hours postinjection in 4T1 tumor-bearing mice. Tumor inhibition efficacy with various treatments (NS = normal saline; PHP = non-radiolabeled nanogels; PBA-PHP = non-radiolabeled phenylboronic acid nanogels; 131 I-PHP = radiolabeled nanogels; 131 I-PBA-PHP = radiolabeled phenylboronic acid nanogels) showing C) relative tumor volume, D) body weight and E) survival rate of 4T1 tumor-bearing mice within 47 d. Reproduced with permission [231]. Copyright 2022, Frontiers.…”