Design and Synthesis of New Sulfur-Containing Hyperbranched Polymer and Theranostic Nanomaterials for Bimodal Imaging and Treatment of Cancer.

In this study, we have synthesized a new hyperbranched polyester polymer containing sulfur-pendants (HBPE-S) in the branching points. This HBPE-S polymer is composed of spherical shaped, aliphatic three-dimensional architecture with carboxylic acid groups on the surface. The presence of sulfur pendants in the polymeric cavities demonstrated important role in the effective encapsulation of Bi-DOTA complexes ([Bi] = 5.21 μM), when compared to the previously reported polymer without sulfur pendants (HBPE, [Bi] = 1.07 x 10-3 μM). Higher X-ray blocking capability and excellent X-ray contrast images were obtained from Bi-DOTA encapsulating HBPE-S polymeric nanoparticles when compared with that of HBPE nanoparticles. In addition, the HBPE-S polymer's spherical structure with amphiphilic cavities allow for the successful encapsulation of anti-tumor drugs and optical dyes, indicating suitable for delivery of wide-range of theranostic agents for cancer diagnosis and treatment. Therapeutic drug taxol encapsulating, folic acid decorated HBPE-S-Fol nanoparticles showed more than 80% of lung carcinoma cell death within 24 h of incubation. Cell viability and microscopic experiments also confirmed for the targeted delivery, thereby minimizing toxicity to healthy tissues. Taken together, new HBPE-S polymer and multimodal theranostic nanoplatforms were synthesized with enhanced X-ray blocking capability for the effective cancer targeting and treatment monitoring.