Development of modified polymer dot as stimuli-sensitive and 67Ga radio-carrier, for investigation of in vitro drug delivery, in vivo imaging and drug release kinetic.

A polymer dot modified histidine-functionalized graphene quantum dot carrier, PD@His.GQD, was synthesized to investigate the in vitro sunitinib (STB) deliveryvia luminescence spectrometer. The carrier's synthesis, with an average size of 34 nm, was proved by Fourier transform infrared (FTIR), Transmission Electron Microscopy (TEM), and Dynamic Light Scattering (DLS) analyses. In the in vitro, STB delivery investigation showed that for healthy tissue, the STB was loaded at pH  = 7.2 and at 25  = 5.4 at 37 °C with a maximum loading efficiency percentage of 99 % while it was released at pH = 5.4 at 37 °C with a release percentage of 97 %. In the sequel, the STB loaded carrier was labeled with Gallium-67 (67Ga-STB.PD@His.GQD) to produce exceedingly transparent radio-carrier for in vivo kidney cancerous mice imaging via the single photon emission computed tomography (SPECT) device. The radiochemical purity of the 67Ga-STB.PD@His.GQD was obtained as 95 % by Radio Thin Layer Chromatography (RTLC) and High-Performance Liquid Chromatography (HPLC) analysis. All obtained results affirmed that the synthesized PD@His.GQD is an STB stimuli-sensitive and selective targeting carrier. All cancerous mice in vivo images at 10 and 20 h of 67Ga-STB.PD@His.GQD post-injection and its bio-distribution calculations showed its most accumulation in the kidney cancerous tissue. Also, the STB release kinetic was studied via Zero-order, First-order, Higuchi, and Korsmeyer-Peppas models, and the release data were fitted with Korsmeyer-Peppas model that expresses the STB release mechanism is controlled by diffusion.