RESUMO
A series of push-pull type meso-ester substituted BODIPY dyes 1-4 with intense near-infrared absorption, largely enhanced photoacoustic (PA) activity and excellent photo-stability were synthesized. The impact of the electronic structure on the PA activity was also discussed. Moreover, the in vitro and in vivo PA imaging were investigated, which suggested a passive targeting capacity in the tumor site.
RESUMO
Photoacoustic imaging (PAI) has emerged as an advantageous modality with high resolution and deep tissue penetration. However, its application is limited by the lack of available contrast agents. In this work, we report the synthesis of a naphthalene fused BODIPY dimer Na-BD, and the impact of the electronic structure on the oxidative cyclo-dehydrogenation process was systematically studied. Na-BD exhibited intense NIR absorption, much better photo-stability and higher PA activity compared to commercial ICG dye, which makes it an excellent contrast agent for PAI. Moreover, the in vivo PAI studies based on Na-BD loaded BSA nanoparticles were carried out and they demonstrated a significant passive targeting capacity by exploiting the enhanced permeability and retention effect in the tumor region.
RESUMO
PURPOSE: 32P BioSilicon is a new, implantable, radiological medical device that comprises particles of highly pure silicon encapsulating 32phosphorus (32P) for the treatment of unresectable solid tumors. Prior to administration, the device particles are suspended in a formulant which provides an even suspension of the intended dose for implantation. The primary objective of this animal trial study was to investigate the effects of intratumoral injection of 32)P BioSilicon on human hepatocellular (HepG2) and pancreatic carcinoma (2119) xenografts implanted in nude mice (BALB/c). A secondary objective was the histopathologic examination of the tumor foci and surrounding tissue during the study. METHODS: Cultured human carcinoma cells (HepG2 and 2119) were injected s.c. into the gluteal region of nude mice. When the implanted tumors were approximately 1 cm in diameter, 32P BioSilicon (0.5, 1.0, and 2.0 MBq) or formulant was injected into the tumors. Implanted tumor size was measured once a week for 10 weeks. At study termination, the tumor and surrounding normal tissue were collected and fixed in 10% formalin and processed for histopathologic analysis. RESULTS: 32P BioSilicon produced a reduction in HepG2 tumor volume when compared with formulant control, and complete response was observed among tumors in the 1.0 and 2.0 MBq treatment groups after week 8. There was also significant reduction in 2119 tumor volume in all treated groups, with the complete response rate of 67% in the 2.0 MBq group. CONCLUSION: 32P BioSilicon suppressed the growth of both human hepatocellular and pancreatic carcinoma xenografts implanted in nude mice and complete responses were also observed in tumors at higher radiation doses.