Ninth People's Hospital affiliated to Shanghai Jiaotong University Medical College, School of Stomatology, Department of Oral Maxillofacial Surgery, Shanghai Institute of Stomatology, Shanghai Key Point Laboratory of Stomatology, Shanghai 200011, China.
Photodiagnosis Photodyn Ther. 2012 Mar;9(1):76-82. doi: 10.1016/j.pdpdt.2011.08.001. Epub 2011 Oct 4.
Hyperbranched polymers represent a new class of drug-delivery vehicle that can be used to prepare nanoparticles with uniform size distribution.
In this study we prepared covalent conjugates between the photosensitizer chlorin(e6) and hyperbranched poly(ether-ester), HPEE. HPEE-ce6 nanoparticles were synthesized by carbodiimide-mediated reaction between HPEE and ce6, and characterized by ultraviolet-visible absorption spectroscopy (UV-Vis), and transmission electron microscopy (TEM). The uptake and phototoxicity of HPEE-ce6 nanoparticles towards human oral tongue cancer CAL-27 cells was detected by confocal laser scanning microscopy (CLSM) and MTT assay, respectively.
The absorption peak of HPEE-ce6 nanoparticles was red-shifted 12-nm compared with ce6, and TEM showed uniform nanoparticles with a diameter of 50-nm. HPEE-ce6 nanoparticles were taken up by CAL-27 cells after 4h incubation and localized in the cytoplasm. The MTT assay showed a significantly (P<0.05) higher phototoxicity compared to free ce6 after 12 J/cm² of 660-nm laser illumination.
This is the first time to our knowledge that hyperbranched polymers have been used in PDT drug delivery.
超支化聚合物是一类新型的药物输送载体,可用于制备具有均匀粒径分布的纳米粒子。
在本研究中,我们制备了光敏剂氯(e6)与超支化聚(醚-酯),HPEE 的共价缀合物。通过 HPEE 和 ce6 之间的碳二亚胺介导反应合成了 HPEE-ce6 纳米粒子,并通过紫外-可见吸收光谱(UV-Vis)和透射电子显微镜(TEM)进行了表征。通过共聚焦激光扫描显微镜(CLSM)和 MTT 测定法分别检测了 HPEE-ce6 纳米粒子对人舌癌细胞 CAL-27 的摄取和光毒性。
HPEE-ce6 纳米粒子的吸收峰比 ce6 红移了 12nm,TEM 显示出直径为 50nm 的均匀纳米粒子。HPEE-ce6 纳米粒子在孵育 4 小时后被 CAL-27 细胞摄取,并定位于细胞质中。与 660nm 激光照射 12J/cm²后的游离 ce6 相比,MTT 测定法显示出显著更高的光毒性(P<0.05)。
据我们所知,这是首次将超支化聚合物用于 PDT 药物输送。