Zhang Guo-Dong, Harada Atsushi, Nishiyama Nobuhiro, Jiang Dong-Lin, Koyama Hiroyuki, Aida Takuzo, Kataoka Kazunori
Department of Materials Science and Engineering, Graduate School of Engineering, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, 113-8656, Japan.
J Control Release. 2003 Dec 5;93(2):141-50. doi: 10.1016/j.jconrel.2003.05.002.
Photosensitizers play a crucial role in the photodynamic therapy (PDT) of cancer. In this study, a third-generation aryl ether dendrimer porphyrin with 32 primary amine groups on the periphery, [NH2CH2CH2NHCO]32DPZn, and pH-sensitive, polyion complex micelles (PIC) composed of the porphyrin dendrimer and PEG-b-poly(aspartic acid), were evaluated as new photosensitizers (PSs) for PDT in the Lewis Lung Carcinoma (LLC) cell line. The preliminary photophysical characteristics of [NH2CH2CH2NHCO]32DPZn and the corresponding micelles were investigated. Electrostatic assembly resulted in a red-shift of the Soret peak of the porphyrin core and the enhanced fluorescence. Compared to the dendrimer porphyrin [NH2CH2CH2NHCO]32DPZn, relatively low cellular uptake of dendrimer porphyrin [NH2CH2CH2NHCO]32DPZn incorporated in the PIC micelle was observed, yet the latter exhibited enhanced photodynamic efficacy on the LLC cell line. Importantly, the use of PIC micelles as a delivery system reduced the dark toxicity of the cationic dendrimer porphyrin, probably due to the biocompatible PEG shell of the micelles.
光敏剂在癌症的光动力疗法（PDT）中起着至关重要的作用。在本研究中，对一种在周边带有32个伯胺基团的第三代芳基醚树枝状大分子卟啉[NH2CH2CH2NHCO]32DPZn，以及由该卟啉树枝状大分子和聚乙二醇-b-聚天冬氨酸组成的pH敏感型聚离子复合物胶束（PIC）作为Lewis肺癌（LLC）细胞系中光动力疗法（PDT）的新型光敏剂进行了评估。研究了[NH2CH2CH2NHCO]32DPZn及其相应胶束的初步光物理特性。静电组装导致卟啉核心的Soret峰发生红移并增强了荧光。与树枝状大分子卟啉[NH2CH2CH2NHCO]32DPZn相比，观察到掺入PIC胶束中的树枝状大分子卟啉[NH2CH2CH2NHCO]32DPZn的细胞摄取相对较低，但后者对LLC细胞系表现出增强的光动力疗效。重要的是，使用PIC胶束作为递送系统降低了阳离子树枝状大分子卟啉的暗毒性，这可能是由于胶束具有生物相容性的聚乙二醇外壳。
