Departament de Farmacologia, Toxicologia i Química Terapèutica and Institut de Nanociència i Nanotecnologia UB (IN2UB), Universitat de Barcelona, Avda. Joan XXIII 27-31, 08028 Barcelona, Spain.
School of Chemistry, University of East Anglia, Norwich Research Park, Norwich, Norfolk NR4 7TJ, UK.
J Colloid Interface Sci. 2017 Jun 15;496:100-110. doi: 10.1016/j.jcis.2017.02.006. Epub 2017 Feb 8.
Photodynamic therapy (PDT) is a treatment of cancer by which tumour cells are destroyed using reactive oxygen species produced by photosensitizers following activation with visible or near infrared light. Successful PDT depends on the solubility and the targeting ability of the photosensitizers. In this work, the synthesis of a porphyrin-based water soluble nanoparticle conjugate containing a targeting agent that recognizes the erbB2 receptor overexpressed on the surface of particular cancer cells is reported. The nanoparticle conjugates were synthesized following two different protocols, viz. a biphasic and a monophasic method, with the aim to determine which method yielded the optimal nanosystem for potential PDT applications. The nanoparticles were characterized using UV-Vis absorption and fluorescence spectroscopies together with transmission electron microscopy and zeta potential measurements; and their ability to produce singlet oxygen following irradiation was investigated following the decay in absorption of a singlet oxygen probe. The nanoparticles synthesized using the monophasic method were shown to produce the highest amount of singlet oxygen and were further functionalized with anti-erbB2 antibody to target the erbB2 receptors expressed on the surface of SK-BR-3 human breast cancer cells. The water soluble, antibody-porphyrin nanoparticle conjugates were shown to elicit targeted PDT of the breast cancer cells.
光动力疗法（PDT）是一种通过使用光敏剂在可见光或近红外光激活下产生的活性氧来破坏肿瘤细胞的癌症治疗方法。成功的 PDT 取决于光敏剂的溶解度和靶向能力。在这项工作中，报道了一种基于卟啉的水溶性纳米颗粒缀合物的合成，其中包含一种靶向剂，该靶向剂识别在特定癌细胞表面过表达的 erbB2 受体。纳米颗粒缀合物通过两种不同的方法（双相法和单相法）进行合成，目的是确定哪种方法可以产生最适合潜在 PDT 应用的纳米系统。使用紫外可见吸收光谱、荧光光谱以及透射电子显微镜和zeta 电位测量对纳米颗粒进行了表征；并通过吸收单线态氧探针的衰减来研究其在照射后产生单线态氧的能力。结果表明，使用单相法合成的纳米颗粒产生的单线态氧最多，并且进一步用抗 erbB2 抗体进行功能化，以靶向 SK-BR-3 人乳腺癌细胞表面表达的 erbB2 受体。水溶性、抗体-卟啉纳米颗粒缀合物被证明可以引发针对乳腺癌细胞的靶向 PDT。
