School of Pharmaceutical Sciences, University of Lausanne/Geneva, Geneva, 30, quai Ernest Ansermet, Geneva CH-1211, Switzerland.
Molecules. 2011 Dec 23;17(1):98-144. doi: 10.3390/molecules17010098.
The purpose of this review is to compile preclinical and clinical results on phthalocyanines (Pcs) as photosensitizers (PS) for Photodynamic Therapy (PDT) and contrast agents for fluorescence imaging. Indeed, Pcs are excellent candidates in these fields due to their strong absorbance in the NIR region and high chemical and photo-stability. In particular, this is mostly relevant for their in vivo activation in deeper tissular regions. However, most Pcs present two major limitations, i.e., a strong tendency to aggregate and a low water-solubility. In order to overcome these issues, both chemical tuning and pharmaceutical formulation combined with tumor targeting strategies were applied. These aspects will be developed in this review for the most extensively studied Pcs during the last 25 years, i.e., aluminium-, zinc- and silicon-based Pcs.
本次综述旨在汇总酞菁(Pc)作为光敏剂(PS)用于光动力疗法(PDT)和荧光成像对比剂的临床前和临床研究结果。实际上,由于酞菁在近红外区域具有较强的吸收能力和较高的化学和光稳定性,因此非常适合应用于这些领域。特别是,这对于它们在更深组织区域的体内激活尤为重要。然而,大多数酞菁存在两个主要的局限性,即强烈的聚集倾向和低水溶性。为了克服这些问题,人们应用了化学调谐和药物制剂,并结合肿瘤靶向策略。本综述将针对过去 25 年来研究最广泛的铝、锌和硅基酞菁,对这些方面进行阐述。