van Leengoed H L, van der Veen N, Versteeg A A, Ouellet R, van Lier J E, Star W M
Dr. Daniel den Hoed Cancer Center, Rotterdam, The Netherlands.
Photochem Photobiol. 1993 Aug;58(2):233-7. doi: 10.1111/j.1751-1097.1993.tb09554.x.
The fluorescence pharmacokinetics of a series of metallosulfophthalocyanines, chelated with either aluminum or zinc and sulfonated to different degrees, was studied by fluorescence measurements in vivo. Dyes were administered systemically to female WAG/RIJ rats with an isogeneic mammary carcinoma transplanted into the subcutis in a transparent observation chamber located on their backs. Following an intravenous injection of 2.5 mumol/kg of the dye, fluorescence dynamics was observed up to 7 h postinjection. The phthalocyanines were excited at 610 nm with a power density of 0.1 mW/cm2 without causing photodynamic damage to the vasculature. Fluorescence was detected above 665 nm using a fluorescence imaging system based on an image intensifier. Dye retention in the blood vessels and tumor tissue was expressed as ratios relative to the fluorescence signal of the surrounding subcutaneous tissue. Phthalocyanines chelated with aluminum gave the highest fluorescence signal with tumor-over-subcutis ratios of up to a value of 4. The zinc complexes exhibited the highest vascular-over-subcutis ratios with maximum values exceeding a value of 6. They also displayed the longest retention times in the vascular system of well over 7 h. Overall, decreasing the degree of sulfonation of the metallophthalocyanines results in lower tumor-over-normal tissue fluorescence ratios, and furthermore aluminum-based dyes seem superior tumor localizers over zinc-based dyes. The advantages of phthalocyanines over porphyrins with respect to tumor localization and photodynamic therapy are discussed.
通过体内荧光测量研究了一系列与铝或锌螯合且磺化程度不同的金属磺基酞菁的荧光药代动力学。将染料全身给药于雌性WAG/RIJ大鼠，这些大鼠背部皮下移植了同基因乳腺癌，并置于透明观察室中。静脉注射2.5 μmol/kg染料后，在注射后7小时内观察荧光动力学。酞菁在610 nm处以0.1 mW/cm²的功率密度激发，不会对脉管系统造成光动力损伤。使用基于图像增强器的荧光成像系统在665 nm以上检测荧光。血管和肿瘤组织中的染料保留率以相对于周围皮下组织荧光信号的比率表示。与铝螯合的酞菁产生最高的荧光信号，肿瘤与皮下组织的比率高达4。锌配合物表现出最高的血管与皮下组织比率，最大值超过6。它们在血管系统中的保留时间也最长，超过7小时。总体而言，金属酞菁磺化程度的降低导致肿瘤与正常组织的荧光比率降低，此外，铝基染料似乎比锌基染料更能有效地定位肿瘤。讨论了酞菁相对于卟啉在肿瘤定位和光动力治疗方面的优势。
