Fabris C, Ometto C, Milanesi C, Jori G, Cook M J, Russell D A
Department of Biology, University of Padova, Italy.
J Photochem Photobiol B. 1997 Jul;39(3):279-84. doi: 10.1016/s1011-1344(97)00018-3.
Zn(II)-octapentyl-phthalocyanine (ZnOPPc), incorporated into a Cremophor oil emulsion, was found to be a highly selective tumour-targeting agent (50-fold larger concentration in the tumour than in the peritumoral tissue) when injected at a dose of 1.46 mumol (kg body weight)-1 in Balb/c mice bearing an intramuscularly transplanted MS-2 fibrosarcoma. The pharmacokinetic properties of this phthalocyanine were closely similar to those found for the analogous octadecyl derivative, whereas the unsubstituted Zn(II)-phthalocyanine showed a lower efficiency and selectivity of tumour targeting than the octaalkyl-substituted phthalocyanines. Irradiation of the ZnOPPc-loaded tumour with 620-700 nm light 24 h after injection caused a significant delay of tumour growth with a gradual shrinkage of the neoplastic mass; the damage involved important contributions from both random necrosis and apoptosis of malignant cells.
将锌（II）-八戊基-酞菁（ZnOPPc）掺入聚氧乙烯蓖麻油乳剂中，当以1.46 μmol/（kg体重）的剂量注射到患有肌肉移植MS-2纤维肉瘤的Balb/c小鼠体内时，发现它是一种高度选择性的肿瘤靶向剂（肿瘤中的浓度比肿瘤周围组织中的浓度大50倍）。这种酞菁的药代动力学特性与类似的十八烷基衍生物非常相似，而未取代的锌（II）-酞菁显示出比八烷基取代的酞菁更低的肿瘤靶向效率和选择性。注射后24小时，用620-700 nm光照射负载ZnOPPc的肿瘤，导致肿瘤生长显著延迟，肿瘤块逐渐缩小；损伤涉及随机坏死和恶性细胞凋亡的重要作用。
