Pharmacokinetic studies with zinc(II)-phthalocyanine in tumour-bearing mice.

Zn(II)-phthalocyanine (Zn-Pc) incorporated into unilamellar liposomes of dipalmitoylphosphatidylcholine has been injected intraperitoneally (0.5mgkg-1) to BALB/c mice bearing a transplanted MS-2 fibrosarcoma. The drug is specifically transported by serum lipoproteins and cleared from the serum via the bile-gut pathway in a biphasic process: ˜60% of Zn-Pc is eliminated with a serum half-life of ˜9 hours, while the remaining aliquot is eliminated at a very slow rate. Several normal tissues take up the drug within 3 hours after administration but release it almost completely after 24-48 hours. On the other hand, the tumour shows a maximum concentration of Zn-Pc (˜0.6.µgg-1 of tissue) after 18-24 hours; at this time, the ratio between the Zn-Pc levels in the tumour and the muscle (which represents the surrounding normal tissue) is ˜7.5. The results are discussed in terms of a possible use of Zn-Pc as a photosensitizer in the photodynamic therapy of tumours. © 1987 The Macmillan Press Ltd.