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. 1987 Nov;56(5):597–600. doi: 10.1038/bjc.1987.247

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

E Reddi 1, G Lo Castro 1, R Biolo 1, G Jori 1
PMCID: PMC2001878  PMID: 3426922

Abstract

Zn(II)-phthalocyanine (Zn-Pc) incorporated into unilamellar liposomes of dipalmitoylphosphatidylcholine has been injected intraperitoneally (0.5 mg kg-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: approximately 60% of Zn-Pc is eliminated with a serum half-life of approximately 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 (approximately 0.6 microgram g-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 approximately 7.5. The results are discussed in terms of a possible use of Zn-Pc as a photosensitizer in the photodynamic therapy of tumours.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Barel A., Jori G., Perin A., Romandini P., Pagnan A., Biffanti S. Role of high-, low- and very low-density lipoproteins in the transport and tumor-delivery of hematoporphyrin in vivo. Cancer Lett. 1986 Aug;32(2):145–150. doi: 10.1016/0304-3835(86)90112-6. [DOI] [PubMed] [Google Scholar]
  2. Ben-Hur E., Rosenthal I. The phthalocyanines: a new class of mammalian cells photosensitizers with a potential for cancer phototherapy. Int J Radiat Biol Relat Stud Phys Chem Med. 1985 Feb;47(2):145–147. doi: 10.1080/09553008514550211. [DOI] [PubMed] [Google Scholar]
  3. Chan W. S., Svensen R., Phillips D., Hart I. R. Cell uptake, distribution and response to aluminium chloro sulphonated phthalocyanine, a potential anti-tumour photosensitizer. Br J Cancer. 1986 Feb;53(2):255–263. doi: 10.1038/bjc.1986.43. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Dougherty T. J. Hematoporphyrin as a photosensitizer of tumors. Photochem Photobiol. 1983 Sep;38(3):377–379. doi: 10.1111/j.1751-1097.1983.tb02687.x. [DOI] [PubMed] [Google Scholar]
  5. Dougherty T. J. Photodynamic therapy (PDT) of malignant tumors. Crit Rev Oncol Hematol. 1984;2(2):83–116. doi: 10.1016/s1040-8428(84)80016-5. [DOI] [PubMed] [Google Scholar]
  6. Goldstein J. L., Anderson R. G., Brown M. S. Coated pits, coated vesicles, and receptor-mediated endocytosis. Nature. 1979 Jun 21;279(5715):679–685. doi: 10.1038/279679a0. [DOI] [PubMed] [Google Scholar]
  7. Jori G., Beltramini M., Reddi E., Salvato B., Pagnan A., Ziron L., Tomio L., Tsanov T. Evidence for a major role of plasma lipoproteins as hematoporphyrin carriers in vivo. Cancer Lett. 1984 Oct;24(3):291–297. doi: 10.1016/0304-3835(84)90025-9. [DOI] [PubMed] [Google Scholar]
  8. Jori G., Tomio L., Reddi E., Rossi E., Corti L., Zorat P. L., Calzavara F. Preferential delivery of liposome-incorporated porphyrins to neoplastic cells in tumour-bearing rats. Br J Cancer. 1983 Aug;48(2):307–309. doi: 10.1038/bjc.1983.186. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Kessel D. Sites of photosensitization by derivatives of hematoporphyrin. Photochem Photobiol. 1986 Oct;44(4):489–493. doi: 10.1111/j.1751-1097.1986.tb04697.x. [DOI] [PubMed] [Google Scholar]
  10. LIPSON R. L., BALDES E. J., OLSEN A. M. The use of a derivative of hematoporhyrin in tumor detection. J Natl Cancer Inst. 1961 Jan;26:1–11. [PubMed] [Google Scholar]
  11. Moan J. Porphyrin photosensitization and phototherapy. Photochem Photobiol. 1986 Jun;43(6):681–690. doi: 10.1111/j.1751-1097.1986.tb05647.x. [DOI] [PubMed] [Google Scholar]
  12. Netland P. A., Zetter B. R., Via D. P., Voyta J. C. In situ labelling of vascular endothelium with fluorescent acetylated low density lipoprotein. Histochem J. 1985 Dec;17(12):1309–1320. doi: 10.1007/BF01002528. [DOI] [PubMed] [Google Scholar]
  13. Rousseau J., Ali H., Lamoureux G., Lebel E., van Lier J. E. Synthesis, tissue distribution and tumor uptake of 99mTc- and 67Ga-tetrasulfophthalocyanine. Int J Appl Radiat Isot. 1985 Sep;36(9):709–716. doi: 10.1016/0020-708x(85)90041-9. [DOI] [PubMed] [Google Scholar]
  14. Spikes J. D., Bommer J. C. Zinc tetrasulphophthalocyanine as a photodynamic sensitizer for biomolecules. Int J Radiat Biol Relat Stud Phys Chem Med. 1986 Jul;50(1):41–45. doi: 10.1080/09553008614550421. [DOI] [PubMed] [Google Scholar]
  15. Spikes J. D. Phthalocyanines as photosensitizers in biological systems and for the photodynamic therapy of tumors. Photochem Photobiol. 1986 Jun;43(6):691–699. doi: 10.1111/j.1751-1097.1986.tb05648.x. [DOI] [PubMed] [Google Scholar]
  16. Tomio L., Zorat P. L., Jori G., Reddi E., Salvato B., Corti L., Calzavara F. Elimination pathway of hematoporphyrin from normal and tumor-bearing rats. Tumori. 1982 Aug;68(4):283–286. doi: 10.1177/030089168206800402. [DOI] [PubMed] [Google Scholar]
  17. Tralau C. J., MacRobert A. J., Coleridge-Smith P. D., Barr H., Bown S. G. Photodynamic therapy with phthalocyanine sensitisation: quantitative studies in a transplantable rat fibrosarcoma. Br J Cancer. 1987 Apr;55(4):389–395. doi: 10.1038/bjc.1987.78. [DOI] [PMC free article] [PubMed] [Google Scholar]
  18. Valduga G., Reddi E., Jori G. Spectroscopic studies on Zn(II)-phthalocyanine in homogeneous and microheterogeneous systems. J Inorg Biochem. 1987 Jan;29(1):59–65. doi: 10.1016/0162-0134(87)80012-0. [DOI] [PubMed] [Google Scholar]
  19. Zalar G. L., Poh-Fitzpatrick M., Krohn D. L., Jacobs R., Harber L. C. Induction of drug photosensitization in man after parenteral exposure to hematoporphyrin. Arch Dermatol. 1977 Oct;113(10):1392–1397. [PubMed] [Google Scholar]

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