Correlation of distribution of sulphonated aluminium phthalocyanines with their photodynamic effect in tumour and skin of mice bearing CaD2 mammary carcinoma

Abstract

Summan-A chemical extraction assax-and fluorescence microscopi incorporating a light-sensitive thermoelectnically cooled charge-coupled device (CCD) camera was used to study the kinetics of uptake. retention and localisation of disulphonated aluminium phthalocyanine (AIPcS-) and tetrasulphonated aluminium phthalocvanine (AlPcS4) at different time inten-als after an i.p. injection at a dose of 10 mg kg`body w-eight (b.Ax in tumour and surrounding normal skin and muscle of female C-D F, mice bearing CaD2 mammary carcinoma. Moreover. the photodymamic effect on the tumour and normal skin using sulphonated aluminium phthalocvanines (AIPcS,. AIPcS:. AlPcS4) and Photofrin was compared w-ith respect to dye, dve dose and time interval betu-een dve administration and light exposure. The maximal concentrations of AlPcS in the tumour tissue w-ere reached 2-24 h after injection of the dve. while the amounts of AIPcS4 peaked 1-2 h after the dve administration. AlPcS, was simultaneouslv localised in the interstitium and in the neoplastic cells of the tumour. uhereas AlPcS4 appeared to localise only in the stroma of the tumour. The photodynamic efficiency (light A-as applied 24 h after dye injection at a dose of 10 mg kg-' b.wu. of the tumours u-as found to decrease in the folloWing order: AlPcS > AIPcS4> Photofrin > AlPcSl. Furthermore. photodynamic efficacyv was strongly dependent upon dye doses and time intervals betw-een dye administration and light exposure: the higher the dose. the higher the photodynamic efficiency. The most efficient photodynamic therapy (PDT) of the tumour u-as reached (day 20 tumour-free) when light exposure took place 2 h after injection of AlPcS, (10 mg k-.) A dual intratumoral localisation pattern of the dye. as found for AlPcS:. seems desirable to obtain a high photodynamic efficiency. The kinetic patterns of uptake. retention and localisation of AlPcS, and AIPcS4 are roughly correlated w-ith their photodynamic effect on the tumour and normal skin.

Photodynamic parameters in the chick chorioallantoic membrane (CAM) bioassay for topically applied photosensitizers

“…The present study is limited to four compounds: sulfonated chloro-aluminum phthalocyanine (AlPcS n ) [14], benzoporphyrin derivative monoacid ring A (BPD-MA) [15,16], lutetium texaphyrin (Lutex) [17][18][19], and aminolevulinic acid (ALA), a precursor of the endogenous sensitizer protoporphyrin IX (PpIX) [20]. In Table 1 Thursday we present some published results of the PDT efficiency, relative to Photofrin, of these selected sensitizers [21][22][23][24][25][26][27][28][29][30][31][32][33][34][35][36][37][38].…”

Inhibition of protease-resistant prion protein formation by porphyrins and phthalocyanines

“…Important therapeutic parameters likely will include not only the specificity and affinity of PrP binding of these compounds, but also the pharmacokinetics, side effects, toxicity, and delivery to the brain. Many of the tetrapyrrole inhibitors found here are known to be well tolerated in animals, e.g., PcTS-Al (19,21,(44)(45)(46)(47)(48). An ability to penetrate the blood-brain barrier is expected to be helpful although an inhibitor could be useful prophylactically by preventing PrPres formation outside the central nervous system.…”

Photosensitized Inactivation of Cyst Forms of the Freshwater Amoeba Vahlkampfia hartmanni by Aluminium (III) Phthalocyanine Tetrasulfonate

“…On the other hand, hydrophilic phthalocyanines have a low affinity to epithelial tissues and a low dark toxicity (at concentrations <5 µM) as they are rapidly eliminated from cells (Peng et al, 1991;Peng and Moan, 1995;Ceburkov and Gollnick, 2000).…”