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A novel tetracationic phthalocyanine as a potential skin phototherapeutic agent
Author(s) -
Fabris Clara,
Soncin Marina,
Mazzon Emanuela,
CalzavaraPinton Piergiacomo,
Lia Fantetti,
Giacomo Chiti,
Dei Donata,
Tampucci Silvia,
Roncucci Gabrio,
Jori Giulio
Publication year - 2005
Publication title -
experimental dermatology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.108
H-Index - 96
eISSN - 1600-0625
pISSN - 0906-6705
DOI - 10.1111/j.0906-6705.2005.00339.x
Subject(s) - phthalocyanine , photosensitivity , photodynamic therapy , irradiation , phototoxicity , dermis , chemistry , hairless , photochemistry , dermatology , epidermis (zoology) , biophysics , materials science , medicine , pathology , optoelectronics , organic chemistry , biochemistry , biology , anatomy , physics , nuclear physics , in vitro
An amphiphilic tetracationic derivative of Zn(II)‐phthalocyanine (RLP068) was prepared by means of chemical synthesis and was showed to possess efficient photophysical and photosensitizing properties against model biological substrates. RLP068 was incorporated into a gel formulation, which allowed its ready penetration into the epidermal layers, but not into the dermis, of both Balb/c and hairless SKH1 mice after 1–2 h of topical deposition. Pharmacokinetic studies showed that the phthalocyanine thus formulated does not enter the general blood circulation. The epidermis‐associated amount of phthalocyanine was sufficient to cause an important cutaneous damage upon irradiation with red light (600–700 nm; 100–180 mW/cm 2 , 160 J/cm 2 ); the latter was confined to the epidermal area with no apparent diffusion to the underlying dermal layers or appearance of photosensitivity in distal skin areas. A systematic investigation of the interplay among the different parameters (deposition time of the formulated phthalocyanine on mouse skin, irradiation fluence rate and total light fluence) allowed us to identify the minimal phototoxic dose, as well as to define irradiation protocols allowing the repeatability of the phototherapeutic treatment. The potential of RLP068 to act as a PDT agent for cutaneous diseases is briefly discussed.