Abstract
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/cm2, 160 J/cm2); 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.
| Original language | English |
|---|---|
| Pages (from-to) | 675-683 |
| Number of pages | 9 |
| Journal | Experimental Dermatology |
| Volume | 14 |
| Issue number | 9 |
| DOIs | |
| Publication status | Published - Sep 2005 |
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Keywords
- Cutaneous diseases
- Minimal phototoxic dose
- Photodynamic therapy
- Photosensitization
- Pthalocyanines
- Singlet oxygen
ASJC Scopus subject areas
- Dermatology
Cite this
A novel tetracationic phthalocyanine as a potential skin phototherapeutic agent. / Fabris, Clara; Soncin, Marina; Mazzon, Emanuela; Calzavara-Pinton, Piergiacomo; Lia, Fantetti; Giacomo, Chiti; Dei, Donata; Tampucci, Silvia; Roncucci, Gabrio; Jori, Giulio.
In: Experimental Dermatology, Vol. 14, No. 9, 09.2005, p. 675-683.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - A novel tetracationic phthalocyanine as a potential skin phototherapeutic agent
AU - Fabris, Clara
AU - Soncin, Marina
AU - Mazzon, Emanuela
AU - Calzavara-Pinton, Piergiacomo
AU - Lia, Fantetti
AU - Giacomo, Chiti
AU - Dei, Donata
AU - Tampucci, Silvia
AU - Roncucci, Gabrio
AU - Jori, Giulio
PY - 2005/9
Y1 - 2005/9
N2 - 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/cm2, 160 J/cm2); 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.
AB - 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/cm2, 160 J/cm2); 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.
KW - Cutaneous diseases
KW - Minimal phototoxic dose
KW - Photodynamic therapy
KW - Photosensitization
KW - Pthalocyanines
KW - Singlet oxygen
UR - http://www.scopus.com/inward/record.url?scp=23844526909&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=23844526909&partnerID=8YFLogxK
U2 - 10.1111/j.0906-6705.2005.00339.x
DO - 10.1111/j.0906-6705.2005.00339.x
M3 - Article
C2 - 16098127
AN - SCOPUS:23844526909
VL - 14
SP - 675
EP - 683
JO - Experimental Dermatology
JF - Experimental Dermatology
SN - 0906-6705
IS - 9
ER -