The pharmacokinetic behaviour and phototherapeutic effectiveness of 2,3-dihydro-5,15-di(3,5-dihydroxyphenyl)porphyrin (SIM01), a new diphenylchlorin photosensitizer incorporated into dimyristoyl phosphatidylcholine (DMPC) liposomes, were studied in vivo in nude mice bearing HT29 human adenocarcinoma. The photophysical and photochemical specificity of SIM01 are a strong absorption at 647 nm, high photosensitizing efficiency and a rapid pharmacokinetic profile making SIM01 an attractive candidate for PDT. The pharmacokinetics in vivo, as determined by fiber spectrofluorimetry, showed that tumor concentration was found maximal for SIM01 and SIMOI-DMPC 12 h after injection, with better uptake for the liposomal formulation. With a 2 mg kg(-1) dye dose, optimal PDT response occurred when the interval between injection and irradiation was 12 h for both formulations, with laser irradiation of 300 J cm(-2) (650 nm, 300 mW). At day 12 after treatment involving a 12-h interval between injection and irradiation, tumor growth was decreased by 26% for SIM01 (P = 0.005) and 35% for SIMOI-DMPC (P = 0.001) as compared to the untreated group. SIM01 would appear to be a powerful sensitizer characterized by high in vivo phototoxicity and rapid tissue uptake and elimination. Our results suggest that SIM01 delivered in a liposomal dispersion is as effective as the raw formulation, something that would open new delivery routes and PDT applications. (C) 2003 Elsevier Science Ltd. All rights reserved.
Bourré, L., Thibaut, S., Fimiani, M., Ferrand, Y., Simonneaux, G., Patrice, T. (2003). In vivo photosensitizing efficiency of a diphenylchlorin sensitizer: interest of a DMPC liposome formulation. PHARMACOLOGICAL RESEARCH, 47(3), 253-261 [10.1016/S1043-6618(02)00312-2].
In vivo photosensitizing efficiency of a diphenylchlorin sensitizer: interest of a DMPC liposome formulation
Fimiani, M.;
2003-01-01
Abstract
The pharmacokinetic behaviour and phototherapeutic effectiveness of 2,3-dihydro-5,15-di(3,5-dihydroxyphenyl)porphyrin (SIM01), a new diphenylchlorin photosensitizer incorporated into dimyristoyl phosphatidylcholine (DMPC) liposomes, were studied in vivo in nude mice bearing HT29 human adenocarcinoma. The photophysical and photochemical specificity of SIM01 are a strong absorption at 647 nm, high photosensitizing efficiency and a rapid pharmacokinetic profile making SIM01 an attractive candidate for PDT. The pharmacokinetics in vivo, as determined by fiber spectrofluorimetry, showed that tumor concentration was found maximal for SIM01 and SIMOI-DMPC 12 h after injection, with better uptake for the liposomal formulation. With a 2 mg kg(-1) dye dose, optimal PDT response occurred when the interval between injection and irradiation was 12 h for both formulations, with laser irradiation of 300 J cm(-2) (650 nm, 300 mW). At day 12 after treatment involving a 12-h interval between injection and irradiation, tumor growth was decreased by 26% for SIM01 (P = 0.005) and 35% for SIMOI-DMPC (P = 0.001) as compared to the untreated group. SIM01 would appear to be a powerful sensitizer characterized by high in vivo phototoxicity and rapid tissue uptake and elimination. Our results suggest that SIM01 delivered in a liposomal dispersion is as effective as the raw formulation, something that would open new delivery routes and PDT applications. (C) 2003 Elsevier Science Ltd. All rights reserved.
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https://hdl.handle.net/11365/29340
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