Photodynamic therapy involves the concomitant action of three components, light with an appropriate wavelength, molecular oxygen, and a molecule, able to absorb an electromagnetic radiation, called photosensitizer (PS). A fundamental aspect is the bioavailability of the PS that is directly related to some physicochemical properties of the PS itself as it should feature a certain degree of lipophilicity to easily cross the cell membrane, however, at the same time, should be sufficiently water-soluble to navigate in the bloodstream. Consequently, the use of a system for drug delivery becomes essential when photosensitizers with a high degree of lipophilicity are considered. In this work, we present three different drug delivery systems, microemulsions, emulsions and liposomes all capable of carrying a PS belonging to the porphyrin family: the tetraphenyl porphyrin (TPP) and the 4-hydroxyphenyl porphyrin (THPP), which show a relevant different degree of lipophilicity. A series of microemulsions (ME) and emulsions (E) were prepared, among which two formulations, one for THPP and one for TPP, have been chosen. The stability of these two carriers was monitored over time and under various temperature conditions. With the same criteria, two liposomal formulations have been also identified and analyzed. The four formulations mentioned above (one ME, one E and two liposomes) have been tested on SKOV3 tumor cell line comparing the photodynamic activity of the porphyrin formulations versus the aqueous/organic (DMSO) solution of the same two PSs. The results show that all the formulations have proved to be excellent carriers and that the liposomal formulation enhance the photodynamic efficacy of both porphyrins.

Drug delivery systems for the photodynamic application of two photosensitizers belonging to the porphyrin family

Malacarne M. C.;Banfi S.;Rugiero M.;Caruso E.
2021

Abstract

Photodynamic therapy involves the concomitant action of three components, light with an appropriate wavelength, molecular oxygen, and a molecule, able to absorb an electromagnetic radiation, called photosensitizer (PS). A fundamental aspect is the bioavailability of the PS that is directly related to some physicochemical properties of the PS itself as it should feature a certain degree of lipophilicity to easily cross the cell membrane, however, at the same time, should be sufficiently water-soluble to navigate in the bloodstream. Consequently, the use of a system for drug delivery becomes essential when photosensitizers with a high degree of lipophilicity are considered. In this work, we present three different drug delivery systems, microemulsions, emulsions and liposomes all capable of carrying a PS belonging to the porphyrin family: the tetraphenyl porphyrin (TPP) and the 4-hydroxyphenyl porphyrin (THPP), which show a relevant different degree of lipophilicity. A series of microemulsions (ME) and emulsions (E) were prepared, among which two formulations, one for THPP and one for TPP, have been chosen. The stability of these two carriers was monitored over time and under various temperature conditions. With the same criteria, two liposomal formulations have been also identified and analyzed. The four formulations mentioned above (one ME, one E and two liposomes) have been tested on SKOV3 tumor cell line comparing the photodynamic activity of the porphyrin formulations versus the aqueous/organic (DMSO) solution of the same two PSs. The results show that all the formulations have proved to be excellent carriers and that the liposomal formulation enhance the photodynamic efficacy of both porphyrins.
Drug delivery; Emulsion; Liposome; Microemulsion; Photodynamic activity; Cell Line, Tumor; Drug Carriers; Humans; Liposomes; Photosensitizing Agents; Porphyrins; Photochemotherapy
Malacarne, M. C.; Banfi, S.; Rugiero, M.; Caruso, E.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11383/2115544
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