Comparison of a new nanoform of the photosensitizer chlorin e6, based on plant phospholipids, with its free form

Photodynamic therapy is an advanced method of treating cancer and various benign diseases, including infections. It uses light-activated molecules [photosensitizers (PSs)] to generate reactive oxygen species (ROS) when irradiated with light of a specific wavelength. This study examined the photophysical and photosensitizing activity of the PS chlorin e6 incorporated in a delivery system based on plant phospholipids. This new nanoform of chlorin e6 comprised particles with a diameter of 18.4 ± 2.5 nm and zeta potential of -34.6 ± 3.0 mV. Incorporation of chlorin e6 in phospholipid nanoparticles was observed to cause a bathochromic shift of Q-band absorption maximum by 14 nm without an absorption change in the range of the Soret band. Fluorescence intensity of chlorin e6 embedded in the phospholipid nanoparticles increased 1.7-fold. Chlorin e6 in phospholipid nanoparticles, when irradiated, was able to generate ROS as shown by oxidation of polyunsaturated fatty acids of the phospholipid matrix of the delivery system and reduced l-glutathione. In vivo it was demonstrated that the new nanoform of chlorin e6 provides more accumulation of PSs in tumor tissue than its free form. Moreover, its accumulation in the skin was lower and its elimination from the skin almost five times faster than when administered in free form. The observed differences of this new nanoform of chlorin e6 should lead to enhancement of antitumor efficacy and a decrease in phototoxicity.