New cationic liposomes as vehicles of m-tetrahydroxyphenylchlorin in photodynamic therapy of infectious diseases

Antimicrobial photodynamic therapy is emerging as a promising therapeutic modality for bacterial infections. For optimizing the antibacterial activity of the photosensitizer m-tetrahydroxy-phenylchlorin, it has been encapsulated in mixed cationic liposomes composed of different ratios of dimyristoyl-sn-glycero-phosphatidylcholine and any of four cationic surfactants derived from L-prolinol. The delivery efficiency of the different liposomes formulations has been evaluated on a methicillin-resistant Staphylococcus aureus bacterial strain (MRSA), and one of the tested formulations shows a biological activity comparable to that of the free chlorin. In order to rationalize the physicochemical parameters of the carriers that control the biological activity, the new liposome formulations have been characterized by measuring (a) the zeta potential, (b) their capability of chlorin entrapping efficiency, i.e. entrapment efficacy, (c) the effect of storage on chlorin entrapment and (d) the localization of chlorin in the bilayer. The correlation of the physicochemical and biological features of formulations has allowed us to rationalize, to some extent, some of the parameters that may control the interactions with the biological environment. © 2008 American Chemical Society.