NON-POLAR PHOTOSENSITIZER FORMULATIONS FOR PHOTODYNAMIC THERAPY

摘要

A pharmaceutical liposomal formulation for photodynamic therapy comprising a non-polar porphyrin photosensitizer and one or more phospholipids, which are stable in storage without requiring freeze-drying is described. The liposoma l formulation provides therapeutically effective amounts of the photosensitize r for intravenous administration. The phospholipids may be modified by pegylation, i.e. they contain poly ethylene glycol as an integral part of th e phospholipids. The formed liposomes contain the non-polar photosensitizer within the membrane and are useful for the combined targeting of a nonpolar photosensitizer and a second polar substance. When a formulation includes th e presence of monosaccharides or polyalcohols, it can be efficiently freeze- dried preserving the size of the liposomal vehicles and the content of a therapeutically effective amount of the photosensitizing agent. The inventio n also relates to the liposome composition formed upon reconstitution with an aqueous vehicle. The freeze-dried formulation upon reconstitution with a suitable aqueous vehicle forms liposomes that are also useful for intravenou s administration.