Anti-PSMA labeled liposomes loaded with Actinium-225 for potential antivascular alpha-radiotherapy

We study targeted liposomes loaded with the alpha-particle generator Actinium-225 (225Ac) to selectively kill prostate-specific-membrane-antigen-(PSMA)-expressing cells with the aim to evaluate their potential for targeted antivascular alpha-radiotherapy. This bottom-up design contains the following: The targeted moiety is PSMA which is unique to human tumor vasculature for several different types of primary human cancers. The therapeutic radionuclide,225Ac, emits a total of four alpha-particles per decay providing highly lethal and localized irradiation of targeted cells with minimal exposure of surrounding healthy tissues. Finally, the delivery carrier is a lipid-based nanocarrier (a liposome). Liposomes can be loaded with high levels of radioactivity, and, in terms of toxicities, liposomes can be easily engineered to become rapidly cleared from circulation with the aim to shift the distribution of normal organ toxicities away from the kidneys (the dose limiting organ for 225Ac-labeled antibodies) and toward the spleen and/or liver.

ZHU Charles;  BANDEKAR Amey;  BANERJEE Sangeeta Ray;  POMPER Martin;  BRUCHERTSEIFER Frank;  MORGENSTERN Alfred;  SOFOU Stavroula; 

2014-07-31

SOC NUCLEAR MEDICINE INC

JRC88668

0161-5505,   

https://publications.jrc.ec.europa.eu/repository/handle/JRC88668,