Zoledronic acid (ZOL), a third generation aminobisphosphonate (A-BP), is a drug whose potent anticancer activity is limited by its short plasma half-life and rapid uptake and accumulation within bone. We have recently proposed new delivery systems to avoid ZOL accumulation into the bone, thus improving extra-skeletal bioavailability. In this work, we have developed selfassembly PEGylated nanoparticles (NPs) containing ZOL. ZOL-containing NPs showed good technological characteristics and the possibility to be prepared before use. These NPs showed a higher anti-cancer activity, evaluated in nude mice xenografted with prostate cancer PC3 cells, compared with that induced by free ZOL. In addition, NPs induced, in a significant number of animals, the complete remission of tumour xenografts and an increase of survival time.
New self-assembling nanoparticles for bisphosphonate delivery in cancer.
SALZANO, GIUSEPPINA;LA ROTONDA, MARIA IMMACOLATA;DE ROSA, GIUSEPPE
2011
Abstract
Zoledronic acid (ZOL), a third generation aminobisphosphonate (A-BP), is a drug whose potent anticancer activity is limited by its short plasma half-life and rapid uptake and accumulation within bone. We have recently proposed new delivery systems to avoid ZOL accumulation into the bone, thus improving extra-skeletal bioavailability. In this work, we have developed selfassembly PEGylated nanoparticles (NPs) containing ZOL. ZOL-containing NPs showed good technological characteristics and the possibility to be prepared before use. These NPs showed a higher anti-cancer activity, evaluated in nude mice xenografted with prostate cancer PC3 cells, compared with that induced by free ZOL. In addition, NPs induced, in a significant number of animals, the complete remission of tumour xenografts and an increase of survival time.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
