Zoledronic acid (ZOL), a third generation amino-bisphosphonate (A-BP), is a drug whose potent anti-cancer activity is limited by its short plasma half-life and rapid uptake and accumulation within bone1. Here we propose new delivery systems able to avoid ZOL accumulation into the bone, thus improving extra-skeletal bioavailability. In particular, we developed new self-assembling PEGylated nanoparticles (NPs) containing ZOL that can be prepared before use. In nude mice xenografted with prostate cancer PC3 cells, ZOL-encapsulating NPs showed an enhanced anti-cancer activity, when 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, G., M., M., S., Z., M., P., C., L., A., A., LA ROTONDA, M.I., M., C., DE ROSA, G.. - (2012), pp. 0-0. (8th World Meeting on Pharmaceutics, Biopharmaceutics and Pharmaceutical Technology. Istanbul (Turchia) 19-22 marzo 2012).
New self-assembling nanoparticles for bisphosphonate delivery in cancer.
SALZANO, GIUSEPPINA;LA ROTONDA, MARIA IMMACOLATA;DE ROSA, GIUSEPPE
2012
Abstract
Zoledronic acid (ZOL), a third generation amino-bisphosphonate (A-BP), is a drug whose potent anti-cancer activity is limited by its short plasma half-life and rapid uptake and accumulation within bone1. Here we propose new delivery systems able to avoid ZOL accumulation into the bone, thus improving extra-skeletal bioavailability. In particular, we developed new self-assembling PEGylated nanoparticles (NPs) containing ZOL that can be prepared before use. In nude mice xenografted with prostate cancer PC3 cells, ZOL-encapsulating NPs showed an enhanced anti-cancer activity, when 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.
