Nanotechnologies to use bisphosphonates as potent anticancer agents: The effects of zoledronic acid encapsulated into liposomes - Abstract

Department of Biochemistry and Biophysics, Second University of Naples, Naples, Italy.


Zoledronic acid (ZOL) is a potent amino-bisphosphonate used for the treatment of bone metastases with recently reported antitumor activity. However, the short plasma half-life and rapid accumulation in bone limits the use of ZOL as an antitumor agent in extraskeletal tissues. Therefore, we developed stealth liposomes encapsulating ZOL (LipoZOL) to increase extraskeletal drug availability. Compared to ZOL, LipoZOL induced a stronger inhibition of growth of a range of different cancer cell lines in vitro. LipoZOL also caused significantly larger inhibition of tumor growth and increased the overall survival in murine models of human prostate cancer and multiple myeloma, in comparison with ZOL. Moreover, a strong inhibition of vasculogenetic events without evidence of necrosis in the tumor xenografts from prostate cancer was recorded after treatment with LipoZOL. We demonstrated both antitumor activity and tolerability of LipoZOL in preclinical animal models of both solid and hematopoietic malignancies, providing a rationale for early exploration of use of LipoZOL as a potential anticancer agent in cancer patients.

Written by:
Marra M, Salzano G, Leonetti C, Tassone P, Scarsella M, Zappavigna S, Calimeri T, Franco R, Liguori G, Cigliana G, Ascani R, La Rotonda MI, Abbruzzese A, Tagliaferri P, Caraglia M, De Rosa G.   Are you the author?

Reference: Nanomedicine. 2011 Mar 29. Epub ahead of print.
doi: 10.1016/j.nano.2011.03.004

PubMed Abstract
PMID: 21453789 Prostate Cancer Section