Open AccessStealth liposomes for the delivery of zoledronic acid into tumors enhance the anticancer activity of the drug
Author(s) -
Silvia Zappavigna,
Amalia Luce,
Manuela Porru,
Alessia Maria Cossu,
Carmela Ferri,
Sara Lusa,
Marianna Abate,
Giuseppe De Rosa,
Michele Caraglia
Publication year - 2017
Publication title -
translational medicine reports
Language(s) - English
Resource type - Journals
ISSN - 2532-1250
DOI - 10.4081/tmr.6596
Subject(s) - zoledronic acid , liposome , pharmacology , drug , cancer research , in vitro , bisphosphonate , pharmacokinetics , cytotoxicity , drug delivery , chemistry , medicine , biochemistry , osteoporosis , organic chemistry
Zoledronic acid (ZOL) is a third generation aminobisphosphonate, commonly used for the treatment of bone metastases. Several studies have shown a direct in vitro antitumor activity of ZOL but a clear evidence of clinical activity is still lacking. Unfortunately, the use of ZOL as an anticancer agent in extraskeletal tissues is limited probably because it is rapidly removed from the blood and tends to accumulate in the bone. On these bases, we developed stealth liposomes encapsulating ZOL (Lipo- ZOL) to improve the pharmacokinetic profile of the drug. Compared to free ZOL, Lipo-ZOL induced a stronger inhibition of growth in two different cancer cell lines H460 and CG5. Moreover, Lipo-ZOL also significantly caused a larger inhibition of tumor growth and increased the overall survival in murine models of human lung and breast cancer, in comparison with free ZOL. These results suggest the use of Lipo-ZOL as a potential anticancer agent in patients with neoplastic disease.