Lipid bilayer-gated mesoporous silica nanocarriers for tumor-targeted delivery of zoledronic acid in vivo

A1 Journal article (refereed)

Internal Authors/Editors

Publication Details

List of Authors: Desai D, Zhang J, Sandholm J, Lehtimäki J, Grönroos T, Tuomela J, Rosenholm JM
Publisher: American Chemical Society
Publication year: 2017
Journal: Molecular Pharmaceutics
Volume number: 14
Issue number: 9
Start page: 3218
End page: 3227
ISSN: 1543-8384


Zoledronic acid (ZOL) is a nitrogen-containing bisphosphonate used for
the treatment of bone diseases and calcium metabolism. Anticancer
activity of ZOL has been established, but its extraskeletal effects are
limited due to its rapid uptake and accumulation to bone hydroxyapatite.
In this work, we report on the development of tethered lipid
bilayer-gated mesoporous silica nanocarriers (MSNs) for the
incorporation, retention, and intracellular delivery of ZOL. The in vitro anticancer activity of ZOL-loaded nanocarriers was evaluated by cell viability assay and live-cell imaging. For in vivo
delivery, the nanocarriers were tagged with folic acid to boost the
affinity for breast cancer cells. Histological examination of the liver
revealed no adverse off-target effects stemming from the nanocarriers.
Importantly, nonspecific accumulation of ZOL within bone was not
observed, which indicated in vivo stability of the tethered lipid
bilayers. Further, the intravenously administered ZOL-loaded
nanocarriers showed tumor growth suppression in breast cancer
xenograft-bearing mice.

Last updated on 2019-23-04 at 05:04