Antiangiogenic nanotherapy with lipase-labile Sn-2 fumagillin prodrug.

ABSTRACT:

Background

The chemical instability of antiangiogenic fumagillin, combined with its poor retention during intravascular transit, requires an innovative solution for clinical translation. We hypothesized that an Sn-2 lipase-labile fumagillin prodrug, in combination with a contact-facilitated drug delivery mechanism, could be used to address these problems.

Methods

α(v)β(3)-targeted and nontargeted nanoparticles with and without fumagillin in the prodrug or native forms were evaluated in vitro and in vivo in the Matrigel™ (BD Biosciences, CA, USA) plug model of angiogenesis in mice.

Results

In vitro experiments demonstrated that the new fumagillin prodrug decreased viability at least as efficacious as the parent compound, on an equimolar basis. In the Matrigel mouse ang

SUBMITTER: Pan D 

PROVIDER: S-EPMC3498609 | biostudies-literature | 2012 Oct

REPOSITORIES: biostudies-literature