Microparticle encapsulation prevented PRX302 from immediately interacting with GPI-anchored proteins as demonstrated in a competition assay, which resulted in an increased therapeutic index and significant anti-tumor efficacy following a single dose of PRX302-loaded microparticles in a preclinical model of prostate cancer liver metastasis with no obvious toxicity. These results document PRX302 released from PLGA microparticles demonstrate in vivo anti-tumor efficacy in a clinically-relevant preclinical model of metastatic prostate cancer.