Bone is the most common organ affected by metastatic
breast cancer. Targeting delivery of drugs to bone may not only enhance the treatment efficacy, but also reduce the quantity of drug administered. In order to increase the distribution of
paclitaxel (PTX) in bone, herein, a novel bone
metastasis-targeted glutamic hexapeptide-
folic acid (Glu6-FA) derivative was designed and synthesized as
liposome ligand to deliver PTX to bone
metastasis effectively. The
liposomes were prepared by thin film hydration method and its particle size, zeta potential, encapsulation efficiency, release profile, stability,
hemolysis were also characterized. What's more, the anti-
tumor effects of PTX-Glu6-FA-Lip were confirmed by the detection of cell cycle, migration, and further measurement of microtubule stabilization. In addition, the PTX-Glu6-FA-Lip showed superior targeting ability in vitro and in vivo evaluation as compared to naked PTX, non-coated, singly-modified and co-modified by physical blending
liposomes. All the results suggested that Glu6-FA-modified
liposome showed excellent targeting activity to metastatic
bone cancer. These findings suggested that Glu6-FA-Lip was a promising bone
metastasis-targeting carrier for the delivery of PTX. This study may therefore be conducive to the field of bone-targeting drugs delivery.