Gestational trophoblastic neoplasia (GTN) can result from the over-proliferation of trophoblasts. Treatment of
choriocarcinoma, the most aggressive GTN, currently requires high doses of systemic chemotherapeutic agents, which result in indiscriminate drug distribution and severe toxicity. To overcome these disadvantages and enhance the chemotherapeutic efficacy,
chondroitin sulfate A (CSA)-binding nanoparticles were developed for the targeted delivery of
doxorubicin (DOX) to
choriocarcinoma cells using a synthetic CSA-binding
peptide (CSA-BP), derived from malarial
protein, which specifically binds to the CSA exclusively expressed in the placental trophoblast. CSA-BP-conjugated nanoparticles rapidly bonded to
choriocarcinoma (JEG3) cells and were efficiently internalized into the lysosomes. Moreover, CSA-BP modification significantly increased the anti-
cancer activity of the DOX-loaded nanoparticles in vitro.
Intravenous injections of CSA-BP-conjugated nanoparticles loaded with
indocyanine green (CSA-INPs) were rapidly localized to the
tumor. The CSA-targeted nanoparticles loaded with DOX (CSA-DNPs) strongly inhibited primary
tumor growth and, more importantly, significantly suppressed
metastasis in vivo. Collectively, our results highlight the potential of the CSA-BP-decorated nanoparticles as an alternative targeted delivery system of chemotherapeutic agents for treating
choriocarcinoma and for developing new GTN
therapies based on drug targeting.