Dehydrocurvularin-loaded mPEG-PLGA Nanoparticles for Targeted Breast Cancer Drug Delivery: Preparation, Characterization, in Vitro and in Vivo Evaluation.

Dehydrocurvularin (DCV) is a promising lead compound for anti-cancer therapy. Unfortunately, the development of DCV-based drugs has been hampered by its poor solubility and bioavailability. Herein, we prepared a DCV-loaded mPEG-PLGA nanoparticles (DCV-NPs) with improved drug properties and therapeutic efficacy. The spherical and discrete particles of DCV-NPs had a uniform diameter of 101.8 ± 0.45 nm and negative zeta potential of -22.5 ± 1.12 mV (pH =7.4), and its entrapment efficiency (EE) and drug loading (DL) were approximately 53.28 ± 1.12% and 10.23 ± 0.30%, respectively. In vitro the release of DCV-NPs lasted for more than 120 h in a sustained-release pattern, its antiproliferation efficacy towards breast cancer cell lines (MCF-7, MDA-MB-231 and 4T1) was better than that of starting drug DCV, and it could be efficiently and rapidly internalized by breast cancer cells. In vivo DCV-NPs were gradually accumulated in tumor areas of mice and significantly suppressed tumor growth. In summary, loading water-insoluble DCV onto nanoparticles has the potential to be an effective agent for breast cancer therapy with injectable property and tumor targeting capacity.