Human Serum Albumin Nanoparticles as a Novel Delivery System for Cabazitaxel.

Background: Due to use of Tween-80 as an enhancer of solubility, the current clinical formulation of cabazitaxel (CBT) (Jevtana (R)) causes hypersensitivity, neurotoxicity and other severe side-effects. To reduce these vehicle-related effects, a suitable nanocarrier is needed. Materials and Methods: Human serum albumin (HSA) was used to encapsulate CBT by a simple self-assembly method. Physicochemical properties of HSA-CBT nanoparticles were characterized. In vitro release property and cytotoxicity were also determined. In vivo imaging system was used to study nanocarrier distribution in vivo. The safety profile was assessed by hemolysis and acute-toxicity study. Finally, the antitumor efficacy in vivo was investigated in tumor-bearing mice. Results: The average size of HSA-CBT nanoparticles was about 240 nm and the encapsulation efficiency reached 97%. The hemolysis and acute-toxicity experiments confirmed biocompatibility of HSA-CBT nanoparticles. Conclusion: HSA nanoparticles are a safe and effective drug delivery system for hydrophobic anticancer drugs such as CBT.