Monoolein cubic nanoparticles as novel carriers for docetaxel

Abstract

Docetaxel is considered as an effective anticancer agent that can be used for the treatment of various human cancers and is more potent than its structural analogue paclitaxel. In spite of these advantages, there are few limitations of using docetaxel, such as its high hydrophobicity and systemic toxicity due to nonspecific distribution. These limitations could be overcome by incorporating docetaxel into nanoparticles such as cubic nanoparticles (cubosomes). Monoolein cubic nanoparticles containing docetaxel were prepared by top-down procedures using the homogenization technique with different amphiphile concentrations. Characterization of docetaxel cubic nanoparticles was carried out by measuring particle size, entrapment efficiency, small angle X-ray diffraction and in-vitro release of docetaxel from these cubic nanoparticles. Docetaxel release was determined by an advanced technique using multilamellar vesicles (MLV) as acceptor particles. In vitro cytotoxicity and in vivo antitumor activity were evaluated for docetaxel cubosmes and compared with those of docetaxel solution. Particle size and X-ray measurements confirmed the presence of cubic nanoparticles. The entrapment efficiency exceeded 85%. Cubic nanoparticles loaded with docetaxel showed a slow drug release over 24 h. The efficacy of tumor inhibition was higher for docetaxel cubosmes compared with that of docetaxel solution.In conclusion, monoolein cubic nanoparticles seem to be a good carrier for docetaxel due to their particle size and release behavior. Furthermore, the amphiphile concentration of these nanoparticles obviously affects their behavior. Finally, an obvious tumor regression was achieved by these cubic nanoparticles.