Paclitaxel-functionalized aspragalan-calcium phosphate nanoparticles
Q. He, X.Z. Zhang, W.M. Yaun, D.M. Zhau, Z.Q. Fang, X.H. Gang
Nanjing Medical University, CN
Keywords: aspragalan, calcium phosphate, nanoparticles
Abstract:Paclitaxel (PTX) is an important anticancer agent. Its aqueous solubility is very low; hence the available formulation of PTX for clinical use consists of Cremophor EL, which has been associated with several hypersensitivity reactions. In order to avoid the use of Cremophor EL, we developed a Cremophor EL free aspragalan-calcium phosphate nanoparticle delivery system containing paclitaxel and tested its efficacy and safety. The Cremophor EL-free aspragalan-calcium phosphate -containing the PTX were prepared by simple nanoprecipitation. The chemical and physical characteristics of the nanoparticles including the chemical composition, particle size, zeta potential, and surface morphology, as well as quantification of drug, were measured. The results are: 1. The release behavior of paclitaxel exhibited a biphasic pattern characterized by an initial burst release followed by a slower and continuous release. 2. The size of nanoparticle was in 100-250nm range. 3. Through in vivo study, the paclitaxel -loaded Cremophor EL-free aspragalan-calcium phosphate nanoparticles shown greater tumor growth inhibition effect on hepatocarcinoma and fewer side effects compared with Taxol (R). Therefore, paclitaxel -loaded aspragalan-calcium phosphate nanoparticles may be considered as an effective anticancer drug delivery system for cancer chemotherapy.