Paclitaxel-functionalized aspragalan-calcium phosphate nanoparticles

Paclitaxel (PTX) is an important anticancer agent widely applied in the treatment of breast, ovarian and lung cancer. Its water 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 reduce the systemic toxicity of PTX as well as to avoid the use of Cremophor EL, we developed a Cremophor EL-free aspragalan-calcium phosphate nanoparticle delivery system containing PTX and tested its efficacy. Calcium phosphate nanoparticles have attracted attention as a drug delivery system in recent years, and aspragalan polysaccharides extracted from Chinese herbs have been reported to provide protection against tumors. Cremophor EL-free aspragalan-calcium phosphate PTX-containing nanoparticles were prepared by an adsorption and an incorporation technique. The physicochemical characteristics of the nanoparticles, including particle size, zeta potential, and surface morphology, as well as quantification of drug, were measured. The results were: 1. The loading efficiency of PTX was higher with the incorporation technique than with the adsorption technique. 2. The release behavior of PTX exhibited a biphasic pattern characterized by an initial burst release followed by a slower and continuous release. 3. The size of nanoparticle was in 100-500nm range. 4. In an in vivo study, the PTX-loaded Cremophor EL-free aspragalan-calcium phosphate nanoparticles shown tumor growth inhibition effect on hepatocarcinoma and few side effects. Therefore, PTX -loaded aspragalan-calcium phosphate nanoparticles may be considered as an effective anticancer drug delivery system for cancer chemotherapy. Keyword: aspragalan: calcium phosphate nanoparticles; paclitaxel; antitumor