Physicochemical properties and acute lung toxicity of paclitaxel / oleyl chitosan nanoparticles / 中国药学杂志

ABSTRACT

OBJECTIVE: To prepare paclitaxel / oleyl chitosan nanoparticles (PTX / OCS-NPs) and to examine its physicochemical properties and acute lung toxicity. METHODS: The morphology and size were determined by transmission electron microscope (TEM). The average diameters and polydispersity index were evaluated by dynamic light scattering (DLS). Encapsulation efficiency (EE) and in vitro release were determined by high performance liquid chromatography (HPLC). RESULTS: The RESULTS of PTX/OCS-NPs were spherical in shape, uniform particle size and dispersed uniformly. The diameters of NPs were(292.4±20)nm, PDI less than 0.246 and Zeta potential was about 25 mV. The drug loading of PTX was 15.06%. The encapsulation efficiency of PTX was 48.96%. In vitro release study showed that the cumulative release of PTX from NPs were 41.41% and 56.23% respectively, within 48 h in phosphate buffered saline (PBS) pH 7.4 and pH 4.5. Acute toxicity showed that there was no change in the number of white blood cells in the blood, and the content of LDH in the bronchoalveolar lavage fluid was not changed. The RESULTS indicated that the drug delivery system has a good biosafety and biocompatibility. CONCLUSION: PTX / OCS-NPs have excellent physicochemical properties, high drug loading, with sustained release, no acute lung toxicity, that is expected to be a good delivery of paclitaxel and other difficult anti-cancer drug delivery system.