Preparation, characterization and in vitro anti-tumor activities of evodiamine phospholipids complex / 中国药学杂志

ABSTRACT

OBJECTIVE: To prepare evodiamine phospholipids complex, investigate its physicochemical properties and study its anti-tumor activities in vitro. METHODS: Evodiamine phospholipids complex was prepared and optimized by solvent evaporation method and central composite design, physicochemical characteristics of the complex were investigated by means of apparent solubility studies, Fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC) ,the Particle size and zeta-potential were also investigated. MTT assay was employed to evaluate the anti-tumor activities of the complex in vitro. RESULTS: The optimal formulation protocol for evodiamine phospholipids complex were as follows: mixture (1:1, v/v) of ethanol and tetrahydrofuran was taken as the reaction medium, phospholipids-to-evodiamine molar ratio, reaction concentration of evodiamine, reaction temperature and time were 2:1, 2.5 mg · mL-1, 60°C and 3 h, respectively. The complex rate, particle size and Zeta potential for the optimized EVO-PLC was 94.15%, 243.4 nm and -44.21 mV, respectively. IR and DSC analysis indicated that evodiamine might interact with phospholipids by apolar interactions. MTT assay showed that the anti-tumor activities of evodiamine phospholipids complex on LLC cells was less effective than evodiamine in vitro. CONCLUSION: Evodiamine phospholipids complex was successfully developed under the optimized protocol, possessing high complex rate and enhanced solubility in water, which was a fundamental formulation for the further research of evodiamine. Copyright 2012 by the Chinese Pharmaceutical Association.