title: Preparation and physicochemical properties of vinblastine microparticles by supercritical antisolvent process.
abstract: The objective of the study was to prepare vinblastine microparticles by supercritical antisolvent process using N-methyl-2-pyrrolidone as solvent and carbon dioxide as antisolvent and evaluate its physicochemical properties. The effects of four process variables, pressure, temperature, drug concentration and drug solution flow rate, on drug particle formation during the supercritical antisolvent process, were investigated. Particles with a mean particle size of 121 ± 5.3 nm were obtained under the optimized process conditions (precipitation temperature 60 °C, precipitation pressure 25 MPa, vinblastine concentration 2.50 mg/mL and vinblastine solution flow rate 6.7 mL/min). The vinblastine was characterized by scanning electron microscopy, X-ray diffraction,  Fourier-transform infrared spectroscopy, mass spectrometry and dissolution test. It was concluded that physicochemical properties of crystalline vinblastine could be improved by physical modification, such as particle size reduction and generation of amorphous state using the supercritical antisolvent process. Furthermore, the supercritical antisolvent process was a powerful methodology for improving the physicochemical properties of vinblastine.
authors.affiliation: State Engineering Laboratory for Bio-Resource Eco-Utilization, Northeast Forestry University, 150040 Harbin, China. zygorl@sohu.com.
authors.forename: Xiaonan
authors.initials: X
authors.lastname: Zhang
authors.forename: Xiuhua
authors.initials: X
authors.lastname: Zhao
authors.forename: Yuangang
authors.initials: Y
authors.lastname: Zu
authors.forename: Xiaoqiang
authors.initials: X
authors.lastname: Chen
authors.forename: Qi
authors.initials: Q
authors.lastname: Lu
authors.forename: Yuliang
authors.initials: Y
authors.lastname: Ma
authors.forename: Lei
authors.initials: L
authors.lastname: Yang
mesh_terms: D002245:Carbon Dioxide / Q000737:chemistry; D025924:Chromatography, Supercritical Fluid; D013058:Mass Spectrometry; D008855:Microscopy, Electron, Scanning; D010316:Particle Size; D011312:Pressure; D011760:Pyrrolidinones / Q000737:chemistry; D012997:Solvents / Q000737:chemistry; D017550:Spectroscopy, Fourier Transform Infrared; D013696:Temperature; D014747:Vinblastine / Q000737:chemistry*; D014961:X-Ray Diffraction
chemical_list: D011760:Pyrrolidinones; D012997:Solvents; D002245:Carbon Dioxide; D014747:Vinblastine; C038678:N-methylpyrrolidone