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.
Highlights
Catharanthus roseus is a well-known medicinal tropical perennial sub-shrub belonging to the family Apocynaceae
Physical modifications often aim to increase the surface area and dissolution rate of the particles, current research is focused on generation of amorphous states or particle size reduction
The result showed that the precipitation pressure has significant effect on the mean particle size (MPS) of micronized vinblastine during the supercritical antisolvent process, whereas the other three factors showed some effect but insignificantly affected the result
Summary
Catharanthus roseus is a well-known medicinal tropical perennial sub-shrub belonging to the family Apocynaceae. It is regarded as a rich source of pharmaceutically important terpenoid indole alkaloids [1]. Vinblastine has poor water solubility, in this case, its dissolution in biological liquids is practically poor and has a low bioavailability [5]. Many approaches have been developed to improve solubility and to enhance the bioavailability of poorly soluble drugs. These include solid dispersion [6], salt formation [7], inclusion complex [8,9] and microemulsion [10]. Physical modifications often aim to increase the surface area and dissolution rate of the particles, current research is focused on generation of amorphous states or particle size reduction
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