Micro and nanosizing of Tamsulosin drug via supercritical CO2 antisolvent (SAS) process

Abstract

Supercritical anti-solvent (SAS) method is a solvent-free approach where supercritical carbon dioxide (SC-CO2) is used as anti-solvent and one can control the output particle size without disturbing the nature of the particles. The primary objective of this study is to develop SAS method for the production of Tamsulosin (TML) nanoparticles and investigate the parameters affecting the resultant particle size. In order to optimize the production of nano-sized particles, response surface methodology (RSM) based on Box-Behnken design (BBD (was used. Using dynamic light scattering (DLS) and scanning electron microscopy (SEM) analyses, morphologies and mean diameter ranges were examined. To look into how the SAS process affects TML's chemical and physical characteristics, Fourier-transform infrared spectroscopy (FT–IR), X-ray diffraction analysis (XRD) and differential scanning calorimetry (DSC) were further performed. The acquired results demonstrated that the pressure imposes the largest impact on the TML particle production, with the particle size exhibiting an inverse correlation to the pressure. Observations further indicated an increase in particle size with increasing the temperature from 35 to 50 °C. By increasing the flow rate of the drug solution, the average particle size exhibited an initial decrease followed by an increasing trend. Results of the optimization of the SAS process showed that at a pressure, temperature, and injection rate of 25 MPa, 41.3 °C, and 2.9 mL/min, respectively, the TML particles shrink to an average size of 600 nm.

Keywords

• Supercritical carbon dioxide
• Supercritical anti-solvent
• Tamsulosin
• Nano-scale particles
• Response surface methodology
• Dynamic light scattering