Drop-by-drop solvent hot antisolvent interaction method for engineering nanocrystallization of sulfamethoxazole to enhanced water solubility and bioavailability

摘要

In this study, we investigated the drop-by-drop solvent hot antisolvent interaction (DBD-SAI) method for the production of sulfamethoxazole (SMZ) nanoparticles. We thoroughly investigated the effect of different experimental parameters. Hydroxypropyl methylcellulose (HPMC), polyacrylic acid (PAA), polyvinyl alcohol (PVA), polyvinylpyrrolidone (PVP), and sodium dodecyl sulfate (SDS) were used as additives. From particle size and shape analysis, it was confirmed that the obtained nanoparticles of SMZ were less than 220?nm with spherical morphology, and thin circular-shaped flakes (4–5?μm) demonstrated in the presence of the additive PVP. It was observed that particle size increased with the pressure of drug solution and drug concentration and decreased with increased rate of stirring. The formulated samples demonstrated an enhanced solubility, drug-release percentage, and anti-bacterial activity compared with raw SMZ. The solubility increased a minimum of 7 times and a maximum of 18 times compared with those of raw SMZ for nano-SMZ and SMZ-PVA, respectively. The drug-release profile showed that more than 95% of SMZ was released within 1?h. Anti-bacterial activity was evaluated against gram positive bacteriaStaphylococcus aureusand gram negative bacteria Escherichia Coli. SMZ-PVA showed nearly doubled anti-bacterial activity compare to raw-SMZ.