Analysis of nucleation kinetics of poorly water-soluble drugs in presence of ultrasound and hydroxypropyl methyl cellulose during antisolvent precipitation

Organic nanoparticles

“…126 The kinetics of nanoparticle nucleation by the example of four drugs insoluble in water was analyzed. 127 The effect of sonication and of hydroxypropylmethylcellulose (HPMC) on the particle deposition in the presence of an antisolvent (water) was studied. The antifungal drug Itraconazole, the antibiotic griseofulvin, the non-steroidal antiinflammatory drug Ibuprofen and the antibacterial drug Sulfamethoxazole were tested, which made it possible to assess how the physicochemical properties affect the nucleation rate and the particle size determined by the light scattering technique.…”

NanoCluster Itraconazole Formulations Provide a Potential Engineered Drug Particle Approach to Generate Effective Dry Powder Aerosols

“…A study by Dalvi and Dave (31) also found that precipitated itraconazole showed amorphous character due to high nucleation rates and rapid precipitation of itraconazole particles. They mentioned that hydrophobic molecules such as ITZ had a higher supersaturation compared to moderately water-soluble molecules, due to a very low equilibrium solubility in anti-solvent-solvent mixtures.…”

Bioavailability Improvement Strategies for Poorly Water-Soluble Drugs Based on the Supersaturation Mechanism: An Update

“…The reason is that the ultrasonic can improve the rate of diffusion, and HPMC can reduce the interfacial tension of the solid-liquid. Additionally, the lower the solubility of a drug, the easier it is to reduce the interfacial tension and thus to generate the drug particles at a sub-micron scale (108). The incorporation of polyethylene glycol (PEG) or its methoxylated derivative (MPEG) as a stabilizer can produce smaller NPs with narrower particle size distribution and enhanced apparent solubility (109).…”