Particle size reduction of water-insoluble drug in water-assisted extrusion of hydroxypropyl methyl cellulose

• Published in: Macromolecular research Vol. 19; no. 1; pp. 38 - 43
• Main Authors: Kim, Myeong Jun, Park, Mee-Young, Lee, Young Chul, Lee, Jonghwi
• Format: Journal Article
• Language: English
• Published: Heidelberg The Polymer Society of Korea 2011; 한국고분자학회
• Subjects: Characterization and Evaluation of Materials; Chemistry; Chemistry and Materials Science; Complex Fluids and Microfluidics; Nanochemistry; Nanotechnology; Physical Chemistry; Polymer Sciences; Soft and Granular Matter; 고분자공학; hydroxypropyl methyl cellulose; itraconazole; hot melt extrusion; waterinsoluble drugs; drug nanoparticles; granules
• ISSN: 1598-5032; 2092-7673
• DOI: 10.1007/s13233-011-0110-y

Recent advances in the preparation of nanoparticles of water-insoluble drugs, while remarkable, still largely require a secondary drying step to produce solid dosage forms. This report describes the novel extrusion of crystalline drug particles in a polymer/water matrix, which was developed as a comminution technique for particle size reduction. Itraconazole and hydroxypropyl methyl cellulose were used as a model drug and a matrix polymer, respectively. Nanocomposites of 400 nm itraconazole crystals were prepared successfully with significantly improved release kinetics. The water and polymer content should be optimized, and the repeated extrusion runs were beneficial for effective particle size reduction. This process produced nanocomposite granules, containing stable crystalline drug particles, which can be processed readily into a solid dosage form with a high drug content without a drying step.