3 years ago

Development of fine solid-crystal suspension with enhanced solubility, stability, and aerosolization performance for dry powder inhalation

Development of fine solid-crystal suspension with enhanced solubility, stability, and aerosolization performance for dry powder inhalation
Dry powder for inhalation (DPI) is an attractive approach for the treatment of local lung diseases. However, the application of drugs with poor water solubility is often limited due to the dissolution obstacles in the fluid layer of the lung lining. In this study, fine solid-crystal suspension (FSCS) was proposed as a solvent-free method to improve the solubility of a drug with poor solubility (itraconazole) and achieve high deposition efficiency simultaneously. The FSCS, in which the crystalline drug particle was highly dispersed in the crystalline excipient, was initially prepared as drug-excipient extrudate by hot melt extrusion, followed by jet milling into fine particles. Unlike the amorphous solid dispersion in the high-energy state, which is liable to recrystallize and aggregate, the FSCS was expected not only to improve the solubility of itraconazole, but also to maintain excellent physical stability. As evidenced in the solubility and stability studies, the solubility of itraconazole in the FSCS was approximately 145-fold greater than that of the raw material, and the crystalline form of itraconazole in the FSCS was also unchanged after storage in the accelerated condition for 6 months (40°C and 75% relative humidity [RH]). The improved solubility might be ascribed to the reduced crystal size and increased wettability, as confirmed by the particle size and contact angle test. The FSCS also showed an encouragingly high fine-particle fraction of 50.59±0.67%, which might have benefited from the appropriate particle size. Therefore, the FSCS was suggested as a promising DPI for delivery of drugs with poor water solubility.

Publisher URL: www.sciencedirect.com/science

DOI: S0378517317308797

You might also like
Discover & Discuss Important Research

Keeping up-to-date with research can feel impossible, with papers being published faster than you'll ever be able to read them. That's where Researcher comes in: we're simplifying discovery and making important discussions happen. With over 19,000 sources, including peer-reviewed journals, preprints, blogs, universities, podcasts and Live events across 10 research areas, you'll never miss what's important to you. It's like social media, but better. Oh, and we should mention - it's free.

  • Download from Google Play
  • Download from App Store
  • Download from AppInChina

Researcher displays publicly available abstracts and doesn’t host any full article content. If the content is open access, we will direct clicks from the abstracts to the publisher website and display the PDF copy on our platform. Clicks to view the full text will be directed to the publisher website, where only users with subscriptions or access through their institution are able to view the full article.