2010/07/20 by Thorsteinn Loftsson, Þorsteinn Loftsson, Marcus E. Brewster +1 · 4 citations
Medicine · Pharmacology, Toxicology and Pharmaceutics · #Advanced Drug Delivery Systems #Drug Solubulity and Delivery Systems #Pharmaceutical studies and practices
paper · pdf · doi:10.1111/j.2042-7158.2010.01030.x
openalex publication_date 2010/07/20 · crossref created 2010/07/20 · crossref issued 2010/11/01 · crossref published 2010/11/01 · crossref published-online 2010/11/01 · crossref published-print 2010/11/01 · crossref deposited 2024/10/30 · openalex created_date 2025/10/10 · crossref indexed 2026/07/30 · openalex updated_date 2026/08/03
OBJECTIVES: Drug pipelines are becoming increasingly difficult to formulate. This is punctuated by both retrospective and prospective analyses that show that while 40% of currently marketed drugs are poorly soluble based on the definition of the biopharmaceutical classification system (BCS), about 90% of drugs in development can be characterized as poorly soluble. Although a number of techniques have been suggested for increasing oral bioavailability and for enabling parenteral formulations, cyclodextrins have emerged as a productive approach. This short review is intended to provide both some basic science information as well as data on the ability to develop drugs in cyclodextrin-containing formulations. KEY FINDINGS: There are currently a number of marketed products that make use of these functional solubilizing excipients and new product introduction continues to demonstrate their high added value. The ability to predict whether cyclodextrins will be of benefit in creating a dosage form for a particular drug candidate requires a good working knowledge of the properties of cyclodextrins, their mechanism of solubilization and factors that contribute to, or detract from, the biopharmaceutical characteristics of the formed complexes. SUMMARY: We provide basic science information as well as data on the development of drugs in cyclodextrin-containing formulations. Cyclodextrins have emerged as an important tool in the formulator's armamentarium to improve apparent solubility and dissolution rate for poorly water-soluble drug candidates. The continued interest and productivity of these materials bode well for future application and their currency as excipients in research, development and drug product marketing.