Cyclodextrins and their pharmaceutical applications

Cyclodextrins were first described by Villiers in 1891. Schardinger laid the foundation of the cyclodextrin chemistry in 1903–1911 and identified both α- and β-cyclodextrin. In the 1930s, Freudenberg identified γ-cyclodextrin and suggested that larger cyclodextrins could exist. Freudenberg and co-wo...

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Bibliographic Details
Published in:International journal of pharmaceutics 2007-02, Vol.329 (1), p.1-11
Main Authors: Loftsson, Thorsteinn, Duchêne, Dominique
Format: Article
Language:English
Subjects:
Biological and medical sciences
Complexation
Cyclodextrin
Cyclodextrins - pharmacology
Drug delivery
Formulation
General pharmacology
History
History, 19th Century
History, 20th Century
History, 21st Century
Humans
Medical sciences
Pharmaceutical technology. Pharmaceutical industry
Pharmacology, Clinical - history
Pharmacology. Drug treatments
Regulatory
Toxicology
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Summary:Cyclodextrins were first described by Villiers in 1891. Schardinger laid the foundation of the cyclodextrin chemistry in 1903–1911 and identified both α- and β-cyclodextrin. In the 1930s, Freudenberg identified γ-cyclodextrin and suggested that larger cyclodextrins could exist. Freudenberg and co-workers showed that cyclodextrins were cyclic oligosaccharides formed by glucose units and somewhat later Cramer and co-workers described their ability to form inclusion complexes. By the early 1950s the basic physicochemical characteristics of cyclodextrins had been discovered, including their ability to solubilize and stabilize drugs. The first cyclodextrin-related patent was issued in 1953 to Freudenberg, Cramer and Plieninger. However, pure cyclodextrins that were suitable for pharmaceutical applications did not come available until about 25 years later and at the same time the first cyclodextrin-containing pharmaceutical product was marketed in Japan. Later cyclodextrin-containing products appeared on the European market and in 1997 also in the US. New cyclodextrin-based technologies are constantly being developed and, thus, 100 years after their discovery cyclodextrins are still regarded as novel excipients of unexplored potential.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2006.10.044