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[Novel approach of cyclodextrin-based pharmaceutical formulation].

The α-, β-, and γ-CyDs are the most common natural CyDs, consisting of six, seven, and eight glucose units, respectively. Among the natural CyDs, bioadaptable γ-cyclodextrin (γ-CyD) is useful to improve the undesired properties of drug molecules through the formation of inclusion complex. Recently, various kinds of CyD derivatives such as hydrophilic, hydrophobic, amphiphatic and anionic CyDs have been developed, anticipating the design of CyD-based drug delivery system. The objective of this contribution is to outline our recent findings on the combinational use of γ-CyD and functional ingredients, focusing on the ability to increase the drug absorption, the ability to control the rate and time profiles of drug release, and the ability to deliver a drug to a targeted site. In addition, the multi-functional characteristic of hydroxyalkylated CyDs, in particular, 2-hydroxypropyl-β-CyD (HP-β-CyD) is applicable to design the novel pharmaceutical formulation, focusing on the ability to form hydrophilic nano-particles. Moreover, some amphiphatic CyDs such as 2,6-di-O-methyl-β-CyD (DM-β-CyD) and 2-hydroxybutyl-β-CyD (HB-β-CyD) are useful to control the crystallization and polymorphic transition of solid drugs and will provide an opportunity to isolate labile intermediate metastable polymorphs. On the basis of above-mentioned knowledge, this review explores the use of CyDs to better understand their pharmaceutical applications as well as their limitations in the approach of CyD-based drug delivery system.