Methyl-β-cyclodextrin

Methyl-β-cyclodextrin (Methyl-beta-cyclodextrin) is a cyclic heptasaccharide used to deliver hydrophobic drugs based on its property of solubilizing non-polar substances. Methyl-β-cyclodextrin is also extensively used as a cholesterol-depleting reagent^[1]. Methyl-β-cyclodextrin strongly reduces clathrin-dependent endocytosis^[2]. Methyl-β-cyclodextrin blocks cell migrasome formation^[3]. In Vitro:Methyl-β-cyclodextrin is extensively used to increase the permeability of cells, and thereby increase the uptake of small molecules such as glucose and nano-particles^[4].
Cyclodextrins are a family of cyclic oligosaccharides with a hydrophilic outer surface and a lipophilic central cavity. Cyclodextrins molecules are relatively large with a number of hydrogen donors and acceptors and, thus in general, they do not permeate lipophilic membranes. In the pharmaceutical industry, cyclodextrins have mainly been used as complexing agents to increase aqueous solubility of poorly soluble drugs and to increase their bioavailability and stability. Cyclodextrins are used in pharmaceutical applications for numerous purposes, including improving the bioavailability of drugs^[4].
Methyl-β-cyclodextrin quickly induces caspase-dependent apoptosis in PEL cells via cholesterol depletion from the plasma membrane. Methyl-β-cyclodextrin inhibits the growth of all PEL cell lines in a dose-dependent manner. The IC₅₀ is 3.33-4.23 mM in each cell line^[5].
Methyl-β-cyclodextrin is a highly water soluble cyclic heptasaccharide consisting of a β-glucopyranose unit, has been reported as the most effective agent for the depletion of cholesterol from cells among the various cholesterol-depleting agents^[5]. In Vivo:In a PEL xenograft mouse model, Methyl-β-cyclodextrin significantly inhibits the growth and invasion of PEL cells without apparent adverse effects. Methyl-β-cyclodextrin-treated mice appears to be healthy, whereas non-treated mice has a distended abdominal region. The body weights of control are significantly higher than those of Methyl-β-cyclodextrin treated mice. Methyl-β-cyclodextrin-treated mice has a significantly lower volume of ascites than that of non-treated mice^[4].
Studies in both humans and animals have shown that cyclodextrins can be used to improve drug delivery from almost any type of drug formulation. Currently, there are approximately 30 different pharmaceutical products worldwide containing drug/cyclodextrins complexes in the market^[6].