How cyclodextrins can mask their toxic effect on the blood-brain barrier

Céline Binkowski-Machut (1) , Frédéric Hapiot (1) , Patrick Martin (2) , Roméo Cecchelli (2) , Eric Monflier (3)

1 LPCIA - Laboratoire de physico-chimie des interfaces et applications
2 LBHE - Laboratoire de Physiopathologie de la Barrière Hémato-Encéphalique
3 UCCS Artois - Unité de Catalyse et Chimie du Solide - Equipes du Site Artois

The toxicity of monosubstituted n-alkyldimethylammonium-β-cyclodextrins (DMA-C_n-CD with n = 2, 4 and 12) towards endothelial cells of an in vitro model of the blood-brain barrier (BBB) was evaluated and compared to that of the native β-CD. DMA-C₁₂-CD was found to be non-toxic below 10 mM due to the self-inclusion of the alkyl chain in the CD cavity. A high percentage of passage (30%) of DMA-C₁₂-CD through the endothelial cells has been measured.

Keywords: Cyclodextrins; Blood-brain barrier; Toxicity; Permeability; Endothelial cells; In vitro model

Domains: Biochemistry, Molecular Biology

Céline Binkowski-Machut, Frédéric Hapiot, Patrick Martin, Roméo Cecchelli, Eric Monflier. How cyclodextrins can mask their toxic effect on the blood-brain barrier. Bioorganic and Medicinal Chemistry Letters, 2006, 16 (7), p. 1784-1787. ⟨hal-00543314⟩