Viability and permeability across Caco-2 cells of CBZ solubilized in fully dilutable microemulsions.

Citation:

Anna Kogan, Kesselman, Ellina , Danino, Dganit , Aserin, Abraham , and Garti, Nissim. . 2008. “Viability And Permeability Across Caco-2 Cells Of Cbz Solubilized In Fully Dilutable Microemulsions.”. Colloids And Surfaces, B: Biointerfaces, 66, 1, Pp. 1–12. doi:10.1016/j.colsurfb.2008.05.006.

Abstract:

The viability and permeability of carbamazepine (CBZ) solubilized in fully dilutable non-ionic microemulsions across Caco-2 cells used as a model for intestinal epithelium. Maximum solubilization capacity (SC) of CBZ was detd. within water-in-oil (W/O), bicontinuous and oil-in-water (O/W) structures formed upon diln. The effect of the nature of the oil phase, surfactant type, and the ratio between the oil phase and surfactant on the quantity of solubilized CBZ, droplets size, the viability of the cells and drug permeability was elucidated. Several fully dilutable microemulsions based on pharma-grade ingredients can be loaded with very significant amts. of CBZ, and W/O microemulsions (10 wt% water) exhibit up to 3-fold higher solubilization capacity over the drug's soly. in oil (triacetin). CBZ in the O/W microemulsions (80 wt% water) exhibit up to 29-fold higher solubilization than in water, and the O/W droplets of the examd. systems are 9-11 nm in size, and the highest permeability was obtained in systems contg. triacetin/$\alpha$-tocopherol acetate/ethanol in 3/1/4 wt% ratio as oil phase and Tween 60 as surfactant. The replacement of $\alpha$-tocopherol acetate by $\alpha$-tocopherol inhibits CBZ release and replacement of a satd. chain of Tween 60 by an unsatd. (Tween 80) or shorter chain (Tween 40) inhibited drug release. The decrease in the oil phase to surfactant ratio leads to enhancement of drug release (diln. line 64 \textgreater diln. line 73). [on SciFinder(R)]
Last updated on 06/28/2020