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Synthetic cathinones, such as methylone and pentedrone, are psychoactive derivatives of cathinone, sold in the internet as “plant food” or “bath salts”.However, the level at which these compounds and their enantiomers cross the intestinal barrier has not been yet determined. Thus, the present study aimed to analyze the enantioselectivity on the permeability of these drugs through the intestinal barrier by using the Caco-2 cell line, a widely used in vitro model for drug permeability studies. To achieve this goal, an UHPLC-UV method was developed and validated to quantify both synthetic cathinones.The developed UHPLC-UV method revealed high selectivity and a linearity from 1 to 500 μM with correlation coefficients always higher than 0.999. The method has an accuracy that ranged between 89 and 107%, inter-day and intra-day precisions with coefficients of variation below 10%, limits of detection and quantification of 0.31 μM and 0.93 μM for methylone and 0.17 μM and 0.52 μM for pentedrone, respectively. In Caco-2 cells, a differentiated passage of the enantiomers across monolayer was observed for both cathinones. For pentedrone, the difference was observed after the first hour, being R-(−)-pentedrone the most permeable compound. Regarding methylone, the difference was noted after one hour and 30 min, with S-(−)-methylone being the most absorbed enantiomer.In conclusion, a fully validated method was successfully applied for studying the permeability of methylone and pentedrone enantiomers in an in vitro model of human intestine, which allowed to discover, for the first time, the enantioselectivity in drug permeability of this class of drugs.UHPLC method was validated for quantification of pentedrone and methylone in HBSS.Caco-2 permeability assay is suitable assessing high and low permeability profiles.Papp of both cathinones indicated a relatively low transport across cell monolayer.Cathinones enantiomers have a differentiated passage through the intestinal membrane.The R-(−)-pentedrone and S-(−)-methylone are the most permeable compounds.