BackgroundsSurfactants are amphiphilic molecules of large interest in the pharmaceutical field. An interesting technological application of surfactants is their use as permeability enhancers. At this end, different amphiphilic compounds have been investigated both iAimsThe aim of the study was to evaluate the effect of N-acyl serine and N-acyl alanine on Caco-2 cell monolayer permeability of fluorescein isothiocyanate–dextran 4kDa (as model for macromolecular drug) in comparison to SDS, a well-knMethodsN-acyl serine and N-acyl alanine, with different lengths of the hydrocarbon chains (from C10 to C16) were synthesized. Transepithelial electrical resistance (TEER) at not-toxic concentrations (100% cell viability) across Caco-2 cell monoResultsA decrease in TEER was observed after exposure to N-acyl surfactants. Particularly, the decrease in TEER was proportional to the length of the hydrocarbon chain, reaching values comparable to SDS, when C16 derivatives were tested. Permeability studies refSummary/ConclusionThis study demonstrated that N-acyl serine and N-acyl alanine can act as permeability enhancers for oral absorption of macromolecular drugs.
Effect of amino acid-based surfactants on Caco-2 cell permeability of macromolecular drugs
Perinelli Diego Romano;Logrippo Serena.
2017-01-01
Abstract
BackgroundsSurfactants are amphiphilic molecules of large interest in the pharmaceutical field. An interesting technological application of surfactants is their use as permeability enhancers. At this end, different amphiphilic compounds have been investigated both iAimsThe aim of the study was to evaluate the effect of N-acyl serine and N-acyl alanine on Caco-2 cell monolayer permeability of fluorescein isothiocyanate–dextran 4kDa (as model for macromolecular drug) in comparison to SDS, a well-knMethodsN-acyl serine and N-acyl alanine, with different lengths of the hydrocarbon chains (from C10 to C16) were synthesized. Transepithelial electrical resistance (TEER) at not-toxic concentrations (100% cell viability) across Caco-2 cell monoResultsA decrease in TEER was observed after exposure to N-acyl surfactants. Particularly, the decrease in TEER was proportional to the length of the hydrocarbon chain, reaching values comparable to SDS, when C16 derivatives were tested. Permeability studies refSummary/ConclusionThis study demonstrated that N-acyl serine and N-acyl alanine can act as permeability enhancers for oral absorption of macromolecular drugs.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
