Evaluation of Sucrose Laurate as an Intestinal Permeation Enhancer for Macromolecules: Ex Vivo and In Vivo Studies

Evaluation of Sucrose Laurate as an Intestinal Permeation Enhancer for Macromolecules: Ex Vivo and In Vivo Studies

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Oral delivery of macromolecules requires permeation CRANK SET enhancers (PEs) adaptable to formulation.Sucrose laurate (SL) (D1216), a food grade surfactant, was assessed in Caco-2 monolayers, isolated rat intestinal tissue mucosae, and rat intestinal instillations.Accordingly, 1 mM SL increased the apparent permeability coefficient (Papp) of [14C]-mannitol and reduced transepithelial electrical resistance (TEER) across monolayers.

It altered expression of the tight junction protein, ZO-1, increased plasma membrane potential, and decreased mitochondrial membrane potential in Caco-2 cells.The concentrations that increased flux were of the same order as those that induced cytotoxicity.In rat colonic tissue mucosae, the same patterns emerged in respect to the concentration-dependent increases in paracellular marker fluxes and TEER reductions with 5 mM being the key concentration.

While the histology revealed some perturbation, ion transport capacity was retained.In rat jejunal and colonic instillations, 50 and 100 mM SL co-administered with insulin induced blood glucose reductions and achieved relative bioavailability values of Used Skates 2.4% and 8.

9%, respectively, on a par with the gold standard PE, sodium caprate (C10).The histology of the intestinal loops revealed little damage.In conclusion, SL is a candidate PE with high potential for emulsion-based systems.

The primary action is plasma membrane perturbation, leading to tight junction openings and a predominant paracellular flux.