Polyarginine nanocapsules: A versatile nanocarrier with potential in transmucosal drug delivery

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Abstract

The objective of this work was to investigate the potential utility of nanocapsules composed of an oily core decorated with a single polyarginine (PARG), or double PARG/polyacrylic acid (PAA) layer as oral peptide delivery carrier. A step-by-step formulation optimization process was designed, which involved the study of the influence of the surfactants, oils and polymer shells (PARG of different molecular weight and PAA) on the nanocapsules physicochemical properties, peptide loading efficiency, stability in simulated intestinal fluids (SIF) and capacity to enhance the permeability of the intestinal epithelium. Despite the lipophilic nature of the nanocapsules, it was possible to achieve a moderate loading of the hydrophilic model peptide salmon calcitonin and control its release in SIF, by adjusting the formulation conditions. Finally, studies in the Caco-2 epithelial cell line showed the capacity of the nanocapsules to reduce the transepithelial electric resistance of the monolayer, without compromising their viability. Overall, these properties suggest the capacity of polyarginine nanocapsules for enhancing the transport of peptides across epithelia.

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