Counter polyelectrolytes (PEs) having degradable polyamide backbone and controlled thiolation were prepared from a common, amino acid-based precursor. Upon mixing as aqueous solutions, these thiolated counter-PEs formed polyelectrolyte complexes (PECs) having sub-200nm diameters. These PECs were stabilized through spontaneous and reagent-less disulfide cross-linking under ambient conditions. The large positive zeta potential conferred onto these PECs provided colloidal stability for months, and regenerability after centrifugation. Figure 1 schematically depicts the disulfide crosslinking of these polyamide polyelectrolytes. These PECs resist degradation by proteolytic enzymes and are stable to large variations of electrolyte- and proton-concentrations, similar to those encountered in biological milieu. However, they are unraveled in reductive conditions. These features profoundly expand the potential of these PECs to act as vectors for delivering entrapped cargo to the reductive environment of colon and cytosol. These PECs entrap with high efficiency, and controllably-release, FITC-insulin (model peptide) in vitro. Potent cellular internalization of this model peptide within human lung cancer cells along with high cell viability at high polymer loadings was demonstrated.

Disulfide-crosslinked nanocomplexes of polyamide polyelectrolytes for potent cellular internalization of entrapped peptides

248th National Meeting (2014)

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