Opinion
Cyclosporin is a lipophilic cyclic peptide that form gels to clump together
Author(s): Robert Zheng*
Cyclic peptides are promising prospects for orally administered medicines, but limited intestinal permeability has hampered their development. Although certain biological mechanisms that affect cyclic peptide intestinal permeability have been identified, the impact of the mucus barrier, a key stumbling block to epithelial medication delivery, on cyclic peptide bioavailability remains unknown. We show that the lipophilic cyclic peptide cyclosporin A (CsA) interacted with polymeric, gel-forming mucins (MUC2, MUC5AC, and MUC5B), which support the mucus gel-networks in the gastrointestinal tract, and likely caused aggregation. Two additional cyclic peptides (daptomycin and polymyxin B) did not produce mucin aggregation under the same circumstances. Purified MUC2, MUC5AC, and MUC5B mucins sedimented quicker in the presence of CsA using rate-zonal centrifugation, with a substantial increase.. Read More»
DOI:
10.37532/puljbb.22.6(2).18-19
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