Methods and compositions to enhance epithelial drug transport

Abstract

Methods and compositions provided for enhancing the transport of drugs (including peptides, oligonucleotides, proteins and conventional drugs) across epithelial cells at mucosal sites. The methods and compositions include the use of a peptide comprising at least two amino acids, such as Pro-Leu-Gly-Pro-Arg or Pro-Leu, and a protective group such as phenylazo-benzyloxycarbonyl, N-methyl, t-butyloxycarbonyl, fluoroenylmethyloxycarbonyl or carbobenzoxy, at the N-terminus, or in a mixture of such peptides in a sufficient amount to enhance the drug transport across epithelial cells at mucosal sites. Preferably, the peptide comprises 2 to 5 amino acids; the N-terminal amino acids are preferably Pro-Leu. The peptide with the drug are introduced to the mucosal site in a physical mixture, a conjugated form or by a microcapsule, microsphere, liposome, cell, bacteria, virus or food vesicle carrier by an oral, nasal, pulmonary, buccal, rectal, transdermal, vaginal or ocular route.

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