Method and composition for enhancing transport across biological membranes
AssigneeThe Board of Trustees of the Leland Stanford Junior University
InventorsJonathan B. Rothbard, Paul A. Wender
Life of this patent
Estimating the term…
Abstract
Methods and compositions for transporting drugs and macromolecules across biological membranes are disclosed. In one embodiment, the invention includes a method for enhancing transport of a selected compound across a biological membrane, wherein a biological membrane is contacted with a conjugate containing a biologically active agent that is covalently attached to a transport polymer. In one embodiment, the polymer consists of from 6 to 25 subunits, at least 50% of which contain a guanidino or amidino sidechain moiety. The polymer is effective to impart to the attached agent a rate of trans-membrane transport across a biological membrane that is greater than the rate of trans-membrane transport of the agent in non-conjugated form.
Claims18
A conjugate for administration, to a mammalian subject, of an antimicrobial agent whose efficacy in non-conjugated form is limited by its solubility in aqueous liquid or its inability to cross biological membranes to manifest biological activity, said conjugate comprises a transport peptide covalently attached by a linker to the antimicrobial agent, said linker being cleaved in vivo to release the antimicrobial agent from the linker and the transport peptide, wherein the attached transport peptide:
- (a) consists of from 6 to 25 amino acid residues, at least 50% of which contain a guanidino sidechain having the structure
- or an amidino sidechain having the structure
- wherein n is 2, 3, 4 or 5;
- (b) contains at least 6 contiguous amino acid residues containing said guanidino or amidino sidechain;
- and
- (c) increases the delivery of the antimicrobial agent across a biological membrane relative to the delivery of the antimicrobial agent in non-conjugated form.
Dependencies are inferred from the claim text.