Compositions and methods for enhanced transepithelial and transendothelial transport or active agents
First Claim
1. A method for enhancing transcellular or transmembrane transport of an active agent, said method comprising:
- forming a conjugate of said active agent with a cell-surface receptor ligand for a transferrin receptor; and
administering said conjugate and a transfer enhancing amount of a transfer enhancement agent which enhances transcytosis of a cell-surface receptor/ligand complex.
2 Assignments
0 Petitions
Accused Products
Abstract
Compositions and methods for use in enhancement of transmembrane and transcellular transport of an active agent, in particular a peptide or protein, in which at least one carrier for transmembrane or transcellular transport of an active agent which is a ligand for a cell-surface receptor is used to form a ligand/active agent conjugate and at least one transfer enhancement agent which enhances transcytosis of the resultant cell-surface receptor/ligand complex is administered to accelerate transcytosis. As an example, the effects of brefeldin A and monensin on transferrin (Tf) transcellular transport, Tf receptor (TfR) distribution and TfR-mediated endocytosis in filter-grown MDCK cells are described. The transfer enhancement agents markedly enhanced the transcytosis of ligand/active agent complexes in both the apical-to-basal and the basal-to-apical directions, but did not increase the transcytosis of agents which were not bound to a cell-surface receptor ligand as carrier. Furthermore, this enhanced transcytosis was abolished by competition with excess unlabeled Tf, confirming that it was a TfR-mediated process.
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Citations
2 Claims
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1. A method for enhancing transcellular or transmembrane transport of an active agent, said method comprising:
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forming a conjugate of said active agent with a cell-surface receptor ligand for a transferrin receptor; and administering said conjugate and a transfer enhancing amount of a transfer enhancement agent which enhances transcytosis of a cell-surface receptor/ligand complex. - View Dependent Claims (2)
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Specification