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Details for Patent: 6,099,856

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Details for Patent: 6,099,856

Title: Active agent transport systems
Abstract:Methods for transporting a biologically active agent across a cellular membrane or a lipid bilayer. A first method includes the steps of: (a) providing a biologically active agent which can exist in a native conformational state, a denatured conformational state, and an intermediate conformational state which is reversible to the native state and which is conformationally between the native and denatured states; (b) exposing the biologically active agent to a complexing perturbant to reversibly transform the biologically active agent to the intermediate state and to form a transportable supramolecular complex; and (c) exposing the membrane or bilayer to the supramolecular complex, to transport the biologically active agent across the membrane or bilayer. The perturbant has a molecular weight between about 150 and about 600 daltons, and contains at least one hydrophilic moiety and at least one hydrophobic moiety. The supramolecular complex comprises the perturbant non-covalently bound or complexed with the biologically active agent. In the present invention, the biologically active agent does not form a microsphere after interacting with the perturbant. A method for preparing an orally administrable biologically active agent comprising steps (a) and (b) above is also provided as are oral delivery compositions. Additionally, mimetics and methods for preparing mimetics are contemplated.
Inventor(s): Milstein; Sam J. (Larchmont, NY), Barantsevitch; Evgueni (New Rochelle, NY), Leone-Bay; Andrea (Ridgefield, CT), Wang; Nai Fang (Long Island City, NY), Sarubbi; Donald J. (Bronxville, NY), Santiago; Noemi B (Hawthorne, NY)
Assignee: Emisphere Technologies, Inc. (Tarrytown, NY)
Filing Date:Dec 10, 1996
Application Number:08/763,183
Claims:1. A method for preparing an agent which is transportable across a cellular membrane or a lipid-bilayer and which is bioavailable after crossing said membrane or bilayer, said method comprising

(a) providing a biologically active agent which can exist in (i) a native conformational state, (ii) a denatured conformational state, and (iii) an intermediate conformational state, said intermediate conformational state being reversible to said native state and said intermediate conformational state being between said native and denatured states; and

(b) exposing said biologically active agent to a complexing perturbant to reversibly transform said biologically active agent to said intermediate state and to form a transportable supramolecular complex,

said perturbant having a molecular weight ranging from about 150 to about 600 daltons, and having at least one hydrophilic moiety and at least one hydrophobic moiety,

said supramolecular complex comprising said perturbant non-covalently complexed with said biologically active agent, and

said biologically active agent not forming a microsphere with said perturbant; and

(c) preparing a mimetic of said supramolecular complex.

2. A method as defined in claim 1, wherein said biologically active agent comprises a peptide and said mimetic comprises a peptide mimetic.

3. A method for preparing an agent which is transportable across a cellular membrane or a lipid-bilayer, and which is bioavailable after crossing said membrane or bilayer, said method comprising

(a) providing a biologically active agent which can exist in (i) a native conformational state, (ii) a denatured conformational state, and (iii) an intermediate conformational state, said intermediate conformational state being reversible to said native state and said intermediate conformational state being between said native and denatured states; and

(b) exposing said biologically active agent to perturbant to reversibly transform said biologically active agent to said intermediate state; and

(c) preparing a mimetic of said intermediate state.

4. A method as defined in claim 3, wherein said perturbant comprises a pH changing agent, an ionic strength changing agent, or guanidine hydrochloride.
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