Oral delivery composition comprising supramolecular complex
First Claim
1. A method for preparing an orally administrable biologically active agent, said method comprising:
- exposing a biologically active agent, which can exist in (i) a native conformational state, (ii) a denatured conformational state. and (iii) an intermediate conformational state, to acomplexing perturbant to reversibly transform said biologically active agent to said intermediate state and to form a transportable suprarnolecular complex,said intermediate conformational state being reversible to said native state and said intermediate conformational state being between said native and denatured states,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.
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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.
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Citations
20 Claims
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1. A method for preparing an orally administrable biologically active agent, said method comprising:
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exposing a biologically active agent, which can exist in (i) a native conformational state, (ii) a denatured conformational state. and (iii) an intermediate conformational state, to acomplexing perturbant to reversibly transform said biologically active agent to said intermediate state and to form a transportable suprarnolecular complex, said intermediate conformational state being reversible to said native state and said intermediate conformational state being between said native and denatured states, 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. - View Dependent Claims (2, 3, 4, 5, 15, 17)
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6. An oral delivery composition comprising a supramolecular complex comprising:
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(a) a biologically active agent in an intermediate conformational state non-covalently complexed with (b) a complexing perturbant having a molecular weight ranging from about 150 to about 600 and having at least one hydrophilic moiety and at least one hydrophobic moiety; said intermediate conformational state being reversible to a native state, said intermediate conformational state being between said native conformational state and a denatured conformational state of said biologically active agent, said composition not being a microsphere. - View Dependent Claims (7, 8, 9, 10, 18)
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11. 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
exposing a biologically active agent, which can exist in (i) a native conformational state, (ii) a denatured conformational state, and (iii) an intermediate conformational state, to a complexing perturbant to reversibly transform said biologically active agent to said intermediate state and to form a transportable supramolecular complex, said intermediate conformational state being reversible to said native state and said intermediate conformational state being between said native and denatured states, 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. - View Dependent Claims (12, 19)
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13. 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
exposing a biologically active agent, which can exist in (i) a native conformational state, (ii) a denatured conformational state, and (iii) an intermediate conformational state, to a perturbant to reversibly transform said biologically active agent to said intermediate state, said intermediate conformational state being reversible to said native state and said intermediate conformational state being between said native and denatured states; - and
(c) preparing a mimetic of said intermediate state. - View Dependent Claims (14, 20)
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16. An oral delivery composition comprising a peptide mimetic of a peptidic biologically active agent having a native state, a denatured state, and an intermediate state conformationally between said native and denatured states, wherein said intermediate state is reversible to said native state.
Specification