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.
