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US 5,620,708 AGranted
Compositions and methods for the oral delivery of active agents
AssigneeAlza Corporation
InventorsAlfred A. Amkraut, Heechung Yang
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AssigneeAlza Corporation
InventorsAlfred A. Amkraut, Heechung Yang
Estimating the term…
Compositions and methods for the oral administration of drugs and other active agents are provided. The compositions comprise an active agent carrier particle attached to a binding moiety which binds specifically to a target molecule present on the surface of a mammalian enterocyte. The binding moiety binds to the target molecule with a binding affinity or avidity sufficient to initiate endocytosis or phagocytosis of the particulate active agent carrier so that the carrier will be absorbed by the enterocyte. The active agent will then be released from the carrier to the host's systemic circulation. In this way, degradation of degradation-sensitive drugs, such as polypeptides, in the intestines can be avoided while absorption of proteins and polypeptides from the intestinal tract is increased.
A composition comprising a matrix carrier particle composed of a material which resists proteolytic degradation and which is sufficiently small to be absorbed by a mammalian enterocyte, covalently attached to a binding moiety which binds specifically to a target molecule present on the surface of a mammalian enterocyte, the target molecule being an endocytosis- or phagocytosis-promoting receptor, said composition further comprises a polypeptide drug protectively retained by the carrier particle.
A composition comprising a matrix carrier particle composed of a material which resists proteolytic degradation and which is sufficiently small to be absorbed by a mammalian enterocyte, attached to a binding moiety selected from the group consisting of oligopeptides containing the sequence RGD, invasin molecules or fragments thereof, EGF or fragments thereof, and antibodies or fragments thereof, which bind specifically to a target molecule present on the surface of a mammalian enterocyte, the target molecule being an endocytosis- or phagocytosis- promoting receptor.
A pharmaceutical composition comprising:
A composition for oral administration comprising a matrix carrier particle composed of a material which resists proteolytic degradation when passing through the environment of the intestines and stomach and which is sufficiently small to be absorbed by a mammalian enterocyte, attached to a binding moiety which binds specifically to a target molecule present on the surface of a mammalian enterocyte with sufficient affinity or avidity to initiate endocytosis or phagocytosis, the target molecule being an endocytosis- or phagocytosis- promoting receptor.
Dependencies are inferred from the claim text.