Method and compositions for lipidization of hydrophilic molecule

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

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514 2, 514 9, 514 19, 514 23, 530300, 530303, 530307, 530315, 530317, 530331, 530333, 530350, A61K 3828

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060936924

ABSTRACT:
Fatty acid derivatives of disulfide-containing compounds (for example, disulfide-containing peptides or proteins) comprising fatty acid-conjugated products with a disulfide linkage are employed for delivery of the compounds to mammalian cells. This modification markedly increases the absorption of the compounds by mammalian cells relative to the rate of absorption of the unconjugated compounds, as well as prolonging blood and tissue retention of the compounds. Moreover, the disulfide linkage in the conjugate is quite labile in vivo and thus facilitates intracellular or extracellular release of the intact compounds from the fatty acid moieties.

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