Vitamin E conjugates, and their uses as antioxidants and prodrug delivery vehicles

William Baumgartner, Benedict, Dirk, Astete, Carlos E, Sabliov, Cristina M.  |  6/13/2017 6:43:28 PM

Astete, Carlos E.; Sabliov, Cristina M.; Spivak, David
Patent Status: Issued
Issue Date: 12/29/2015
Patent Number: 9,220,787

Abstract:
Tocopherol conjugates are disclosed that are useful as antioxidants or as pro-drug delivery vehicles. The conjugates are amphiphilic, and tend to localize at the interface between water domains and lipid domains. A prototype embodiment disclosed is an alpha tocopherol-linker-carnosine conjugate that has been designated VECAR.

Description:
We have discovered novel conjugates of vitamin E that are useful, for example, as antioxidants or as pro-drug delivery vehicles. The conjugates are amphiphilic, and tend to localize at the interface between water domains and lipid domains. Vitamin E is covalently conjugated with a hydrophilic antioxidant, for example carnosine, joined by a bio-stable linker. The resulting conjugates possess potent antioxidant properties, and can inhibit oxidation in polyunsaturated fatty acids (PUFAs) and LDL [Low-density lipoprotein].

The limitations of lipophilic natural antioxidants have been overcome with the novel antioxidants, which may be formed by covalently conjugating a hydrophobic antioxidant with a hydrophilic antioxidant, joined by a bio-stable linker. The hydrophobic component, the hydrophilic component, or both may be natural-occurring antioxidants. The novel structure provides better antioxidant performance in both the hydrophilic and hydrophobic regimes (e.g., in both the hydrophilic and the hydrophobic portions of LDL particles). The novel structure affords synergetic effects from antioxidant-coantioxidant interactions.

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