pH sensitive lipids based on ortho ester linkers,...

Details pH sensitive lipids based on ortho ester linkers,... pH sensitive lipids based on ortho ester linkers,...

2005-05-24

2005-05-24

Nguyen, Dave T. (Department: 1635)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

C514S04400A, C424S450000

Reexamination Certificate

active

06897196

ABSTRACT:
The invention comprises lipid derivatives that rapidly degrade in the pH range from 4.0 to 7.0 and lipidic delivery systems that contain them. These lipid derivatives can be used to modify the delivery properties of the lipidic delivery systems to enable prolonged circulation times or more rapid drug unloading in the target tissue. The lipid derivatives are amphipathic compounds comprising a hydrophilic head group joined to a hydrophobic group by an acid-labile ortho ester linkage. The delivery systems of the invention exhibit degradation of less than 10% within 3 hours at a pH of 7.4 and degradation greater than 50% within 60 min at a pH of 5.0.

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