Bolaamphiphilic compounds, compositions and uses thereof
AssigneeLauren Sciences LLC
InventorsCharles Linder, Sarina Grinberg, Eliahu Heldman
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Abstract
Bolaamphiphilic compounds are provided according to formula I: HG2-L1-HG1 I where HG1, HG2 and L1 are as defined herein. Provided bolaamphiphilic compounds and the pharmaceutical compositions thereof are useful for delivering HIV active drugs into animal or human brain.
Claims5
A formulation containing vesicles comprising one or more bolaamphiphilic compounds, cholesteryl hemisuccinate, cholesterol, stearyl amine, and an active agent which is tenofovir or fosamprenavir ({[(2R,3S)-1-[N-(2-methylpropyl)(4-aminobenzene)sulfonamido]-3-({[(3S)-oxolan-3-yloxy]carbonyl}amino)-4-phenylbutan-2-yl]oxy}phosphonic acid), wherein the pH has been adjusted to a pH of 7.5 or 8 using a buffer to maximize tenofovir encapsulation
- wherein for 1 mL of formulation the components are:
- 10 mg GLH 19 and GLH 20 in a ratio of 2/1, 1 mg GLH-55b, 2.4 mg cholesteryl hemisuccinate, 1.6 mg cholesterol, 2.5 mg stearyl amine, and 5 mg tenofovir or fosamprenavir ({[(2R,3S)-1-[N-(2-methylpropyl)(4-aminobenzene)sulfonamido]-3-({[(3S)-oxolan-3-yloxy]carbonyl}amino)-4-phenylbutan-2-yl]oxy}phosphonic acid);
- and the buffer is a HEPES, wherein
- GLH 19 is
- wherein
- HG is
- each p1 and p2 is an integer from 1-400, and R7a is H or an acyl group.
Dependencies are inferred from the claim text.