Controlling release from the lipidic cubic phase by selective alkylation

摘要: The lipidic cubic phase can be viewed as a molecular sponge consisting of interpenetrating nanochannels filled with water and coated by lipid bilayers. It has been used delivery matrix for low-molecular-weight drugs. For those that are water-soluble, release is fast unregulated. This study seeks to exploit the bilayer compartment location within in which 'hydrophobically' anchor water-soluble drug. was accomplished controlling partitioning into, thus from, aqueous phase. Tryptophan surrogate drug alkylation implemented regulate release. By adjusting alkyl chain length, exquisite control realized. Without alkylation, 20% tryptophan released under standard conditions (infinite sink 30-mg source at pH 7 20 degrees C) over period 30 min (t(20)). In case derivatives chains two eight carbon atoms long, t(20) values 3 13 days, respectively, were observed. Eliminating charge on completely produced derivative became irreversibly lodged bilayer. behavior short-chain mathematically modeled parameters describing transport have obtained. Cubic partition coefficients its measured facilitate modeling. implications these findings regard related systems, vaccine efficacy discussed.