abstract |
A method for encapsulating one or more therapeutic agents in a neutral lipid nanoparticle, said method comprising the steps of: (a) loading a lipid nanoparticle comprising at least one reducible cationic lipid with the one or more therapeutic agents; and (b) contacting the lipid nanoparticle with one or more reducing agents such that the lipid nanoparticle is neutralized; wherein said reducible cationic lipid has the structure: ** (See formula) ** wherein R1 is a releasable polar head group and is selected from the group consisting of imidazole, guanidine, imine, enamine, amino, optionally an alkyl amino substituted and an optionally substituted pyridyl; wherein R2 is selected from the group consisting of ** (See formula) ** wherein R3 and R4 are each independently selected from the group consisting of an optionally substituted, variably saturated or unsaturated C6-C20 alkyl and a C6- acyl C20 optionally substituted, variably saturated or unsaturated; where n is zero or any positive integer. |