Core crosslinkable polymeric micelles from PEG-lipid amphiphiles as drug carriers

Core crosslinkable micelles were prepared based on PEG - lipid amphiphiles. The branched hydrophobic domain was prepared by acylation of 2,2-bis( hydroxymethyl) propionic acid ( DMPA) with 10-undecenoyl chloride and pyridine as catalyst. Monohydroxyl poly( ethylene glycol) (m-PEG) was conjugated onto the hydrophobic domain to form the branched polymeric amphiphiles. Following micelle formation of the amphiphiles, the vinylic groups at the peripheral ends of the 10-undecenoyl acid chains were polymerized with AIBN to crosslink the hydrophobic domains in aqueous solution. The solution properties of the crosslinked micelles were evaluated in various solvents and temperatures; relative to the uncrosslinked micelle controls, the core crosslinked micelles demonstrated improved thermodynamic stability in solution to high temperatures and nonselective solvents. Furthermore, the core crosslinked micelles show much higher drug loading capacity ( nearly 80 wt%) than the uncrosslinked micelles (ca. 10 wt%).