An amphiphilic dendrimer-based nanocarrier was designed and synthesized to study the collaboration of two protein stimuli triggered disassembly. On each amphiphilic unit of dendron was attached a hydrophilic pentaethylene glycol (PEG) moiety and a hydrophobic coumarin ester moiety, which allows for the formation of micelle-type assemblies in aqueous milieu with an equilibrium between assembly and its dendron state through hydrophilic-lipophilic balance (HLB). High stability of dendritic assembly makes the equilibrium favor the assembly state, which makes the hydrophobic interior difficult to be accessed by outside trigger. To overcome this, a protein-specific ligand is attached on the terminus of one PEG moiety. This design results in a dendron-protein complex, thus breaking the HLB and shifting the equilibrium to favor the monomer state, and leading to an increased accessibility of hydrophobic ester moiety by outside triggers. An enzyme can liberate a fluorescent form of coumarin that can be detected and quantified. Dye release results have shown that dual triggers boost the initial rate dramatically. We present herein a method of designing a dual stimuli responsive system which will respond with significant dye release only when both stimuli are present. Advantages such as assembly stability and response to primary biological changes, coupled with efficient targeting and faster and complete guest release make this system a promising candidate for applications such as sensing and drug delivery.

Dual protein stimuli triggered dendritic nanocarrier disassembly

247th National Meeting (2014)

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