pH-Sensitive Vesicles with Tunable Membrane Permeability for Drug Delivery

By synergizing multiscale simulations, we investigate the assembly of amphiphilic copolymers PAE-g-PEGLA into vesicles and the loading/release of DOX∙HCl. During the formation of bilayer-structured vesicles, the interior size and membrane thickness are substantially affected by the exchange rate between tetrahydrafuran and water. At pH = 7, DOX∙HCl is loaded into the vesicle interior and the loading efficiency increases with polymer concentration. At pH < 7, PAE blocks are protonated, which tunes membrane permeability for DOX∙HCl release. To mimic controlled release, a mixture of two copolymers is proposed, which form hybrid vesicles and lead to a moderate release rate of DOX∙HCl. After multiple sequential pH variations between acidic and neutral circulatory environment, DOX∙HCl is gradually released from the hybrid vesicles. This study identifies the key factors governing vesicle formation and drug loading/release, and provides bottom-up insights toward the design and optimization of new amphiphilic polymers for high-efficacy drug delivery.

 

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This work has been published in Macromolecules on August 12, 2016 (10.1021/acs.macromol.6b01211)

Corresponding author: Jianwen Jiang ( This email address is being protected from spambots. You need JavaScript enabled to view it. )
Corresponding author Webpage: http://cheed.nus.edu.sg/stf/chejj/