A Simple Dual-pH Responsive Prodrug-Based Polymeric Micelles for Drug Delivery

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• 作者：Jie Mao ; Yang Li ; Tong Wu ; Conghui Yuan ; Birong Zeng ; Yiting Xu ; Lizong Dai
• 刊名：ACS Applied Materials & Interfaces
• 出版年：2016
• 出版时间：July 13, 2016
• 年：2016
• 卷：8
• 期：27
• 页码：17109-17117
• 全文大小：623K
• 年卷期：0
• ISSN：1944-8252

文摘

To precisely deliver drug molecules at a targeted site and in a controllable manner, there has been great interest in designing a synergistical drug delivery system that can achieve both surface charge-conversion and controlled release of a drug in response to different stimuli. Here we outline a simple method to construct an intelligent drug carrier, which can respond to two different pH values, therefore achieving charge conversion and chemical-bond-cleavage-induced drug release in a stepwise fashion. This drug carrier comes from the self-assembly of a block copolymer-DOX conjugate synthesized through a Schiff base reaction between poly(2-(diisopropylamino)ethyl methacrylate-b-poly(4-formylphenyl methacrylate-co-polyethylene glycol monomethyl ether methacrylate) (PDPA-b-P(FPMA-co-OEGMA)) and DOX. The surface charge of the BCP-DOX micelles reversed from negative to positive when encountering a weakly acidic environment due to the protonation of PDPA segments. In vitro cellular uptake measurement shows that the cellular uptake and internalization of the BCP-DOX micelles can be significantly enhanced at pH ∼ 6.5. Moreover, this drug carrier exhibits a pH-dependent drug release owing to the cleavage of the imine bond at pH < 5.5. With this dual-pH responsive feature, these micelles may have the ability to precisely deliver DOX to the cancer cells.