A Simple Dual-pH Responsive Prodrug-Based Polymeric Micelles for Drug Delivery.
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.
College of Materials, Xiamen University , Xiamen 361005, People's Republic of China.
Jie
J
Mao
College of Materials, Xiamen University , Xiamen 361005, People's Republic of China.
Yang
Y
Li
College of Materials, Xiamen University , Xiamen 361005, People's Republic of China.
Tong
T
Wu
College of Materials, Xiamen University , Xiamen 361005, People's Republic of China.|Fujian Provincial Key Laboratory of Fire Retardant Materials, Xiamen University , Xiamen 361005, People's Republic of China.
Conghui
C
Yuan
College of Materials, Xiamen University , Xiamen 361005, People's Republic of China.|Fujian Provincial Key Laboratory of Fire Retardant Materials, Xiamen University , Xiamen 361005, People's Republic of China.
Birong
B
Zeng
College of Materials, Xiamen University , Xiamen 361005, People's Republic of China.|Fujian Provincial Key Laboratory of Fire Retardant Materials, Xiamen University , Xiamen 361005, People's Republic of China.
Yiting
Y
Xu
College of Materials, Xiamen University , Xiamen 361005, People's Republic of China.|Fujian Provincial Key Laboratory of Fire Retardant Materials, Xiamen University , Xiamen 361005, People's Republic of China.
Lizong
L
Dai
D004317:Doxorubicin; D004337:Drug Carriers; D016503:Drug Delivery Systems; D006863:Hydrogen-Ion Concentration; D008823:Micelles; D011108:Polymers / Q000737:chemistry*; D011355:Prodrugs
D004337:Drug Carriers; D008823:Micelles; D011108:Polymers; D011355:Prodrugs; D004317:Doxorubicin
charge-conversion; controlled release; pH response; polymer-drug conjugate; self-assembly