pH-sensitive polyion complex micelles for tunable intracellular drug delivery

来源 :The Third Symposium on Innovative Polymers for Controlled De | 被引量 : 0次 | 上传用户:qncy1230s
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  The capability of smart response to the extracellular or intracellular microenviroments,such as overexpressed enzymes,and glutathione and pH differences,has become a necessary character of the anticancer drug delivery nanovehicles in recent years [1-3].In this work,four pH-responsive DOX-loaded polyion complex (PIC) micelles (noted as SAD,CDAD,CAD and DMMAD) were prepared for adjustable intracellular drug delivery.As shown in Scheme 1,due to the difference in the amide bond linkages,these PIC micelles were proved to have gradient pH-sensitivity in the following order:(a) SAD < (b) CDAD < (c) CAD < (d) DMMAD.As soon as the DOX-loaded micelles finally reached the acidic intmcellular microenvironment,the degradable amide bonds were cleaved with different rates.The negatively charged block copolymers became positively charged,thus the PIC micelles dissociated due to electrostatic repulsion and released the payload with different rates.The in vitro drug release rate was consistent with the sensitivity order of the PIC micelles.The cell uptakes and cytotoxicities of the PIC micelles can also be adjusted by the sensitivities ofcopolymers.
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