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pH‐Responsive Nanoparticles for Controllable Curcumin Delivery: The Design of Polycation Core with Different Structures
Authors:Hailiang Feng  Changrong Wang  Junhui Zhou  Jinjian Liu  Jianhua Zhang  Ruiwei Guo  Jianfeng Liu  Anjie Dong  Liandong Deng
Affiliation:1. Department of Polymer Science and Technology, Key Laboratory of Systems Bioengineering of the Ministry of Education, School of Chemical Engineering and Technology, Tianjin University, Tianjin, China;2. Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Tianjin, China;3. Tianjin Key Laboratory of Radiation and Molecular Nuclear Medicine, Institute of Radiation Medicine, Chinese Academy of Medical Science and Peking Union College, Tianjin, China
Abstract:To achieve low leakage at pH 7.4, pH‐controlled drug release remains a major challenge of cancer nanomedicine. Here, pH‐responsive mPEG113b‐polycaprolactone (PCL)xb‐PAEMAy (PELAx) nanoparticles (NPs)‐pH7.4 with different poly(2‐azepane ethyl methacrylate) (PAEMA) lengths and PELA4 nanoparticles (NPs)‐pHx with different pH conditions of preparing NPs based on mPEG113b‐PCLxb‐PAEMAy are prepared to investigate influences of PAEMA lengths and pH condition of preparing NPs on properties of NPs. PELAx NPs‐pH7.4 and PELA4 NPs‐pHx both undergo differently sharp property changes of size, charge, pH‐responsive drug release, cellular uptake, and cytotoxicity, because of the protonation of PAEMA block (pKa ≈ 6.5–6.7). Among PELAx NPs‐pH7.4 and PELA4 NPs‐pHx, it can be found that the NPs prepared at pKa value of PAEMA exhibited exciting pH‐responsive drug release, improving cellular uptake ability and obvious high cytotoxicity toward HepG‐2 cells. This system not only holds great potential for drug delivery but also provides a new strategy to prepare pH‐responsive NPs.
Keywords:curcumin delivery  drug delivery systems  PAEMA  pH‐responsive release  polycation core structures
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