pH-Responsive Polycarbonate Copolymer-based Nanoparticles for Targeted Anticancer Drug Delivery

doi:10.1007/s40242-018-8147-5

高等学校化学研究 ›› 2018, Vol. 34 ›› Issue (6): 1041-1050.doi: 10.1007/s40242-018-8147-5

pH-Responsive Polycarbonate Copolymer-based Nanoparticles for Targeted Anticancer Drug Delivery

LI Yunxia¹, DU Wenjuan², FU Zhiguang¹, WANG Huanhuan¹, WANG Jiexin³, LE Yuan³, ZHANG Jianjun³, WEN Ning¹

1. Department of Stomatology, the General Hospital of Chinese PLA, Beijing 100853, P. R. China;
2. Department of Oncology, the General Hospital of Chinese PLA, Beijing 100853, P. R. China;
3. College of Chemical Engineering, Beijing University of Chemical Technology, Beijing 100029, P. R. China

收稿日期:2018-05-07 出版日期:2018-12-01 发布日期:2018-09-29
通讯作者: ZHANG Jianjun, WEN Ning E-mail:wenningchn@163.com;zhangjj@mail.buct.edu.cn
基金资助:
Supported by the National High Technolgy Researeh and Development Program of China(No.2013AA032201), the National Natural Science Foundation of China(Nos.81703003, 51303009, 21476018, 21622601) and the National Key R&D Program of China(No.2015CB932101).

pH-Responsive Polycarbonate Copolymer-based Nanoparticles for Targeted Anticancer Drug Delivery

LI Yunxia¹, DU Wenjuan², FU Zhiguang¹, WANG Huanhuan¹, WANG Jiexin³, LE Yuan³, ZHANG Jianjun³, WEN Ning¹

1. Department of Stomatology, the General Hospital of Chinese PLA, Beijing 100853, P. R. China;
2. Department of Oncology, the General Hospital of Chinese PLA, Beijing 100853, P. R. China;
3. College of Chemical Engineering, Beijing University of Chemical Technology, Beijing 100029, P. R. China

Received:2018-05-07 Online:2018-12-01 Published:2018-09-29
Contact: ZHANG Jianjun, WEN Ning E-mail:wenningchn@163.com;zhangjj@mail.buct.edu.cn
Supported by:
Supported by the National High Technolgy Researeh and Development Program of China(No.2013AA032201), the National Natural Science Foundation of China(Nos.81703003, 51303009, 21476018, 21622601) and the National Key R&D Program of China(No.2015CB932101).

摘要/Abstract

摘要： A smart polycarbonate(PCA) copolymer-based nanoparticle(NanoPCA) with pH-responsive, long-term stability, and tumor targeting ability was successfully developed by synthesizing and assembling a series of functional PCA-based copolymers including poly(2-amino-1,3-propanediol carbonate-co-L-lactide)[P(CA-co-LA)], poly(2-amino-1,3-propanediol carbonate-co-L-lactide)-g-methoxy-poly(ethylene glycol)[P(CA-co-LA)-g-MPEG], and poly(2-amino-1,3-propanediol carbonate-co-L-lactide)-g-poly(ethylene glycol)-cyclic(Arg-Gly-Asp-D-Phe-Lys)[P(CA-co-LA)-g-PEG-cRGD] for targeted anticancer drug delivery. pH-Responsive studies demonstrated that the loading doxorubicin(DOX) released faster from NanoPCA at acidic conditions due to protonation effects of P(CA-co-LA) copolymers. Furthermore, the in vitro and in vivo investigations demonstrate that the DOX-loaded NanoPCA exhibited significant tumor targeting ability, outstanding antitumor effect and excellent biological safety in the treatment of oral squamous cell carcinoma(OSCC). Therefore, this work provides a promising drug delivery platform for cancer therapy and other applications.

关键词: Polycarbonate copolymer-based nanoparticle(NanoPCA), pH-Responsive, Tumor targeting ability, Oral squamous cell carcinoma(OSCC)

Abstract: A smart polycarbonate(PCA) copolymer-based nanoparticle(NanoPCA) with pH-responsive, long-term stability, and tumor targeting ability was successfully developed by synthesizing and assembling a series of functional PCA-based copolymers including poly(2-amino-1,3-propanediol carbonate-co-L-lactide)[P(CA-co-LA)], poly(2-amino-1,3-propanediol carbonate-co-L-lactide)-g-methoxy-poly(ethylene glycol)[P(CA-co-LA)-g-MPEG], and poly(2-amino-1,3-propanediol carbonate-co-L-lactide)-g-poly(ethylene glycol)-cyclic(Arg-Gly-Asp-D-Phe-Lys)[P(CA-co-LA)-g-PEG-cRGD] for targeted anticancer drug delivery. pH-Responsive studies demonstrated that the loading doxorubicin(DOX) released faster from NanoPCA at acidic conditions due to protonation effects of P(CA-co-LA) copolymers. Furthermore, the in vitro and in vivo investigations demonstrate that the DOX-loaded NanoPCA exhibited significant tumor targeting ability, outstanding antitumor effect and excellent biological safety in the treatment of oral squamous cell carcinoma(OSCC). Therefore, this work provides a promising drug delivery platform for cancer therapy and other applications.

Key words: Polycarbonate copolymer-based nanoparticle(NanoPCA), pH-Responsive, Tumor targeting ability, Oral squamous cell carcinoma(OSCC)

LI Yunxia, DU Wenjuan, FU Zhiguang, WANG Huanhuan, WANG Jiexin, LE Yuan, ZHANG Jianjun, WEN Ning. pH-Responsive Polycarbonate Copolymer-based Nanoparticles for Targeted Anticancer Drug Delivery[J]. 高等学校化学研究, 2018, 34(6): 1041-1050.

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pH-Responsive Polycarbonate Copolymer-based Nanoparticles for Targeted Anticancer Drug Delivery

pH-Responsive Polycarbonate Copolymer-based Nanoparticles for Targeted Anticancer Drug Delivery

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