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 functiona...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-l,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 plat-form for cancer therapy and other applications.展开更多
基金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 ）.
文摘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-l,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 plat-form for cancer therapy and other applications.
