Synthesis of Size‐Tunable Hollow Polypyrrole Nanostructures and Their Assembly into Folate‐Targeting and pH‐Responsive Anticancer Drug‐Delivery Agents. Issue 68 (14th November 2017)

• Record Type: Journal Article
• Authors: Chen, Jian; Li, Xiufang; Sun, Yanhua; Hu, Yuwei; Peng, Yulong; Li, Yimin; Yin, Gang; Liu, Hui; Xu, Jiangfeng; Zhong, Shian
• Is Part Of: Chemistry. Volume 23:Issue 68(2017)
• Page Start: 17279
• Page End: 17289
• Publication Date: 2017-11-14
• Subjects: cancer -- drug delivery -- nanotubes -- polymers -- template synthesis; Chemistry -- Periodicals; 540
• DOI: 10.1002/chem.201702945
• Languages: English
• ISSNs: 0947-6539

Abstract

Abstract: Chemotherapeutic drugs currently used in clinical settings have high toxicity, low specificity, and short half‐lives. Herein, polypyrrole‐based anticancer drug nanocapsules were prepared by tailoring the size of the nanoparticles with a template method, controlling drug release by means of an aromatic imine, increasing nanoparticle stability through PEGylation, and improving tumor‐cell selectivity by folate mediation. The nanoparticles were characterized by TEM and dynamic light scattering. α‐Folate receptor expression levelsof tumor cells and normal cells were investigated by western blot and quantitative polymerase chain reaction analyses. Flow cytometry and fluorescence imaging were used to verify the cell uptake of the different‐sized nanoparticles. From the different‐sized polypyrrole nanoparticles, the optimally functionalized nanoparticles of 180 nm hydrodynamic diameter were chosen and further usedfor in vitroandin vivotests. The nanoparticles showed excellent biocompatibility and the drug‐loaded nanoparticles exhibited effective inhibition of tumor cell growth in vitro. Moreover, the drug‐loaded nanoparticles showed substantially enhanced accumulation in tumor regions and effectively inhibitedin vivotumor growth. Furthermore, the nanoparticles showed reduced doxorubicin‐induced toxicity andno significant side effects in normal organs of tumor‐bearing mice, as measured by body‐weight shifts and evaluationof drug distribution. Overall, the functionalized nanoparticles are promising nanocarriers for tumor‐targeting drug delivery. Abstract : Anticancer nanocapsules : By using a template method, polypyrrole (PPy)@tetra‐arm aldehyde (TAA)@polyethylene glycol (PEG)@folate (FA) nanoparticle drug carriers were synthesized (see figure). In vitro cytotoxicity assays showed that doxorubicin (Dox)‐loaded PPy@TAA@PEG@FA nanoparticles induced death of Skov3 tumor cells, and in vivo studies demonstrated that Dox/PPy@TAA@PEG@FA nanoparticles exhibited higher antitumor activity than free Dox (see scheme).