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| 1 | Synthesis of multifunctional ABC stars with a reduction-labile arm by consecutive ROP, RAFT and ATRP processes显示文摘This study aims at versatile synthesis of 3-arm ABC-type(A=poly(?-caprolactone), PCL; B=poly(N-isopropylacrylamide), PNIPAM; C=poly(tert-butyl acrylate), Pt BA, or poly(acrylic acid), PAA) miktoarm star copolymers with a reducible disulfide linkage. Using 2-((2-((2-hydroxymethyl-2-((2-bromo-2-methyl)propionyloxy)methyl)propionyloxy)ethyl)disulfanyl)ethyl 4-cyano-4-(phenylcarbonothioylthio)pentanoate(HBCP) as a heterotrifunctional initiator, consecutive ring-opening polymerization(ROP) of ?-caprolactone(CL), reversible addition-fragmentation chain transfer(RAFT) polymerization of N-isopropylacrylamide(NIPAM) and atom transfer radical polymerization(ATRP) of tert-butyl acrylate(t BA) afforded ABC1 star, and followed by a subsequent hydrolysis to give ABC2 star. 1H nuclear magnetic resonance(1H NMR) and gel permeation chromatography(GPC) analyses revealed the desired stars and their precursors had well-controlled molecular weight and relatively low polydispersity(PDI?1.12). As confirmed by GPC analysis, the disulfide linkage in ABC1 star could be efficiently cleaved upon reductive stimulus, during which the topology was converted from star terpolymer to mixtures of homopolymer(B) and diblock copolymer(AC1). In addition to acting as nanocarriers for stimuli-triggered drug delivery systems, ABC stars with terminal bromide, dithiobenzoate and hydroxyl functionalities are expected to form other reduction-cleavable multicomponent copolymers such as(BC-graft-A)m and dendritic graft copolymers via postpolymerization modification. Our research affords a straightforward 'core-first' method to construct multifunctional star terpolymers with stimuli-responsive arms and reduction-labile linkage. | Huanhuan Liu Dandan Tang Rupei Tang Youliang Zhao | 2015 | Science China Chemistry2015，58，11： | 2 |
| 2 | Synthesis of new conjugted polyfluorene derivatives bearing triphenylamine moiety through a vinylene bridge and their stable blue electroluminescence显示文摘 | Tang Rupei Tan Zhaoao Li Yongfang | 2006 | Chem Mater2006，18，4： | 1 |
| 3 | Preparation and Aggregation of Polypseudorotaxane from Dendronized Poly(Methacrylate)-Poly(Ethylene Oxide) Diblock Copolymer and α-Cyclodextrin显示文摘 | CHENG Cai-xia TANG Rupei XI Fu | 2005 | Macromol Rapid Commun2005，26，： | 1 |
| 4 | Dialdehyde starch-crosslinked chitosan films and their antimicrobial effects显示文摘 | Tang Rupei Du Yumin Fan Lihong | 2003 | Jof Polym Sci Part B Polym Phys2003，41，9： | 1 |
| 5 | Synthesis, electroluminescence, and photovoltaic properties of dendronized poly(p-phenylene vinylene) derivatives 显示文摘 | Tang Rupei Tan Zhanao Cheng Caixia | 2005 | Polymer2005，46，14： | 1 |
| 6 | Synthesis, characterization, and electroluminescent properties of pyridi-nylene vinylene-modified phenylene vinylene copolymers显示文摘 | Tang Rupei Zhang Wenqing Qian Deping | 2012 | J Electron Mater2012，41，9： | 1 |
| 7 | Preparation and Characterization of Soy Protein Isolate-carboxymethylated Konjac Glucomannan Blend Films 显示文摘 | Tang Rupei Du Yumin Zheng Hua | 2003 | Journal of Applied Polymer Science2003，88，5： | 1 |
| 8 | Synthesis of new conjugated polyfluorene derivatives bearing triphenylamine moiety through a vinylene bridge and their stable blue electroluminescence显示文摘 | Tang Rupei Tan Zhaoao Li Yongfang | 2006 | Chem Mater2006，18，4： | 1 |
| 9 | Carrier-free prodrug nanoparticles based on dasatinib and cisplatin for efficient antitumor in vivo显示文摘Carrier-free drug self-delivery systems consisting of amphiphilic drug-drug conjugate(ADDC)with well-defined structure and nanoscale features have drawn much attention in tumor drug delivery.Herein,we report a simple and effective strategy to prepare ADDC using derivatives of cisplatin(CP)and dasatinib(DAS),which further selfassembled to form reduction-responsive nanoparticles(CP-DDA NPs).DAS was modified with succinic anhydride and then connected with CP derivative by ester bonds.The size,micromorphology and in vitro drug release of CP-DDA NPs were characterized.The biocompatibility and bioactivity of these carrier-free nanoparticles were then investigated by HepG2 cells and H22-tumor bearing mice.In vitro and in vivo experiments proved that CPDDA NPs had excellent anti-tumor activity and significantly reduced toxicities.This study provides a new strategy to design the carrier-free nanomedicine composed of CP and DAS for synergistic tumor treatment. | Lu Yang Jiaxi Xu Zheng Xie Faquan Song Xin Wang Rupei Tang | 2021 | Asian Journal of Pharmaceutical Sciences2021，16，6： | 0 |
| 10 | pH-sensitive micelles self-assembled from star-shaped TPGS copolymers with ortho ester linkages for enhanced MDR reversal and chemotherapy显示文摘TPGS approved by FDA can be used as a P-gp inhibitor to effectively reverse multi-drug resistance(MDR)and as an anticancer agent for synergistic antitumor effects.However,the comparatively high critical micelle concentration(CMC),low drug loading(DL)and poor tumor target limit its further clinical application.To overcome these drawbacks,the pH-sensitive star-shaped TPGS copolymers were successfully constructed via using pentaerythritol as the initial materials,ortho esters as the pH-triggered linkages and TPGS active-ester as the terminated MDR material.The amphiphilic star-shaped TPGS copolymers could self-assemble into free and doxorubicin(DOX)-loaded micelles at neutral aqueous solutions.The micelles exhibited the lower CMC(8.2×10^(−5) mg/ml),higher DL(10.8%)and long-term storage and circulation stability,and showed enhanced cellular uptake,apoptosis,cytotoxicity,and growth inhibition for in vitro MCF-7/ADR and/or MCF-7/ADR multicellular spheroids and in vivo MCF-7/ADR tumors via efficiently targeted drug release at tumoral intracellular pH(5.0),MDR reversal of TPGS,and synergistic effect of DOX and TPGS.Therefore,the pH-sensitive micelles self-assembled from star-shaped TPGS copolymers with ortho ester linkages are potentially useful to clinically transform for enhanced MDR cancer treatment. | Yong Xu Shi Wang Longshun Yang Yuhang Dong Yafang Zhang Guoqing Yan Rupei Tang | 2021 | Asian Journal of Pharmaceutical Sciences2021，16，3： | 0 |
| 11 | pH-triggered dynamic erosive small molecule chlorambucil nano-prodrugs mediate robust oral chemotherapy显示文摘Currently,the dynamic erosive small molecule nano-prodrug is of great demand for oral chemotherapy,owing to its precise structure,high drug loading and improved oral bioavailability via overcoming various physiologic barriers in gastrointestinal tract,blood circulation and tumor tissues compared to other oral nanomedicines.Herein,this work highlights the successful development of pH-triggered dynamic erosive small molecule nano-prodrugs based on in vivo significant pH changes,which are synthesized via amide reaction between chlorambucil and star-shaped ortho esters.The precise nano-prodrugs exhibit extraordinarily high drug loading(68.16%),electric neutrality,strong hydrophobicity,and dynamic large-to-small size transition from gastrointestinal pH to tumoral pH.These favorable physicochemical properties can effectively facilitate gastrointestinal absorption,blood circulation stability,tumor accumulation,cellular uptake,and cytotoxicity,therefore achieving high oral relative bioavailability(358.72%)and significant tumor growth inhibition while decreasing side effects.Thus,this work may open a new avenue for robust oral chemotherapy attractive for clinical translation. | Xin Liu Zhexiang Wang Xiaodie Ren Xinyang Chen Jinjin Tao Yuanhui Guan Xuefeng Yang Rupei Tang Guoqing Yan | 2023 | Asian Journal of Pharmaceutical Sciences2023，18，4： | 0 |
| 12 | Dual-stimuli-sensitive poly(ortho ester disulfide urethanes)-based nanospheres with rapid intracellular drug release for enhanced chemotherapy显示文摘Herein, new poly(ortho ester disulfide urethanes)(POEDU) and poly(ortho ester urethanes)(POEU) were successfully synthesized via polycondensation between active esters of 1,6-hexandiol(HD) and dual-stimuli-sensitive ortho ester disulfide diamine or p H-senstive ortho ester diamine. The corresponding POEDU and POEU nanospheres were easily fabricated using an oil-in-water emulsion technique. In vitro degradation experiments indicated that POEDU nanospheres degraded faster than POEU nanospheres in mildly acidic and reductive environments. Doxorubicin(DOX) as a model antitumor drug was successfully incorporated into these nanospheres to give DOX-loaded nanoparticles(POEDU-DOX and POEU-DOX). In vitro drug release studies showed that release of DOX from dual-stimuli-sensitive POEDU-DOX was accelerated compared with release from the p H-sensitive POEU-DOX under DL-dithiothreitol(DTT) and mildly acidic conditions. In addition, in vitro uptake and cytotoxicity assays revealed that POEDU-DOX exhibited more efficient antitumor effect than POEU-DOX did against both twodimensional(2 D) cells and three-dimensional(3 D) multicellular tumor spheroids(MCTS). Finally, in a mice H22 tumor model,POEDU-DOX exhibited preferable antitumor capability. In conclusion, the pH and redox dual-stimuli-sensitive POEDU nanospheres can be superior drug carriers for cancer treatment. | Yan Huang Jiejie Qin Jun Wang Guoqing Yan Xin Wang Rupei Tang | 2018 | Science China Chemistry2018，61，11： | 0 |
| 13 | Self-assembled ternary hybrid nanodrugs for overcoming tumor resistance and metastasis显示文摘Traditional chemotherapy exhibits a certain therapeutic effect toward malignant cancer,but easily induce tumor multidrug resistance(MDR),thereby resulting in the progress of tumor recurrence or metastasis.In this work,we deigned ternary hybrid nanodrugs(PEI/DOX@CXB-NPs)to simultaneously combat against tumor MDR and metastasis.In vitro results demonstrate this hybrid nanodrugs could efficiently increase cellular uptake at pH 6.8 by the charge reversal,break lysosomal sequestration by the proton sponge effect and trigger drugs release by intracellular GSH,eventually leading to higher drugs accumulation and cell-killing in drug-sensitive/resistant cells.In vivo evaluation revealed that this nanodrugs could significantly inhibit MDR tumor growth and simultaneously prevent A549 tumor liver/lung metastasis owing to the specifically drugs accumulation.Mechanism studies further verified that hybrid nanodrugs were capable of down-regulating the expression of MDR or metastasis-associated proteins,lead to the enhanced anti-MDR and anti-metastasis effect.As a result,the multiple combination strategy provided an option for effective cancer treatment,which could be potentially extended to other therapeutic agents or further use in clinical test. | Xu Cheng Dapeng Li Jiaxi Xu Bing Wei Qin Fang Longshun Yang Yanbing Xue Xin Wang Rupei Tang | 2021 | Acta Pharmaceutica Sinica B2021，11，11： | 0 |
| 14 | Dynamic crosslinked polymeric nano-prodrugs for highly selective synergistic chemotherapy显示文摘To achieve highly selective synergistic chemotherapy attractive for clinical translation,the precise polymeric nano-prodrugs(PPD-NPs)were successfully constructed via the facile crosslinking reaction between p H-sensitive poly(ortho ester)s and reduction-sensitive small molecule synergistic prodrug(Pt(IV)-1).PPD-NPs endowed the defined structure and high drug loading of cisplatin and demethylcantharidin(DMC).Moreover,PPD-NPs exhibited steady long-term storage and circulation via the crosslinked structure,suitable negative potentials and low critical micelle concentration(CMC),improved selective tumour accumulation and cellular internalization via dynamic size transition and surficial amino protonation at tumoural extracellular p H,promoted efficient disintegration and drug release at tumoural intracellular p H/glutathione,and enhanced cytotoxicity via the synergistic effect between cisplatin and DMC with the feed ratio of 1:2,achieving significant tumour suppression while decreasing the side effects.Thus,the dynamic crosslinked polymeric nano-prodrugs exhibit tremendous potential for clinically targeted synergistic cancer therapy. | Shi Wang Yining Song Jingge Ma Xinyang Chen Yuanhui Guan Hui Peng Guoqing Yan Rupei Tang | 2022 | Asian Journal of Pharmaceutical Sciences2022，17，6： | 0 |
| 15 | Dynamic micelles with detachable PEGylation at tumoral extracellular pH for enhanced chemotherapy显示文摘Although surface PEGylation of nanomedicines can decrease serum protein adsorption in vivo,it also blocks uptake by tumor cells.This dilemma could be overcome by employing detachably PEGylated strategy at tumoral extracellular microenvironment to achieve improved cellular uptake while prolonged circulation times.Herein,the amphiphilic graft copolymers with p H-sensitive ortho ester-linked m PEG in side chains and polyurethanes in backbone,can self-assemble into the free and doxorubicin(DOX)-loaded micelles.The p H-sensitive micelles could undergo several characteristics as follows:(i)PEGylated shells for stability in sodium dodecyl sulfonate(SDS)solution;(ii)De PEGylation via degradation of ortho ester linkages at tumoral extracellular pH(6.5)for gradually dynamic size changes and effective release of DOX;and(iii)enhanced cellular uptake and cytotoxicity via positive DOX.Moreover,the dynamic micelles with detachable PEGylation could quickly penetrate the centers of SH-SY5 Y multicellular spheroids(MCs)and strongly inhibit tumor growth in vitro and in vivo,and might be considered as promising and effective drug carriers in tumor therapy. | Guoqing Yan Panpan Zhang Jun Wang Xin Wang Rupei Tang | 2020 | Asian Journal of Pharmaceutical Sciences2020，15，6： | 0 |
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