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| 1 | A lipophilic prodrug of Danshensu:preparation,characterization,and in vitro and in vivo evaluation显示文摘Danshensu [3-(3, 4-dihydroxyphenyl) lactic acid, DSS], one of the significant cardioprotective components, is extracted from the root of Salvia miltiorrhiza. In the present study, an ester prodrug of Danshensu(DSS), palmitoyl Danshensu(PDSS), was synthesized with the aim to improve its oral bioavailability and prolong its half-life. The in vitro experiments were carried out to evaluate the physicochemical properties and stability of PDSS. Although the solubility of PDSS in water was only 0.055 mg·mL^(-1), its solubility in Fa SSIF and Fe SSIF reached 4.68 and 9.08 mg·mL^(-1), respectively. Octanol-water partition coefficient(log P) was increased from-2.48 of DSS to 1.90 of PDSS. PDSS was relatively stable in the aqueous solution in pH range from 5.6 to 7.4. Furthermore, the pharmacokinetics in rats was evaluated after oral administration of PDSS and DSS. AUC and t1/2 of PDSS were enhanced up to 9.8-fold and 2.2-fold, respectively, compared to that of DSS. Cmax was 1.67 ± 0.11 μg·mL^(-1) for PDSS and 0.81 ± 0.06 μg·m L-1 for DSS. Thus, these results demonstrated that PDSS had much higher oral bioavailability and longer circulation time than its parent drug. | GUO Xue-Jiao FAN Xue-Jiao QIAO Bin GE Zhi-Qiang | 2017 | Chinese Journal of Natural Medicines2017，15，5： | 5 |
| 2 | PEPT1-mediated prodrug strategy for oral delivery of peramivir显示文摘Peramivir was a novel and highly potent neuraminidase(NA) inhibitor for the treatment of influenza A and B. However, it exhibited a very low oral bioavailability(only 3%) due to the high polarity(log P of-1.4) and the low membrane permeability across the intestine. To utilize the PEPT1-mediated prodrug strategy to improve the oral absorption and develop the oral alternative, seven amino acid ester prodrugs and seven amino acid amide prodrugs have been synthesized. The permeability of these prodrugs across Caco-2 cells were screened. Peramivr-(CH_2)_2-l-Val and Peramivir-l-Ile were of the highest permeability in ester prodrugs and amide prodrugs, respectively, and then they were selected for further studies. Glycylsarcosine(gly-sar) uptake by Caco-2 could be inbihited by Peramivir-(CH_2)_2-l-Val and Peramivir-l-Ile in a concentration-dependent manner, and the IC 50 was 1.34 ± 0.31 m M and 1.78 ± 0.48 m M, respectively. The direct uptake of Peramivir-(CH_2)_2-l-Val and Peramivirl-Ile in MDCK-PEPT1 cells were significantly higher than in MDCK mock cells, and could be markedly inhibited by gly-sar. The uptake of Peramivir-(CH_2)_2-l-Val and Peramivir-l-Ile(0.01 to 50 m M) in MDCK-hPEPT1 cells conformed to Michaelis–Menten Equation. The oral bioavailability of peramivir was 65.3% and 37.3% after the oral administration of Peramivir-(CH_2)_2-l-Val and Peramivir-l-Ile to rats, respectively. The oral absorption and bioactivation of Peramivir-(CH_2)_2-l-Val was rapid and extensive, and no Peramivir-(CH_2)_2-l-Val was found in plasma. Because the amide bond was relatively stable, Peramivir-l-Ile could not be totally converted to the parent drug in vivo. Peramivir-(CH_2)_2-l-Val with good oral profiles and rapid bioactivation might be a promising prodrug for the further clinic development. The present study also corroborated the idea that the PEPT1-mediated prodrug approach has enormous promise for improving the oral absorption of poorly absorbed drug. | Yongbing Sun Wei Gan Mingdao Lei Wei Jiang Meng Cheng Junwei He Qi Sun Wan Liu Lvjiang Hu Yi Jin | 2018 | Asian Journal of Pharmaceutical Sciences2018，13，6： | 4 |
| 3 | Intestinal OCTN2-and MCT1-targeted drug delivery to improve oral bioavailability显示文摘Various drug transporters are widely expressed throughout the intestine and play important roles in absorbing nutrients and drugs,thus providing high quality targets for the design of prodrugs or nanoparticles to facilitate oral drug delivery.In particular,intestinal carnitine/organic cation transporter 2(OCTN2)and mono-carboxylate transporter protein 1(MCT1)possess high transport capacities and complementary distributions.Therefore,we outline recent developments in transporter-targeted oral drug delivery with regard to the OCTN2 and MCT1 proteins in this review.First,basic information of the two transporters is reviewed,including their topological structures,characteristics and functions,expression and key features of their substrates.Furthermore,progress in transporter-targeting prodrugs and nanoparticles to increase oral drug delivery is discussed,including improvements in the oral absorption of anti-inflammatory drugs,antiepileptic drugs and anticancer drugs.Finally,the potential of a dual transporter-targeting strategy is discussed. | Gang Wang Lichun Zhao Qikun jiang Yixin Sun Dongyang Zhao Mengchi Sun Zhonggui He Jin sun Yang Wang | 2020 | Asian Journal of Pharmaceutical Sciences2020，15，2： | 3 |
| 4 | Amino acid transporters: Emerging roles in drug delivery for tumor-targeting therapy显示文摘Amino acid transporters,which play a vital role in transporting amino acids for the biosynthesis of mammalian cells,are highly expressed in types of tumors.Increasing studies have shown the feasibility of amino acid transporters as a component of tumortargeting therapy.In this review,we focus on tumor-related amino acid transporters and their potential use in tumor-targeting therapy.Firstly,the expression characteristics of amino acid transporters in cancer and their relationship with tumor growth are reviewed.Secondly,the recognition requirements are discussed,focusing on the“acidbase”properties,conformational isomerism and structural analogues.Finally,recent developments in amino acid transporter-targeting drug delivery strategies are highlighted,including prodrugs and nanocarriers,with special attention to the latest findings of molecular mechanisms and targeting efficiency of transporter-mediated endocytosis.We aim to offer related clues that might lead to valuable tumor-targeting strategies by the utilization of amino acid transporters. | Ling Zhang Chengguang Sui Wenhan Yang Qiuhua Luo | 2020 | Asian Journal of Pharmaceutical Sciences2020，15，2： | 3 |
| 5 | Facile preparation of pH-responsive PEGylated prodrugs for activated intracellular drug delivery显示文摘PEGylated prodrug,covalent attaching polyethylene glycol(PEG) polymer chains to therapeutic drugs,is one of the most promising techniques to improve the water-solubility,stability,and therapeutic effect of drugs.In this study,three PEGylated acid-sensitive prodrugs DOX-PEG-DOX with different molecular weights,were prepared via Schiff-base reaction between aldehyde-modified PEG and the amino groups of doxorubicin(DOX).This kind of amphiphilic polymeric prodrug could be self-assemble into nanoparticles in aqueous solution.The average particle size and morphologies of the prodrug nanoparticles under different pH conditions were observed by dynamic light scattering(DLS) and transmission electron microscopy(TEM),re s pectively.It turned out that the nanoparticles could be kept stable in the physiological environment,but degraded in acidic medium.Subsequently,we also investigated in vitro drug release behavior and found that the prodrug had acid-sensitive property.The cytotoxicity and intracellular uptake assays revealed that the prodrugs could rapidly internalized by HeLa or HepG2 cells to release DOX and effectively inhibited the proliferation of the tumor cells,which have the potential for use in cancer therapy. | Yue Song Dian Li Jinlin He Mingzu Zhang Peihong Ni | 2019 | Chinese Chemical Letters2019，30，12： | 3 |
| 6 | Kidney-targeted drug delivery systems显示文摘Kidney-targeted drug delivery systems represent a promising technology to improve drug efficacy and safety in the treatment of renal diseases.In this review,we summarize the strategies that have been employed to develop kidney-targeted drug delivery systems.We also describe how macromolecular carriers and prodrugs play crucial roles in targeting drugs to particular target cells in the kidney.New technologies render it possible to create renal targeting conjugates and other delivery systems including nanoparticles and liposomes present promising strategies to achieve the goal of targeting drugs to the kidney. | Peng Zhou Xun Sun Zhirong Zhang | 2014 | Acta Pharmaceutica Sinica B2014，4，1： | 3 |
| 7 | Current prodrug strategies for improving oral absorption of nucleoside analogues显示文摘Nucleoside analogues are first line chemotherapy in various severe diseases:AIDS(acquired immunodeficiency disease syndrome),cytomegalovirus infections,cancer,etc.However,many nucleoside analogues exhibit poor oral bioavailability because of their high polarity and low intestinal permeability.In order to get around this drawback,prodrugs have been utilized to improve lipophilicity by chemical modification of the parent drug.Alternatively,prodrugs targeting transporters present in the intestine have been applied to promote the transport of the nucleoside analogues.Valacyclovir and valganciclovir are two classic valine ester prodrugs transported by oligopeptide transporter 1.The ideal prodrug achieves delivery of a parent drug by attaching a non-toxic moiety that is stable during transport,but is readily degraded to the parent drug once at the target.This article presents advances of prodrug approaches for enhancing oral absorption of nucleoside analogues. | Youxi Zhang Yikun Gao Xiaojing Wen Haiying Ma | 2014 | Asian Journal of Pharmaceutical Sciences2014，9，2： | 3 |
| 8 | The design and synthesis of dextran-doxorubicin prodrug-based pH-sensitive drug delivery system for improving chemotherapy efficacy显示文摘Tumor cells show acidic conditions compared with normal cells,which further inspires scientist to build nanocarrier responsive to tumor microenvironment(TME)for enhancing tumor therapeutic efficacy.Here,we report a pH-sensitive and biocompatible polyprodrug based on dextran-doxorubicin(DOX)prodrug(DOXDT)for enhanced chemotherapy.Highdensity DOX component was covalently decorated on the nanocarrier and the drug molecules could be effectively released in the acidic tumor tissue/cells,improving chemotherapy efficacy.Specifically,a dextran-based copolymer was preliminarily prepared by one-step atom transfer radical polymerization(ATRP);then DOX was conjugated on the copolymer component via pH-responsive hydrazone bond.The structure of DOXDT can be well-controlled.The resulting DOXDT was able to further self-assemble into nanoscale micelles with a hydration diameter of about 32.4 nm,which presented excellent micellar stability.Compared to lipid-based drug delivery system,the DOXDT prodrug showed higher drug load capacity up to 23.6%.In addition,excellent stability and smaller size of the nanocarrier contributed to better tissue permeability and tumor suppressive effects in vivo.Hence,this amphipathic DOXDT prodrug is promising in the development of translational DOX formulations,which would be widely applied in cancer therapy. | Xiaoli Zhang Tian Zhang Xianbin Ma Yajun Wang Yi Lu Die Jia Xiaohua Huang Jiucun Chen Zhigang Xu Feiqiu Wena | 2020 | Asian Journal of Pharmaceutical Sciences2020，15，5： | 3 |
| 9 | Albumin-bound paclitaxel dimeric prodrug nanoparticles with tumor Qr redox heterogeneity-triggered drug release for synergistic photothermal/ chemotherapy显示文摘In spired by the clinically approved albumin based PTX formulatio n(Abraxa ne)and high-drug-loading dimeric prodrug tactics,herein we report a theranostic HAbraxane-likeH prodrug formulation,which is comprised of human serum albumin(HSA),a paclitaxel(PTX)dimer bridged with thioether liner(PTX2-S),and photosensitizer IR780 iodide.Nanoparticles(NPs)with PTX2-S and IR780 as the core and HSA as the stealth shell are formed.Compared with HSA-based PTX clinical formulation(Abraxane),the dimeric molecules not only constitute the bulk structure of the particles,but also act as crossi ng age nt,thus realizing drug loadi ng content in creasi ng from 6.6 wt.%to 48.7 wt.%with high loadi ng efficie ncy(>90%)and excellent stability in biological conditions.Importa ntly,the thioether lin kage dually resp onds to the tumor redox heteroge neity and the NPs gradually releases the pare nt drug PTX for chemotherapy.Mea nwhile,PTX2-S facilitates the en capsulatio n of IR780 iodide due to their π-π stacki ng interaction and IR780 iodide gen erates spatio-temporal hyperthermia un der light irradiation to kill cancer cells for photothermal therapy.The described craft integrates the biomimetic trait of HSA,high drug loading,tumor redox heterogeneity-initiated on-dema nd drug release,and combi nation therapy into one formulati on and the developed nan oparticles are promising for cancer treatment. | Qing Pei Xiuli Hu Xiaohua Zheng Rui Xia Shi Liu Zhigang Xie Xiabin Jing | 2019 | Nano Research2019，12，4： | 3 |
| 10 | Determination of the mitigating effect of colon-specific bioreversible codrugs of mycophenolic acid and aminosugars in an experimental colitis model in Wistar rats显示文摘AIM To design colon-targeted codrugs of mycophenolic acid(MPA) and aminosugars as a safer option to mycophenolate mofetil(MMF) in the management of inflammatory bowel disease. METHODS Codrugs were synthesized by coupling MPA with aminosugars(D-glucosamine and D-galactosamine) using EDCI coupling. The structures were confirmed by infrared radiation, nuclear magnetic resonance, mass spectroscopy and elemental analysis. The release profile of codrugs was extensively studied in aqueous buffers, upper gastrointestinal homogenates, faecal matter and caecal homogenates(in vitro) and rat blood(in vitro). Anti-colitic activity was assessed in 2,4,6-trinitrobezenesulfonic acid-induced colitis in Wistar rats by the estimation of various demarcating parameters. Statistical evaluation was performed by applying one-way and two-way ANOVA when compared with the disease control.RESULTS The prodrugs resisted activation in HCl buffer(pH 1.2) and stomach homogenates of rats with negligible hydrolysis in phosphate buffer(p H 7.4) and intestinal homogenates. Incubation with colon homogenates(in vitro) produced 76% to 89% release of MPA emphasizing colon-specific activation of codrugs and the release of MPA and aminosugars at the site of action. In the in vitro studies, the prodrug of MPA with D-glucosamine(MGLS) was selected which resulted in 68% release of MPA in blood. in vitro studies on MGLS revealed its colon-specific activation after a lag time of 8 h which could be ascribed to the hydrolytic action of N-acyl amidases found in the colon. The synthesized codrugs markedly diminished disease activity score and revived the disrupted architecture of the colon that was comparable to MMF but superior to MPA. CONCLUSION The significant attenuating effect of prodrugs and individual aminosugars on colonic inflammation proved that the rationale of the codrug approach is valid. | Shakuntala Santosh Chopade Suneela Sunil Dhaneshwar | 2018 | World Journal of Gastroenterology2018，24，10： | 2 |
| 11 | 2D-ultrathin MXene/DOXjade platform for iron chelation chemo-photothermal therapy显示文摘An increased demand for iron is a hallmark of cancer cells and is thought necessary to promote high cell proliferation,tumor progression and metastasis.This makes iron metabolism an attractive therapeutic target.Unfortunately,current iron-based therapeutic strategies often lack effectiveness and can elicit off-target toxicities.We report here a dual-therapeutic prodrug,DOXjade,that allows for iron chelation chemo-photothermal cancer therapy.This prodrug takes advantage of the clinically approved iron chelator deferasirox(ExJade®)and the topoisomerase 2 inhibitor,doxorubicin(DOX).Loading DOXjade onto ultrathin 2D Ti_(3)C_(2) MXene nanosheets produces a construct,Ti_(3)C_(2)-PVP@DOXjade,that allows the iron chelation and chemotherapeutic functions of DOXjade to be photo-activated at the tumor sites,while potentiating a robust photothermal effect with photothermal conversion efficiencies of up to 40%.Antitumor mechanistic investigations reveal that upon activation,Ti_(3)C_(2)-PVP@DOXjade serves to promote apoptotic cell death and downregulate the iron depletion-induced iron transferrin receptor(TfR).A tumor pH-responsive iron chelation/photothermal/chemotherapy antitumor effect was achieved both in vitro and in vivo.The results of this study highlight what may constitute a promising iron chelation-based phototherapeutic approach to cancer therapy. | Yunjie Xu Yingwei Wang Jusung An Adam C.Sedgwick Mingle Li Jianlei Xie Weibin Hu Jianlong Kang Sajal Sen Axel Steinbrueck Bin Zhang Lijun Qiao Swelm Wageh Jonathan F.Arambula Liping Liu Han Zhang Jonathan L.Sessler Jong Seung Kim | 2022 | Bioactive Materials2022，7，8： | 2 |
| 12 | Intracellular enzyme-activatable prodrug for real-time monitoring of chlorambucil delivery and imaging显示文摘Carboxylesterase,a necessary enzyme in various mammalian cells,has been employed in various biological applications.Herein,we designed and synthesized a novel carboxylesterase-based prodrug,which can realize simultaneous drug-release imaging and cancer chemotherapy.This prodrug comprises three parts:coumarin as the fluorophore and the cleavable architecture,chlorambucil as the anticancer drug,and acetyl group as the enzyme-responsive unit.The presence of carboxylesterase leads to the activation of coumarin fluorescence,and this fluorescence serves as the reporting signal for assessing the enzyme level and drug release.Moreover,the prodrug was incorporated in liposome for monitoring drug release and chemotherapeutic effect in living cells.Upon internalization by HeLa cells,the prodrug can release chlorambucil and exhibit high cytotoxicity.This approach may provide some helpful insights for enhancing therapeutic effect and tracking the release of prodrug. | Meng Ni Wen-Jun Zeng Xin Xie Ze-Lin Chen Hao Wu Chang-Min Yu Bo-Wen Li | 2017 | Chinese Chemical Letters2017，28，6： | 2 |
| 13 | Cylindrical polymer brushes-anisotropic unimolecular micelle drug delivery system for enhancing the effectiveness of chemotherapy显示文摘Polymer systems can be designed into different structures and morphologies according to their physical and chemical performance requirements,and are considered as one of the most promising controlled delivery systems that can effectively improve the cancer therapeutic index.However,the majority of the polymer delivery systems are designed to be simple spherical nanostructures.To explore morphology/size-oriented delivery performance optimization,here,we synthesized three novel cylindrical polymer brushes(CPBs)by atom transfer radical polymerization(ATRP),which were cellulose-g-(CPT-b-OEGMA)(CCO)with different lengths(~86,~40,and~21 nm).The CPBs are composed of bio-degradable cellulose as the carrier,poly(ethylene glycol)methyl ether methacrylate(OEGMA)as hydrophily block,and glutathione(GSH)-responsive hydrophobic camptothecin(CPT)monomer as loaded anticancer drug.By controlling the chain length of the initiator,three kinds of polymeric prodrugs with different lengths(CCO-1,CCO-2,and CCO-3)could be self-organized into unimolecular micelles in water.We carried out comparative studies of three polymers,whose results verified that the shorter CPBs exhibited higher drug release efficiency,more cellular uptake,and enhanced tumor permeability,accompanied by shortened blood circulation time and lower tumor accumulation.As evidenced by in vivo experiments,the shorter CPBs exhibited higher anti-tumor efficiency,revealing that the size advantage has a higher priority than the anisotropic structure advantage.This provided vital information as to design an anisotropic polymer-based drug delivery system for cancer therapy. | Shuang Bai Die Jia Xianbin Ma Mengyun Liang Peng Xue Yuejun Kang Zhigang Xu | 2021 | Bioactive Materials2021，6，9： | 2 |
| 14 | Synthesis and delivery characteristics of colon-specific dexamethasone prodrug显示文摘Objective: To discuss the possibility of dexamethasone-dextran as a colon-specific dexamethasone prodrug. Methods: Dexamenthasone-dextran conjugate was synthesized with succinate as a cross-linker. The release of dexamethasone was determined after the incubation of the prodrug with the contents of different parts of gastrointestinal(GI) tract of rats. Results: By HPLC analysis, it was shoWn that dexamethasone-dextran contained 9.2 mg dexamethasone per l00 mg dextran. conjugate. During 160 min incubation, the concentration of dexamethasone released in the contents of colon and cecum was 2.7 times as high as that released in the contents of proximal small intestine and distal small intestine. But no dexametha sone was released in the contents of stomach. Conclusion: Dexamethasone-dextran conjugate can be ed as a colon-specific dexamethasone prodrug to selectively deliver the drug to colon. | 周四元 梅其炳 赵德化 | 2000 | Journal of Medical Colleges of PLA(China)2000，15，2： | 2 |
| 15 | pH-Responsive supramolecular DOX-dimer based on cucurbit[8]uril for selective drug release显示文摘A supramolecular dimer of doxorubicin(DOX)was constructed via ternary host-guest interactions between cucurbit[8]uril(CB[8])and tryptophan modified DOX(DOX-Trp,connected with an acid-labile bond)and we demonstrate for the first time that a supramolecular dimer of DOX can be formed upon homo-dimerization by CB[8],which may act as a stimuli pH-responsive,supramolecular DOX dimer prodrug system.This supramolecular DOX dimer transported DOX efficiently and selectively to cancer cells,thereby exhibiting significantly minimized cytotoxicity against noncancerous cells while maintaining effective cytotoxicity against cancer cells.Under this strategy,many other anticancer drugs could be chemically modified and loaded as a dimeric'ammunition'into CB[8]as supramolecular dimer prodrug systems(or a'jet fighter')for improved cancer therapy. | Qian Cheng Shengke Li Yanlong Ma Hang Yin Ruibing Wang | 2020 | Chinese Chemical Letters2020，31，5： | 2 |
| 16 | Development and validation of a UPLC–MS/MS assay for the determination of gemcitabine and its L-carnitine ester derivative in rat plasma and its application in oral pharmacokinetics显示文摘A simple and rapid UPLC–MS/MS method to simultaneously determine gemcitabine and its L-carnitine ester derivative(2’-deoxy-2’, 2’-difluoro-N-((4-amino-4-oxobutanoyl) oxy)-4-(trimethyl amm-onio) butanoate-cytidine, JDR) in rat plasma was developed and validated.The conventional plasma sample preparation method of nucleoside analogues is solidphase extraction(SPE) which is time-consuming and cost-expensive. In this study, gradient elution with small particles size solid phase was applied to effectively separate gemcitabine and JDR, and protein precipitation pretreatment was adopted to remove plasma protein and extract the analytes with high recovery(>81%). Method validation was performed as per the FDA guidelines, and the standard curves were found to be linear in the range of 5–4000 ng/ml for JDR and 4–4000 ng/ml for gemcitabine, respectively. The lower limit of quantitation(LLOQ)of gemcitabine and JDR was 4 and 5 ng/ml, respectively. The intra-day and inter-day precision and accuracy results were within the acceptable limits. Finally, the developed method was successfully applied to investigate the pharmacokinetic studies of JDR and gemcitabine after oral administration to rats. | Gang Wang Dongyang Zhao Hongxiang Chen Dawei Ding Longfa Kou Lifang Sun Chenxia Hao Xincong Li Kai Jia Qiming Kan Xiaohong Liu Zhonggui He Jin Sun | 2017 | Asian Journal of Pharmaceutical Sciences2017，12，5： | 2 |
| 17 | YPD-30, a prodrug of YPD-29B, is an oral small-molecule inhibitor targeting PD-L1 for the treatment of human cancer显示文摘PD-1 and PD-L1 antibodies have brought about extraordinary clinical benefits for cancer patients,and their indications are expanding incessantly.Currently,most PD-1/PD-L1 agents are administered intravenously,which may be uncomfortable for some cancer patients.Herein,we develop a novel oral-delivered small molecular,YPD-29B,which specifically targets human PD-L1.Our data suggested that YPD-29B could potently and selectively block the interaction between PD-L1 and PD-1,but did not inhibit any other immune checkpoints.Mechanistically,YPD-29B induced human PD-L1 dimerization and internalization,which subsequently activated T lymphocytes and therefore overcomes immunity tolerance in vitro.YDP-29B was modified as the YPD-30 prodrug to improve druggability.Using humanized mice with human PD-1 xenografts of human PD-L1 knock-in mouse MC38 cancer cells,we demonstrated that YPD-30 exhibited significant antitumor activity and was well tolerated in vivo.Taken together,our results indicate that YPD-30 serves as a promising therapeutic candidate for anti-human PD-L1 cancer immunotherapy. | Fangfang Lai Ming Ji Lei Huang Yunchen Wang Nina Xue Tingting Du Kai Dong Xiaoqing Yao Jing Jin Zhiqiang Feng Xiaoguang Chen | 2022 | Acta Pharmaceutica Sinica B2022，12，6： | 1 |
| 18 | Hydroxyethyl starch and its derivatives as nanocarriers for delivery of diagnostic and therapeutic agents towards cancers显示文摘Many types of drugs and agents used for cancer diagnosis and therapy often have low bioavailability and insufficient efficacy,as well as causing various side effects due to their nonspecific delivery.Nanocarriers with purposely-designed compositions and structures have shown varying degrees of abilities to deliver these compounds towards cancers in passive or active manners.Despite the availability of a variety of materials for the construction of nanocarriers,natural polymers with good biocompatibility and biodegradability are preferable for such usage because of their high in vivo safety as well as easy removal of degradation products.Among the natural polymers intended for building nanocarriers,hydroxyethyl starch and its derivatives have gained tremendous attention in the field of drug delivery in the form of nanomedicines over the last decade.There is growing optimism that ever more hydroxyethyl starch-based nanomedicines will be a significant addition to the armoury currently used for cancer diagnosis and therapy. | Ronghua Tan Ying Wan Xiangliang Yang | 2020 | Biomaterials Translational2020，1，1： | 1 |
| 19 | Theranostic hyaluronic acid prodrug micelles with aggregation- induced emission characteristics for targeted drug delivery显示文摘Theranostic hyaluronic acid(HA) prodrug micelles with pH-responsive drug release and aggregation-induced emission(AIE)properties were prepared by chemical graft of biomimetic phosphorylcholine(PC), anticancer drug doxorubicin(DOX) and AIE fluorogen tetraphenylene(TPE) to the HA backbone. DOX was conjugated to the HA backbone by a hydrazone bond which can be hydrolyzed under acidic environment and result in pH-triggered smart release of DOX. The TPE units with typical AIE characteristics were applied for real time drug tracking in cancer cells. The HA-based prodrugs could self-assemble into micelles in aqueous solution as confirmed by the dynamic light scattering(DLS) and transmission electron microscopy(TEM). The intracellular distribution of HA prodrug micelles could be clearly observed by fluorescence microscopy based on the strong fluorescence of TPE. Moreover, after treated with the micelles, stronger fluorescence of TPE in CD44 overexpressed MDA-MB-231 cancer cells was observed, compared to the CD44 negative cell line, NIH3T3 cells, suggesting efficient cell uptake of HA prodrug micelles by receptor-mediated endocytosis. The cell viability results indicated that the prodrug micelles could inhibit the proliferation of the cancer cells effectively. Such pH-triggered theranostic drug delivery system with AIE features can provide a new platform for targeted and image-guided cancer therapy. | Lin Wang Haoke Zhang Anjun Qin Qiao Jin Ben Zhong Tang Jian Ji | 2016 | Science China Chemistry2016，59，12： | 1 |
| 20 | Recent developments in the medicinal chemistry of single boron atom-containing compounds显示文摘Various boron-containing drugs have been approved for clinical use over the past two decades,and more are currently in clinical trials.The increasing interest in boron-containing compounds is due to their unique binding properties to biological targets;for example,boron substitution can be used to modulate biological activity,pharmacokinetic properties,and drug resistance.In this perspective,we aim to comprehensively review the current status of boron compounds in drug discovery,focusing especially on progress from 2015 to December 2020.We classify these compounds into groups showing anticancer,antibacterial,antiviral,antiparasitic and other activities,and discuss the biological targets associated with each activity,as well as potential future developments. | Shu Song Ping Gao Lin Sun Dongwei Kang Jacob Kongsted Vasanthanathan Poongavanam Peng Zhan Xinyong Liu | 2021 | Acta Pharmaceutica Sinica B2021，11，10： | 1 |
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