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| 1 | Erythrocyte membrane-camouflaged carrier-free nanoassembly of FRET photosensitizer pairs with high therapeutic efficiency and high security for programmed cancer synergistic phototherapy显示文摘Phototherapy has been intensively investigated as a non-invasive cancer treatment option.However,its clinical translation is still impeded by unsatisfactory therapeutic efficacy and severe phototoxicity.To achieve high therapeutic efficiency and high security,a nanoassembly of Forster Resonance Energy Transfer(FRET)photosensitizer pairs is developed on basis of dual-mode photosensitizer co-loading and photocaging strategy.For proof-of-concept,an erythrocyte-camouflaged FRET pair co-assembly of chlorine e6(Ce6,FRET donor)and 1,1′-dioctadecyl-3,3,3′,3′-tetramethylindotricarbocyanine iodide(DiR,FRET acceptor)is investigated for breast cancer treatment.Notably,Ce6 in the nanoassemby is quenched by DiR and could be unlocked for photodynamic therapy(PDT)only when DiR is photobleached by 808-nm laser.As a result,Ce6-caused phototoxicity could be well controlled.Under cascaded laser irradiation(808-660 nm),tumor-localizing temperature rise following laser irradiation on DiR not only induces tumor cell apoptosis but also facilitates the tumor penetration of NPs,relieves tumor hypoxia,and promotes the PDT efficacy of Ce6.Such FRET pair-based nanoassembly provides a new strategy for developing multimodal phototherapy nanomedicines with high efficiency and good security. | Xuanbo Zhang Jianchen Xiong Kaiyuan Wang Han Yu Bingjun Sun Hao Ye Zhiqiang Zhao Ning Wang Yuequan Wang Shenwu Zhang Wutong Zhao Haotian Zhang Zhonggui He Cong Luo Jin Sun | 2021 | Bioactive Materials2021，6，8： | 4 |
| 2 | Small changes in the length of diselenide bond-containing linkages exert great influences on the antitumor activity of docetaxel homodimeric prodrug nanoassemblies显示文摘Homodimeric prodrug-based self-assembled nanoparticles,with carrier-free structure and ultrahigh drug loading,is drawing more and more attentions.Homodimeric prodrugs are composed of two drug molecules and a pivotal linkage.The influence of the linkages on the self-assembly,in vivo fate and antitumor activity of homodimeric prodrugs is the focus of research.Herein,three docetaxel(DTX)homodimeric prodrugs are developed using different lengths of diselenide bond-containing linkages.Interestingly,compared with the other two linkages,the longest diselenide bond-containing linkage could facilitate the self-delivery of DTX prodrugs,thus improving the stability,circulation time and tumor targeting of prodrug nanoassemblies.Besides,the extension of linkages reduces the redox-triggered drug release and cytotoxicity of prodrug nanoassemblies in tumor cells.Although the longest diselenide bond-containing prodrug nanoassemblies possessed the lowest cytotoxicity to 4T1 cells,their stable nanostructure maintained intact during circulation and achieve the maximum accumulation of DTX in tumor cells,which finally“turned the table”.Our study illustrates the crucial role of linkages in homodimeric prodrugs,and gives valuable proposal for the development of advanced nano-DDS for cancer treatment. | Lingxiao Li Shiyi Zuo Fudan Dong Tian Liu Yanlin Gao Yinxian Yang Xin Wang Jin Sun Bingjun Sun Zhonggui He | 2021 | Asian Journal of Pharmaceutical Sciences2021，16，3： | 3 |
| 3 | Pure photosensitizer-driven nanoassembly with core-matched PEGylation for imaging-guided photodynamic therapy显示文摘Pure drug-assembled nanomedicines(PDANs)are currently under intensive investigation as promising nanoplatforms for cancer therapy.However,poor colloidal stability and less tumor-homing ability remain critical unresolved problems that impede their clinical translation.Herein,we report a core-matched nanoassembly of pyropheophorbide a(PPa)for photodynamic therapy(PDT).Pure PPa molecules are found to self-assemble into nanoparticles(NPs),and an amphiphilic PEG polymer(PPaPEG_(2K))is utilized to achieve core-matched PEGylating modification via the p-p stacking effect and hydrophobic interaction between the PPa core and the PPa-PEG_(2K) shell.Compared to PCL-PEG_(2K) with similar molecular weight,PPa-PEG_(2K) significantly increases the stability,prolongs the systemic circulation and improves the tumor-homing ability and ROS generation efficiency of PPa-nanoassembly.As a result,PPa/PPa-PEG_(2K) NPs exert potent antitumor activity in a 4T1 breast tumor-bearing BALB/c mouse xenograft model.Together,such a core-matched nanoassembly of pure photosensitizer provides a new strategy for the development of imaging-guided theragnostic nanomedicines. | Shenwu Zhang Yuequan Wang Zhiqiang Kong Xuanbo Zhang Bingjun Sun Han Yu Qin Chen Cong Luo Jin Sun Zhonggui He | 2021 | Acta Pharmaceutica Sinica B2021，11，11： | 3 |
| 4 | Influence of anchorage length and pretension on the working resistance of rock bolt based on its tensile characteristics显示文摘In coal mining roadway support design,the working resistance of the rock bolt is the key factor affecting its maximum support load.Effective improvement of the working resistance is of great significance to roadway support.Based on the rock bolt’s tensile characteristics and the mining roadway surrounding rock deformation,a mechanical model for calculating the working resistance of the rock bolt was established and solved.Taking the mining roadway of the 17102(3)working face at the Panji No.3 Coal Mine of China as a research site,with a quadrilateral section roadway,the influence of pretension and anchorage length on the working resistance of high-strength and ordinary rock bolts in the middle and corner of the roadway is studied.The results show that when the bolt is in the elastic stage,increasing the pretension and anchorage length can effectively improve the working resistance.When the bolt is in the yield and strain-strengthening stages,increasing the pretension and anchorage length cannot effectively improve the working resistance.The influence of pretension and anchorage length on the ordinary and high-strength bolts is similar.The ordinary bolt’s working resistance is approximately 25 kN less than that of the high-strength bolt.When pretension and anchorage length are considered separately,the best pretensions of the high-strength bolt in the middle of the roadway side and the roadway corner are 41.55 and 104.26 kN,respectively,and the best anchorage lengths are 1.54 and 2.12 m,respectively.The best anchorage length of the ordinary bolt is the same as that of the high-strength bolt,and the best pretension for the ordinary bolt in the middle of the roadway side and at the roadway corner is 33.51 and 85.12 kN,respectively.The research results can provide a theoretical basis for supporting the design of quadrilateral mining roadways. | Jucai Chang Kai He Dongdong Pang Dong Li Chuanming Li Bingjun Sun | 2021 | International Journal of Coal Science & Technology2021，8，6： | 2 |
| 5 | Origin and effect of surface oxygen-containing species on electrochemical CO or CO_(2) reduction reactions显示文摘Renewable-energy-powered electrochemical CO or CO_(2)reduction reactions(CO_(2)RR)provide one of the most promising strategies to upgrade CO_(2)to valuable products.In the past decade,the existence and the mechanistic role of oxygen-containing species,such as(sub)surface oxide,hydroxide and oxyhydroxide species,at the electrode–electrolyte interface under reductive conditions have emerged as a topic of acute discussion within the CO_(2)RR field.Oxide-derived Cu attracted the most attention,while other surfaces,including Au,Ag and Sn,were also widely investigated.This review identifies likely causes for contrasting results and views in the literature,summarizes possible oxygen sources for the interfacial oxygen-containing species at the CO_(2)RR conditions,and discusses potential roles these species could play in affecting the rate and product distribution.Finally,perspectives on future efforts to reveal the identity and role of oxygen-containing species in the CO_(2)RR are presented. | Xiaoxia Chang Ming He Qi Lu Bingjun Xu | 2023 | Science China Chemistry2023，66，1： | 1 |
| 6 | Minor change in the length of carbon chain has a great influence on the antitumor effect of paclitaxel-fatty alcohol prodrug nanoassemblies:Small roles,big impacts显示文摘Prodrug-based nanoassembly emerges as a hopeful way for the efficient delivery of antitumor drugs,with carrier-free structure and ultra-high drug loading.Carbon chains are widely used to design self-assembling prodrugs.The impacts of the length of carbon chains on the self-assembly stability,drug delivery efficiency and antitumor effect of prodrugs have not been fully elucidated.Here,three paclitaxel prodrugs were synthesized by conjugating paclitaxel with octanol(C_(8)),decanol(C_(10))or dodecanol(C_(12))through disulfide bond.The three prodrugs could form homogeneous nanoparticles,with over 50%drug loading and redox dual-responsivity.Interestingly,the length extension of carbon chains ameliorates the self-assembly and the colloidal stability of prodrugs,thus improving the drug delivery efficiency.The optimal paclitaxel-dodecanol prodrug nanoassemblies exhibit better antitumor efficacy than Taxol and Abraxane.These findings are meaningful for the rational design of advanced nanomedicines in cancer therapy. | Xin Wang Lingxiao Li Danping Wang Shiyi Zuo Tian Liu Fudan Dong Xuanbo Zhang Zhonggui He Bingjun Sun Jin Sun | 2022 | Nano Research2022，15，4： | 1 |
| 7 | Effect of Metal Additives on Performance of Low-Carbon Magnesia-Carbon Materials显示文摘In this paper,both oxidation and corrosion resistance of low-carbon magnesia-carbon materials containing 4.0wt% graphite with metallic Al and Mg-Al alloy powders as antioxidants were investigated.Meanwhile,the microstructures of samples corroded by slag were observed with optical microscope as well.The test results revealed the properties of oxidation and corrosion resistance of low-carbon magnesia-carbon materials could be improved obviously by adding metal Al powder and Mg-Al alloy powder.The rule of improving oxidation resistance was illegibility when metal Al powder and Mg-Al alloy powder were added together.It was harmful to corrosion resistance by mixed adding metal Al powder and Mg-Al alloy powder into the materials,at the same time,the corrosion resistance would decreased with the increasing of Mg-Al alloy content.The corrosion resistance of samples with 0.5wt% or 3.0wt% Mg-Al alloy was better. The oxidation resistance and corrosion resistance of materials with metal Al or Mg-Al alloy respectively were better than that with mixed metal Al and Mg-Al alloy. As a result, Mg-Al alloy was more suitable for low-carbon composite materials than metal Al as additives. | PENG Xiaoyan LI Lin HE Zhiyong LIU Kaiqi WANG Bingjun | 2007 | China's Refractories2007，16，1： | 1 |
| 8 | Impact of the amount of PEG on prodrug nanoassemblies for efficient cancer therapy显示文摘PEGylation has been widely used to improve the pharmacokinetic properties of prodrug self-assembled nanoparticles(prodrug-SANPs).However,the impacts of the amount of PEG on the self-assemble stability,cellular uptake,pharmacokinetics,and antitumor efficacy of prodrug-SANPs are still unknown.Herein,selenoether bond bridged docetaxel dimeric prodrug was synthesized as the model prodrug.Five prodrug-SANPs were designed by using different mass ratios of prodrugs to PEG(W_(prodrug)/W_(DSPE-mPEG2000)=10:0,9:1,8:2,7:3 and 6:4),and defined as Pure drug NPs,9:1NPs,8:2NPs,7:3 NPs and 6:4 NPs,respectively.Interestingly,8:2 NPs formed the most compact nanostructure,thus improving the self-assemble stability and pharmacokinetics behavior.In addition,the difference of these prodrug-SANPs in cellular uptake was investigated,and the influence of PEG on cytotoxicity and antitumor efficacy was also clarified in details.The 8:2 NPs exhibited much better antitumor efficacy than other prodrug-SANPs and even commercial product.Our findings demonstrated the pivotal role of the amount of PEG on prodrug-SANPs. | Yaqiao Li Lingxiao Li Qianhui Jin Tian Liu Jin Sun Yongjun Wang Zhijun Yang Zhonggui He Bingjun Sun | 2022 | Asian Journal of Pharmaceutical Sciences2022，17，2： | 1 |
| 9 | Integration of phospholipid-drug complex into self-nanoemulsifying drug delivery system to facilitate oral delivery of paclitaxel显示文摘Self-nanoemulsifying drug delivery system(SNEDDS) has emerged as a promising platform to improve oral absorption of drugs with poor solubility and low permeability. However,large polarity molecules with insufficient lipid solubility,such as paclitaxel(PTX),would suffer from inferior formulation of SNEDDS due to poor compatibility. Herein,phospholipid-drug complex(PLDC) and SNEDDS were integrated into one system to facilitate oral delivery of PTX. First,PTX was formulated into PLDC in response to its inferior physicochemical properties. Then,the prepared PLDC was further formulated into SNEDDS by integrating these two drug delivery technologies into one system(PLDC-SNEDDS). After PLDC-SNEDDS dispersed in aqueous medium,nanoemulsion was formed immediately with an average particle size of ~30 nm. Furthermore,the nanomulsion of PLDC-SNEDDS showed good colloidal stability in both HCl solution(0.1 mol/l,p H 1.0) and phosphate buffer solution(PBS,p H 6.8). In vivo,PTX-PLDC-SNEDDS showed distinct advantages in terms of oral absorption efficiency,with a3.42-fold and 2.13-fold higher bioavailability than PTX-PLDC and PTX solution,respectively.Our results suggest that the integration of PLDC into SNEDDS could be utilized to facilitate the oral delivery of hydrophobic drugs with large polarity. | Dawei Ding Bingjun Sun Weiping Cui Qin Chen Xuanbo Zhang Haotian Zhang Zhonggui He Jin Sun Cong Luo | 2019 | Asian Journal of Pharmaceutical Sciences2019，14，5： | 1 |
| 10 | Textual Metaphor from the Perspective of Relator显示文摘 | Qingshun He Bingjun Yang Binli Wen | 2015 | Australian Journal of Linguistics2015，，： | 1 |
| 11 | A Study of Transfer Directions in Grammatical Metaphor显示文摘 | Qingshun He Bingjun Yang | 2014 | Australian Journal of Linguistics2014，，： | 1 |
| 12 | Precisely engineering a dual-drug cooperative nanoassembly for proteasome inhibition-potentiated photodynamic therapy显示文摘Photodynamic therapy(PDT) has been widely investigated for cancer therapy. The intracellular accumulation of reactive oxygen species(ROS)-damaged protein facilitates tumor cell apoptosis. However, there is growing evidence that the ubiquitin-proteasome pathway(UPP) significantly impedes PDT by preventing the enrichment of ROS-damaged proteins in tumor cells. To tackle this challenge, we report a facile dual-drug nanoassembly based on the discovery of an interesting co-assembly of bortezomib(BTZ, a proteasome inhibitor) and pyropheophorbide a(PPa) for proteasome inhibition-mediated PDT sensitization.The precisely engineered nanoassembly with the optimal dose ratio of BTZ and PPa demonstrates multiple advantages, including simple fabrication, high drug co-loading efficiency, flexible dose adjustment,good colloidal stability, long systemic circulation, favorable tumor-specific accumulation, as well as significant enrichment of ROS-damaged proteins in tumor cells. As a result, the cooperative nanoassembly exhibits potent synergistic antitumor activity in vivo. This study provides a novel dual-drug engineering modality for multimodal cancer treatment. | Fujun Yang Qingyu Ji Rui Liao Shumeng Li Yuequan Wang Xuanbo Zhang Shenwu Zhang Haotian Zhang Qiming Kan Jin Sun Zhonggui He Bingjun Sun Cong Luo | 2022 | Chinese Chemical Letters2022，33，4： | 1 |
| 13 | Structurally defined tandem-responsive nanoassemblies composed of dipeptide-based photosensitive derivatives and hypoxia-activated camptothecin prodrugs against primary and metastatic breast tumors显示文摘Substantial progress in the use of chemo-photodynamic nano-drug delivery systems(nanoDDS) for the treatment of the malignant breast cancer has been achieved. The inability to customize precise nanostructures, however, has limited the therapeutic efficacy of the prepared nano-DDS to date. Here,we report a structurally defined tandem-responsive chemo-photosensitive co-nanoassembly to eliminate primary breast tumor and prevent lung metastasis. This both-in-one co-nanoassembly is prepared by assembling a biocompatible photosensitive derivative(pheophorbide-diphenylalanine peptide, PPADA) with a hypoxia-activated camptothecin(CPT) prodrug [(4-nitrophenyl) formate camptothecin, NCPT]. According to computational simulations, the co-assembly nanostructure is not the classical core-shell type, but consists of many small microphase regions. Upon exposure to a 660 nm laser,PPA-DA induce high levels of ROS production to effectively achieve the apoptosis of normoxic cancer cells. Subsequently, the hypoxia-activated N-CPT and CPT spatially penetrate deep into the hypoxic region of the tumor and suppress hypoxia-induced tumor metastasis. Benefiting from the rational design of the chemo-photodynamic both-in-one nano-DDS, these nanomedicines exhibit a promising potential in the inhibition of difficult-to-treat breast tumor metastasis in patients with breast cancer. | Mengchi Sun Hailun Jiang Tian Liu Xiao Tan Qikun Jiang Bingjun Sun Yulong Zheng Gang Wang Yang Wang Maosheng Cheng Zhonggui He Jin Sun | 2022 | Acta Pharmaceutica Sinica B2022，12，2： | 1 |
| 14 | Iron-doxorubicin prodrug loaded liposome nanogenerator programs multimodal ferroptosis for efficient cancer therapy显示文摘Ferroptosis is a new mode of cell death,which can be induced by Fenton reactionmediated lipid peroxidation.However,the insufficient H2O2 and high GSH in tumor cells restrict the efficiency of Fenton reaction-dependent ferroptosis.Herein,a self-supplying lipid peroxide nanoreactor was developed to co-delivery of doxorubicin(DOX),iron and unsaturated lipid for efficient ferroptosis.By leveraging the coordination effect between DOX and Fe3+,trisulfide bond-bridged DOX dimeric prodrug was actively loaded into the core of the unsaturated lipids-rich liposome via iron ion gradient method.First,Fe3+could react with the overexpressed GSH in tumor cells,inducing the GSH depletion and Fe2+generation.Second,the cleavage of trisulfide bond could also consume GSH,and the released DOX induces the generation of H2O2,which would react with the generated Fe2+in step one to induce efficient Fenton reaction-dependent ferroptosis.Third,the formed Fe3+/Fe2+couple could directly catalyze peroxidation of unsaturated lipids to boost Fenton reaction-independent ferroptosis.This iron-prodrug liposome nanoreactor precisely programs multimodal ferroptosis by integrating GSH depletion,ROS generation and lipid peroxidation,providing new sights for efficient cancer therapy. | Yinxian Yang Shiyi Zuo Linxiao Li Xiao Kuang Jinbo Li Bingjun Sun Shujun Wang Zhonggui He Jin Sun | 2021 | Asian Journal of Pharmaceutical Sciences2021，16，6： | 1 |
| 15 | Metal-organic layers induce in situ nano-structuring of Cu surface in electrocatalytic CO_(2)reduction显示文摘Cu-based catalysts have attracted widespread attention for its capability in electrocatalytically reducing CO_(2)to a variety of products.Surface modification of Cu has become an interesting method for tuning the catalytic performance.Here,we use Zrbased metal-organic layers(MOLs)as the additive of the Cu surface,which enhanced the Faradaic efficiency of CH4 by two times as compared to the untreated polycrystalline Cu foil.Unexpectedly,the MOLs were found to induce in situ nano-structuring of the Cu foil surface within seconds in the electrolysis,as revealed by a combination of scanning electron microscopy(SEM),grazing incidence X-ray diffractometry(GIXRD),and linear sweep voltammetry(LSV)measurements.These surface changes are responsible for the shift of product selectivity.Control experiments suggest that negatively chargedμ3-O−on the Zr-cluster in the MOL might interact with CO-covered Cu surface and induce roughing and nano-structuring.This work reveals a potential role of additive on Cu to induce surface nano-structuring that tunes catalytic activity and selectivity. | Xinru He Jiawei Chen Yifei Xu Yan Shen Yifan Zeng Jieyu Zhu Bingjun Xu Cheng Wang | 2023 | Nano Research2023，16，4： | 0 |
| 16 | Evaluation on therapeutic effects of orthotopic liver transplantation by megnetic resonance imaging in patients with portal hypertension显示文摘 | Wang Jin Liang Yingying Yan Ronghua Jiang Zaibo Liu Jingjing Hu Bing He Bingjun Ren Linglan Chen Jingbiao Shan Hong | 2014 | Chinese Medical Journal2014，，19： | 0 |
| 17 | The effect of lengths of branched-chain fatty alcohols on the efficacy and safety of docetaxel-prodrug nanoassemblies显示文摘The self-assembly prodrugs are usually consisted of drug modules,activation modules,and assembly modules.Keeping the balance between efficacy and safety by selecting suitable modules remains a challenge for developing prodrug nanoassemblies.This study designed four docetaxel(DTX)prodrugs using disulfide bonds as activation modules and different lengths of branched-chain fatty alcohols as assembly modules(C_(16),C_(18),C_(20),and C_(24)).The lengths of the assembly modules determined the self-assembly ability of prodrugs and affected the activation modules’sensitivity.The extension of the carbon chains improved the prodrugs’self-assembly ability and pharmacokinetic behavior while reducing the cytotoxicity and increased cumulative toxicity.The use of C_(20) can balance efficacy and safety.These results provide a great reference for the rational design of prodrug nanoassemblies. | Shuo Wang Tian Liu Yuetong Huang Chaoying Du Danping Wang Xiyan Wang Qingzhi Lv Zhonggui He Yinglei Zhai Bingjun Sun Jin Sun | 2024 | Acta Pharmaceutica Sinica B2024，14，3： | 0 |
| 18 | Cancer-specific calcium nanoregulator suppressing the generation and circulation of circulating tumor cell clusters for enhanced anti-metastasis combinational chemotherapy显示文摘Tumor metastasis is responsible for chemotherapeutic failure and cancer-related death.Moreover,circulating tumor cell(CTC)clusters play a pivotal role in tumor metastasis.Herein,we develop cancer-specific calcium nanoregulators to suppress the generation and circulation of CTC clusters by cancer membrane-coated digoxin(DIG)and doxorubicin(DOX)co-encapsulated PLGA nanoparticles(CPDDs).CPDDs could precisely target the homologous primary tumor cells and CTC clusters in blood and lymphatic circulation.Intriguingly,CPDDs induce the accumulation of intracellular Ca^(2+) by inhibiting Na^(+)/K^(+)-ATPase,which help restrain cellecell junctions to disaggregate CTC clusters.Meanwhile,CPDDs suppress the epithelialemesenchymal transition(EMT)process,resulting in inhibiting tumor cells escape from the primary site.Moreover,the combination of DOX and DIG at a mass ratio of 5:1 synergistically induces the apoptosis of tumor cells.In vitro and in vivo results demonstrate that CPDDs not only effectively inhibit the generation and circulation of CTC clusters,but also precisely target and eliminate primary tumors.Our findings present a novel approach for anti-metastasis combinational chemotherapy. | Dan Li Yingli Wang Chang Li Qiu Wang Bingjun Sun Haotian Zhang Zhonggui He Jin Sun | 2021 | Acta Pharmaceutica Sinica B2021，11，10： | 0 |
| 19 | Investigating the crucial roles of aliphatic tails in disulfide bond-linked docetaxel prodrug nanoassemblies显示文摘Disulfide bond-bridging strategy has been extensively utilized to construct tumor specificity-responsive aliphatic prodrug nanoparticles(PNPs) for precise cancer therapy. Yet, there is no research shedding light on the impacts of the saturation and cis-trans configuration of aliphatic tails on the self-assembly capacity of disulfide bond-linked prodrugs and the in vivo delivery fate of PNPs. Herein, five disulfide bond-linked docetaxelfatty acid prodrugs are designed and synthesized by using stearic acid, elaidic acid, oleic acid, linoleic acid and linolenic acid as the aliphatic tails, respectively. Interestingly, the cistrans configuration of aliphatic tails significantly influences the self-assembly features of prodrugs, and elaidic acid-linked prodrug with a trans double bond show poor self-assembly capacity. Although the aliphatic tails have almost no effect on the redox-sensitive drug release and cytotoxicity, different aliphatic tails significantly influence the chemical stability of prodrugs and the colloidal stability of PNPs, thus affecting the in vivo pharmacokinetics, biodistribution and antitumor efficacy of PNPs. Our findings illustrate how aliphatic tails affect the assembly characteristic of disulfide bond-linked aliphatic prodrugs and the in vivo delivery fate of PNPs, and thus provide theoretical basis for future development of disulfide bond-bridged aliphatic prodrugs. | Yuequan Wang Cong Luo Shuang Zhou Xinhui Wang Xuanbo Zhang Shumeng Li Shenwu Zhang Shuo Wang Bingjun Sun Zhonggui He Jin Sun | 2021 | Asian Journal of Pharmaceutical Sciences2021，16，5： | 0 |
| 20 | Fine-tuning the structure-tolerance-antitumor efficacy axis of prodrug nanoassemblies via branched aliphatic functionalization显示文摘Small-molecule prodrug nanoassemblies have emerged as efficient antitumor drug delivery systems.However,in the case of camptothecins-based prodrug nanoassemblies,linear aliphatic side chain modification often results in rod-shaped or irregularly shaped nanoassemblies,which are highly unfavorable for sterilization through filtration,and may cause capillary blockage upon intravenous injection.The rational design of camptothecins-based prodrug nanoassemblies remains a challenge.Herein,we propose that branched aliphatic alcohol(BAA)functionalization could fine-tune the structure-tolerance-antitumor efficacy axis of prodrug nanoassemblies.Correspondingly,four SN38-BAA prodrugs were synthesized by conjugating 7-ethyl-10-hydroxycamptothecin(SN38)with BAAs of varying lengths via a tumor redox-responsive disulfide bond,which self-assemble into uniform spherical nanoparticles.The length of BAA was found to significant impact the multiple drug delivery process,including colloidal stability,drug release profiles and pharmacokinetics.Overall,SN38-C21 NPs(SN38-11-heneicosanol nanoparticles),featuring the longest BAA,showcased multiple therapeutic advantages,ultimately culminating the optimal antitumor efficacy and tolerance.The findings underscore the potential of BAA functionalization in strengthening the therapeutic outcomes of prodrug nanoassemblies,and provide valuable insights for developing translational camptothecins-based nanomedicines. | Guanting Li Fengli Xia Hongying Xiao Shunzhe Zheng Shuwen Fu Han Qiao Qianhui Jin Xuanbo Zhang Dun Zhou Chutong Tian Jin Sun Zhonggui He Bingjun Sun | 2024 | Nano Research2024，17，4： | 0 |
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