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Science China Chemistry 2025年第3期 1185-1198页

作者： Erwei Zhao Lingxiao Li Jingyi Zhang Yaqiao Li Rong Chai Bowen Zhang Jialin Xing Minglong Huang Lurong Zhang Xiaohui Pu Zhonggui He Bingjun Sun department of Pharmaceutics Wuya College of InnovationShenyang Pharmaceutical University department of Bioengineering Graduate School of EngineeringThe University of Tokyo Peking Union Pharmaceutical Factory Ltd. State Key Laboratory of Antiviral drugs School of PharmacyHenan University Joint International Research Laboratory of Intelligent drug Delivery systems Ministry of EducationShenyang Pharmaceutical University

Forming electrostatic nanocomplexes(ENCs) with counter-ions can improve the delivery efficiency of chemotherapy ***,water-soluble chemotherapy drugs like mitoxantrone(MTO),have limited affinity for counter-ions,posing challenges in the creation of stable ***,MTO was connected to fatty alcohols of varying chain lengths(C8,C12,C16) via disulfide bonds,forming hydrophobic *** found that conjugating MTO to fatty alcohols significantly improved its affinity for the counter-ion sodium cholesterol sulfate(SCS).Among the designed prodrugs,conjugated to fatty alcohols with longer carbon chain lengths exhibited heightened affinity for SCS,resulting in the formation of more stable ***,extending the carbon chain also slowed the rate of drug ***,compared with MTO solution,these ENCs demonstrated comparable therapeutic efficacy while causing minimal damage to healthy tissues,especially for MTO-SS-C16 *** research provides new insights for constructing stable and safe ENCs for hydrophilic drugs like MTO.

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Sequential delivery of PD-1/PD-L1 blockade peptide and IDO inhibitor for immunosuppressive microenvironment remodeling via an MMP-2 responsive dual-targeting liposome

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Acta Pharmaceutica Sinica B 2023年第5期13卷 2176-2187页

作者： Chuan Hu Yujun Song Yiwei Zhang Siqin He Xueying Liu Xiaotong Yang Tao Gong Yuan Huang Huile Gao Key Laboratory of drug Targeting and drug Delivery systems West China School of PharmacySichuan UniversityChengdu 610041China

Intelligent responsive drug delivery system opens up new avenues for realizing safer and more effective combination ***,a kind of tumor cascade-targeted responsive liposome(NLG919@Lip-pep1)is developed by conjugating polypeptide inhibitor of PD-1 signal pathway(AUNP-12),which is also a targeted peptide that conjugated with liposome carrier through matrix metalloproteinase-2(MMP-2)cleavable peptide(GPLGVRGD).This targeted liposome is prepared through a mature preparation process,and indoleamine-2,3-dioxygenase(IDO)inhibitor NLG919 was encapsulated into ***,mediated by the enhanced permeability and retention effect(EPR effect)and AUNP-12,NLG919@Lip-pep1 first targets the cells that highly express PD-L1 in tumor *** the same time,the over-expressed MMP-2 in the tumor site triggers the dissociation of AUNP-12,thus realizing the precise block of PD-1 signal pathway,and restoring the activity of T *** exposure of secondary targeting moduleⅡVRGDC-NLG919@Lip mediated tumor cells targeting,and further relieved the immunosuppressive ***,this study offers a potentially appealing paradigm of a high efficiency,low toxicity,and simple intelligent responsive drug delivery system for targeted drug delivery in breast cancer,which can effectively rescue and activate the body's anti-tumor immune response and furthermore achieve effective treatment of metastatic breast cancer.

关键词： Immunotherapy Cascade targeting Liposome MMP-2 responsive Breast cancer ICBs IDO inhibitors Immunosuppressive microenvironment

Hollow copper sulfide nanoparticles carrying ISRIB for the sensitized photothermal therapy of breast cancer and brain metastases through inhibiting stress granule formation and reprogramming tumor-associated macrophages

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Acta Pharmaceutica Sinica B 2023年第8期13卷 3471-3488页

作者： Fan Tong Haili Hu Yanyan Xu Yang Zhou Rou Xie Ting Lei Yufan Du Wenqin Yang Siqin He Yuan Huang Tao Gong Huile Gao Key Laboratory of drug Targeting and drug Delivery systems West China School of PharmacySichuan UniversityChengdu 610041China

As known,the benefits of photothermal therapy(PTT)are greatly limited by the heat tolerance of cancer cells resulting from overexpressed heat shock proteins(HSPs).Then HSPs further trigger the formation of stress granules(SGs)that regulate protein expression and cell viability under various stress *** of SG formation can sensitize tumor cells to ***,we developed PEGylated pH(low)insertion peptide(PEG-pHLIP)-modified hollow copper sulfide nanoparticles(HCuS NPs)encapsulating the SG inhibitor ISRIB,with the phase-change material lauric acid(LA)as a gatekeeper,to construct a pH-driven and NIR photo-responsive controlled smart drug delivery system(IL@H-PP).The nano medicine could specifically target slightly acidic tumor *** irradiation,IL@H-PP realized PTT,and the light-controlled release of ISRIB could effectively inhibit the formation of PTT-induced SG to sensitize tumor cells to PTT,thereby increasing the antitumor effect and inducing potent immunogenic cell death(ICD).Moreover,IL@H-PP could promote the production of reactive oxygen species(ROS)by tumor-associated macrophages(TAMs),repolarizing them towards the M1 phenotype and remodeling the immunosuppressive *** vitro/vivo results revealed the potential of PTT combined with SG inhibitors,which provides a new paradigm for antitumor and antimetastases.

关键词： Hollow coppersulfide nanoparticles Sensitized PTT SG inhibition TAMs repolarization pH-driven targeting Photothermal responsiveness Immunotherapy Anti-metastases

A chitosan-mediated inhalable nanovaccine against SARS-CoV-2

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Nano Research 2022年第5期15卷 4191-4200页

作者： Shao-Hua Zhuo Jun-Jun Wu Lang Zhao Wen-Hao Li Yu-Fen Zhao Yan-Mei Li Key Lab of Bioorganic Phosphorus Chemistry&Chemical Biology Department of ChemistryTsinghua UniversityBeijing 100084China Beijing Institute for Brain Disorders Beijing 100069China Center for Synthetic and systems Biology Tsinghua UniversityBeijing 100084China Institute of drug discovery Technology Ningbo UniversityNingbo 315221China

Severe acute respiratory syndrome coronavirus 2(SARS-CoV-2),with several antigenic variants,has grown into a global challenge,and the rapid establishment of an immune barrier is crucial to achieving long-term control of the *** has led to a great demand for easy preparation and scalable vaccines,especially in low-income ***,we present an inhalable nanovaccine comprising chitosan and SARS-CoV-2 spike *** chitosan-mediated nanovaccine enabled a strong spike-specific antibody immune response and augmented local mucosal immunity in bronchoalveolar lavage and lungs,which might be capable of protecting the host from infection without systemic *** addition,the enhanced adaptive immunity stimulated by chitosan showed potential protection against ***,inhalation of the nanovaccine induced a comparable antibody response compared to intramuscular *** inhalable nanovaccine against SARS-CoV-2 offers a convenient and compliant strategy to reduce the use of needles and the need for medical staff.

关键词： severe acute respiratory syndrome coronavirus 2(SASR-CoV-2) inhalation nanovaccine chitosan

Synthesis of 5-（Sulfamoylmethyl）indoles by Mild Negishi Coupling and Their Application in Almotriptan

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Chemical Research in Chinese Universities 2015年第4期31卷 539-542页

作者： LI Xiaolong QIU Rui WAN Weili CHENG Xu HE Yi HAI Li WUYong Key Laboratory of drug-Targeting and drug-Delivery systems of Ministry of Education Department of Medicinal Chemistry West China School of Pharmacy Sichuan University Chengdu 610041 P R. China

A new synthetic route of almotriptan was described. The application of Negishi coupling reaction simpli- fied the process and significantly improved the yield. The synthetic route was also expected to be general for t... 详细信息

关键词： Negishi coupling Almotriptan 5-(Sulfamoylmethyl)indole

Nanoparticles for targeted delivery of therapeutics and small interfering RNAs in hepatocellular carcinoma

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World Journal of Gastroenterology 2015年第42期21卷 12022-12041页

作者： Jaleh Varshosaz Maryam Farzan department of Pharma-ceutics Faculty of Pharmacy and Novel Drug Delivery Systems Research Centre Isfahan University of Medical Sciences

Hepatocellular carcinoma(HCC) is the 5th most common malignancy which is responsible for more than half million annual mortalities; also, it is the third leading cause of cancer related death. Unfavorablesystemic side-effects of chemotherapeutic agents and susceptibility to the degradation of small interfering RNAs(si RNAs), which can knock down a specific gene involved in the disease, have hampered their clinical application. So, it could be beneficial to develop an efficient carrier for the stabilization and specific delivery of drugs and si RNA to cells. Targeted nanoparticles have gained considerable attention as an efficient drug and gene delivery system, which is due to their capability in achieving the highest accumulation of cytotoxic agents in tumor tissue, modifiable drug pharmacokinetic- and bio-distribution, improved effectiveness of treatment, and limited sideeffects. Recent studies have shed more light on the advantages of novel drug loaded carrier systems vs free drugs. Most of the animal studies have reported improvement in treatment efficacy and survival rate using novel carrier systems. Targeted delivery may be achieved passively or actively. In passive targeting, no ligand as homing device is used, while targeting is achieved by incorporating the therapeutic agent into a macromolecule or nanoparticle that passively reaches the target organ. However, in active targeting, the therapeutic agent or carrier system is conjugated to a tissue or cell-specific receptor which is overexpressed in a special malignancy using a ligand called a homing device. This review covers a broad spectrum of targeted nanoparticles as therapeutic and nonviral si RNA delivery systems, which are developed for enhanced cellular uptake and targeted gene silencing in vitro and in vivo and their characteristics and opportunities for the clinical applications of drugs and therapeutic si RNA are discussed in this article. Asialoglycoprotein receptors, low-density lipoprotein, gangl

关键词： Small interfering RNA Targeted delivery Nanopartic

Synthesis of a dendritic estrogen cluster:A potential tool for studies of nuclear versus extranuclear pathways of estrogen actions

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Chinese Chemical Letters 2012年第12期23卷 1319-1322页

作者： Jian Chen Hu Zheng Yan Song Yu Feng Liang Qing Rong Qi Functional Food(drug) Laboratory Institute of Agro-Product Processing Science and TechnologySichuan Academy of Agricultural Science Key Laboratory of drug-Targeting and drug-Delivery systems of the Ministry of Education Department of Medicinal ChemistryWest China School of PharmacySichuan University

A novel estrogen dendrimer has been synthesized through a combination of divergent and convergent approaches in 9 practical steps and in good yields. It was characterized and confirmed by elemental analysis, FT-IR, MS, 1H NMR, 13C NMR. The dendrimer contains 16 estrone units and is potentially a useful tool for the studies of estrogen actions.

关键词： Estrogen dendrimer Synthesis Nuclear and extranuclear Receptor

Rationally designed amyloid inhibitors based on amyloid-related structural studies

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Chinese Chemical Letters 2023年第2期34卷 7-17页

作者： Jinjian Hu Yufen Zhao Yanmei Li department of Chemistry Key Lab of Bioorganic Phosphorus Chemistry&Chemical BiologyTsinghua UniversityBeijing 100084China Beijing Institute for Brain Disorders Beijing 100069China Center for Synthetic and systems Biology Tsinghua UniversityBeijing 100084China Institute of drug discovery Technology Ningbo UniversityNingbo 315221China

Amyloid proteins correlate with a series of degenerative diseases. Targeting amyloid aggregation has remained a hot topic in therapeutic studies. Numerous inhibitors have been developed, but very few have been approved for marketing. Meanwhile, the growing knowledge of amyloid structural characteristics provides a basis for the rational design of inhibitors. Here we introduce the high-resolution structural findings of amyloid fibrils in recent years and discuss the reported strategies toward rationally designed inhibitors based on amyloid-related structural studies.

关键词： Amyloid Amyloid structure Degenerative disease Amyloid inhibitor Rational design

Fine-tuning the activation behaviors of ternary modular cabazitaxel prodrugs for efficient and on-target oral anti-cancer therapy

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Asian Journal of Pharmaceutical Sciences 2024年第2期19卷 188-203页

作者： Mingyang Zhang Yifan Miao Can Zhao Tong Liu Xiyan Wang Zixuan Wang Wenxin Zhong Zhonggui He Chutong Tian Jin Sun department of Pharmaceutics Wuya College of InnovationShenyang Pharmaceutical UniversityShenyang 110016China Key Laboratory of Advanced drug Delivery systems of Zhejiang Province Hangzhou 310058China Joint International Research Laboratory of Intelligent drug Delivery systems Ministry of EducationShenyang 110016China Liaoning Provincial Institute of drug Inspection and Testing Shenyang 110036China

The disulfide bond plays a crucial role in the design of anti-tumor prodrugs due to its exceptional tumor-specific redox responsiveness. However, premature breaking of disulfide bonds is triggered by small amounts of reducing substances (e.g., ascorbic acid, glutathione, uric acid and tea polyphenols) in the systemic circulation. This may lead to toxicity, particularly in oral prodrugs that require more frequent and high-dose treatments. Fine-tuning the activation kinetics of these prodrugs is a promising prospect for more efficient on-target cancer therapies. In this study, disulfide, steric disulfide, and ester bonds were used to bridge cabazitaxel (CTX) to an intestinal lymph vessel-directed triglyceride (TG) module. Then, synthetic prodrugs were efficiently incorporated into self-nanoemulsifying drug delivery system (corn oil and Maisine CC were used as the oil phase and Cremophor EL as the surfactant). All three prodrugs had excellent gastric stability and intestinal permeability. The oral bioavailability of the disulfide bond-based prodrugs (CTX-(C)S-(C)S-TG and CTX-S-S-TG) was 11.5- and 19.1-fold higher than that of the CTX solution, respectively, demonstrating good oral delivery efficiency. However, the excessive reduction sensitivity of the disulfide bond resulted in lower plasma stability and safety of CTX-S-S-TG than that of CTX-(C)S-(C)S-TG. Moreover, introducing steric hindrance into disulfide bonds could also modulate drug release and cytotoxicity, significantly improving the anti-tumor activity even compared to that of intravenous CTX solution at half dosage while minimizing off-target adverse effects. Our findings provide insights into the design and fine-tuning of different disulfide bond-based linkers, which may help identify oral prodrugs with more potent therapeutic efficacy and safety for cancer therapy.

关键词： Steric disulfide bond Triglyceride-like pr odrugs Cabazitaxel Lymphatic transport Oral chemotherapy

Smart drug delivery systems to overcome drug resistance in cancer immunotherapy

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Cancer Biology & Medicine 2023年第4期20卷 248-267页

作者： Wenzhe Yi Dan Yan Dangge Wang Yaping Li State Key Laboratory of drug Research&Center of Pharmaceutics Shanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China University of Chinese Academy of Sciences Beijing 100049China department of Pharmaceutics School of PharmacyNanjing Medical UniversityNanjing 211116China Yantai Key Laboratory of Nanomedicine&Advanced Preparations Yantai Institute of Materia MedicaYantai 264000China Shandong Laboratory of Yantai drug discovery Bohai Rim Advanced Research Institute for Drug DiscoveryYantai 264000China

Cancer immunotherapy,a therapeutic approach that inhibits tumors by activating or strengthening anti-tumor immunity,is currently an important clinical strategy for cancer treatment;however,tumors can develop drug resistance to immune surveillance,resulting in poor response rates and low therapeutic *** addition,changes in genes and signaling pathways in tumor cells prevent susceptibility to immunotherapeutic ***,tumors create an immunosuppressive microenvironment via immunosuppressive cells and secrete molecules that hinder immune cell and immune modulator infiltration or induce immune cell *** address these challenges,smart drug delivery systems(SDDSs)have been developed to overcome tumor cell resistance to immunomodulators,restore or boost immune cell activity,and magnify immune *** combat resistance to small molecules and monoclonal antibodies,SDDSs are used to co-deliver numerous therapeutic agents to tumor cells or immunosuppressive cells,thus increasing the drug concentration at the target site and improving ***,we discuss how SDDSs overcome drug resistance during cancer immunotherapy,with a focus on recent SDDS advances in thwarting drug resistance in immunotherapy by combining immunogenic cell death with immunotherapy and reversing the tumor immunosuppressive *** that modulate the interferon signaling pathway and improve the efficacy of cell therapies are also ***,we discuss potential future SDDS perspectives in overcoming drug resistance in cancer *** believe that this review will contribute to the rational design of SDDSs and development of novel techniques to overcome immunotherapy resistance.

关键词： Cancer immunotherapy drug resistance smart drug delivery system immunosuppressive microenvironment immune cell