International Journal of Pharmaceutics: X最新文献

pH/NIR dual-responsive implantable patch for combined photothermal and chemotherapy of tumors. pH/NIR双响应植入式贴片用于肿瘤光热化疗联合治疗。

IF 7.9 2区医学

International Journal of Pharmaceutics: X Pub Date : 2026-06-06 eCollection Date: 2026-06-01 DOI: 10.1016/j.ijpx.2026.100582

Wenjie Sun, Xi Zhang, Yili Zhao, Bixiang Ye, Wen Gao, Guangyi Jiang, Xin Li, Xiaoji Lin

{"title":"pH/NIR dual-responsive implantable patch for combined photothermal and chemotherapy of tumors.","authors":"Wenjie Sun, Xi Zhang, Yili Zhao, Bixiang Ye, Wen Gao, Guangyi Jiang, Xin Li, Xiaoji Lin","doi":"10.1016/j.ijpx.2026.100582","DOIUrl":"10.1016/j.ijpx.2026.100582","url":null,"abstract":"<p><p>The treatment of malignant solid tumors still faces challenges including the high risk of surgical resection and the severe side effects of chemotherapy. Moreover, existing clinical strategies often fail to meet the treatment needs of patients with inoperable tumors. In this study, a safe and efficient nanofiber patch was designed via electrospinning for combined photothermal-chemotherapy of abdominal tumors. By loading copper sulfide nanoparticles and polydopamine, the patch achieved efficient photothermal effects under safe NIR II laser irradiation. Moreover, the patch exhibited pH/NIR dual-responsive drug release through polydopamine protonation and photothermally enhanced diffusion. With these superior properties, the implantable patch can non-invasively ablate solid tumors via photothermal therapy and eliminate residual cancer cells through controllable chemotherapy, while maintaining low systemic toxicity. Notably, this safe and effective therapeutic strategy exhibited significantly higher tumor apoptosis (68.6%) than the control of only chemotherapy patch (29.3%) or photothermal therapy patch (42.5%). The DPPCP patch + NIR group exhibited dramatically decreased signal intensity, demonstrating superior antitumor efficacy. Moreover, the DPPCP patch enabled 100% survival of nude mice over 90 days. In this work, the patch-mediated combined photothermal-chemotherapy strategy holds promise as an alternative to clinical surgical resection and postoperative chemotherapy, addressing the treatment needs of diverse cancer patients.</p>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"100582"},"PeriodicalIF":7.9,"publicationDate":"2026-06-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13262176/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148251478","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

ROS-responsive tegafur-pheophorbide a conjugate-loaded microneedles for deep drug delivery and chemo-photodynamic therapy of superficial tumors. 一种用于深部药物传递和浅表肿瘤化学光动力治疗的偶联负载微针。

IF 7.9 2区医学

International Journal of Pharmaceutics: X Pub Date : 2026-06-02 eCollection Date: 2026-06-01 DOI: 10.1016/j.ijpx.2026.100580

Anning Li, Yingjie Ma, Yunfeng Dai, Yibin Guo, Yanjun He, Sihan Chen, Xinjie Su, Chenxi Fang, Long Chen, Meitao Duan, Ming Chen, Jungang Ren, Li Wang, Chen Wang, Zhiqiang Zhang

{"title":"ROS-responsive tegafur-pheophorbide a conjugate-loaded microneedles for deep drug delivery and chemo-photodynamic therapy of superficial tumors.","authors":"Anning Li, Yingjie Ma, Yunfeng Dai, Yibin Guo, Yanjun He, Sihan Chen, Xinjie Su, Chenxi Fang, Long Chen, Meitao Duan, Ming Chen, Jungang Ren, Li Wang, Chen Wang, Zhiqiang Zhang","doi":"10.1016/j.ijpx.2026.100580","DOIUrl":"10.1016/j.ijpx.2026.100580","url":null,"abstract":"<p><p>Superficial tumors, including breast cancer, melanoma, and oral carcinoma, pose significant treatment challenges due to their anatomical location and the inherent limitations of conventional therapies, such as systemic toxicity and poor tumor specificity. Chemotherapy often leads to severe side effects, while photodynamic therapy (PDT) is hindered by the limited tissue penetration of both light and photosensitizers. To address these issues, we developed an innovative reactive oxygen species (ROS)-responsive drug delivery system based on a conjugate of tegafur (TF) and pheophorbide a (PPa) linked <i>via</i> a thioether bond. This prodrug (TF-TA-PPa) integrates chemotherapy and PDT into a single molecular entity, enabling synergistic anti-tumor effects. To enhance localized delivery and patient compliance, the conjugate was encapsulated into polymeric micelles and further incorporated into soluble microneedles (MNs) containing cell-penetrating peptides. The resulting TF-TA-PPa@PMN system enables painless transdermal administration, deep tumor penetration, and on-demand drug release triggered by near-infrared laser irradiation through ROS-mediated cleavage of the thioether linker. Comprehensive <i>in vitro</i> and <i>in vivo</i> evaluations demonstrated excellent biocompatibility, sustained drug release profiles, enhanced cellular uptake, and potent tumor suppression in a 4 T1 breast cancer model, achieving a remarkable tumor inhibition rate of 89.2% with minimal systemic toxicity. This integrated platform represents a promising strategy for the localized, combinatory treatment of superficial tumors with improved efficacy and reduced side effects.</p>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"100580"},"PeriodicalIF":7.9,"publicationDate":"2026-06-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13264333/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148251594","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Ligand-modified liposomes as drug delivery systems for the active targeting of pancreatic cancer 配体修饰脂质体作为主动靶向胰腺癌的药物递送系统

IF 6.4 2区医学

International Journal of Pharmaceutics: X Pub Date : 2026-06-01 Epub Date: 2026-01-02 DOI: 10.1016/j.ijpx.2026.100483

Yerin Jang , Jaehee Jang , Jaewoo Son , Hee-Young Lee , Jonghoon Choi

{"title":"Ligand-modified liposomes as drug delivery systems for the active targeting of pancreatic cancer","authors":"Yerin Jang , Jaehee Jang , Jaewoo Son , Hee-Young Lee , Jonghoon Choi","doi":"10.1016/j.ijpx.2026.100483","DOIUrl":"10.1016/j.ijpx.2026.100483","url":null,"abstract":"<div><div>Pancreatic cancer is among the most fatal malignancies worldwide. The aggressive nature of this disease, coupled with late-stage diagnosis and limited therapeutic options, highlights the urgent need for innovative treatment approaches. Targeted therapy has emerged as a promising strategy to enhance therapeutic efficacy while minimizing systemic toxicity. Liposomes, as versatile nanoparticles, have shown significant potential to contribute to the develpment of drug delivery system. These lipid-based vesicles encapsulate chemotherapeutic drugs, shield them from degradation, and promote greater accumulation within tumor cites. Furthermore, liposomes can be surface-modifed with various ligands to improve their specificity and cellular uptake. Research on liposome-based targeted chemotherapy for pancreatic cancer has explored useful ligand-based strategies to enhance drug delivery to pancreatic cancer cells. In this review, liposome-based targeted strategies for pancreatic cancer are classified by ligand type, including antibodies, aptamers, carbohydrates, proteins and peptides, and integrates case studies to demonstrate how different targeting approaches translate into improved cellular uptake, therapeutic efficacy, and antitumor effects. In addition, emerging formulations such as dual-targeting liposomes are described, highlighting their potential to further strengthen treatment performance. The review summarizes the current research landscape of liposome-based targeted drug delivery systems for pancreatic cancer, providing insights into promising biomarkers and ligand-mediated targeting strategies. It further discusses broader opportunities for target exploration and liposomal design optimization, as well as future research directions aimed at overcoming existing limitations and improving therapeutic outcomes.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100483"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145921844","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Enhancing islet transplantation outcomes in T1DM: The promise of mesenchymal stem cells and exosomes 增强胰岛移植治疗T1DM的结果：间充质干细胞和外泌体的前景

IF 6.4 2区医学

International Journal of Pharmaceutics: X Pub Date : 2026-06-01 Epub Date: 2026-01-31 DOI: 10.1016/j.ijpx.2026.100498

Ying Zhang , Xiaoyue Chen , Zhuoxun Huang , Yifan Qiu , Longfa Kou , Qing Yao

{"title":"Enhancing islet transplantation outcomes in T1DM: The promise of mesenchymal stem cells and exosomes","authors":"Ying Zhang , Xiaoyue Chen , Zhuoxun Huang , Yifan Qiu , Longfa Kou , Qing Yao","doi":"10.1016/j.ijpx.2026.100498","DOIUrl":"10.1016/j.ijpx.2026.100498","url":null,"abstract":"<div><div>Islet transplantation represents a promising therapeutic strategy for type 1 diabetes mellitus (T1DM), yet its clinical application is constrained by hypoxia, oxidative stress, and immune rejection during islet isolation, culture, and post-transplantation. In recent years, mesenchymal stem cells (MSCs) have demonstrated the ability to enhance islet survival and function through immunomodulation, anti-inflammatory effects, and paracrine signaling. Among the secreted components, exosomes have emerged as key mediators of MSC function, capable of delivering nucleic acids, proteins, and lipids to target cells with high biocompatibility and low immunogenicity. This review highlights recent advances in utilizing MSCs and MSC-derived exosomes to improve islet engraftment and long-term function. Particular emphasis is placed on exosome engineering strategies—such as therapeutic cargo loading and targeted delivery—as well as encapsulation techniques that facilitate sustained release and graft protection. Despite encouraging preclinical results, the field remains in its early stages, and further research is required to standardize exosome isolation, elucidate mechanisms of action, and ensure clinical translatability. Harnessing the full potential of MSC-derived exosomes may offer a next-generation approach for achieving durable glycemic control and β-cell regeneration in T1DM.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100498"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146188934","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Brain-targeted delivery of siRNA via non-viral delivery systems, the therapeutic strategy for Alzheimer's disease—Unveiling challenges and prospects 通过非病毒传递系统的siRNA脑靶向递送，阿尔茨海默病的治疗策略-揭示挑战和前景

IF 6.4 2区医学

International Journal of Pharmaceutics: X Pub Date : 2026-06-01 Epub Date: 2026-02-05 DOI: 10.1016/j.ijpx.2026.100503

Lili Gu , Jiayi Liu , Can Wang , Xiaoqin Shan , Siyi Li , Xinyue Zhang , Lijie Xia , Jinyao Li

{"title":"Brain-targeted delivery of siRNA via non-viral delivery systems, the therapeutic strategy for Alzheimer's disease—Unveiling challenges and prospects","authors":"Lili Gu , Jiayi Liu , Can Wang , Xiaoqin Shan , Siyi Li , Xinyue Zhang , Lijie Xia , Jinyao Li","doi":"10.1016/j.ijpx.2026.100503","DOIUrl":"10.1016/j.ijpx.2026.100503","url":null,"abstract":"<div><div>Alzheimer's disease (AD) is a neurodegenerative disorder characterized by cognitive and behavioral issues, posing significant public health challenges. Small interfering RNAs (siRNAs) offer the potential to selectively silence AD-related pathogenic genes. This review first outlines the diverse pathogenic mechanisms and hallmark pathologies of AD, then spotlights the key genes now being silenced by siRNA for therapeutic intervention. These genes encompass those directly implicated in amyloidogenesis, tau phosphorylation, and neuroinflammation, along with those aberrantly up-regulated and associated with AD pathology. Finally, it summarizes recent research on non-viral and local siRNA delivery strategies including lipid, polymer, quantum dots, inorganic materials, extracellular vesicles, and conjugates aimed at effectively penetrating the blood-brain barrier while overcoming intra- and extracellular barriers to target key AD pathways. These findings underscore the promise of siRNA therapy in addressing AD pathology and provide valuable insights into overcoming delivery challenges.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100503"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146188935","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Stabilization strategies and advancements in lyophilization to preserve integrity and efficacy of next-generation biologicals 冷冻干燥的稳定策略和进展，以保持下一代生物制品的完整性和有效性

IF 6.4 2区医学

International Journal of Pharmaceutics: X Pub Date : 2026-06-01 Epub Date: 2026-05-26 DOI: 10.1016/j.ijpx.2026.100575

Ravi Maharjan , Chang Yell Shin , Seon-Kwang Lee , Eun-Sol Ha , Heejun Park , Jeong-Soo Kim , Ki Hyun Kim , Nam Ah. Kim , Min-Soo Kim , Seong Hoon Jeong

{"title":"Stabilization strategies and advancements in lyophilization to preserve integrity and efficacy of next-generation biologicals","authors":"Ravi Maharjan , Chang Yell Shin , Seon-Kwang Lee , Eun-Sol Ha , Heejun Park , Jeong-Soo Kim , Ki Hyun Kim , Nam Ah. Kim , Min-Soo Kim , Seong Hoon Jeong","doi":"10.1016/j.ijpx.2026.100575","DOIUrl":"10.1016/j.ijpx.2026.100575","url":null,"abstract":"<div><div>The success of mRNA-lipid nanoparticles (LNPs) vaccines during the COVID-19 pandemic has significantly increased global demand for stable, thermo-resistant biologicals. Lyophilization remains a cornerstone technology for enhancing the stability of these formulations; however, the freezing and drying processes impose major stresses that can compromise the integrity of fragile LNPs. This review systematically explores the molecular mechanisms by which lyoprotectants, including sugars, polyols, amino acids, and polymers, mitigate challenges such as ice-induced denaturation, dehydration-driven aggregation, and interfacial destabilization. This review emphasizes the importance of optimized sucrose-trehalose combinations and effective ice-nucleation control in preserving encapsulation efficiency and maintaining particle integrity. Furthermore, the review discusses advanced process optimization tools, including digital twin modeling and in-line Raman spectroscopy, which enhance lyophilization efficiency by reducing primary drying times by up to 40% while ensuring critical quality attributes are preserved. Additionally, emerging applications utilizing novel excipient combinations are highlighted, showcasing their potential to enable refrigerated storage of viral vectors. With 85% of commercial conjugates relying on lyophilization, recent advancements in continuous freeze-drying technology, such as spin-freeze approaches, have achieved cycle times that are three-fold faster. These developments provide a comprehensive roadmap for overcoming cold chain limitations while addressing the stabilization needs of next-generation biologicals, CRISPR-based systems, and personalized medicines.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100575"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148184151","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Data-efficient prediction in tableting using word embeddings and empirically-guided neural networks 使用词嵌入和经验引导神经网络的数据高效预测

IF 6.4 2区医学

International Journal of Pharmaceutics: X Pub Date : 2026-06-01 Epub Date: 2025-12-03 DOI: 10.1016/j.ijpx.2025.100458

Najeeb Abdelrahman, Stefan Klinken-Uth

{"title":"Data-efficient prediction in tableting using word embeddings and empirically-guided neural networks","authors":"Najeeb Abdelrahman, Stefan Klinken-Uth","doi":"10.1016/j.ijpx.2025.100458","DOIUrl":"10.1016/j.ijpx.2025.100458","url":null,"abstract":"<div><div>The development of robust oral tablet formulations remains time-consuming, often limited by scarce data and the difficulty of incorporating categorical formulation variables into predictive models. Traditional regression methods are interpretable but struggle with nonlinear interactions, whereas modern machine learning approaches offer higher predictive power at the expense of transparency. In this study, we present a neural network framework that employs word embedding layers to represent categorical formulation factors, such as active pharmaceutical ingredients (APIs), as trainable semantic vectors. These embeddings are integrated with empirically-guided output functions and a deep ensemble strategy to predict tablet quality attributes, including tensile strength and density as well as ejection force, and dosing height, based solely on formulation composition, compression pressure, and tablet weight. The model achieved predictive accuracy comparable to or exceeding classical regression while reliably avoiding physically implausible outputs. Analysis of the learned embedding vectors revealed meaningful clustering of APIs, enabling transfer learning across materials and robust predictions even for APIs with few or no training data. Furthermore, information gain analysis demonstrated that low-concentration formulations can substantially enhance predictive accuracy, supporting more material-efficient experimental designs. These results highlight embedding-based, empirically-guided neural networks as explainable and practical tools that could accelerate pharmaceutical formulation development in the future.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100458"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145977954","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Nanoparticle carriers in the treatment of intracellular bacterial infections: Current approaches and challenges 纳米颗粒载体治疗细胞内细菌感染：目前的方法和挑战

IF 6.4 2区医学

International Journal of Pharmaceutics: X Pub Date : 2026-06-01 Epub Date: 2026-05-20 DOI: 10.1016/j.ijpx.2026.100574

Zheng Lu , Bin He , Zhixin Lei , Lijun Wu , Dongyang Ye , Dan Xu , Shanqin Chen , Xiaotian Zhang , Ziqi Weng

{"title":"Nanoparticle carriers in the treatment of intracellular bacterial infections: Current approaches and challenges","authors":"Zheng Lu , Bin He , Zhixin Lei , Lijun Wu , Dongyang Ye , Dan Xu , Shanqin Chen , Xiaotian Zhang , Ziqi Weng","doi":"10.1016/j.ijpx.2026.100574","DOIUrl":"10.1016/j.ijpx.2026.100574","url":null,"abstract":"<div><div>Pathogenic bacterial intracellular infection by <em>Mycobacterium tuberculosis</em> and <em>Staphylococcus aureus</em> is a major complication to treatment because of resistance to immune actions and the ability to withstand traditional antibiotics. Failure of existing therapies is usually due to inefficient intracellular penetration of drugs and inappropriate targeting of subcellular sites. We discuss the nanoparticle drug delivery systems (NDDSs) here that enhance intracellular delivery of antibiotics using customized carrier materials, targeted internalization processes and stimuli-responsive release of antibiotics. These systems enhance specificity of pathogen targeting and efficacy of drugs and overcome barriers of microenvironment. We also address translational challenges such as toxicity, heterogeneity of infection, scalability of manufacturing, and scanty clinical data. Future trends include versatile hybrid vehicles, combination with immunomodulators or gene-editing applications and AI-enhanced personalized nanomedicine. The potential to tackle pathogen-specific issues with nanotechnology advances can provide possible solutions to the treatment of persistent intracellular infections and antibiotic resistance, which are the prospects with NDDSs.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100574"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148184152","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Improving the bioavailability of nintedanib by formulating inhalable ufasomes as a targeted therapy for non-small cell lung cancer 提高尼达尼布的生物利用度，通过制定可吸入的非小细胞肺癌的靶向治疗

IF 6.4 2区医学

International Journal of Pharmaceutics: X Pub Date : 2026-06-01 Epub Date: 2025-12-30 DOI: 10.1016/j.ijpx.2025.100482

Salman M. Ghazwani , Sami Alhazmi , Salhah M. Ghazwani , Hussam M. Shubaily , Ahmed M. Wafi , Naifa Alenazi , Marwa Qadri , Amal Naif Alshammari , Wedad Mawkili , Jobran M. Moshi , Zenat Khired , Salama A. Salama

{"title":"Improving the bioavailability of nintedanib by formulating inhalable ufasomes as a targeted therapy for non-small cell lung cancer","authors":"Salman M. Ghazwani , Sami Alhazmi , Salhah M. Ghazwani , Hussam M. Shubaily , Ahmed M. Wafi , Naifa Alenazi , Marwa Qadri , Amal Naif Alshammari , Wedad Mawkili , Jobran M. Moshi , Zenat Khired , Salama A. Salama","doi":"10.1016/j.ijpx.2025.100482","DOIUrl":"10.1016/j.ijpx.2025.100482","url":null,"abstract":"<div><div>The safety and effectiveness of nintedanib in treating non-small cell lung cancer (NSCLC) have been evaluated in several clinical trials. However, nintedanib exhibits low oral bioavailability due to its poor solubility and first-pass metabolism. To enhance the sustainability, targeting, bioavailability, and effectiveness of nintedanib, a targeted therapy for NSCLC was developed in the form of nebulized nintedanib ufasomes (NLU). Various NLU formulations were optimized utilizing the Design Expert software. The selected NLU was then evaluated for its aerodynamics, cytotoxicity, bioavailability, and targeting capabilities. To evaluate the effectiveness and safety of the optimal NLU formulation, a dose-dependent study was conducted using a mouse model of lung cancer induced by Lewis lung carcinoma (LLC) cell lines. The selected NLU formulation increased the sustainability, bioavailability, and targeting capability of nintedanib by 49.5 %, 6.63-fold, and 8.99-fold, respectively. Additionally, it decreased the IC<sub>50</sub> value by 4.7-fold. The nebulized NLU showed better anti-tumor, anti-inflammatory, and anti-oxidative effects than oral nintedanib in terms of LDH, CEA, AFP, MDA, TNF-α, and IL-1β. The histopathological analysis confirmed these results. The safety and efficacy studies demonstrated that the nebulized NLU formulation at a dose of 100 mg/kg could serve as a viable therapy for NSCLC.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100482"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146034577","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Can therapeutic potency of a cancer nanomedicine be predicted by pain-related behavioral test in subcutaneous tumor model? 皮下肿瘤模型疼痛相关行为测试能否预测纳米肿瘤药物的治疗效果？

IF 6.4 2区医学

International Journal of Pharmaceutics: X Pub Date : 2026-06-01 Epub Date: 2025-11-17 DOI: 10.1016/j.ijpx.2025.100450

Ye Tao , Xiaohui Cai , Zhongping Chen

{"title":"Can therapeutic potency of a cancer nanomedicine be predicted by pain-related behavioral test in subcutaneous tumor model?","authors":"Ye Tao , Xiaohui Cai , Zhongping Chen","doi":"10.1016/j.ijpx.2025.100450","DOIUrl":"10.1016/j.ijpx.2025.100450","url":null,"abstract":"<div><div>Cancer nanomedicines have shown great potential in fighting against cancer. While the development of cancer nanomedicines is advancing rapidly, preclinical assessment approaches for their therapeutic potency have stagnated. In view of high prevalence of cancer pain in cancer patients, we aim to determine whether therapeutic potency of a cancer nanomedicine can be predicted by pain-related behavioral test in subcutaneous tumor model, the simplest and most widely used tumor model in oncology. Behavioral profiles reveal that subcutaneous tumor, probably irrespective of tumor type, presents with spontaneous pain (open field test) and evoked pain (von Frey test for mechanical allodynia; Hargreaves test, hot plate test, and tail flick test for thermal hyperalgesia; cold plate test and acetone drop test for thermal allodynia). Using doxorubicin (DOX)-loaded lipid nanoparticles (LNPs) (LNPs/DOX) as a representative cancer nanomedicine and ropivacaine (ROP)-loaded LNPs (LNPs/ROP) as a pain nanomedicine, it is validated that inhibiting subcutaneous tumor growth can relieve cancer pain, while delaying the growth cannot, despite a significant difference found compared with non-treatment group. Moreover, behavioral results in all the tests are consistent and von Frey test is suggested the most sensitive among them. It is strongly suggested that pain-related behavioral test can serve as a powerful tool to predict therapeutic potency of a cancer nanomedicine <em>in vivo</em> in treating subcutaneous tumor.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100450"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145921846","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0