International Journal of Pharmaceutics: X最新文献_第3页

Chitosan-based nanozyme hydrogels: Advanced antioxidant and sustained-release systems for the prevention and treatment of skin photoaging 壳聚糖基纳米酶水凝胶：先进的抗氧化和缓释系统，用于预防和治疗皮肤光老化

IF 6.4 2区医学

International Journal of Pharmaceutics: X Pub Date : 2026-06-01 Epub Date: 2026-01-13 DOI: 10.1016/j.ijpx.2026.100491

Qucheng Huang , Xiaojun Zhang , YuanYuan Zuo , Leiyi Wang , Huan Sun , Hewei Xu , Miao Yu , Chang Liu

{"title":"Chitosan-based nanozyme hydrogels: Advanced antioxidant and sustained-release systems for the prevention and treatment of skin photoaging","authors":"Qucheng Huang , Xiaojun Zhang , YuanYuan Zuo , Leiyi Wang , Huan Sun , Hewei Xu , Miao Yu , Chang Liu","doi":"10.1016/j.ijpx.2026.100491","DOIUrl":"10.1016/j.ijpx.2026.100491","url":null,"abstract":"<div><div>Photoaging of the skin is a chronic damage process caused by prolonged exposure to ultraviolet radiation, characterized by increased oxidative stress, activation of inflammatory responses, and collagen degradation. However, photoaging of the skin presents challenges in prevention, limited efficacy of therapeutic agents, and difficulties in repairing the damage. In recent years, chitosan-based hydrogels, which exhibit excellent biocompatibility, biodegradability, film-forming properties, and the ability to deliver sustained-release medication, have progressively emerged as cutting-edge therapeutic agents for treating photoaging of the skin. Nanozymes are nanomaterials possessing enzymatic functions that effectively scavenge reactive oxygen species generated by ultraviolet irradiation, exhibiting excellent antioxidant properties. Loading nanozymes into chitosan-based hydrogels not only combines the biocompatibility of chitosan hydrogels with the antioxidant properties of nanozymes to enhance therapeutic efficacy but also enables stable loading and controlled release of drugs and active ingredients. This further improves treatment efficiency while fully leveraging the moisturizing and restorative properties of the hydrogel matrix. This paper systematically summarizes the construction methods, performance optimization, and mechanism of action of chitosan-based nanozyme hydrogels in preventing and treating skin photoaging. It focuses on analyzing research advances in their capacity to scavenge free radicals, alleviate inflammation, and promote skin barrier repair, while exploring their application prospects and challenges in skin repair and the cosmetics sector.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100491"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145977959","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

Functionalized polysaccharides for infection-resistant and regenerative therapies in gynecology 用于妇科抗感染和再生治疗的功能化多糖。

IF 6.4 2区医学

International Journal of Pharmaceutics: X Pub Date : 2026-06-01 Epub Date: 2026-05-16 DOI: 10.1016/j.ijpx.2026.100568

Yingying Hao , Daming Chu , Hui Li , Lufeng Zheng , Yan Liu , Qi Xi , Sishi Liu

{"title":"Functionalized polysaccharides for infection-resistant and regenerative therapies in gynecology","authors":"Yingying Hao , Daming Chu , Hui Li , Lufeng Zheng , Yan Liu , Qi Xi , Sishi Liu","doi":"10.1016/j.ijpx.2026.100568","DOIUrl":"10.1016/j.ijpx.2026.100568","url":null,"abstract":"<div><div>Gynecological infections and implant-related complications, such as bacterial vaginosis (BV), pelvic inflammatory disease (PID), and endometritis, are exacerbated by biofilm-forming pathogens such as <em>G. vaginalis</em>, <em>E. coli</em>, and <em>S. aureus</em>, posing significant clinical challenges worldwide. These biofilms, resistant to antibiotics, contribute to chronic infections and device failures in gynecological implants. Rising antibiotic resistance underscores the need for innovative biomaterials. Chitosan, hyaluronic acid (HA) and alginate are three representative natural polysaccharides, showing broad application potential in antibacterial materials and tissue engineering due to their excellent biocompatibility, biodegradability and modifiable structures. In their natural forms, they exhibit a certain degree of anti-biofilm activity by inhibiting bacterial adhesion and disrupting bacterial membranes. Functional modification significantly enhances their antibacterial performance such as AMPs grafting, cross-linking, quaternization, and nanocomposites. This review explores the antibacterial mechanisms of natural polysaccharides in the vaginal microbiome and endometrial tissue, highlighting advances in functionalization with antimicrobial peptides, nanoparticles, and chemical modifications to enhance antibacterial efficacy. The toxicological effects of natural polysaccharide materials on gynecological tissues generally show the characteristics of mainly protective and restorative effects, rather than causing damage. Natural polysaccharides and their applications offer promising potential for infection-resistant, regenerative therapies in gynecology, promising safer and more effective interventions.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100568"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148156392","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

3D-printed polypills for personalized medicine and precision oral drug delivery in pharmaceutical practice: A review 在制药实践中用于个性化医疗和精确口服给药的3d打印复方药丸：综述

IF 6.4 2区医学

International Journal of Pharmaceutics: X Pub Date : 2026-06-01 Epub Date: 2025-12-19 DOI: 10.1016/j.ijpx.2025.100474

Mahesha Keerikkadu, Sathvik Chennamsetty, Akshay Shetty, Vamshi Krishna Tippavajhala, Mahalaxmi Rathnanand

{"title":"3D-printed polypills for personalized medicine and precision oral drug delivery in pharmaceutical practice: A review","authors":"Mahesha Keerikkadu, Sathvik Chennamsetty, Akshay Shetty, Vamshi Krishna Tippavajhala, Mahalaxmi Rathnanand","doi":"10.1016/j.ijpx.2025.100474","DOIUrl":"10.1016/j.ijpx.2025.100474","url":null,"abstract":"<div><div>3D-printed polypills have considerably changed the way oral medications can be delivered. They offer a way to create a single dosage form that can be customized to meet the needs of individual patients, while also allowing multiple drugs to be stored in distinct compartments, layers, or designs. Using 3D printing techniques such as fused deposition modeling (FDM), inkjet printing, stereolithography (SLA), selective laser sintering (SLS), and Arburg Plastic Freeforming (APF), it is possible to create tablet structures that provide control over various aspects of dissolution and drug release through engineered porosity and density of the material used during fabrication. Several technologies have been developed to enable the fabrication of polypills, along with methods for selecting the correct excipients, controlling drug release through various mechanisms, and considering the principles of quality-by-design when creating a polypill. In recent years, new material innovations have significantly enhanced the ability of polypills to deliver drugs with improved mechanical strength, stability, and accuracy upon printing. The ability to provide personalized medication regimens for patients with chronic diseases requiring precise titration or a complex regimen is expected to have a great impact on the management of patients taking 3D-printed polypills. 3D-printed polypills have significant translational challenges due to inconsistent production, difficulty obtaining regulatory approval, the inability to scale up batch manufacture, and inadequate long-term stability of the final product.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100474"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145921834","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

ROS-triggered smart hydrogel adhesives for modulating the inflammatory microenvironment and promoting tendon-bone interface regeneration ros触发的智能水凝胶粘合剂用于调节炎症微环境和促进肌腱-骨界面再生

IF 6.4 2区医学

International Journal of Pharmaceutics: X Pub Date : 2026-06-01 Epub Date: 2026-01-30 DOI: 10.1016/j.ijpx.2026.100502

Hebei He , Yifen Lin , Jia Fang , Kai He , Wenjun Li , Min Du , Shilong Lin , Xiaofei Zheng , Hanyu Lu

{"title":"ROS-triggered smart hydrogel adhesives for modulating the inflammatory microenvironment and promoting tendon-bone interface regeneration","authors":"Hebei He , Yifen Lin , Jia Fang , Kai He , Wenjun Li , Min Du , Shilong Lin , Xiaofei Zheng , Hanyu Lu","doi":"10.1016/j.ijpx.2026.100502","DOIUrl":"10.1016/j.ijpx.2026.100502","url":null,"abstract":"<div><div>Currently, suture surgery for rotator cuff repair is unable to regenerate the original functional fibrocartilage layer at the tendon-bone interface, resulting in high postoperative retear rates. In this study, a ROS-triggered smart hydrogel adhesive (DPQP@ME) was designed to synergistically enhance the functional repair of the tendon-bone interface during suture surgery by modulating the inflammatory microenvironment, promoting cell differentiation, and providing mechanically adaptive support. Metal-phenolic nanoparticles (ME) with multiple bioactivities were formed through the self-assembly of epigallocatechin gallate (EGCG) and Mg<sup>2+</sup>. Subsequently, ME, dithiothreitol (DTT), polyethylene glycol diacrylate (PEGDA), and boronic acid-modified quaternary ammonium chitosan (QCS-PBA) were crosslinked <em>via</em> borate ester bonds, thioether bonds, and photo-crosslinking to form a bioactive hydrogel adhesive with ROS responsiveness and favorable mechanical properties. Based on the ROS sensitivity of the borate ester bonds and thioether bonds, DPQP@ME exhibited favorable ROS-responsive drug release properties, with ME release reaching 73.15 ± 1.35% in H<sub>2</sub>O<sub>2</sub>-containing PBS <em>versus</em> 33.15 ± 1.65% in PBS alone. <em>In vitro</em> cellular experiments demonstrated that DPQP@ME could effectively reduce intracellular ROS levels, regulate macrophage polarization toward an anti-inflammatory phenotype, and promote osteogenic differentiation as well as cartilage formation. Animal studies further demonstrated that DPQP@ME significantly attenuated inflammatory responses and promoted functional reconstruction of the tendon-bone interface. In conclusion, this novel smart hydrogel adhesives provides a promising therapeutic strategy for tendon healing.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100502"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146188931","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

Comparing the efficacy of nanocarriers for cutaneous and follicular delivery of poorly water-soluble molecules: A case study with ciclosporin A 比较纳米载体对皮肤和滤泡递送水溶性较差分子的功效：环孢素A的案例研究

IF 6.4 2区医学

International Journal of Pharmaceutics: X Pub Date : 2026-06-01 Epub Date: 2026-02-10 DOI: 10.1016/j.ijpx.2026.100505

Aditya R. Darade , Maria Lapteva , Yogeshvar N. Kalia

{"title":"Comparing the efficacy of nanocarriers for cutaneous and follicular delivery of poorly water-soluble molecules: A case study with ciclosporin A","authors":"Aditya R. Darade , Maria Lapteva , Yogeshvar N. Kalia","doi":"10.1016/j.ijpx.2026.100505","DOIUrl":"10.1016/j.ijpx.2026.100505","url":null,"abstract":"<div><div>Therapeutic agents approved for the topical treatment of dermatological diseases have diverse physicochemical properties, but they are frequently poorly water-soluble, which makes it a challenge to prepare stable aqueous formulations with good delivery characteristics. Several types of nanocarrier have been reported to facilitate formulation and to enhance cutaneous delivery but there are few direct comparisons of nanocarriers in terms of their ability to deliver a specific molecule to the skin under the same controlled conditions. The present study aimed to address this by developing, optimizing, and comparing different nanocarriers with respect to their ability to deliver ciclosporin A (CsA) to the skin and the hair follicle. Nanoconstructs were categorized as vesicular carriers (micelles and liposomes), emulsion-based systems (microemulsions and nanoemulsions), and nanoparticle systems (e.g. polymeric nanoparticles, solid lipid nanoparticles, nanostructured lipid carriers). Formulations were optimized using a design of experiments approach and were characterized with respect to size, morphology and incorporation efficiency. Cutaneous and follicular delivery experiments were performed using porcine skin. CsA deposition, cutaneous biodistribution, follicular delivery and targeting potential (ratio of delivery to skin with and without pilosebaceous units) were assessed. Nanoemulsions, kinetically stable systems with high thermodynamic activity, showed the highest cutaneous delivery of CsA among the nanosystems tested followed by solid lipid nanoparticles and mPEG-dihexPLA micelles – i.e. three different types of nanocarrier. The results confirmed the pivotal role of thermodynamic activity in determining delivery efficiency of a nanocarrier and its greater importance than other routinely studied morphological parameters such as nanocarrier size: the smallest nanocarriers did not yield the highest delivery.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100505"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146188932","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

Engineering exosomes for cancer therapy - Modification technologies and subcellular targeting strategies: A review 用于癌症治疗的工程外泌体-修饰技术和亚细胞靶向策略：综述

IF 6.4 2区医学

International Journal of Pharmaceutics: X Pub Date : 2026-06-01 Epub Date: 2025-12-31 DOI: 10.1016/j.ijpx.2025.100473

Fengbo Liu, Chengxing Xia, Hang Yu, Xiaofang Yang, Liping Ge, Chunwei Ye

{"title":"Engineering exosomes for cancer therapy - Modification technologies and subcellular targeting strategies: A review","authors":"Fengbo Liu, Chengxing Xia, Hang Yu, Xiaofang Yang, Liping Ge, Chunwei Ye","doi":"10.1016/j.ijpx.2025.100473","DOIUrl":"10.1016/j.ijpx.2025.100473","url":null,"abstract":"<div><div>Exosomes are secreted lipid bilayer vesicles of 30–150 nm in diameter. Their low immunogenicity, excellent biocompatibility, and inherent targeting capability make them a promising drug delivery vehicle for cancer therapeutics. However, the use of natural exosomes is still challenging for therapeutic applications, including limited targeting precision and drug-loading efficiency, necessitating engineered modification strategies to optimize their performance. To further enhance exosome targeting capacity, recent studies have explored precision delivery strategies targeting subcellular structures such as lysosomes, nuclei, mitochondria, and the endoplasmic reticulum, thereby improving exosome therapeutic potential. This review systematically summarizes the core advantages of exosomes as drug carriers, elaborates on their engineering modification methods, and highlights recent advances in strategies to improve exosomes targeting of subcellular structures to enhance antitumor efficacy. The review aims to provide a theoretical foundation and technical guidance for developing exosome-based precision therapies for cancer.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100473"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145921845","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

3D printed system using ex vivo porcine eye globes to investigate intracorneal absorption of dexpanthenol from contact lens care solution and eye drops 3D打印系统使用离体猪眼球来研究隐形眼镜护理液和眼药水中葡聚糖醇的角膜内吸收

IF 6.4 2区医学

International Journal of Pharmaceutics: X Pub Date : 2026-06-01 Epub Date: 2025-12-17 DOI: 10.1016/j.ijpx.2025.100472

Verena Santer , Adyl-Michaёl El Guamra , Tohru Kawaguchi , Mouad Lamrani , Yogeshvar N. Kalia

{"title":"3D printed system using ex vivo porcine eye globes to investigate intracorneal absorption of dexpanthenol from contact lens care solution and eye drops","authors":"Verena Santer , Adyl-Michaёl El Guamra , Tohru Kawaguchi , Mouad Lamrani , Yogeshvar N. Kalia","doi":"10.1016/j.ijpx.2025.100472","DOIUrl":"10.1016/j.ijpx.2025.100472","url":null,"abstract":"<div><div>Reduction of the use of animal models in research is encouraged for the sake of animal wellbeing. However, available <em>in vitro</em> models in the specific case of topical ocular delivery/penetration studies are often oversimplified by the use of excised corneal or scleral tissue and the frequent lack of dynamic barriers such as the lacrimal outwash. This is why we have developed our novel <em>ex vivo</em> porcine eye globe 3D printed laboratory setup with simulated tear flow, using enucleated porcine eyes. This setup was employed to investigate the penetration of a common topical formulation excipient Dexpanthenol (Dxp). First, Dxp deposition in soft contact lenses following usage of SOLOCARE AQUA® care solution was quantified by UHPLC-MS/MS. The subsequent penetration into corneal tissue and aqueous humour of Dxp from SOLOCARE AQUA® care solution treated contact lenses was compared to that following application of eye drop solutions Bepanthen® and Siccaprotect®, containing equivalent Dxp concentrations. The results showed that the Dxp concentration in the anterior segment was three-fold higher after application of the Dxp-containing eye drops as compared to contact lens application. Given that Dxp uptake was greater following the application of the marketed eye drops, this confirmed the safety of the Dxp-containing contact lens care solution. This research demonstrates how topical delivery studies on the ocular surface can be simulated in our novel <em>ex vivo</em> porcine eye globe model without the need to sacrifice laboratory animals<strong>.</strong></div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100472"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145799374","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

Application of ultrasound and ultrasound-responsive materials in wounds: A systematic review 超声及超声反应材料在伤口中的应用综述

IF 6.4 2区医学

International Journal of Pharmaceutics: X Pub Date : 2026-06-01 Epub Date: 2026-01-08 DOI: 10.1016/j.ijpx.2026.100485

Jialei Luo , Liwan Song , Xinyi Yan , Xiaolu Ma , Jianqing Gao , Ying Luo , Gaoyi Yang

{"title":"Application of ultrasound and ultrasound-responsive materials in wounds: A systematic review","authors":"Jialei Luo , Liwan Song , Xinyi Yan , Xiaolu Ma , Jianqing Gao , Ying Luo , Gaoyi Yang","doi":"10.1016/j.ijpx.2026.100485","DOIUrl":"10.1016/j.ijpx.2026.100485","url":null,"abstract":"<div><div>Wound healing is a multifaceted biological process that is highly susceptible to disruption by numerous internal and external factors, resulting in delayed tissue repair. Recent advancements have highlighted the therapeutic potential of ultrasound, especially when integrated with emerging smart materials, which together offer promising strategies for enhancing wound care outcomes. Low- and high-intensity ultrasound (US) use mechanisms such as cavitation, acoustic streaming, and radiation forces to disrupt biofilms, improve drug permeability, and promote tissue regeneration. When combined with US-responsive materials, such as scaffolds, piezoelectric composites, microbubbles, microneedles, and flexible patches, these systems enable targeted functions, including controlled drug release, antimicrobial activity, and enhanced deep tissue penetration. These responsive materials effectively overcome the limitations of conventional wound dressings, which often suffer from poor drug bioavailability, susceptibility to infection, and a lack of personalized therapeutic capabilities. This review systematically explores 5 categories of advanced materials, with a focus on their synergistic interactions with ultrasound to enhance wound healing outcomes. By elucidating the interactions between material-US and their translational implications, this review offers new perspectives to advance the clinical development of precision-based, next-generation wound therapies.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100485"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145939598","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

Transferrin-modified multicomponent liposomes encapsulating paclitaxel-loaded β-elemene microemulsion enhance therapeutic efficacy in non-small-cell lung cancer 转铁蛋白修饰的多组分脂质体包封紫杉醇β-榄香烯微乳可提高非小细胞肺癌的治疗效果

IF 6.4 2区医学

International Journal of Pharmaceutics: X Pub Date : 2026-06-01 Epub Date: 2026-01-12 DOI: 10.1016/j.ijpx.2026.100488

Yunyan Chen , Ziwei Zhang , Rui Xiong , Yuqing Cao , Qian Liu

{"title":"Transferrin-modified multicomponent liposomes encapsulating paclitaxel-loaded β-elemene microemulsion enhance therapeutic efficacy in non-small-cell lung cancer","authors":"Yunyan Chen , Ziwei Zhang , Rui Xiong , Yuqing Cao , Qian Liu","doi":"10.1016/j.ijpx.2026.100488","DOIUrl":"10.1016/j.ijpx.2026.100488","url":null,"abstract":"<div><div>To achieve efficient accumulation and facilitate profound penetration of anti-tumor agents within neoplastic tissues stands as one of the most critical determinants influencing the efficacy of anticancer therapies. Herein, a multicomponent-based liposomes (Tf-PEM/L) by transferrin-modified encapsulating paclitaxel (PTX)-loaded <em>β</em>-elemene microemulsion (PEM) was fabricated, demonstrating significantly enhanced therapeutic efficacy against non-small cell lung cancer (NSCLC). Leveraging the synergistic mechanism of transferrin-mediated active targeting coupled with the enhanced permeability and retention (EPR) effect, Tf-PEM/L demonstrates a pronounced propensity for efficient and substantial accumulation at the tumor site. Following accumulation, the subsequently released PEM enables highly efficient deep penetration within tumor tissue, thereby achieving favorable anti-tumor therapeutic efficacy. Characterization of Tf-PEM/L revealed a mean particle size approximately (144.76 ± 9.34) nm, while the zeta potential exhibited a measurement of (−12.52 ± 0.28) mV. Notably, the transmission electron microscopy (TEM) images revealed the small-sized PEM were encapsulated within large-sized liposomes. In vitro cytotoxicity assays demonstrated that Tf-PEM/L elicited synergistic antitumor effects against A549 cells, underscoring its combinatorial therapeutic potential. In vivo studies, Tf-PEM/L demonstrated exceptional tumor-targeting capabilities as evidenced by quantitative biodistribution analyses. Moreover, Tf-PEM/L exhibited superior antitumor efficacy with tumor inhibition rate of (81.36 ± 3.87)% while markedly attenuating systemic toxicity, positioning it as a promising therapeutic strategy for NSCLC. Collectively, the Tf-PEM/L represents a promising targeted therapeutic strategy for NSCLC, with enhanced efficacy and safety profiles.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100488"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145978488","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

A prostate-specific membrane antigen targeted small molecule-drug conjugate for efficient prostate cancer therapy at a low dosage 一种前列腺特异性膜抗原靶向小分子药物偶联物，用于低剂量有效治疗前列腺癌

IF 6.4 2区医学

International Journal of Pharmaceutics: X Pub Date : 2026-06-01 Epub Date: 2026-01-26 DOI: 10.1016/j.ijpx.2026.100496

Jingjing Zhang , Fanchun Hu , Caiting Deng , Yuhan Ding , Yuchen Yang , Shupeng Han , Jun Liu , Feifei An , Mingsong Shi

{"title":"A prostate-specific membrane antigen targeted small molecule-drug conjugate for efficient prostate cancer therapy at a low dosage","authors":"Jingjing Zhang , Fanchun Hu , Caiting Deng , Yuhan Ding , Yuchen Yang , Shupeng Han , Jun Liu , Feifei An , Mingsong Shi","doi":"10.1016/j.ijpx.2026.100496","DOIUrl":"10.1016/j.ijpx.2026.100496","url":null,"abstract":"<div><div>Prostate-specific membrane antigen (PSMA), which is overexpressed in most prostate cancer cells, serves as an ideal target for precision therapy. The clinical utility of the potent chemotherapeutic agent SN38 is hindered by its poor water solubility and systemic toxicity. Herein, we present a novel, fully water-soluble small-molecule drug conjugate (SMDC), SN38-SS-3PEG<sub>24</sub>-3PSMA (SPP), designed for enhanced prostate cancer targeting and tumor-selective drug release. SPP integrates three PSMA-targeting ligands, a glutathione (GSH)-responsive disulfide linker, and three monodisperse polyethylene glycol (PEG) chains, achieving exceptional water solubility (>1 mM) and tumor-specific payload activation. In vivo fluorescence imaging revealed efficient tumor accumulation with minimal hepatic distribution, as evidenced by predominant renal clearance, thereby reducing hepatotoxicity risks. Remarkably, SPP demonstrated potent tumor growth inhibition at low doses (20 nmol) in PSMA-positive xenograft models, outperforming controls without PEG spacers or disulfide linkers. The GSH-triggered release of SN38 within the tumor cells ensured high cytotoxicity against cancer cells while maintaining stability in circulation, thereby minimizing off-target toxicity. Collectively, this study highlights SPP as a promising therapeutic candidate, combining enhanced water solubility, precise tumor targeting, and low-dose efficacy with an excellent safety profile, offering a transformative strategy for prostate cancer treatment.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100496"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146074027","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