International Journal of Pharmaceutics: X最新文献

{"title":"Ligand-modified liposomes as drug delivery systems for the active targeting of pancreatic cancer","authors":"Yerin Jang ,&nbsp;Jaehee Jang ,&nbsp;Jaewoo Son ,&nbsp;Hee-Young Lee ,&nbsp;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}

{"title":"Enhancing islet transplantation outcomes in T1DM: The promise of mesenchymal stem cells and exosomes","authors":"Ying Zhang ,&nbsp;Xiaoyue Chen ,&nbsp;Zhuoxun Huang ,&nbsp;Yifan Qiu ,&nbsp;Longfa Kou ,&nbsp;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}

{"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 ,&nbsp;Jiayi Liu ,&nbsp;Can Wang ,&nbsp;Xiaoqin Shan ,&nbsp;Siyi Li ,&nbsp;Xinyue Zhang ,&nbsp;Lijie Xia ,&nbsp;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}

{"title":"Data-efficient prediction in tableting using word embeddings and empirically-guided neural networks","authors":"Najeeb Abdelrahman,&nbsp;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}

{"title":"Can therapeutic potency of a cancer nanomedicine be predicted by pain-related behavioral test in subcutaneous tumor model?","authors":"Ye Tao ,&nbsp;Xiaohui Cai ,&nbsp;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}

{"title":"Improving the bioavailability of nintedanib by formulating inhalable ufasomes as a targeted therapy for non-small cell lung cancer","authors":"Salman M. Ghazwani ,&nbsp;Sami Alhazmi ,&nbsp;Salhah M. Ghazwani ,&nbsp;Hussam M. Shubaily ,&nbsp;Ahmed M. Wafi ,&nbsp;Naifa Alenazi ,&nbsp;Marwa Qadri ,&nbsp;Amal Naif Alshammari ,&nbsp;Wedad Mawkili ,&nbsp;Jobran M. Moshi ,&nbsp;Zenat Khired ,&nbsp;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 IC₅₀ 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}

{"title":"PEGylated gold nanoparticles regulate metabolic flux in erythrocytes by inducing hemoglobin deoxygenation","authors":"Zeng He ,&nbsp;Wanjing Li ,&nbsp;Qin Zhao ,&nbsp;Doudou Hao ,&nbsp;Rui Zhong ,&nbsp;Hong Wang ,&nbsp;Xiaojie Zhang ,&nbsp;Libo Du ,&nbsp;Xiaodong Wu ,&nbsp;Jiaxin Liu","doi":"10.1016/j.ijpx.2026.100495","DOIUrl":"10.1016/j.ijpx.2026.100495","url":null,"abstract":"<div><div>Nanomedicines based on polyethylene glycol-functionalized gold nanoparticles (Au@PEG NPs) are usually administered by intravenous injection to improve bioavailability. It is widely accepted that surface modification with PEG can prevent direct interactions between AuNPs and proteins. Therefore, the interaction of Au@PEG NPs with plasma proteins and blood cells has not received enough attention. Our previous study demonstrated that Au@PEG NPs affect the oxygen-carrying capacity and deformability of erythrocytes through oxidative stress; however, the molecular mechanism of oxidative damage induced by Au@PEG NPs remains unclear. Due to the absence of cell organelles such as the nucleus and mitochondria in mature erythrocytes, we hypothesise that Au@PEG NPs primarily generate oxidative stress by interfere with metabolic flux in erythrocytes. We have employed dynamic light scattering (DLS), isothermal titration calorimetry (ITC) and surface plasmon resonance imaging (SPRi) to investigate the interaction between proteins and 30 nm Au@PEG NPs. ITC and SPRi data revealed that hemoglobin exhibits a higher affinity for 30 nm Au@PEG NPs compared to albumin (Ka: 1.46 × 10⁻⁴ <em>vs</em> 1.08 × 10⁻⁴ M⁻¹). Circular dichroism (CD) spectrum demonstrated a significant conformational shift in hemoglobin following incubation with 30 nm Au@PEG NPs, characterized by an increase in α-helix [(65.9 ± 0.6) % to (68.2 ± 0.6) %] and a decrease in β-sheet [(4.8 ± 0.3) % to (1.7 ± 0.2) %], which is consistent with its transition toward a deoxygenated state. By combining ICP-MS and four specific endocytosis inhibitors, we investigated the endocytic mechanism of Au@PEG NPs entering erythrocytes. The data revealed that the uptake efficiency of 30 nm Au@PEG NPs by erythrocytes was 68.2 ± 0.6 ng/10⁹ RBCs, with approximately 75% of the Au@PEG NPs were uptaked by erythrocytes through a mechanism involving caveolin- and clathrin-mediated endocytosis. Metabolomics and NADP⁺/NADPH analysis revealed that Au@PEG NPs induce hemoglobin deoxygenation, which in turn inhibits the pentose phosphate pathway and disrupts redox homeostasis, as reflected by the decrease of intracellular NADPH from 3.53 ± 0.50 nmol/10¹² RBCs to 2.67 ± 0.46 nmol/10¹² RBCs. However, tail vein injection of Au@PEG NPs did not impair the liver oxygen supply since mice can compensate for the hemoglobin deoxygenation effect of Au@PEG NPs by decreasing systolic blood pressure and increasing tissue perfusion. Our findings showed that Au@PEG NPs interfere with metabolic flux and generate oxidative stress in erythrocytes by changing the oxygenation state of hemoglobin, and these results suggest that future studies should pay more attention to hemocompatibility evaluations of nanomedicines before their clinical application.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100495"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146074140","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}

{"title":"Encapsulating GSH/NQO1-responsive SN38 prodrug micelles with Timosaponin AIII-based multifunctional liposomes for tumor-targeted chemotherapy","authors":"Xu Luo ,&nbsp;Ziqiong Yang ,&nbsp;Jianqiu Chen ,&nbsp;Mengqi Shen ,&nbsp;Kun Wang ,&nbsp;Qian Du","doi":"10.1016/j.ijpx.2026.100497","DOIUrl":"10.1016/j.ijpx.2026.100497","url":null,"abstract":"<div><div>Colorectal cancer chemotherapy faces challenges with low intratumoral drug accumulation and off-target toxicity. Micellar liposome complex carriers are a promising anti-cancer platform due to their high encapsulation efficiency, responsive release, and multi-targeting capabilities. This study explores a novel tumor-targeted chemotherapy approach by encapsulating GSH/NQO1-responsive SN38 prodrug micelles into cholesterol-replacement multifunctional liposomes. Timosaponin AIII (TAIII), a steroid saponin with anticancer activity, substitutes cholesterol to stabilize liposomes, benefiting from its steroidal aglycone structure. Additionally, TAIII mimics PEGylation via its glucose moiety, enhancing tumor targeting via the overexpression of glucose transporter 1 (GLUT1) on cancer cells. Molecular docking studies with AutoDock revealed that GLUT1 residues stabilize TAIII in the binding pocket through hydrogen bonding, hydrophobic, and polar interactions, promoting its transmembrane transport. A specific amphiphilic SN38 prodrug, PEG-SS-SN38-QPA (PSSQ), was synthesized and self-assembled into micelles via a solvent injection-dialysis method for GSH/NQO1-responsive controlled drug release in the tumor microenvironment. PSSQ micelles were integrated into the hydrophilic cavity of TAIII-based liposomes (TLP, prepared by the thin-film hydration method) through passive encapsulation to form PSSQ@TLP. In vitro release study exhibiting GSH/NQO1-triggered release under simulated tumor microenvironment. In vitro cytotoxicity evaluation was performed using the MTT assay on HCT116, LOVO, CT26.WT cell lines. Following in vivo evaluations of biodistribution, anti-tumor efficacy, and biosafety in CT26.WT xenograft tumor-bearing mice, PSSQ@TLP demonstrated enhanced intratumoral accumulation, robust tumor suppression, and minimized systemic toxicity, underscoring its promise as a targeted therapeutic strategy for colorectal cancer.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100497"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146074141","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}

{"title":"Ensuring vaccine cold chain integrity: A rapid and low-cost test for identifying heat-exposed sucrose-containing vaccines","authors":"Benediktus Yohan Arman ,&nbsp;Andrea Magri ,&nbsp;Matteo N. Barbaglia ,&nbsp;Lawrence Petherbridge ,&nbsp;Jennifer Brook ,&nbsp;Tehmina Bharucha ,&nbsp;Isabelle Legge ,&nbsp;John Walsby-Tickle ,&nbsp;Michael Deats ,&nbsp;Sneha Banerjee ,&nbsp;Sara Mosca ,&nbsp;Rajender Jena ,&nbsp;Dnyanesh S. Ranade ,&nbsp;Shrikrishna R. Chunekar ,&nbsp;Kundan D. Patil ,&nbsp;Sunil Gairola ,&nbsp;Hamid A. Merchant ,&nbsp;Robert Stokes ,&nbsp;Rutendo Kuwana ,&nbsp;Alexandrine Maes ,&nbsp;Bevin Gangadharan","doi":"10.1016/j.ijpx.2025.100467","DOIUrl":"10.1016/j.ijpx.2025.100467","url":null,"abstract":"<div><div>Maintaining cold-chain integrity is vital for vaccines to ensure that they remain within the recommended temperature limits during routine storage and transportation. This ensures vaccine stability, efficacy, and avoids degradation. Here, we propose rapid and low-cost tests based on simple glucose assays to detect heat-exposed degraded sucrose-containing vaccines through sucrose's inherent gradual conversion to glucose when exposed to elevated temperatures. Bioluminescent and colorimetric assays and a clinical biochemical analyser for urine samples could successfully determine effects of heat exposure on vaccines by detecting a significant increase in glucose levels. We show that this increase in glucose also correlates with the loss of vaccine potency. When vaccines were incubated at 37 and 45 °C, the bioluminescent assay was able to detect an increase in glucose levels from 12 h of heat exposure. The biochemical analyser could successfully detect increased glucose levels in a COVID-19 vaccine which had been exposed to 37 and 45 °C. Most importantly, the colorimetric assay has the advantage of producing a colour change visually upon simply mixing the vaccine with a reagent without the need for a plate reader or any other sophisticated devices. To our knowledge, this is the first simple, rapid and device-free test of its kind to detect heat-exposed substandard vaccines, making it a potential test for deploying at key points in the supply chain in warm and hot countries to check the integrity of vaccine cold-chain. Although this test does not replace the more definitive lot release assays such as potency assays, it could initially be used as a rapid and low-cost test to identify substandard sucrose-containing vaccines within supply chains, in support of WHO's Prevent, Detect, and Respond strategy.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100467"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145765679","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}

{"title":"Development and evaluation of clotrimazole microemulsions for topical application: Effects of HLB value of surfactant mixture and cosurfactant type on formulation design","authors":"Chih-Wun Fang ,&nbsp;Yu-Wen Lin ,&nbsp;I-Hui Chiu ,&nbsp;Pao-Chu Wu","doi":"10.1016/j.ijpx.2025.100469","DOIUrl":"10.1016/j.ijpx.2025.100469","url":null,"abstract":"<div><div>Clotrimazole is a synthetic imidazole with broad-spectrum antimycotic effect that has been widely used for the topical treatment for athlete's foot (tinea pedis), oropharyngeal and vulvovaginal candidiasis. The objective of the study was to develop a nano-delivery system containing to improve the penetration capacity of Clotrimazole. Microemulsions were formulated and the chemophysical properties, permeability through rat skin and irritancy examined by HET-CAM test of drug-loaded formulations and stability were evaluated. The average droplet size and viscosity of all clotrimazole-loaded microemulsion formulations were respectively between 126.7–228.13 nm with PDI value less than 0.31 and 24.53–155.16 mPa·s. The penetration capacity of clotrimazole was markedly improved by using microemulsion formulations as delivery carriers: the 24-h cumulative permeated amount from the optimized microemulsion was approximately three-fold higher than that from the clotrimazole solution (drug dissolved in 30 % ethanol) and about 6.5-fold higher than that from the commercial product. The HET-CAM test showed the irritancy on skin of designed clotrimazole-loaded formulation was acceptable compared to the positive control of 0.8 % paraformaldehyde aqueous solution. The stability studies showed that the physicochemical characteristics and residual drug percentage (about 95.3 %) of F2 clotrimazole-loaded formulation were fairly stable after thermodynamic and storage tests, indicating designed microemulsions as a delivery carrier could be considered as a potential strategy for clotrimazole topical dosage form deployment.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"11 ","pages":"Article 100469"},"PeriodicalIF":6.4,"publicationDate":"2026-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145799440","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}