Shihao Yang, Chengmao Wang, Wenke Yang, Pengwei Li
{"title":"Controllable Fabrication of Highly Elastic and Drug-Loading Alginate-Chitosan Composite Embolic Microspheres.","authors":"Shihao Yang, Chengmao Wang, Wenke Yang, Pengwei Li","doi":"10.2174/0115672018506722260820114246","DOIUrl":"https://doi.org/10.2174/0115672018506722260820114246","url":null,"abstract":"<p><strong>Background: </strong>Transcatheter arterial embolization (TAE) is a minimally invasive therapeutic strategy for treating hypervascular tumors, which relies on the intravascular delivery of embolic agents to obstruct blood supply. Embolic microspheres have emerged as promising agents due to their spherical shape and uniform size, which ensure predictable occlusion levels and targeted delivery. There is a pressing need for a controllable strategy to engineer multifunctional embolic microspheres.</p><p><strong>Methods: </strong>A novel droplet microfluidics-based method for the controllable fabrication of monodisperse alginate-chitosan composite (ACC) microspheres was developed. The mechanical and drugloading properties of the ACC microspheres were systematically characterized. The embolization performance of the optimized microspheres was visually evaluated in a microvascular chip model.</p><p><strong>Results: </strong>The microfluidic platform enabled the generation of highly monodisperse emulsion templates, leading to ACC microspheres with excellent size uniformity. Mechanical characterization revealed that the elasticity of the microspheres could be finely tuned, allowing for the production of highly elastic microspheres suitable for catheter injection. The ACC microspheres demonstrated favorable drug-loading capacity and sustained release characteristics. In the in vitro chip, the microspheres exhibited superior embolization performance.</p><p><strong>Discussion: </strong>The successful fabrication of monodisperse ACC microspheres underscores the precision of droplet microfluidics in creating complex biomaterial structures. The high elasticity is particularly critical for clinical embolization, as it prevents catheter clogging and ensures deep, uniform vessel occlusion. The demonstrated drug-loading capability positions these ACC microspheres as effective drug-eluting beads (DEBs) for combined embolization and local chemotherapy. The visual confirmation of effective embolization in the in vitro chip validates the functional performance of the microspheres.</p><p><strong>Conclusions: </strong>This study presents a robust microfluidic strategy for the controllable synthesis of monodisperse alginate-chitosan composite microspheres with tunable elasticity and favorable drugloading properties. The fabricated microspheres demonstrated excellent embolization performance in an in vitro model, validating their potential as advanced embolic agents. The findings offer valuable insights and a practical methodology for the rational design and preparation of next-generation multifunctional microspheres, which are highly desired for applications in embolization therapy.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-08-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148892851","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Gianna Dipalma, Angelo M Inchingolo, Francesca Elena Dell'Anna, Annarita Savino, Lucia Pia Zaminga, Francesco Inchingolo, Daniela Di Venere, Andrea Palermo, Grazia Marinelli, Giuseppe Minervini, Alessio D Inchingolo
{"title":"Therapeutic Use of Botulinum Toxin Type A in Temporomandibular Myofascial Disorders: A Systematic Review.","authors":"Gianna Dipalma, Angelo M Inchingolo, Francesca Elena Dell'Anna, Annarita Savino, Lucia Pia Zaminga, Francesco Inchingolo, Daniela Di Venere, Andrea Palermo, Grazia Marinelli, Giuseppe Minervini, Alessio D Inchingolo","doi":"10.2174/0115672018444786260820110530","DOIUrl":"https://doi.org/10.2174/0115672018444786260820110530","url":null,"abstract":"<p><strong>Background: </strong>This review explores the clinical role of botulinum toxin type A (BoNT-A) in treating Temporomandibular Disorders (TMDs) with a myofascial component, focusing on effectiveness, safety, injection protocols, and psychological and functional impact.</p><p><strong>Methods: </strong>Fourteen publications were retained for qualitative assessment after reviewing titles, summaries, and complete manuscripts. The risk of bias was appraised employing the ROBINS instrument.</p><p><strong>Results: </strong>BoNT-A treatment showed meaningful reductions in pain scores, especially in patients with high baseline pain or limited response to conservative care. Pain levels decreased significantly. Studies also reported improvements in jaw mobility, reduced muscle hyperactivity, and enhanced psychosomatic well-being. Some studies reported reductions in somatization and improvements in sleep quality. The depressive index remained unchanged, but functional disability improved significantly post-injection. Adverse effects, such as transient muscle soreness or facial changes, were rare and self-limiting. EMG data confirmed temporary neuromuscular relaxation lasting up to 22 weeks in some cases.</p><p><strong>Discussion: </strong>BoNT-A represents a valuable adjunctive or alternative therapy for myofascial TMDs, particularly in patients unresponsive to conventional treatments. It modulates pain perception and muscle overactivity via local and central mechanisms. However, variability in dosing, diagnostic criteria, and follow-up protocols underscores the need for standardized, well-designed clinical trials to optimize treatment strategies.</p><p><strong>Conclusion: </strong>BoNT-A is a valuable alternative for patients unresponsive to standard therapies. It helps reduce muscle overactivity and pain perception through local and central mechanisms. However, lack of standardized dosing, variable diagnostic frameworks, and inconsistent follow-up protocols highlight the need for further well-designed clinical trials to guide optimal use (ID: 1106625).</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-08-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148892871","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Synergistic Nanomedicine-Microcarrier for Transarterial Chemoembolization Against Hepatocellular Carcinoma.","authors":"Qin Shi, Wen Zhang, Licheng Yang, Minjie Yang, Jingqin Ma, Jiaze Yu, Yongbin Cao, Jianjun Luo, Shengxiang Rao, Lingxiao Liu, Zhiping Yan","doi":"10.2174/0115672018451596260518200520","DOIUrl":"https://doi.org/10.2174/0115672018451596260518200520","url":null,"abstract":"<p><strong>Introduction: </strong>Transarterial chemoembolization (TACE) has become a crucial treatment method for hepatocellular carcinoma (HCC) in recent years. However, its effect is limited by low sensitivity to chemotherapy and unsatisfactory loading performance of the embolic agent. This study aimed to explore a promising treatment strategy that combines nanomedicine with a microcarrier to enhance the efficacy of TACE.</p><p><strong>Methods: </strong>In this work, the porous microcarrier was used to carry doxorubicin-loaded zeolitic imidazolate framework-8 nanoparticles (M@ZIF-8-DOX) according to a conventional drug loading method. The physical and chemical properties were characterized. An in vitro cell assay was used to assess the cytotoxicity and cellular uptake ability of the embolic agent. To evaluate the antitumor performance and safety, the M@ZIF-8-DOX was delivered by the standard interventional procedure in the rabbit VX2 liver tumor model.</p><p><strong>Results: </strong>The M@ZIF-8-DOX effectively slowed the release of DOX in the bloodstream and extended the blood circulation time. In vitro studies revealed that ZIF-8-DOX showed high tumor cellular uptake and increased the intracellular DOX concentration. Furthermore, it was observed that M@ZIF-8-DOX could significantly inhibit tumor growth and proliferation while promoting tumor cell necrosis. Safety evaluation further confirmed that the M@ZIF-8-DOX had negligible toxicity to major organs and hepatorenal function.</p><p><strong>Discussion: </strong>The structures of the nanoparticles can be disrupted by the acidic and hypoxic tumor microenvironment to release drugs in a short time. They usually increase intracellular drug concentrations to improve chemotherapy sensitivity and reduce systemic toxicity. Moreover, the combination of embolic agents and nanomedicine has demonstrated an excellent synergistic effect, providing a new strategy for TACE.</p><p><strong>Conclusion: </strong>The M@ZIF-8-DOX is a simple and highly effective embolic agent for TACE, and the concept of nano platform synergistically enhanced embolization therapy may be profound effect in the development of nanodrugs for HCC.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-08-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148809725","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"pH-responsive Nanomedicine Delivery Platform Based on Silicon Nanoparticles for Imaging and Photodynamic Therapy of Tumor Cells.","authors":"Jiahui Lu, Yihao Zhang, Changan Hao, Zhaoqian Chen, Yiting Yang, Yakun Dou","doi":"10.2174/0115672018487892260727155707","DOIUrl":"https://doi.org/10.2174/0115672018487892260727155707","url":null,"abstract":"<p><strong>Introduction: </strong>Fluorescent silicon nanoparticles (Si NPs) are attractive bioimaging probes, but their emission is mainly confined to the blue-green region, resulting in poor penetration into tissues and strong autofluorescence interference. Moreover, most systems based on Si NPs are designed for single-function imaging or sensing, which limits their use in the delivery and treatment of tumortargeted drugs.</p><p><strong>Methods: </strong>Long wavelength fluorescent Si NPs with high physicochemical stability have been synthesised and incorporated into mesoporous silica nanoparticles (MSNs) for drug delivery. Chlorine e6 (Ce6) has been encapsulated as a photosensitizer. The resulting nanocomposites were coated with polydopamine (PDA) and functionalised with folic acid (FA) to realize active tumor-targeting capability.</p><p><strong>Results: </strong>The synthesized Si NPs showed stable long-wavelength fluorescence suitable for biological imaging. The FA-Si NPs-MSNs-PDA@Ce6 nanocomposite benefited from the FA-mediated targeting, increased permeability and retention effects and demonstrated increased tumor accumulation and cellular uptake. This strategy achieved tumor-specific fluorescence imaging, permitted real-time tracking of tumor cells, and boosted intracellular Ce6 delivery, thereby significantly elevating the photodynamic therapy (PDT) efficiency Discussion: This study presents a multifunctional nanoplatform that combines long-wave fluorescence imaging and pH-sensitive photodynamic therapy, thereby overcoming the significant limitations of traditional silicon nanoparticle-based systems. Targeted delivery and controlled release of drugs improve the accuracy of therapy and the effectiveness of imaging, and offer a promising strategy for tumor theranostics.</p><p><strong>Conclusion: </strong>A multifunctional drug delivery nanoplatform based on Si NPs integrating targeted fluorescence imaging and photodynamic therapy has been successfully developed. This system holds great promise for tumor-targeted drug delivery and integrated theranostic applications.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-08-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148809747","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Rama Tyagi, Jahanavi Bhar, Neeraj Kumar, Vikram Sharma, Swati Madan, Ahmed M Aljameeli, Fahaad S Alenazi, Mashael M Alaradi, Afaf F AlMaqati, Abdulkareem Ali Alanezi, Mohammed Helmy Faris Shalayel, Ghassab M Al-Mazaideh, Nadeem Ahmad Siddique
{"title":"Rutin and Scopoletin Co-Loaded Niosomes for Intranasal Brain Delivery: Formulation Optimization and <i>Ex Vivo</i> Evaluation.","authors":"Rama Tyagi, Jahanavi Bhar, Neeraj Kumar, Vikram Sharma, Swati Madan, Ahmed M Aljameeli, Fahaad S Alenazi, Mashael M Alaradi, Afaf F AlMaqati, Abdulkareem Ali Alanezi, Mohammed Helmy Faris Shalayel, Ghassab M Al-Mazaideh, Nadeem Ahmad Siddique","doi":"10.2174/0115672018473163260713051930","DOIUrl":"https://doi.org/10.2174/0115672018473163260713051930","url":null,"abstract":"<p><strong>Introduction/objective: </strong>Rutin (R) and scopoletin (S) are natural flavonols, which have been shown to reduce heart disease, improve blood circulation, reduce inflammation, and even prevent diabetes. Certain physicochemical properties, such as poor solubility and poor oral bioavailability of RS, diminish their therapeutic effectiveness. This study aims to develop the RS niosomes formulation (RS-Ns-Opt) to improve the bioavailability and solubility of RS.</p><p><strong>Methods: </strong>Lipid-derived vesicles enclosing RS were developed by the thin-film hydration method, whereas surfactants and cholesterol formed the RS niosome. RS-Ns-Opt were developed and evaluated using the thin-film hydration method, drug release, DPPH assay, confocal laser scanning microscopy (CLSM), ex vivo nasal mucosa permeation, UV analysis, and differential scanning calorimetry (DSC).</p><p><strong>Results: </strong>Nanosize vesicles (55.22 nm) of RS-Ns-Opt were formed within an acceptable polydispersity index (PDI) (0.234). In contrast, the entrapment efficiency of R (72.64%) and S (72.44%) indicates efficient uniformity and automatic surface interaction. Moreover, RS-Ns-Opt exhibited notable drug release (79.96 ± 0.68%) and effective antioxidant activity (70.11 ± 3.07%) compared with RS suspension drug release (23.49 ± 2.11%) and antioxidant potential (75.59 ± 0.75%).</p><p><strong>Discussion: </strong>The CLSM study found that RS-Ns-Opt loaded with rhodamine B showed superior penetration compared to the control.</p><p><strong>Conclusion: </strong>The planned RS-Ns-Opt niosomes can improve the bioavailability of RS and are expected to gain wide consideration in the near future for healthcare applications.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148611577","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Folic Acid-functionalized Liposomal Covalent Organic Framework for Enhanced Photothermal Cancer Therapy.","authors":"Xinying He, Shengli Wan, Qingze Fan, Die Gao, Xiaoqin Zhang, Xinyue Yang, Xiaoying Zhao, Jianming Wu, Yu Jiang","doi":"10.2174/0115672018469694260715113353","DOIUrl":"https://doi.org/10.2174/0115672018469694260715113353","url":null,"abstract":"<p><strong>Introduction: </strong>ICG suffers from poor photostability and rapid clearance in PTT. This study constructs an FA-modified, pH/NIR responsive COF nanodelivery system for targeted ICG delivery and precise controlled release.</p><p><strong>Methods: </strong>FA-Lip-IC was prepared by solvent evaporation. TEM and dynamic light scattering characterized morphology and size. Drug release was evaluated under different pH conditions with or without an 808 nm laser. Photothermal properties were assessed by an 808 nm laser. CLSM and flow cytometry analyzed FR-mediated cellular uptake. Biocompatibility was evaluated using an MTT assay, a hemolysis test, and a zebrafish model. Pharmacokinetics was monitored by blood fluorescence intensity in rats.</p><p><strong>Results: </strong>FA-Lip-IC showed uniform spherical morphology with a size of 577.4 ± 9.42 nm. The cumulative drug release reached 92.56 ± 0.81% at pH 5.5 with NIR irradiation. FA modification increased cellular uptake by ID8 and 4T1 cells. Under 808 nm laser irradiation, FA-Lip-IC induced a local temperature increase of > 20°C, with significantly higher cytotoxicity than free ICG. Hemolysis rate was < 3%, normal cell viability > 87%, zebrafish hatching rate > 90%, and blood circulation time was prolonged.</p><p><strong>Discussion: </strong>This platform integrates the high loading capacity of COFs with liposome biocompatibility. FA targeting and pH/NIR-responsive release enhance treatment precision. A limitation is the lack of in vivo efficacy data.</p><p><strong>Conclusion: </strong>FA-Lip-IC combines photothermal stability, active tumor targeting, and stimuliresponsive release, offering a promising strategy to overcome the limitations of conventional PTT and advance precision cancer therapy.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148611609","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Fahad Zubair, Muhammad Arfat Yameen, Sanaa Anjum, Yali Zhu
{"title":"Nystatin-Loaded Chitosan Nanoparticles Coated Fabric: A Promising Approach for the Management of Diabetic Foot Fungal Infections.","authors":"Fahad Zubair, Muhammad Arfat Yameen, Sanaa Anjum, Yali Zhu","doi":"10.2174/0115672018465558260701062442","DOIUrl":"https://doi.org/10.2174/0115672018465558260701062442","url":null,"abstract":"<p><strong>Introduction: </strong>One of the major complications in diabetic patients is foot disease. The microbial infections associated with this condition lead to skin infections, nail disease, and diabetic dermopathy. Nano-coating of textile fabric can be an approach to producing antimicrobial surfaces used as prophylactic agents to combat this foot disease.</p><p><strong>Method: </strong>Nystatin-loaded chitosan nanoparticles were impregnated onto cotton fabric. The nanoparticles were prepared using the ionic gelation method and coated onto the fabric.</p><p><strong>Results: </strong>Characterization showed a mean particle size of 154.6 nm and a zeta potential of +51.3 mV, indicating high stability. FTIR showed marked changes in peak positions, indicating interactions among chitosan, nystatin, and the fabric. SEM confirmed the presence of nanoparticles on the fabric, and XRD showed a change in the crystalline structure. The antifungal potential of the coated fabric was tested against C. albicans, with a ZOI of 23.5 mm before and 17.16 mm after washing cycles.</p><p><strong>Discussion: </strong>The coated fabric showed an initial burst release of nystatin followed by controlled diffusion, aligning with previous reports. Its antifungal activity remained stable after ten washing cycles, demonstrating superior durability compared to earlier fabric coatings. As this study was limited to in vitro evaluation, further in vivo validation is warranted.</p><p><strong>Conclusion: </strong>The coated fabric showed good antifungal activity with minimal loss of its inherent textile properties and preserved this effect after washing cycles. It can be used to make footwear for diabetic patients as a prophylactic measure.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-07-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148611538","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Intelligent Nanomedicine: AI-Driven Smart Carrier Design for Precision Skin Cancer Therapy.","authors":"Nilesh Meshram, Kuldeep Vinchurkar, Laxmikant Borse, Sudarshan Singh","doi":"10.2174/0115672018449461260428052800","DOIUrl":"https://doi.org/10.2174/0115672018449461260428052800","url":null,"abstract":"<p><p>Skin cancer, one of the most common malignancies globally, continues to present major therapeutic hurdles such as limited drug penetration, high systemic toxicity, and tumor recurrence. Nanomedicine has emerged as a powerful approach to overcome these challenges by enabling targeted, localized, and controlled drug delivery. Within this framework, the integration of Artificial Intelligence (AI) is transforming the way smart carriers are designed and optimized, moving drug development from trial-and-error to predictive, data-driven strategies. AI algorithms, including machine learning and deep learning, can predict drug-nanocarrier interactions, optimize particle size and surface chemistry for dermal penetration, and simulate release kinetics tailored to the tumor microenvironment. Intelligent nanocarriers developed with AI assistance also facilitate combination therapies such as chemo-, immuno-, and photodynamic therapy, offering synergistic benefits against resistant skin cancers. Furthermore, AI enables the personalization of treatment by analyzing patient-specific genomic and clinical data, guiding the creation of safer and more effective nanomedicine formulations. Despite these promising advancements, significant barriers remain in terms of data quality, model validation, and regulatory acceptance of AI-driven nanomedicine. Nonetheless, the convergence of AI and smart carrier technology represents a paradigm shift in precision oncology. This review uniquely emphasizes AI-guided nanocarrier design, optimization, and personalization specifically for skin cancer therapy, distinguishing it from broader AI-oncology reviews by focusing on smart drug-delivery systems rather than general diagnostic or predictive modeling applications.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148521650","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"SNEDDS as a Drug Delivery Carrier for BCS Class III and IV Drugs.","authors":"Jyoti Kumari, Dharmendra Kumar, Pramod Kumar Sharma","doi":"10.2174/0115672018480731260629120132","DOIUrl":"https://doi.org/10.2174/0115672018480731260629120132","url":null,"abstract":"<p><p>Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) are lipid-based systems for drug delivery characterized by poor aqueous solubility and/or limited intestinal permeability, which are overcome by the spontaneous formation of nanosized oil-in-water emulsions upon exposure to gastrointestinal fluids. The progress of SNEDDS over the past years has led to higher levels of solid SNEDDS, supersaturable formulations, and multifunctional platforms incorporating bioenhancers to address both solubility- and permeability-limited absorption, particularly for Biopharmaceutics Classification System (BCS) Class III and IV drugs. This review critically summarizes and synthesizes key developments reported between 2020 and 2025, with emphasis on formulation strategies, mechanistic insights, biorelevant evaluation approaches, and translational considerations. Recent evidence also suggests that optimised SNEDDS may lead to improved drug solubilisation, modification of intestinal membrane permeability, inhibition of efflux transporters, and reduced presystemic metabolism, translating into improved and more consistent oral bioavailability. Preclinical and emerging clinical studies have shown increased systemic exposure, decreased pharmacokinetic variability, and, in some cases, further improved therapeutic outcomes across diverse drug classes. The significance of solidification technologies, digestion-aware formulation design, and quality-by-design frameworks as factors to enhance scalability and achieve reproducibility has also emerged from the review. Nevertheless, despite such great progress, there are still challenges, such as physiological variability in gastrointestinal conditions, surfactant-related tolerability, stability during storage and digestion, regulatory considerations, and the requirement for robust in vitro and in vivo translational models to be established. Taken together, SNEDDS represent a flexible and evolving platform for oral delivery of challenging drug candidates, with continued innovation expected to support their broader clinical translation.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148521656","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Guiping Kong, Yucan Zheng, Yan Lu, Zhifeng Liu, Weixia Cheng
{"title":"Roxadustat-loaded pH-sensitive Anionic Liposomes Ameliorating Experimental Colitis in Mice: Formulation, Cellular Uptake and In vivo Evaluation.","authors":"Guiping Kong, Yucan Zheng, Yan Lu, Zhifeng Liu, Weixia Cheng","doi":"10.2174/0115672018472623260702202237","DOIUrl":"https://doi.org/10.2174/0115672018472623260702202237","url":null,"abstract":"<p><strong>Introduction: </strong>Roxadustat, an inhibitor of hypoxia-inducible factor prolyl hydroxylase, has therapeutic potential for colitis but is limited clinically by poor water solubility and rapid gastrointestinal absorption. This study aimed to develop a pH-responsive, intestinal-targeted nanocarrier to enhance its oral bioavailability and anti-colitis efficacy.</p><p><strong>Methods: </strong>Roxadustat-loaded liposomes (ROX-LP) were prepared via thin-film hydration with DSPG-PEG2000, cholesterol, and sodium cholate, then coated with Kollicoat MAE 100 P to form ROX-MAE@LP. The formulation was evaluated for physicochemical properties, in vitro release, cellular uptake, pharmacokinetics, and in vivo therapeutic efficacy.</p><p><strong>Results: </strong>ROX-MAE@LP showed excellent encapsulation and uniform spherical morphology, with pH-dependent release (markedly increased at pH 6.8 and 7.4). Enhanced cellular uptake was observed in Caco-2 cells under intestinal pH-mimicking conditions. In rats, the oral bioavailability of ROX-LP (150.32±9.22%) and ROX-MAE@LP (255.36±12.82%) was improved compared with roxadustat suspension, and ROX-MAE@LP had a prolonged mean residence time (14.66±1.97 h). In a murine dextran sulfate sodium-induced colitis model, ROX-MAE@LP alleviated inflammation, downregulated pro-inflammatory cytokines, and promoted mucosal repair, outperforming ROX-LP and free roxadustat.</p><p><strong>Discussion: </strong>The pH-responsive coating and intestinal-targeted property of ROX-MAE@LP effectively address the poor solubility and rapid absorption of roxadustat, enhancing local intestinal concentration and therapeutic effect in colitis, showing high potential for oral inflammatory bowel disease therapy.</p><p><strong>Conclusion: </strong>ROX-MAE@LP is an effective intestine-targeted delivery system that improves roxadustat's solubility, bioavailability and therapeutic outcomes in inflammatory bowel disease, while offering additional options for the development of novel roxadustat-based preparations and pHresponsive nanocarriers.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-07-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148521664","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}