{"title":"Methodological advances in liposomal encapsulation efficiency determination: systematic review and analysis.","authors":"Jin-Ping Wang, Zi-Rui Huang, Cheng Zhang, Yi-Ran Ni, Bo-Tao Li, Ying Wang, Jiang-Feng Wu","doi":"10.1080/1061186X.2025.2484773","DOIUrl":"10.1080/1061186X.2025.2484773","url":null,"abstract":"<p><p>Liposomes represent a highly promising drug delivery platform for a wide range of pharmaceutical compounds. Encapsulation efficiency (EE) stands as a critical quality attribute for liposomal formulations. Accurate determination of EE requires quantification of at least two parameters among the three distinct drug populations: total drug content, encapsulated drug fraction, and free drug concentration. However, due to the complex physicochemical characteristics of liposomes, particularly their structural flexibility, surface charge properties, and organic phase composition, direct measurement of encapsulated and free drug fractions presents significant analytical challenges. The ability to precisely quantify both free and total drug concentrations in liposomal formulations enables rapid and reliable evaluation of encapsulation efficiency, which is essential for guiding formulation optimisation and ensuring consistent product quality during scale-up manufacturing processes. This review provides a comprehensive analysis of various analytical techniques for EE determination, including (reverse) dialysis, ultrafiltration centrifugation, differential centrifugation (ultra/low-speed), and size exclusion chromatography, with particular emphasis on their methodological characteristics, applicable ranges, advantages, and limitations. Furthermore, we propose appropriate detection strategies for encapsulation efficiency assessment based on specific laboratory capabilities and the physicochemical properties of the investigational compounds.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-10"},"PeriodicalIF":4.3,"publicationDate":"2025-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143692352","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Punith M, Rajamma Aj, Sateesha Sb, Durgashree Diwakar, E K Girija, Chethan Kumar Kb, Ankith Na, Mousam Bhowmik, Manjunatha Pm
{"title":"Design and Formulation of Fast-Dissolving Microneedles for the Rapid Transdermal Delivery of Lorazepam.","authors":"Punith M, Rajamma Aj, Sateesha Sb, Durgashree Diwakar, E K Girija, Chethan Kumar Kb, Ankith Na, Mousam Bhowmik, Manjunatha Pm","doi":"10.1080/1061186X.2025.2483720","DOIUrl":"https://doi.org/10.1080/1061186X.2025.2483720","url":null,"abstract":"<p><p>This study investigates lorazepam-loaded dissolving microneedles (LMNs) as a fast-acting and minimally invasive treatment for status epilepticus. The LMNs were developed using a micro-molding technique with an optimized combination of PVP K30, Dextran 40, and Pullulan. Their stability was confirmed through FTIR and XRD analysis. The Parafilm® membrane insertion test demonstrated 100% penetration efficiency, verifying their ability to effectively pierce the skin. SEM imaging revealed well-defined microneedles with precise dimensions (800 µm height, 200 µm base, and 500 µm pitch). The LMNs rapidly dissolved in the subdermal layer of porcine skin. An <i>ex-vivo</i> drug diffusion study showed that 3-5% of the encapsulated lorazepam was released within 30 minutes, with a cumulative release of 79.3% over 24 hours. An acute dermal irritation study confirmed the biocompatibility and skin tolerance of the LMNs. Additionally, an <i>in-vivo</i> anti-convulsant efficacy study in albino Wistar rats subjected to maximal electroshock seizures demonstrated significant anticonvulsant effects (p < 0.05), confirming efficient systemic delivery of lorazepam. These findings highlight LMNs as a rapid-acting, non-invasive transdermal drug delivery system for managing status epilepticus, particularly in ambulatory care settings.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-20"},"PeriodicalIF":4.3,"publicationDate":"2025-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143710300","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Rohan Anchan, Anish Ghadi, Mohammed Ali Chauhan, Angel Godad, Sankalp Gharat
{"title":"Understanding the role of Ethosomes in Rheumatoid Arthritis: Innovative Solutions to Challenges in Transdermal Delivery of Synthetic Drugs and Phytoconstituents.","authors":"Rohan Anchan, Anish Ghadi, Mohammed Ali Chauhan, Angel Godad, Sankalp Gharat","doi":"10.1080/1061186X.2025.2477068","DOIUrl":"https://doi.org/10.1080/1061186X.2025.2477068","url":null,"abstract":"<p><p>Rheumatoid Arthritis (RA), an autoimmune disease, is a chronic inflammatory disorder affecting the joints leading to severe damage and cartilage destruction. Current therapies for RA such as DMARDs, NSAIDs, glucocorticoids, and phytoconstituents often face challenges related to solubility and transdermal permeability. Considering the barriers posed by the stratum corneum in transdermal drug delivery, ethosomes have shown promising results in overcoming these hurdles. The presence of ethanol in ethosomes imparts flexibility and disrupts the skin's lipid bilayer, allowing for transdermal penetration. Researchers have explored the potential of ethosomal drug delivery systems loaded with various synthetic drugs and phytoconstituents for the management of RA. Despite promising preclinical findings, these systems have yet to transition from the bench to the bedside, and there is a lack of comprehensive review papers highlighting the potential of ethosomes in RA treatment. Considering the commercial challenges in scaling up such nano systems, this review aims to analyse the current state of the art and advancements in ethosomal formulations loaded with synthetic agents and phytoconstituents. Further, it explores the impact of excipients and processing parameters, on the preparation of ethosomes and their efficacy in overcoming skin barriers, to enhance the permeability of therapeutic agents.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-27"},"PeriodicalIF":4.3,"publicationDate":"2025-03-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143669931","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Redefining hepatocellular carcinoma treatment: nanotechnology meets tumor immune microenvironment.","authors":"Chuanliang Mi, Sai Liu, Zhida Chen","doi":"10.1080/1061186X.2025.2479757","DOIUrl":"10.1080/1061186X.2025.2479757","url":null,"abstract":"<p><p>Hepatocellular carcinoma (HCC) is one of the most lethal malignancies worldwide, characterised by its complex pathogenesis and poor therapeutic outcomes. Despite recent advances in targeted molecular therapies, immune checkpoint inhibitors (ICIs), radiotherapy and conventional chemotherapy, the 5-year survival rate for this neoplasm remains dismally low. The progress in nanotechnology has revolutionised cancer treatment in recent years. These advances provide unprecedented opportunities to overcome the current limitations of different therapeutic modalities. This review provides a comprehensive analysis of how nanotechnology interfaces with the tumour immune microenvironment (TIME) in HCC and can present a new frontier in therapeutic interventions for HCC. We critically overview the latest developments in nanoparticle-based delivery systems for various drugs and also other antitumor agents like thermal therapy and radiotherapy. We also highlight the unique ability of nanoparticles to modulate the immunosuppressive tumour microenvironment (TME) and enhance therapeutic efficacy. Furthermore, we analyse emerging strategies that exploit nanoformulations to overcome biological barriers and enhance drug bioavailability in HCC treatment.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-20"},"PeriodicalIF":4.3,"publicationDate":"2025-03-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143624972","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Cell-based immunotherapy in oesophageal cancer.","authors":"Masoud Lahouty, Amirhossein Soleymanzadeh, Sama Kazemi, Haniyeh Saadati-Maleki, Sanaz Masoudi, Arash Ghasemi, Tohid Kazemi, Sahar Mehranfar, Manouchehr Fadaee","doi":"10.1080/1061186X.2025.2477077","DOIUrl":"10.1080/1061186X.2025.2477077","url":null,"abstract":"<p><p>Oesophageal cancer (EC) is among the most common illnesses globally, and its prognosis is unfavourable. Surgery, radiotherapy and chemotherapy are the primary therapy options for EC. Despite the occasional efficacy of these traditional treatment modalities, individuals with EC remain at a significant risk for local recurrence and metastasis. Consequently, innovative and efficacious medicines are required. In recent decades, clinical practice has effectively implemented cell therapy, which includes both stem cell and non-stem cell-based approaches, as an innovative tumour treatment, offering renewed hope to patients with oesophageal squamous cell carcinoma (ESCC). This paper examines the theoretical framework and contemporary advancements in cell treatment for individuals with EC. We further described current clinical studies and summarised essential data related to survival and safety assessments.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-11"},"PeriodicalIF":4.3,"publicationDate":"2025-03-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143585902","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Silvina Tiburzi, Virginia Lezcano, Gabriel Principe, María Gabriela Montiel Schneider, Alicia B Miravalles, Verónica Lassalle, Ariana Bruzzone, Verónica González-Pardo
{"title":"Quercetin-loaded magnetic nanoparticles: a promising tool for antitumor treatment in human breast cancer cells.","authors":"Silvina Tiburzi, Virginia Lezcano, Gabriel Principe, María Gabriela Montiel Schneider, Alicia B Miravalles, Verónica Lassalle, Ariana Bruzzone, Verónica González-Pardo","doi":"10.1080/1061186X.2025.2477764","DOIUrl":"10.1080/1061186X.2025.2477764","url":null,"abstract":"<p><p>Quercetin (QUE) is a phytoestrogen with known antitumor properties; however, its hydrophobic nature and low bioavailability limit its efficacy as an anticancer drug. To address this, we explored loading QUE onto a non-toxic nanocarrier. This study focused on the biological activity of magnetic iron oxide nanoparticles coated with polyethylene glycol (MAG@PEG) loaded with QUE (MAG@PEG@QUE) in MCF-7 cells. The MAG@PEG nanosystem was synthesised using a hydrothermal method, and QUE was incorporated by adding an alcoholic solution of QUE to an aqueous dispersion of MAG@PEG. QUE incorporation was confirmed qualitatively by FTIR spectroscopy and quantitatively through UV-visible spectroscopy. Cytotoxicity studies showed that MAG@PEG@QUE, at a concentration equivalent to the half-maximal inhibitory concentration (IC<sub>50</sub>) of free QUE, significantly reduced cell proliferation and viability while increasing apoptosis. MCF-7 cells treated with MAG@PEG@QUE also displayed actin cytoskeleton alterations typical of apoptotic cells. Transmission electron microscopy revealed clusters of magnetic nanoparticles within cellular vesicles. Targeted delivery of these nanoparticles was achieved using a static magnetic field, leading to high intracellular accumulation and selective cell death in targeted areas, without affecting adjacent cells. In conclusion, MAG@PEG@QUE shows comparable antitumor effects to free QUE and has the potential to enhance QUE's bioavailability and targeted delivery for breast cancer treatment.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-16"},"PeriodicalIF":4.3,"publicationDate":"2025-03-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143585906","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Jie Chen, Liangquan Liu, Yunxu Yang, Jing Luo, Shengchun Liu
{"title":"Patient-derived organoid models of malignant phyllodes tumours for drug sensitivity testing and identification of targeted therapeutic strategies.","authors":"Jie Chen, Liangquan Liu, Yunxu Yang, Jing Luo, Shengchun Liu","doi":"10.1080/1061186X.2025.2473010","DOIUrl":"10.1080/1061186X.2025.2473010","url":null,"abstract":"<p><strong>Background: </strong>Malignant phyllodes tumours (MPT) of the breast are rare fibroepithelial neoplasms. It exhibits rapid growth, large size, and a high local recurrence rate.</p><p><strong>Methods: </strong>In this study, we established novel patient-derived organoid (PDO) models from two primary MPT samples and conducted comprehensive genetic profiling and drug screening.</p><p><strong>Results: </strong>The PDO models faithfully recapped the histopathological and molecular features of the primary tumours, including stromal overgrowth, leaf-like projections, and the expression of key diagnostic markers. Drug testing revealed significant heterogeneity in response profiles to chemotherapeutic reagents between the two MPT-derived organoids, implying the importance of personalised drug testing. Next-generation sequencing analysis identified recurrent mutations in TP53, RB1, EGFR, ATM, and RECQL4, which correlated with the drug sensitivity profiles observed in the organoid models. Targeted therapeutic drugs, such as Abemaciclib (targeting the RB1 pathway) with an IC<sub>50</sub> value of 1.744 µM, and Alflutinib Mesylate (targeting the EGFR pathway) with an IC<sub>50</sub> value of 0.9150 µM, exhibited significant cytotoxic effects in the MPT2 organoid models.</p><p><strong>Conclusions: </strong>This study highlights the novel application of PDOs for studying the molecular landscape of MPTs and identifying effective therapeutic targets, offering a promising platform for guiding personalised treatment strategies for this rare and challenging cancer.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-11"},"PeriodicalIF":4.3,"publicationDate":"2025-03-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143585904","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"2,2,6,6-tetramethylpiperidin-1-oxyl: a new potential targeted ligand based on lipid peroxidation for targeted drug delivery.","authors":"Xiaofei Zhang, Guohao Yin, Minbo Lan, Hongli Zhao","doi":"10.1080/1061186X.2025.2474639","DOIUrl":"10.1080/1061186X.2025.2474639","url":null,"abstract":"<p><p>The side effects of chemotherapy drugs have prompted the development of targeted therapies. Distinctive abundance of lipid peroxidation (LPO) in tumour cells represents a potential target for drug delivery. However, LPO-based targeted ligands remain under-exploited. In this work, the targeting of 2,2,6,6-tetramethylpiperidin-1-oxyl (TEMPO), was investigated within a mesoporous silica nanoparticle (MSN) loaded with doxorubicin (DOX) and connected with 4-NH<sub>2</sub>-TEMPO obtaining DOX/MSN-TEMPO. A cellular uptake assay showed a faster uptake of DOX/MSN-TEMPO than blank group on Hela, L929 and 4T1 cells, revealing TEMPO's active targeting ability for tumour cells. After observing this phenomenon, the fabrication of a basic copolymer module carrying cyanine5.5 (Cy5.5) and TEMPO was reported. <i>In vivo</i> experiments were conducted on mouse MCF-7 tumour models, displaying selective aggregation of nano micelles at the tumour site and thereby verifying the broad applicability of TEMPO. Since the large amounts of LPO lead to the presence of numerous free radicals, whereas TEMPO, as a free radical capture agent, further selectively targets tumour cells. These findings verify the targeting ability of TEMPO for most tumour cells and collectively underscore the potential of TEMPO and analogous capture agents as innovative targeted ligands for drug delivery.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-12"},"PeriodicalIF":4.3,"publicationDate":"2025-03-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143530986","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Mona A Sawali, Muhammad Ammar Zahid, Shahenda Salah Abdelsalam, Raed M Al-Zoubi, Mohanad Shkoor, Abdelali Agouni
{"title":"The role of PTP1B in cardiometabolic disorders and endothelial dysfunction.","authors":"Mona A Sawali, Muhammad Ammar Zahid, Shahenda Salah Abdelsalam, Raed M Al-Zoubi, Mohanad Shkoor, Abdelali Agouni","doi":"10.1080/1061186X.2025.2473024","DOIUrl":"10.1080/1061186X.2025.2473024","url":null,"abstract":"<p><p>Cardiovascular diseases (CVD) are a global health concern that accounts for a large share of annual mortality. Endothelial dysfunction is the main underlying factor that eventually leads to cardiovascular events. Recent studies have underscored the critical function of Protein Tyrosine Phosphatase 1B (PTP1B) in the onset of endothelial dysfunction, chiefly through its involvement in metabolic diseases such as diabetes, obesity, and leptin resistance. PTP1B attenuates insulin and leptin signalling by dephosphorylating their respective receptors at key tyrosine residues, resulting in resistance-both of which are significant mechanisms underpinning the development of endothelial dysfunction. PTP1B also contributes to the disruption of the endoplasmic reticulum, causing endoplasmic reticulum stress, another molecular driver of endothelial dysfunction. Efforts to inhibit PTP1B activity hold the promise of advancing the prevention and management of CVD and metabolic disorders, as these conditions share common risk factors and underlying cellular mechanisms. Numerous small molecules have been reported as PTP1B inhibitors; however, their progression to advanced clinical trials has been hindered by major challenges such as low selectivity and undesirable side effects. This review provides an in-depth analysis of PTP1B's involvement in metabolic diseases and its interaction with CVD and examines the strategies and challenges related to inhibiting this enzyme.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-16"},"PeriodicalIF":4.3,"publicationDate":"2025-03-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143492236","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Resveratrol in ulcerative colitis: therapeutic mechanisms, animal model evidence and novel approaches.","authors":"Yukta Garg, Nandini Sharma, Shivang Saxena, Nihar Ranjan Sahoo, Sushil Kumar, Sankushdeep Singh, Amandeep Singh","doi":"10.1080/1061186X.2025.2469750","DOIUrl":"https://doi.org/10.1080/1061186X.2025.2469750","url":null,"abstract":"<p><p>Ulcerative colitis is a type of chronic inflammatory bowel disease characterised by abdominal pain, bloody diarrhoea, rectal bleeding and ulcerations in colon. This illness has significant health risks as it easily relapses, thus, providing a considerable threat to human health. A number of inflammatory mediators, oxidative stress and role of gut microbes have been studied thoroughly to understand the exact pathophysiology behind the disease occurrence. Several conventional therapies are available for the treatment of ulcerative colitis but each one of them have one or the other side effect. Therefore, to overcome this limitation, we are moving ahead towards herbal drug therapies. The current review presents the emerging role of Resveratrol, a natural occurring polyphenol derived from plant species. It is associated with potential antioxidative and anti-inflammatory properties. Protective effects of Resveratrol in different ulcerative colitis induced animal models are discussed in this review. Various strategies to improve bioavailability of drug include encapsulation of drug in several nanocarriers. Although many animal models have proved the effectiveness of Resveratrol in the treatment of ulcerative colitis, further research on human subjects is still required to understand the exact mechanism and safety to establish its uses clinically.</p>","PeriodicalId":15573,"journal":{"name":"Journal of Drug Targeting","volume":" ","pages":"1-24"},"PeriodicalIF":4.3,"publicationDate":"2025-03-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143585908","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}