Pharmaceuticals最新文献

{"title":"Efficacy and Safety of Tegoprazan in <i>Helicobacter pylori</i> Eradication: An Umbrella Review of Meta-Analyses.","authors":"Dmitrii N Andreev, Alsu R Khurmatullina, Igor V Maev, Dmitry S Bordin, Andrey V Zaborovskiy, Yury A Kucheryavyy, Filipp S Sokolov, Petr A Beliy","doi":"10.3390/ph19040637","DOIUrl":"10.3390/ph19040637","url":null,"abstract":"<p><p><b>Objective:</b> This umbrella review synthesizes and critically appraises the evidence on the efficacy and safety of tegoprazan-based versus proton pump inhibitor (PPI)-based regimens for <i>Helicobacter pylori</i> (<i>H. pylori</i>) eradication. <b>Methods:</b> This umbrella review was pre-registered in PROSPERO (CRD420251271120). Systematic reviews and meta-analyses published between 1 January 2018 and 10 December 2025 were identified through MEDLINE/PubMed, EMBASE, and the Cochrane Library. Reviews comparing tegoprazan-based and PPI-based eradication regimens in adult patients were included. Methodological quality was assessed using AMSTAR-2, risk of bias with ROBIS, and certainty of evidence with GRADE. Pooled relative risks (RRs) were calculated, with subgroup analyses by study design, treatment duration, and therapeutic regimen. <b>Results:</b> Eight systematic reviews and meta-analyses encompassing 17 primary studies and 12,714 participants were included. Tegoprazan-based regimens were associated with a statistically significant improvement in eradication efficacy compared with PPI-based therapies (RR = 1.019; 95% CI: 1.003-1.035; <i>p</i> = 0.021). In randomized controlled trials, the benefit was more pronounced (RR = 1.037; 95% CI: 1.015-1.061; <i>p</i> = 0.001), whereas no statistically significant benefit was observed in non-randomized studies (RR = 1.014; 95% CI: 0.991-1.037; <i>p</i> = 0.235). The efficacy advantage was mainly confined to quadruple therapy regimens (RR = 1.044; 95% CI: 1.002-1.088; <i>p</i> = 0.038). Tegoprazan-based regimens were associated with a lower incidence of overall adverse events compared with the PPI group (RR = 0.930; 95% CI: 0.885-0.976; <i>p</i> = 0.003). <b>Conclusions:</b> Tegoprazan-containing regimens were associated with a modest but statistically significant improvement in <i>H. pylori</i> eradication compared with PPI-containing regimens, particularly in randomized controlled trials and quadruple therapy regimens.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"19 4","pages":""},"PeriodicalIF":4.8,"publicationDate":"2026-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13118615/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147819865","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Minimally Invasive Therapeutic Drug Monitoring of Immunosuppressants in Children with Kidney Diseases: Validation of Fingerstick Sampling Using LC-MS/MS.","authors":"Marika Ishii, Jun Aoyagi, Natsuka Kimura, Masanori Kurosaki, Tomomi Maru, Kazuya Tanimoto, Mitsuaki Yoshino, Takane Ito, Takahiro Kanai, Hitoshi Osaka, Ryozo Nagai, Kenichi Aizawa","doi":"10.3390/ph19040630","DOIUrl":"10.3390/ph19040630","url":null,"abstract":"<p><p><b>Background/Objectives</b>: Therapeutic drug monitoring (TDM) of immunosuppressants is essential in treating pediatric kidney diseases; however, repeated venipuncture is burdensome in children. We evaluated whether minimally invasive fingerstick capillary sampling combined with liquid chromatography-tandem mass spectrometry (LC-MS/MS) provides results analytically comparable to those of conventional venous sampling. <b>Methods</b>: Capillary whole blood (2.8 µL) was collected via fingersticks from pediatric patients receiving mycophenolate mofetil, with or without tacrolimus (TAC) or cyclosporine A (CsA). Drug concentrations were quantified using a previously validated simultaneous LC-MS/MS method and compared with conventional venous sampling using linear regression and Bland-Altman analyses. <b>Results</b>: Seventy-four paired samples from 21 patients were analyzed. Strong correlations were observed between capillary and venous samples for mycophenolic acid (MPA), TAC, and CsA (R² > 0.90). Hematocrit correction improved agreement for MPA. Bland-Altman analyses demonstrated acceptable bias across analytes. <b>Conclusions</b>: Fingerstick-based microvolume sampling combined with LC-MS/MS provides analytically reliable immunosuppressant quantification in pediatric patients. Although larger clinical validation is required, this minimally invasive approach may reduce procedural burden and may support future outpatient or home-based TDM strategies.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"19 4","pages":""},"PeriodicalIF":4.8,"publicationDate":"2026-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13118987/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147819701","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Ferroptosis in Neuropsychiatric and Neurodegenerative Disorders: Shared Mechanisms and Disease-Specific Signatures.","authors":"Mingxin Liu, Chen Zeng, Zizhen Si","doi":"10.3390/ph19040629","DOIUrl":"10.3390/ph19040629","url":null,"abstract":"<p><p>Neuropsychiatric and neurodegenerative disorders impose a substantial global health burden, yet progress in mechanism-based therapy remains limited by clinical heterogeneity and an incomplete understanding of disease biology. Emerging evidence implicates ferroptosis-an iron-dependent form of lipid peroxidation-driven cell death-as a shared pathogenic process across primary psychiatric disorders and neurodegenerative diseases with prominent neuropsychiatric features. In this review, we synthesize evidence from major depressive disorder, schizophrenia, substance use disorders, Alzheimer's disease (AD), and Parkinson's disease (PD), highlighting ferroptosis as a common mechanism linking iron dyshomeostasis to neuronal dysfunction. Mechanistically, ferroptosis is organized around three interconnected modules: amino acid metabolism, lipid peroxidation, and iron handling. These pathways converge on mitochondrial dysfunction, oxidative damage, and neuroinflammatory amplification. We further propose that each disorder displays a distinct ferroptosis signature, including dopamine quinone-mediated GPX4 loss in PD, AICD-dependent transcriptional reprogramming in AD, and inflammatory-glutamatergic lowering of the ferroptotic threshold in depression and schizophrenia. Together, these insights position ferroptosis as a candidate framework for biomarker development, patient stratification, and mechanism-informed therapeutic intervention across neuropsychiatric disease.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"19 4","pages":""},"PeriodicalIF":4.8,"publicationDate":"2026-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13118317/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147819574","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Ketamine and Esketamine in Obsessive-Compulsive Disorder: A Scoping Review of Clinical and Mechanistic Evidence.","authors":"Maria Marmureanu, Mariana Valy Besoiu, Vlad Dionisie, Mihnea Costin Manea, Catalin Pleșea-Condratovici, Sorana Iulia Voican, Mirela Manea","doi":"10.3390/ph19040628","DOIUrl":"10.3390/ph19040628","url":null,"abstract":"<p><p><b>Background/Objective</b>: A substantial proportion of patients with obsessive-compulsive disorder (OCD) does not respond adequately to first-line treatments such as selective serotonin reuptake inhibitors and cognitive-behavioral therapy. OCD has traditionally been conceptualized as a serotonergic disorder. However, emerging evidence suggests that glutamatergic dysfunction plays an important role. Ketamine and esketamine are NMDA receptor antagonists with rapid antidepressant effects and have therefore attracted interest as potential treatments for OCD. This scoping review aims to map and synthesize the existing preclinical and clinical evidence regarding the therapeutic potential of ketamine and esketamine in OCD. <b>Methods</b>: A scoping review methodology based on the Arksey and O'Malley framework and Joanna Briggs Institute guidance was applied. Searches were conducted in PubMed, Scopus, and Web of Science. Studies that examined ketamine or esketamine in OCD populations or relevant experimental models were included. <b>Results</b>: Twenty-one studies met the inclusion criteria, of which five were preclinical studies and sixteen were clinical investigations. Preclinical evidence suggests that ketamine and esketamine improve compulsive-like behaviors. Clinical studies suggest that ketamine can produce rapid reductions in obsessive symptoms, though results remain inconsistent. Most trials evaluated single administrations, while limited evidence suggests that repeated dosing strategies may provide greater clinical benefit. <b>Conclusions</b>: Ketamine and esketamine show promise as rapid acting interventions for OCD, particularly in treatment refractory cases. However, current evidence remains preliminary and heterogeneous. Future research should prioritize adequately powered randomized trials and investigation of repeated administration protocols with longer follow-up periods to determine efficacy and optimal clinical implementation.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"19 4","pages":""},"PeriodicalIF":4.8,"publicationDate":"2026-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13119091/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147819638","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Repurposing Product Nkabinde for Hepatitis B Virus Therapy: A Network Pharmacology and Molecular Docking Investigation.","authors":"Samuel Chima Ugbaja, Siphathimandla Authority Nkabinde, Magugu Nkabinde, Nceba Gqaleni","doi":"10.3390/ph19040627","DOIUrl":"10.3390/ph19040627","url":null,"abstract":"&lt;p&gt;&lt;p&gt;&lt;b&gt;Background&lt;/b&gt;: Hepatitis B virus (HBV) infection continues to be a major public health concern, especially in sub-Saharan Africa, where widespread epidemics and restricted availability of long-term antiviral therapies result in higher mortality and morbidity rates. Drug repurposing represents a strategic approach to accelerate the discovery of effective therapies by leveraging agents with demonstrated antiviral and immunomodulatory activity. Product Nkabinde (PN) is a patented African polyherbal formulation initially developed for the treatment of HIV. Recent experimental studies demonstrate PN's potent anti-HIV activity and significant immunomodulatory effects in human immune cells, implicating host-directed mechanisms relevant to chronic viral infections. This study combines an integrative application of network pharmacology and molecular docking to evaluate the repurposing potential of PN as a multi-target agent in HBV. &lt;b&gt;Method&lt;/b&gt;: Bioactive components of PN were screened, and compound-associated targets were intersected with HBV-associated genes (proteins) to construct a protein-protein interaction (PPI) network. Topological analysis identified 10 hub targets (STAT1, STAT3, SRC, HCK, EGFR, SYK, PIK3CA, PIK3CB, PIK3R1, and PTPN11). Gene Ontology and KEGG pathway enrichment were performed with an FDR cut-off &lt; 0.05. Significantly enriched pathways included JAK-STAT signaling, chemokine signaling, EGFR-TKI resistance, PI3K complex signaling, and viral infection pathways, particularly those related to Kaposi sarcoma virus and HSV-1, indicating immunoregulatory and antiviral roles. Molecular docking was performed using AutoDock Vina 1.1.2 to evaluate binding affinity and interaction mode of key PN phytochemicals against the hub proteins, and results were compared to their respective co-crystallized ligands. &lt;b&gt;Results&lt;/b&gt;: Molecular docking indicated that major phytochemicals from PN exhibited significant binding affinities across all 10 hub host targets, typically outperforming or closely matching their respective co-crystallized ligands. The strongest contacts were observed for β-sitosterol-PIK3CB (-14.2 kcal/mol) and oleanolic acid-SYK (-14.0 kcal/mol), which were significantly stronger than the co-crystallized ligands (-7.9 and -8.3 kcal/mol, respectively), indicating robust stabilization within catalytic and regulatory pockets. Procyanidin B2 toward HCK (-10.5 vs. -7.9 kcal/mol) and PIK3CA (-9.5 vs. -7.3 kcal/mol), quercetin toward PIK3R1 (-10.6 vs. -8.2 kcal/mol) and PTPN11 (-9.2 vs. -7.5 kcal/mol), rutin toward SRC (-10.5 vs. 7.8 kcal/mol), and diosgenin toward EGFR (-9.4 vs. 8.4 kcal/mol). Procyanidin B2 maintained robust multi-hydrogen bonding networks, demonstrating significant binding, despite STAT1 and STAT3 docking showing identical affinities to co-crystals. Conserved hydrogen bonds, π-cation interactions, and significant hydrophobic packing at ATP-binding clefts and regulatory domains supported these interaction pattern","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"19 4","pages":""},"PeriodicalIF":4.8,"publicationDate":"2026-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13118322/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147819802","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Innovative Buccal Nanofibers for Dual Delivery of Tadalafil and Dapoxetine for Erectile Dysfunction and Premature Ejaculation Conditions.","authors":"Ali A Alamer, Khulud A Alsulami, Abdullah A Alshehri, Fahad A Almughem, Nojoud Al Fayez, Meshal K Alnefaie, Ahmed A Almulaifi, Alhassan H Aodah, Essam A Tawfik","doi":"10.3390/ph19040625","DOIUrl":"10.3390/ph19040625","url":null,"abstract":"<p><p><b>Background</b>: Erectile dysfunction (ED) and premature ejaculation (PE) are prevalent conditions affecting men's sexual health, for which tadalafil and dapoxetine have shown promise in their treatment, respectively. Conventional oral dosage forms face limitations, including variable absorption and delayed onset of action. In this study, we developed electrospun nanofibers using polyvinylpyrrolidone for buccal drug delivery as an alternative dosage form to oral tablets. This route offers advantages such as easy administration, suitability for those with difficulty swallowing, particularly the elderly, and a rapid onset of action via the blood capillaries, which might improve bioavailability. <b>Methods:</b> PVP nanofibers loaded with tadalafil and dapoxetine were fabricated using a modified electrospinning procedure with the Spraybase system, where an 8% (w/v) PVP ethanol solution containing 1.5% dapoxetine and 0.5% tadalafil was electrospun under controlled conditions (800 µL/h flow rate, 15 cm distance, 0.55 mm needle, and 8-10 kV) to produce uniform fibers. <b>Results</b>: The morphology of the nanofibers was characterized using SEM, revealing smooth, uniform fibers with an average diameter of 218 ± 50 nm for drug-loaded nanofibers. This nanofibrous system also demonstrated ultra-rapid disintegration occurring within 4 ± 1 s and consistent drug loading and encapsulation efficiency for both drugs. The release profile showed a burst drug release after 15 min, which accounted for >45% for tadalafil and >50% for dapoxetine, followed by a sustained increment in the drug release that reached > 60% for tadalafil and >78% for dapoxetine after 30 min until a complete drug release (100%) for both drugs after 180 min. In vitro cytotoxicity studies on human dermal fibroblasts confirmed the safety of both medications, with cell viability exceeding 50%, at concentrations of 1.56 to 25 µg/mL for tadalafil and 4.69 to 9.38 µg/mL for dapoxetine after 24 and 48 h of incubation. <b>Conclusions</b>: These findings highlight the potential of PVP-based nanofibers as a novel buccal delivery system for the combined treatment of ED and PE.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"19 4","pages":""},"PeriodicalIF":4.8,"publicationDate":"2026-04-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13119127/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147819653","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Peptide-Based Nanogels for Pharmaceutical and Biotechnological Applications: From Fmoc-FF to Other Peptide Sequences.","authors":"Mariangela Rosa, Sabrina Marino, Giancarlo Morelli, Antonella Accardo, Carlo Diaferia","doi":"10.3390/ph19040624","DOIUrl":"10.3390/ph19040624","url":null,"abstract":"<p><p>Peptide-based materials represent a rapidly growing field in nanotechnology, bridging bottom-up self-assembly and top-down approaches for the development of functional nanostructures. Among these systems, peptide-based nanogels (NGs), namely nanogels in which peptides assume a structural role, have emerged as a promising class of injectable formulations. Typically characterized by a core-shell architecture, these systems are closely related to peptide hydrogels in terms of structural organization. This review provides a state-of-the-art overview of peptides used as core structural elements for NG formulation, focusing on the peptide building blocks employed, the main formulation methodologies, and their current applications, with particular emphasis on pharmaceutical ones. Their potential as drug delivery systems and stimuli-responsive platforms for controlled and targeted release is also reported. For clarity, the reported formulations are classified according to the chemical nature of the core-structuration peptide, distinguishing systems based on Fmoc-FF from those derived from other primary sequences, including Boc-protected tripeptides, dehydropeptides, and chemically crosslinked peptide assemblies.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"19 4","pages":""},"PeriodicalIF":4.8,"publicationDate":"2026-04-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13118838/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147819519","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Recent Advances in Benzimidazole-Triazole Hybrids for Single- and Multi-Target Protein Kinase Inhibition.","authors":"Hamzeh M Abu Al Rub, Ahmed G Eissa","doi":"10.3390/ph19040623","DOIUrl":"10.3390/ph19040623","url":null,"abstract":"<p><strong>Background/objectives: </strong>Protein kinases play a crucial role in cancer initiation, progression, and therapeutic resistance by regulating signalling pathways involved in tumour growth and survival. Consequently, they represent major targets in anticancer drug discovery. Among heterocyclic scaffolds explored in kinase inhibitor design, benzimidazole has emerged as a privileged structure due to its strong hydrogen-bonding capability and structural resemblance to purine moieties. Triazole motifs are also widely incorporated into bioactive molecules because of their metabolic stability, favourable electronic properties, and ability to establish key interactions within kinase active sites. This review aims to summarise and critically discuss benzimidazole- and triazole-based kinase inhibitors, both as individual scaffolds and as hybrid systems, with emphasis on their kinase targets and multitarget potential.</p><p><strong>Methods: </strong>The relevant literature was surveyed from major scientific databases focusing on studies describing the synthesis, biological evaluation, and molecular modelling of benzimidazole- and triazole-containing kinase inhibitors.</p><p><strong>Results: </strong>Numerous studies demonstrate that both benzimidazole and triazole scaffolds exhibit significant kinase inhibitory activity against oncogenic targets, including EGFR, cyclin-dependent kinases (CDKs), and components of the PI3K/Akt/mTOR signalling pathway. Hybrid molecules combining these pharmacophores frequently enhance binding interactions and facilitate the development of multitarget kinase inhibitors. Structure-activity relationship trends indicate that pharmacophore accessibility, substitution patterns, and linker architecture influence inhibitory potency and selectivity.</p><p><strong>Conclusions: </strong>Overall, benzimidazole- and triazole-based scaffolds represent promising platforms for developing next-generation multitarget anticancer agents and provide valuable insights for the rational design of improved kinase inhibitors.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"19 4","pages":""},"PeriodicalIF":4.8,"publicationDate":"2026-04-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13118788/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147819731","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Topical Retinoids in Acne Vulgaris and Acne Scars-From Monotherapy to Combining Regimens.","authors":"Aleksandra Tobiasz, Alina Jankowska-Konsur, Danuta Nowicka","doi":"10.3390/ph19040620","DOIUrl":"10.3390/ph19040620","url":null,"abstract":"<p><p>Topical retinoids are the cornerstone of the treatment of multiple dermatological conditions. Long established in acne therapy, they exert effects on keratinization, inflammation, fibroblast activity, and collagen remodeling, suggesting a potential role in both the prevention and treatment of acne scars. This narrative review summarizes current evidence on the use of topical retinoids in acne vulgaris and acne scarring, focusing on different retinoid molecules, formulation technologies, and combination strategies. A review of published clinical and experimental studies evaluating tretinoin, adapalene, tazarotene, and trifarotene was performed, including their use as monotherapy and in combination with other topical agents or procedural interventions. The available data indicate that topical retinoids have a well-established position in acne treatment, can improve the appearance of atrophic acne scars, reduce the progression of scarring, and support skin remodeling. Advances in formulation technologies have improved tolerability, while combination approaches with agents such as benzoyl peroxide, antibiotics or procedural techniques have shown additive or synergistic effects, particularly in more severe cases. Nevertheless, much of the evidence regarding novel formulations is derived from small or heterogeneous study populations. In conclusion, topical retinoids represent a relevant therapeutic option in acne vulgaris and acne scarring, from monotherapy in mild cases to components of multimodal treatment protocols in more severe disease. Further large-scale, comparative studies are needed to better define the optimal clinical use of advanced drug delivery systems for topical retinoids.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"19 4","pages":""},"PeriodicalIF":4.8,"publicationDate":"2026-04-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13119282/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147819821","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development of Pseudoginsenoside RT2 as a Novel Gut-Selective Agent: Integrated Pharmacodynamic and Pharmacokinetic Evaluation of an Ocotillol Ginsenoside for Ulcerative Colitis.","authors":"Zhuoqiao Li, Junzhe Wu, Jia Wang, Yuwei Liu, Linxuan Liu, Yiyuan Wang, Yanbo Bu, Xiaoyu Geng, Jinping Liu","doi":"10.3390/ph19040622","DOIUrl":"10.3390/ph19040622","url":null,"abstract":"<p><p><b>Background/Objectives</b>: Ulcerative colitis is a chronic inflammatory bowel disease marked by a disrupted intestinal barrier and consequent aberrant immune responses. Pseudoginsenoside RT2, an ocotillol-type ginsenoside abundant in Panax herbs, represents a potential therapeutic candidate, yet its anti-ulcerative colitis efficacy and pharmacokinetic profile remain unclear. This study aimed to elucidate RT2's therapeutic potential for ulcerative colitis through a parallel evaluation of pharmacodynamic efficacy and pharmacokinetic properties. <b>Methods</b>: The anti-ulcerative colitis efficacy and in vivo disposition of RT2 were investigated in a trinitrobenzene sulfonic acid-induced rat colitis model. An ultra-performance liquid chromatography-tandem mass spectrometry method was employed to delineate its pharmacokinetic characteristics and quantify its distribution in various tissues following oral administration. <b>Results</b>: Pharmacodynamically, RT2 demonstrated significant efficacy in the UC rat model by repairing the intestinal barrier (by promoting goblet cell regeneration and upregulating tight junction proteins and mucin) and restoring immune homeostasis (by correcting T-helper 17/regulatory T-cell imbalance and reducing pro-inflammatory cytokines while elevating anti-inflammatory cytokines). Pharmacokinetically, RT2 exhibited rapid absorption, slow elimination, and high colonic accumulation, with concentrations in the inflamed colon being significantly higher than those in healthy rats. Furthermore, the biphasic concentration-time profile may account for its prolonged systemic residence time and enhanced local exposure. In summary, through parallel efficacy and pharmacokinetic studies, this work systematically reveals its characteristics as a therapeutic agent that exhibits high colonic accumulation and acts via barrier repair and immunomodulation. <b>Conclusions</b>: These findings provide a theoretical foundation for the development of RT2 as a novel gut-selective drug candidate for UC.</p>","PeriodicalId":20198,"journal":{"name":"Pharmaceuticals","volume":"19 4","pages":""},"PeriodicalIF":4.8,"publicationDate":"2026-04-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC13119218/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147819830","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}