Inflammopharmacology最新文献

{"title":"Jasminum humile extract mitigates carrageenan-induced paw oedema in rats by modulating inflammatory and antioxidant signalling pathways.","authors":"Mehreen Fatima, Lamya Ahmed Al-Keridis, Mohd Adnan, Nawaf Alshammari, Abdel Moneim Elhadi Sulieman, Muhammad Rashid Khan","doi":"10.1007/s10787-025-01692-3","DOIUrl":"https://doi.org/10.1007/s10787-025-01692-3","url":null,"abstract":"<p><strong>Background: </strong>Jasminum humile is widely used in traditional medicines to treat hard lumps, mouth inflammation, ringworms, and other infections. Leaf decoction of the plant is known to be effective in treating various skin conditions. In addition, root juice is traditionally utilized as a remedy for ringworm infections. Studies have reported that J. humile contains various antioxidant metabolites with analgesic and anti-inflammatory properties. In this study, J. humile chloroform extract (JHC) was investigated for anti-inflammatory effects against carrageenan-induced paw oedema in rat models.</p><p><strong>Methods: </strong>High-performance liquid chromatography was used to examine phenolic compounds present in JHC. The in-vivo anti-inflammatory activities were investigated using carrageenan-induced paw oedema rat models, while indomethacin was referred to as positive control. Therapeutic properties of JHC were examined by assessing paw volumes, motility score, and inflammatory proteins in serum. The anti-inflammatory nature of JHC was further investigated by biochemical and hematological profiles along with genetic expression of inflammatory and antioxidant genes through qRT-PCR analysis.</p><p><strong>Results: </strong>Indomethacin at 10 mg/kg and JHC at 100, 200, and 300 mg/kg doses decreased the concentration of C-reactive protein (CRP) while upregulating the concentration of albumin and myeloperoxidase (MPO). Moreover, JHC administration reduced the expression levels of inflammatory markers, cyclooxygenase-2 (COX2), and inducible nitric oxide synthase (iNOS) compared to the Carr-treated control. However, a significant rise was induced in nuclear factor erythroid 2-related factor 2 (Nrf-2) and heme oxygenase 1 (HO-1) levels after JHC treatment as compared to Carr-treated rats.</p><p><strong>Conclusion: </strong>These results showed significant anti-inflammatory potential of J. humile by increasing the activity levels of enzymatic antioxidants and lowering inflammatory markers. These results confirm the beneficial use of natural plants in the development of new anti-inflammatory drugs.</p>","PeriodicalId":13551,"journal":{"name":"Inflammopharmacology","volume":" ","pages":""},"PeriodicalIF":4.6,"publicationDate":"2025-03-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143556779","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":"Kirenol ameliorates endotoxin-induced acute lung injury by inhibiting the ERK and JNK phosphorylation-mediated NFκB pathway in mice.","authors":"Frank Cheau-Feng Lin, Shih-Pin Chen, Sheng-Chien Lin, Ching-Chi Tseng, Stella Chin-Shaw Tsai, Yu-Hsiang Kuan","doi":"10.1007/s10787-025-01693-2","DOIUrl":"https://doi.org/10.1007/s10787-025-01693-2","url":null,"abstract":"<p><p>Acute lung injury (ALI) is a pathological condition characterised by varying degrees of lung damage in patients. Kirenol exerts anti-inflammatory, immunosuppressive, and antioxidative effects. We investigated the protective effects of kirenol on lipopolysaccharide-induced ALI in mice. Pretreatment with kirenol significantly ameliorated lung oedema and neutrophil infiltration in ALI mice. Kirenol downregulated the chemokines (MIP-2) expression and the adhesion molecules (ICAM-1 and VCAM-1) secretion. Furthermore, kirenol inhibited the production of the proinflammatory mediators nitric oxide and prostaglandin (PG)E2 through the upstream factors iNOS and cyclooxygenase (COX)-2, respectively. Kirenol suppressed the IKK-IκB-NFκB pathway, which is involved in lipopolysaccharide-induced inflammation. Kirenol inhibited the lipopolysaccharide-induced phosphorylation of ERK and JNK, to a lesser extent, p38 MAPK and Akt. In conclusion, our findings suggest that kirenol exerts ameliorative effects against ALI by suppressing the production of chemokines, adhesion molecules, and proinflammatory mediators and inhibiting the IKK-IκB-NFκB pathway and its upstream factors, phosphorylated ERK and JNK.</p>","PeriodicalId":13551,"journal":{"name":"Inflammopharmacology","volume":" ","pages":""},"PeriodicalIF":4.6,"publicationDate":"2025-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143541813","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":"Use quercetin for pulmonary fibrosis: a preclinical systematic review and meta-analysis.","authors":"Xuanyu Wu, Xiang Xiao, Yuchen Su, Yuwei Zhang, Ganggang Li, Fei Wang, Quanyu Du, Han Yang","doi":"10.1007/s10787-025-01678-1","DOIUrl":"https://doi.org/10.1007/s10787-025-01678-1","url":null,"abstract":"<p><strong>Background: </strong>Pulmonary fibrosis (PF) is an age-related interstitial lung disease, which lacks effective drug treatment at present. Quercetin has been shown to have favorable anti-inflammatory and anti-fibrotic properties, and preliminary evidence suggests its potential efficacy and tolerability in PF patients. However, a comprehensive systematic review and evaluation of the protective effects and potential mechanisms of quercetin in PF models remains to be completed. Therefore, we conducted this study.</p><p><strong>Methods: </strong>The PubMed, Cochrane Library, Embase, and Web of Science databases were searched up to the April 1, 2024. CAMARADES was the methodological quality assessment tool. And statistical analyses were conducted with R and Stata 16.0. Origin was used for a three-dimensional (3D) dosage-intervention duration-efficacy model for quercetin treatment of PF.</p><p><strong>Results: </strong>A total of 20 studies, encompassing 44 independent experiments and involving 1019 animals, were included in the analysis. Meta-analysis revealed that quercetin significantly mitigated lung pathological tissue scores and the expression of lung fibrosis markers in PF animal models. Furthermore, quercetin significantly ameliorated inflammatory responses, oxidative stress, epithelial-mesenchymal transition and myofibroblast activation, cell senescence and apoptosis, and the markers expression of extracellular matrix (ECM) deposition. Quercetin did not show significant hepatic and nephrotoxicity. The 3D dosage-intervention duration-efficacy model indicated that a dosing period over 20 days and dosages range of 5-100 mg/kg were appropriate modalities.</p><p><strong>Conclusion: </strong>Herein, our study highlights the potential of quercetin in the treatment of PF and the available mechanisms.</p>","PeriodicalId":13551,"journal":{"name":"Inflammopharmacology","volume":" ","pages":""},"PeriodicalIF":4.6,"publicationDate":"2025-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143556784","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":"Nanostructured lipid carriers in Rheumatoid Arthritis: treatment, advancements and applications.","authors":"Swarnika Sharma, Rashmi Ghosh, Arockia Babu Marianesan, Sumaya Hussain, Jai Deo Pandey, Manish Kumar","doi":"10.1007/s10787-025-01669-2","DOIUrl":"https://doi.org/10.1007/s10787-025-01669-2","url":null,"abstract":"<p><p>Rheumatoid arthritis (RA) is a chronic autoimmune disease that affects the joints and causes pain, swelling, and deformity. Current treatments, including nonsteroidal anti-inflammatory drugs (NSAIDs), corticosteroids, and disease-modifying antirheumatic drugs, often have limited efficacy and adverse side effects. Nanostructured lipid carriers (NLCs) are promising drug delivery agents for treating RA. NLCs are comprised of solid and liquid lipids, forming a nanostructured matrix that enhances drug solubility, stability, and controlled release. They offer advantages over traditional carriers such as improved skin penetration, increased bioavailability, and reduced systemic side effects. Topical NLC formulations show improved stability and skin absorption, targeting drugs specifically to the affected joints, thus reducing the required dose and systemic exposure. Studies on NLCs for delivering anti-inflammatory and antirheumatic drugs, such as methotrexate, indomethacin, and curcumin, in RA animal models indicate the potential for improved therapeutic efficacy and safety. NLCs represent a promising approach for targeted RA drug delivery, offering better efficacy, fewer side effects, and higher patient compliance. However, further research is needed to optimize NLC formulations and evaluate their clinical efficacy and safety in RA patients. The development of NLC-based drug delivery systems for RA treatment may lead to more effective and well-tolerated therapies, thereby improving the quality of life of patients with this debilitating disease.</p>","PeriodicalId":13551,"journal":{"name":"Inflammopharmacology","volume":" ","pages":""},"PeriodicalIF":4.6,"publicationDate":"2025-03-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143537044","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":"Comprehensive multifaceted approach in antibody therapeutics: targeting gut dysbiosis and gastrointestinal oncogenic cells.","authors":"Uddipta Guha","doi":"10.1007/s10787-025-01689-y","DOIUrl":"https://doi.org/10.1007/s10787-025-01689-y","url":null,"abstract":"<p><p>Treatment of biomedicine has advanced significantly in recent years, and it now has a very high success rate with severity of side effects making it so much more compelling to study emerging treatments. A broad concept is proposed, which pools in nominal antibiotics administration nutrition nutritional supplement if requisite and antibodies by maximizing the potential synergy of these elements, that is where conventional methods stop, this paradigm shift starts. The antibiotics act on the pathogen alone and when combined with therapeutic techniques results in increased recovery along with proper body defenses. The first-ever study of its kind combines antibody complex disguising as a carrier for the drugs which improves the palatability, extend retention in body and makes easy to store as well as distribute. This ground-breaking method could really alter the way digestive diseases is treated and provide an alternative to conventional methods.</p>","PeriodicalId":13551,"journal":{"name":"Inflammopharmacology","volume":" ","pages":""},"PeriodicalIF":4.6,"publicationDate":"2025-03-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143537086","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":"Extracellular vesicles as therapeutic agents in rheumatoid arthritis: a systematic review of current evidence.","authors":"Xiaolei Miao, Amirreza Ghafourian, Mahdi Karimi Khaneghah, Seyed Mohammad Ayyoubzadeh, Reza Afrisham, Mahnaz Ahmadi","doi":"10.1007/s10787-025-01670-9","DOIUrl":"https://doi.org/10.1007/s10787-025-01670-9","url":null,"abstract":"<p><p>Rheumatoid arthritis (RA) is defined as a chronic autoimmune disease that severely influences a patient's quality of life. Extracellular vesicles (EVs) have gained much attention in recent years as one of the most potent therapeutic agents for the treatment of RA. A systematic review was performed with the purpose of assessing the current evidence relating to the therapeutic applications of EVs in RA. The systematic search was performed in the databases of PubMed, Scopus, and Web of Science, from inception times to September 2024. All studies investigating the use of EVs for the treatment of RA were included. The quality appraisal of selected articles and data extraction regarding EV characteristics, therapeutic applications, and associated outcomes were performed. Of the 1418 initially identified articles, 59 studies met inclusion criteria. Regarding their cellular origins, most EVs were derived from mesenchymal stem cells, followed by immune cells. The main therapeutic mechanisms included modulation of the immune response, reduction of inflammation, and repair of tissues. Recent trends are toward increasing interest in engineered EVs and combination therapies. Indeed, most studies reported positive outcomes with regard to lowered inflammation and improved joint function. On the other hand, standardization of the metrics of evaluation considerably varied between different studies. EVs are promising therapeutic agents in the treatment of RA by modulating immune responses. Standardization, delivery systems, and clinical translation are challenges yet to be overcome. Future studies will be directed to optimize EV engineering, targeted delivery systems, and large-scale clinical trials.</p>","PeriodicalId":13551,"journal":{"name":"Inflammopharmacology","volume":" ","pages":""},"PeriodicalIF":4.6,"publicationDate":"2025-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143537088","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":"Gefitinib as an antimalarial: unveiling its therapeutic potential.","authors":"Varun Gorki, Neha Sylvia Walter, Monika Chauhan, Neelima Dhingra, Upma Bagai, Sukhbir Kaur","doi":"10.1007/s10787-025-01682-5","DOIUrl":"https://doi.org/10.1007/s10787-025-01682-5","url":null,"abstract":"<p><p>Resistant strains of Plasmodium spp. pose a great threat to healthcare. Drug repurposing is a smart, and an effective way to look for new alternatives for different ailments including malaria. Protein tyrosine kinases (PTKs) play a crucial role in growth, maturation as well as differentiation of Plasmodium and this study explores antimalarial activity of PTKs inhibitor gefitinib using in silico and experimental approaches. The drug showed considerable inhibitory activity against P. falciparum 3D7 (IC₅₀ 0.49 µg/mL) and RKL-9 (IC₅₀ 0.83 µg/mL) strains. Isobologram analysis revealed substantial synergism between gefitinib and artesunate. Gefitinib illustrated highest negative D-score towards phosphoethanolamine methyltransferase followed by PfPK5 and CDPK1. Its acute toxicity was 4 g/kg. Gefitinib (100 mg/kg) exhibited a dose-dependent curative activity against P. berghei with 91.09% chemo-suppression and the combination of gefitinib 100 mg/kg and AS 50 mg/kg exhibited complete parasite clearance with no recrudescence which was also evidenced by cytokine analysis, biochemical as well as histopathological studies. At length, gefitinib illustrated considerable antiplasmodial action by targeting phosphoethanolamine methyltransferase, PfPK5 and CDPK1. The combination of gefitinib (100 mg/kg) and AS (50 mg/kg) holds promise for malaria treatment. Further, research is being done to evaluate its pharmacokinetic properties.</p>","PeriodicalId":13551,"journal":{"name":"Inflammopharmacology","volume":" ","pages":""},"PeriodicalIF":4.6,"publicationDate":"2025-02-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143523332","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":"Unravelling the prophylactic anti-inflammatory potential of Koenigia tortuosa through modulation of cytokine levels and inflammatory markers in LPS-induced localized inflammation in Wistar rat models.","authors":"Ambreena Farooq, Mudasar Nabi, Khalid Bashir Dar, Syed Ishfa Andrabi, Nuzhat Khursheed, Farhat Jabeen, Showkat Ahmad Dar, Aijaz Hassan Ganie, Abdul Wajid Bhat, Showkat Ahmad Ganie","doi":"10.1007/s10787-025-01680-7","DOIUrl":"https://doi.org/10.1007/s10787-025-01680-7","url":null,"abstract":"&lt;p&gt;&lt;p&gt;Chronic inflammation, a pivotal factor in various chronic diseases, necessitates safe and effective treatments to alleviate disease severity and symptoms. Current interventional approaches, including synthetic steroids and non-steroidal anti-inflammatory drugs, pose safety concerns. Consequently, people seek plant-based alternatives as safer substitutes. Koenigia tortuosa, a medicinal plant with rich folklore claims, traditionally treats joint pain, swelling, dysentery and kidney related problems but lacks documentation. This study investigated anti-inflammatory properties of Koenigia tortuosa. Soxhlet extraction method was employed to obtain five different extracts of Koenigia tortuosa viz., hexane (95%), ethyl-acetate (99%), ethanol (99%), methanol (95%) and aqueous. Anti-inflammatory potential of different extracts was determined by both in vitro (including protein denaturation, nitric-oxide scavenging, proteinase inhibition, and erythrocyte membrane stabilization) and in vivo by performing histopathological studies and determining levels of various inflammatory markers like IL-1β, IL-6, IFN-γ and TNF-α using ELISA and, iNOS, PPAR-γ and COX-2 by Western blotting. GC-MS analysis was performed to reveal the bioactive compounds in extracts. At 600 μg/mL, two extracts, ethyl acetate and methanolic extract exhibited maximum inhibition of protein denaturation 75.07% ± 3.28% and 64.97% ± 1.73%, nitric oxide activity 88.06% ± 3.49% and 82.09% ± 3.61%, proteinase activity 82.06% ± 2.98% and 71.06% ± 3.58%, and erythrocyte-membrane haemolysis 84.94% ± 4.14% and 72.97% ± 4.68%, respectively (P &lt; 0.001). In vivo studies using Wistar rats demonstrated no toxic effects of ethyl acetate and methanolic extract upon oral administration. These two extracts modulated cytokine levels and inflammatory markers, showing concentration dependent reductions in levels of IL-6, IL1-β, IFN-γ, TNF-α (P &lt; 0.001), iNOS, COX-2 in LPS -induced inflammation in Wistar rats. At a dose of 100 mg/kgbwt, KTEA administration resulted in a substantial decrease in cytokine levels: IL1β from 68.99 ± 1.83 pg/mL to 31.68 ± 1.90 pg/mL (P &lt; 0.001), IL6 from 80.40 ± 0.70 pg/mL to 39.47 ± 1.85 pg/mL (P &lt; 0.01), TNFα from 71.34 ± 2.35 pg/mL to 29.37 ± 2.20 pg/mL (P &lt; 0.001), and IFNγ from 120.27 ± 4.26 pg/mL to 68.07 ± 2.78 (P &lt; 0.01) pg/mL. Similarly, a concentration dependent decrease in prostaglandins (273.68 pg/mL and 418.96 pg/mL by ethyl acetate and methanolic extract at 100 mg/kgbwt) and leukotrienes (239.37 pg/mL and 302.19 pg/mL by ethyl acetate and methanolic extract at 100 mg/kgBwt) were observed as compared with the LPS induced group (prostaglandins 1129.99 pg/mL and leukotrienes 558.67 pg/mL). We also observed that Koenigia tortuosa extracts improves the levels of lymphocytes and leukocytes. Notably, PPAR-γ expression exhibited a concentration dependent increase, suggesting potential anti-inflammatory effects through nuclear receptor modulation. Histopathological investigati","PeriodicalId":13551,"journal":{"name":"Inflammopharmacology","volume":" ","pages":""},"PeriodicalIF":4.6,"publicationDate":"2025-02-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143515508","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":"Anti-inflammatory and antioxidant effects of baicalein: targeting Nrf2, and NFĸB in neurodegenerative disease.","authors":"Omkar Kumar Kuwar, Nileshwar Kalia","doi":"10.1007/s10787-025-01698-x","DOIUrl":"https://doi.org/10.1007/s10787-025-01698-x","url":null,"abstract":"<p><p>Neurodegenerative diseases, such as Alzheimer's disease, Parkinson's disease, and Huntington's disease, are characterized by progressive loss of neurons in the brain regions, including the hippocampus, cortex, substantia nigra, and striatum. Multiple pathological mechanisms drive this neuronal loss, including oxidative stress, chronic inflammation, mitochondrial dysfunction, protein misfolding, and excitotoxicity. Recent evidence suggests that these processes are intricately linked to the dysregulation of key signalling pathways, such as the IĸB/NFĸB, and KEAP1/Nrf2 pathways, which play central roles in neuroinflammation, oxidative stress, and mitochondrial functions, respectively. At present, no cure exists for neurodegenerative disorders, and available medications focus solely on symptomatic management. While these treatments provide temporary relief, their long-term use is often associated with adverse health effects. In this context, natural Phytoactive constituents like Baicalein, a bioactive flavonoid derived from Scutellaria baicalensis, have gained attention for their promising therapeutic potential. Baicalein has been shown to modulate the IĸB/NFĸB, and KEAP1/Nrf2 pathways, thereby mitigating neuroinflammation and oxidative stress while supporting mitochondrial health. It exerts anti-inflammatory effects by inhibiting NFĸB activation, thereby reducing the production of proinflammatory cytokines, such as TNF-α, IL-1β, IL-6, and NLRP3 inflammasome, and enzymes like COX-2, LOX, and iNOS, which are essential for innate and adaptive immune responses. Simultaneously, baicalein enhances the Nrf2 activation, promoting the expression of antioxidant enzymes like HO-1, NQO1, GPx, and SOD, thus countering oxidative stress. These findings highlight the potential of baiclalein as a complementary approach for managing neurodegenerative diseases, offering a safer and more holistic alternative to conventional therapies.</p>","PeriodicalId":13551,"journal":{"name":"Inflammopharmacology","volume":" ","pages":""},"PeriodicalIF":4.6,"publicationDate":"2025-02-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143515506","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":"Dissolving microneedle patch for transdermal delivery of perindopril erbumine.","authors":"Zunaira Altaf, Zulcaif Ahmad, Asif Mahmood, Saniia Shchinar, Riffat Latif","doi":"10.1007/s10787-025-01696-z","DOIUrl":"https://doi.org/10.1007/s10787-025-01696-z","url":null,"abstract":"<p><p>Perindopril Erbumine is a widely used angiotensin-converting enzyme (ACE) inhibitor for managing hypertension and cardiovascular diseases. Its dual action of lowering blood pressure and mitigating inflammation makes it a cornerstone treatment in these conditions. However, its oral administration often results in suboptimal bioavailability and gastrointestinal side effects. This study aimed to develop and characterize a dissolving microneedle (dMN) patch for the transdermal delivery of Perindopril Erbumine to enhance therapeutic efficacy and patient compliance. A Perindopril Erbumine-loaded microneedle patch was fabricated using chitosan and polyvinyl alcohol (PVA) using the solvent casting method. The microneedle patch was evaluated for physical properties, mechanical strength, drug loading, and moisture content. Ex-vivo permeation through rat skin and in-vivo pharmacokinetic studies in rabbits was conducted to compare its performance with a marketed oral Perindopril Erbumine formulation. The developed patch demonstrated effective skin penetration, controlled drug release, and a six-fold enhancement in cumulative drug permeation (82.45% ± 1.54) compared to the oral solution (14.32% ± 1.60). The pharmacokinetic study revealed prolonged drug release, with a 7.9-fold increase in half-life (7.739 ± 0.243 h vs. 0.986 ± 0.93 h) and a significantly higher area under the curve (AUC) for the microneedle patch. Skin irritation studies confirmed the biocompatibility of the formulation, with no significant adverse effects observed. These findings highlight the potential of Perindopril Erbumine-loaded dissolving microneedles as a promising transdermal delivery system for improved therapeutic outcomes in managing hypertension and inflammation-related vascular conditions, potentially reducing inflammation through enhanced and targeted drug delivery.</p>","PeriodicalId":13551,"journal":{"name":"Inflammopharmacology","volume":" ","pages":""},"PeriodicalIF":4.6,"publicationDate":"2025-02-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143500832","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}