Journal of Pharmaceutical Innovation最新文献

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Formulation and Optimisation of Mucoadhesive Nasal Powder of Celecoxib for Management of Pain Associated with Osteoarthritis 塞来昔布黏附鼻粉治疗骨关节炎疼痛的配方及优化
IF 2.7 4区 医学
Journal of Pharmaceutical Innovation Pub Date : 2025-10-17 DOI: 10.1007/s12247-025-10186-2
Revanshiddh Birajdar, Ashlesha Pandit
{"title":"Formulation and Optimisation of Mucoadhesive Nasal Powder of Celecoxib for Management of Pain Associated with Osteoarthritis","authors":"Revanshiddh Birajdar,&nbsp;Ashlesha Pandit","doi":"10.1007/s12247-025-10186-2","DOIUrl":"10.1007/s12247-025-10186-2","url":null,"abstract":"<div><h3>Purpose</h3><p>Celecoxib, a COX-2 inhibitor used for osteoarthritis pain, has poor aqueous solubility and limited oral bioavailability. Nasal delivery offers rapid systemic absorption and bypasses first-pass metabolism. This study aimed to develop a mucoadhesive nasal powder of celecoxib using HPβCD and PVA to enhance solubility and systemic delivery for effective osteoarthritis pain management.</p><h3>Methods</h3><p>Mucoadhesive nasal powder of celecoxib with hydroxypropyl-β-cyclodextrin (HPβCD) was prepared using the spray drying technique. A central composite design (CCD) was applied to optimize the powder, considering HPβCD (39.32–78.64 mg) and PVA (0.5–1 mg) as independent variables, with response as drug release. The improvement in solubility was evaluated using the flask shake method. In vitro drug release was carried out by using simulated nasal electrolyte solution while drug permeation was performed by using goat nasal mucosa. Mucoadhesivity of powder was evaluated by texture analyser.</p><h3>Result</h3><p>Among nine batches, batch B2 (78.64 mg HPβCD and 1 mg PVA) was selected as optimized, which shows 100% drug release within 5 min. The cumulative permeation of clecoxib (B2) was significantly higher (162.4 µg/cm²) compared to pure celecoxib (40.38 µg/cm²), performed till 75 min at pH 6.4 simulated nasal electrolyte solution (SNES) and maintained at 32 ± 2 ͦC with constant stirring at 277 rpm. PVA-containing formulation exhibited enhanced mucoadhesive strength and effective permeation across goat nasal mucosa, which indicated improved potential for intranasal delivery. HPβCD increased the solubility by 5.36-fold at 1:2 ratio of celecoxib: HPβCD and permeability of celecoxib, while PVA provided mucoadhesivity (higher detachment force at 1019.9 mN) as compared to the formulation without PVA, which enhanced the residence time of powder on nasal mucosa, thus, ultimately enhanced the permeability.</p><h3>Conclusion</h3><p>HPβCD and PVA synergistically improved solubility, release profile, and nasal permeation of celecoxib, highlighting their potential for enhanced drug delivery systems. Thus, this formulation offered a convenient alternative for patients who have difficulty in swallowing oral dosage forms and provided a faster onset of action through nasal drug delivery.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 6","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145316530","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}
引用次数: 0
Iontophoresis-Enhanced Transdermal Delivery of Hyaluronic Acid: Mechanisms, Molecular Weight Effects, and Application Potential 离子渗透增强透明质酸的透皮递送:机制、分子量效应和应用潜力
IF 2.7 4区 医学
Journal of Pharmaceutical Innovation Pub Date : 2025-10-16 DOI: 10.1007/s12247-025-10150-0
Qinghui Zhang, Dangwei Li, Jian Song, Xianmei Meng, Pingping Zhao, Yihua Zhou, Jun Qian
{"title":"Iontophoresis-Enhanced Transdermal Delivery of Hyaluronic Acid: Mechanisms, Molecular Weight Effects, and Application Potential","authors":"Qinghui Zhang,&nbsp;Dangwei Li,&nbsp;Jian Song,&nbsp;Xianmei Meng,&nbsp;Pingping Zhao,&nbsp;Yihua Zhou,&nbsp;Jun Qian","doi":"10.1007/s12247-025-10150-0","DOIUrl":"10.1007/s12247-025-10150-0","url":null,"abstract":"<div><h3>Purpose</h3><p>Hyaluronic acid (HA) is a widely used moisturizing agent, but its strong hydrophilicity and high molecular weight limit its skin permeability. Iontophoresis has been proposed as a strategy to improve HA delivery, but its mechanisms remain unclear. This study aims to investigate how iontophoresis enhances the transdermal transport of HA and to provide a theoretical basis for developing efficient HA delivery systems.</p><h3>Methods</h3><p>Ex vivo pig and rat skin models were used to assess changes in skin electrical properties under iontophoresis. Fluorescein isothiocyanate-labeled HA (FITC-HA) with different molecular weights (3, 10, 35, and 200 kDa) was synthesized to visualize penetration routes and evaluate permeation efficiency. Neutral dextran served as a reference to differentiate the roles of electromigration (EM) and electroosmosis (EO).</p><h3>Results</h3><p>Iontophoresis significantly altered skin electrical behavior, showing polarization and ion accumulation, particularly at the anode with HA. Fluorescence microscopy revealed that HA primarily penetrates through the intercellular pathway, and additionally via hair follicles into the deeper layers of the skin. EM was the primary driving force, with its contribution increasing with applied voltage. Medium-weight HA (10–35 kDa) permeated for 0.5 h under 1 V voltage, showing comparable penetration depth and area to 3 kDa HA under passive conditions.</p><h3>Conclusion</h3><p>Iontophoresis enhances HA transdermal delivery and shows potential as a noninvasive method for skincare and drug delivery applications. Further in vivo studies are needed to support clinical application.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 6","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s12247-025-10150-0.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145296815","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Fusion of Traditional Herbal Drug with Advanced 3-D Printed Dosage Form: Design, Development and Characterization 传统草药与先进3d打印剂型的融合:设计、开发和表征
IF 2.7 4区 医学
Journal of Pharmaceutical Innovation Pub Date : 2025-10-16 DOI: 10.1007/s12247-025-10125-1
Hardik Rana, Dhrusha Patel, Vaishali Thakkar, Tejal Gandhi
{"title":"Fusion of Traditional Herbal Drug with Advanced 3-D Printed Dosage Form: Design, Development and Characterization","authors":"Hardik Rana,&nbsp;Dhrusha Patel,&nbsp;Vaishali Thakkar,&nbsp;Tejal Gandhi","doi":"10.1007/s12247-025-10125-1","DOIUrl":"10.1007/s12247-025-10125-1","url":null,"abstract":"<div><h3>Background</h3><p>The current scenario demands the design of personalized medicine with fewer side effects. The study aims to design a Liquisolid compact containing a 3D printed tablet (LSC-3DPT) of C.pulcherrima (CP) flower extract to treat urolithiasis utilizing the upgraded statistical regulatory framework.</p><h3>Results and Discussion</h3><p>The extraction of terpenes from CP was carried out, and its potency was evaluated in terms of CaCl<sub>2</sub> aggregation, growth, nucleation, and turbidity assays, as well as its ability to inhibit in vitro CaOx crystals. The extract showed reasonable anti-urolithiatic properties, having a p-value &lt; 0.05 with the existing treatment. The observed sticky nature and poor aqueous solubility of the extract were resolved by the liquisolid compact (LSC) technique. The extract was adsorbed into Neusilin (NS). The developed LSC displayed excellent micrometric properties and better solubility. Furthermore, it was loaded into a 3D-printed tablet using FDM technology to make it patient-centric. FMEA scrutinized the percentage infill and layer thickness as critical process parameters, whereas drug release and hardness were identified as critical quality attributes. A central composite design showed the significant effect of process parameters on the quality of LSC-3DPT. The optimized batch exhibited the desired hardness (3.93 ± 0.07), controlled release up to 12 h, and excellent stability.</p><h3>Conclusion</h3><p>LSC-3DPT was used to customize doses, design flexible shapes and sizes, and modulate terpene release thereby enhancing patient compliance. The CP extract was used to treat the patient suffering from urolithiasis. The novel amalgamated, systematically developed LSC-3DPT will be assessed in a pre-clinical study for better assurance.</p><h3>Graphical Abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 6","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145296814","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}
引用次数: 0
A Retrospective Analysis of FDA Warning Letters Issued For Biologics From 2010 To 2025 2010 - 2025年FDA对生物制剂的警告信回顾分析
IF 2.7 4区 医学
Journal of Pharmaceutical Innovation Pub Date : 2025-10-16 DOI: 10.1007/s12247-025-10123-3
Prarthana Radhakrishnan, Dhanabal SP, Ganesh GNK
{"title":"A Retrospective Analysis of FDA Warning Letters Issued For Biologics From 2010 To 2025","authors":"Prarthana Radhakrishnan,&nbsp;Dhanabal SP,&nbsp;Ganesh GNK","doi":"10.1007/s12247-025-10123-3","DOIUrl":"10.1007/s12247-025-10123-3","url":null,"abstract":"<p>To lawfully market any drug products, biosimilars, or vaccines in the United States, the Food and Drug Administration (FDA) must provide a valid license or approval. The FDA takes full responsibility for protecting public health by regulating food and drug substances for their purity, safety, and efficacy. Biologics or biopharmaceuticals represent a rapidly growing field due to recent technological advancements and their targeted therapy advantages. To maintain the quality and safety of approved drugs, the FDA conducts periodic inspections.</p><p>This study aims to analyze the causes and trends of warning letters issued to biologics for current good manufacturing practices (CGMP) and Data integrity violations during 2010–2025, and provide preventive measures to impart knowledge to drug developers, thereby avoiding warning letters.</p><p>The warning letters issued from 2010 to 2025 were pulled from the FDA Compliance and Inspection Dashboard on the FDA website. Complete details on the manufacturer, country, nature of the violation, and other related details were obtained from the warning letter and thoroughly analyzed, summarized, tabulated, and concluded on the most common violations.</p><p>The study reveals that most violations are related to CGMP issues, including compromised data integrity and misbranding. In-depth analysis of CGMP warning letters in the study revealed three major repeated violations, namely, written procedure deviations, stability testing, and gaps in production record review by QC, corresponding to 17%, 15%, and 14%, respectively.</p><p>Review of warning letter analysis depicts that the FDA’s major enforcement actions are on CGMP Violations. Manufacturers should understand the importance and develop an internal checklist to follow the same, improve documentation practices with the latest technology, and conduct regular applicable training, to avoid any possible actions. The globalisation and advancements in technology should be used wisely to plan an upgraded quality management system on par with current guidelines.</p>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 6","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145296869","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}
引用次数: 0
Nanotechnology-Driven Transdermal System for Loxapine Succinate: A Novel Strategy To Improve Pharmacokinetics and Therapeutics in Psychotic Disorders 纳米技术驱动的琥珀酸洛沙平透皮系统:改善精神疾病药代动力学和治疗的新策略
IF 2.7 4区 医学
Journal of Pharmaceutical Innovation Pub Date : 2025-10-15 DOI: 10.1007/s12247-025-10131-3
Gaurav Ghumare, Pramod Salve, Ujban MD Hussain, Amol Tatode, Mohammad Qutub, Tanvi Premchandani, Samiksha Tammewar
{"title":"Nanotechnology-Driven Transdermal System for Loxapine Succinate: A Novel Strategy To Improve Pharmacokinetics and Therapeutics in Psychotic Disorders","authors":"Gaurav Ghumare,&nbsp;Pramod Salve,&nbsp;Ujban MD Hussain,&nbsp;Amol Tatode,&nbsp;Mohammad Qutub,&nbsp;Tanvi Premchandani,&nbsp;Samiksha Tammewar","doi":"10.1007/s12247-025-10131-3","DOIUrl":"10.1007/s12247-025-10131-3","url":null,"abstract":"<div><p>Loxapine succinate, an antipsychotic agent with limited oral bioavailability (30%) due to extensive Hepatic first-pass metabolism, demands innovative delivery strategies to enhance therapeutic efficacy. This study presents a novel transdermal Drug delivery system incorporating loxapine succinate-loaded chitosan nanoparticles designed to overcome these limitations. The nanoparticles, synthesized via ionic gelation, exhibited an optimized average diameter of 261.5 nm, a polydispersity index (PDI) of 0.498, and a Drug entrapment efficiency of 49.5%. These nanoparticles were integrated into pressure-sensitive adhesive (PSA) transdermal patches to facilitate sustained drug release and improved skin adhesion. Characterization studies using Fourier-transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and X-ray diffraction (XRD) confirmed structural compatibility and stability. In vitro Drug release studies demonstrated a progressive diffusion profile, while ex vivo permeation studies using porcine skin achieved a cumulative Drug permeation of 59.52% over 72 h, enhanced by the inclusion of 0.5% w/v limonene as a permeation enhancer. Pharmacokinetic assessments in Wistar rats revealed a sustained plasma concentration of 1540.76 ng/mL for 72 h using a 50 cm² patch, corresponding to a 3.99-fold and 5.2-fold increase in bioavailability compared to intravenous and oral administration, respectively. This nanoparticle-integrated transdermal platform effectively addresses key challenges in loxapine delivery by improving bioavailability, reducing dosing frequency, and promoting patient adherence in the management of psychotic disorders. The findings underscore the potential of nanotechnology-enhanced transdermal systems for advancing therapeutic outcomes in chronic psychiatric conditions.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145315935","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}
引用次数: 0
Computational Evaluation of Solanum Nigrum Phytochemicals for Dermatophyte Inhibition: ADMET, Docking, and Molecular Dynamics Studies 黑茄植物化学物质对皮肤真菌抑制作用的计算评价:ADMET、对接和分子动力学研究
IF 2.7 4区 医学
Journal of Pharmaceutical Innovation Pub Date : 2025-10-15 DOI: 10.1007/s12247-025-10097-2
Payal Panchal, Dimal Shah, Ashish Patel, Drashti Shah
{"title":"Computational Evaluation of Solanum Nigrum Phytochemicals for Dermatophyte Inhibition: ADMET, Docking, and Molecular Dynamics Studies","authors":"Payal Panchal,&nbsp;Dimal Shah,&nbsp;Ashish Patel,&nbsp;Drashti Shah","doi":"10.1007/s12247-025-10097-2","DOIUrl":"10.1007/s12247-025-10097-2","url":null,"abstract":"<div><h3>Purpose</h3><p>Dermatophytosis, a widespread superficial fungal infection affecting nearly a quarter of the global population, presents growing therapeutic challenges due to emerging resistance and tolerance among dermatophyte strains. This study investigates the antifungal potential of phytoconstituents from <i>Solanum nigrum</i> Linn. berries against dermatophytid strains using In-silico methods.</p><h3>Method</h3><p>Ten bioactive compounds—solanine, solasodine, apigenin, catechin, p-coumaric acid, epicatechin, kaempferol, quercetin, rutin, and luteolin—were systematically assessed for drug-likeness, ADMET (absorption, distribution, metabolism, excretion and toxicity) properties, molecular docking, and dynamic simulation. Key fungal protein targets (2CG9, 4QUV, and 5UIV) were selected to evaluate binding efficacy.</p><h3>Results</h3><p>Most compounds exhibited favourable drug-like properties, with molecular weights ranging from 172.224 to 413.646 Da and log P values below 5. ADMET analysis revealed moderate to low water solubility, favourable intestinal absorption, and low skin permeability. None of the compounds were found to cross the blood-brain barrier or inhibit P-glycoprotein I/II. Toxicity predictions indicated no AMES toxicity, hepatotoxicity, or skin sensitization. Molecular docking studies against protein targets 2CG9, 4QUV, and 5UIV showed notable binding affinities for all compounds, with solanine and solasodine demonstrating the highest binding scores. Molecular dynamics simulations of solanine and solasodine with 5UIV revealed stable interactions and structural integrity of the protein-ligand complexes.</p><h3>Conclusion</h3><p>These findings highlight the potential of solanine and solasodine as effective modulators of dermatophytid strains, warranting further experimental validation. This study provides valuable insights into the antifungal activity of <i>Solanum nigrum</i> Linn. berry phytoconstituents and their potential as novel therapeutic agents against dermatophytosis.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145315961","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}
引用次数: 0
Design and Development of a pH-Responsive In-situ Gel of Brinzolamide for Ocular Delivery Using Quality by Design (QbD): Formulation Optimization, Characterization, and In-vivo Evaluation for Sustained Glaucoma Management 基于质量设计(QbD)的ph响应原位布林唑胺凝胶的设计和开发:配方优化、表征和持续青光眼治疗的体内评价
IF 2.7 4区 医学
Journal of Pharmaceutical Innovation Pub Date : 2025-10-14 DOI: 10.1007/s12247-025-10100-w
Sandip A. Bandgar, Riya R. Patil, Anurag R. Panade, Prajakta R. Patil
{"title":"Design and Development of a pH-Responsive In-situ Gel of Brinzolamide for Ocular Delivery Using Quality by Design (QbD): Formulation Optimization, Characterization, and In-vivo Evaluation for Sustained Glaucoma Management","authors":"Sandip A. Bandgar,&nbsp;Riya R. Patil,&nbsp;Anurag R. Panade,&nbsp;Prajakta R. Patil","doi":"10.1007/s12247-025-10100-w","DOIUrl":"10.1007/s12247-025-10100-w","url":null,"abstract":"<div><p>The present investigation aims to develop a Brinzolamide-loaded In-situ gelling ophthalmic system using a Quality by Design (QbD) framework to enhance the therapeutic efficacy in the management of glaucoma. Brinzolamide, a carbonic anhydrase inhibitor, was a preferred drug for lowering intraocular pressure. However, its efficacy through conventional eye drops was compromised due to rapid precorneal elimination and Limited residence time. In-situ gels offer a promising alternative by undergoing a phase transition upon exposure to physiological pH, thereby increasing ocular bioavailability and prolonging drug release. A 3² factorial design was applied to optimize the formulation variables concentrations of Carbopol 934P and HPMC K4M and their impact on viscosity and gelation temperature. The optimized formulation demonstrated favorable physicochemical properties, including pH (6.8 ± 0.1), drug content (97.58 ± 0.5%), viscosity (1125 ± 10 cP), and immediate gelation at ocular pH. In-vitro studies revealed a sustained release profile over 8 h (96.42%) following Korsmeyer–Peppas model. Ocular irritation was evaluated via Draize and HET-CAM tests, confirming the non-irritant nature of the formulation. Accelerated stability studies conducted under ICH Q1A (R2) guidelines demonstrated excellent stability for 30 days. The study confirmed that the developed In-situ gel can significantly improve patient compliance and therapeutic outcomes in glaucoma therapy.</p><h3>Graphical Abstract</h3><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145316058","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}
引用次数: 0
Structure-Based Molecular Screening and Simulation Approaches To Inhibit Marburg Virus VP35 Protein Using Medicinal Phytocompounds for Restoring Host Immune Response 利用药用植物化合物抑制马尔堡病毒VP35蛋白以恢复宿主免疫应答的基于结构的分子筛选和模拟方法
IF 2.7 4区 医学
Journal of Pharmaceutical Innovation Pub Date : 2025-10-14 DOI: 10.1007/s12247-025-10127-z
Mohammed A. Alshehri, Mohammed Alissa, Muhammad Suleman
{"title":"Structure-Based Molecular Screening and Simulation Approaches To Inhibit Marburg Virus VP35 Protein Using Medicinal Phytocompounds for Restoring Host Immune Response","authors":"Mohammed A. Alshehri,&nbsp;Mohammed Alissa,&nbsp;Muhammad Suleman","doi":"10.1007/s12247-025-10127-z","DOIUrl":"10.1007/s12247-025-10127-z","url":null,"abstract":"<div><h3>Purpose</h3><p>The Marburg virus (MARV) is notable for its high mortality rate and potential for widespread transmission. The VP35 protein of MARV is a critical target for therapeutic intervention as it plays a key role in suppressing the host’s immune response, contributing to the virus’s pathogenicity. VP35 binds to viral double-stranded RNA (dsRNA), triggering immunosuppressive actions such as inhibiting the type I interferon (IFN) response, preventing the activation of interferon regulatory factor 3 (IRF-3), and stifling RNA silencing mechanisms.</p><h3>Methods</h3><p>we used structure-based drug design, molecular simulations, and binding free energy approaches, to identify potent phytocompounds from various natural product databases that could inhibit the MARV VP35 protein.</p><h3>Results</h3><p>Through virtual screening of African natural compounds databases against the RNA binding domain of VP35, we identified five potent compounds such as EA/NA-3,083,880 (-6.291 kcal/mol), EA/NA-15,071,544 (-6.062 kcal/mol), EA/NA-5,242,842-VP35 (-5.606 kcal/mol), EA/NA-1057 (-5.247 kcal/mol), and SA-5,281,343 (-5.083 kcal/mol) based on their high docking scores and binding affinities. Further validation through molecular dynamics simulation and dissociation constant analysis confirmed the strong binding affinities of these compounds with the VP35 protein of the MARV. Moreover, the binding free energies for EA/NA-3,083,880, EA/NA-15,071,544, EA/NA-5,242,842-VP35, EA/NA-1057, and SA-5,281,343 were recorded as -32.07 ± 0.21 kcal/mol, -38.44 ± 0.45 kcal/mol, -23.95 ± 0.24 kcal/mol, -47.55 ± 0.22 kcal/mol, and − 26.43 ± 0.22 kcal/mol, respectively, confirming their strong binding affinities with VP35. The chosen compounds demonstrated exceptional water solubility and intestinal absorption, without causing skin sensitization or hepatotoxicity. They also adhered to Lipinski’s rules.</p><h3>Conclusion</h3><p>The strong binding affinities and favourable pharmacokinetic profiles indicate that these compounds are prime candidates for further in-depth research, both in-vitro and in-vivo, with potential for development as therapeutic agents against the MARV.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145316059","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}
引用次数: 0
Application of Box-Behnken Design for the Optimization of Fumaric Acid Loaded Nano-Ethosomes for the Management of Psoriasis in Mice 应用Box-Behnken设计优化富马酸负载纳米质体治疗小鼠银屑病
IF 2.7 4区 医学
Journal of Pharmaceutical Innovation Pub Date : 2025-10-13 DOI: 10.1007/s12247-025-10088-3
Hina Kausar, Mohd. Mujeeb, Abdul Ahad, Mohd. Aqil, Ozair Alam
{"title":"Application of Box-Behnken Design for the Optimization of Fumaric Acid Loaded Nano-Ethosomes for the Management of Psoriasis in Mice","authors":"Hina Kausar,&nbsp;Mohd. Mujeeb,&nbsp;Abdul Ahad,&nbsp;Mohd. Aqil,&nbsp;Ozair Alam","doi":"10.1007/s12247-025-10088-3","DOIUrl":"10.1007/s12247-025-10088-3","url":null,"abstract":"<div><h3>Background</h3><p>Psoriasis is a chronic, inflammatory skin disorder that requires long-term care. Fumaric acid, while useful, is restricted by systemic side effects when taken orally. The purpose of the present research was to develop and optimize a fumaric acid-loaded ethosomes formulation (FA) for better topical use and therapeutic efficacy in psoriasis.</p><h3>Methods</h3><p>The ethosomes formulation was optimized using Box-Behnken Design (BBD), Response Surface Methodology (RSM) software based on vesicle size, polydispersity index (PdI), and entrapment efficiency (EE). The improved ethosomes formulation was characterized using dynamic light scattering and transmission electron microscopy (TEM). Confocal laser scanning microscopy (CLSM), skin penetration studies, in-vitro permeation study, texture analysis, and in vivo evaluation in a psoriasis plaque like psoriasis mice model were conducted to assess performance.</p><h3>Results</h3><p>The optimized formulation had a vesicle size of 153.93 ± 0.05 nm, PdI of 0.362 ± 0.001, and EE of 73.26 ± 0.05%. TEM showed spherical vesicles with a uniform shape. CLSM and skin permeation studies demonstrated enhanced penetration (up to 84.9 μm) compared to the control (59.9 μm). The ethosomes gel exhibited sustained drug release over 24 h and favourable texture properties for topical application. In vivo results indicated significant anti-inflammatory, antioxidant, and anti-psoriatic activities. Skin irritation studies confirmed its safety for topical Application.</p><h3>Conclusion</h3><p>Fumaric acid-loaded ethosomes gel is a potential topical therapy for psoriasis, focusing on local action by delivering high drug concentrations directly to the affected area while minimizing systemic absorption. This targeted approach reduces the risk of systemic side effects, making it well-suited for the treatment of inflammatory skin conditions.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145315970","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}
引用次数: 0
Development of 3D-Printed Mexiletine HCl Tablets: Exploring Formulation Strategies for High-Dose Loading 3d打印盐酸美西汀片剂的研制:探索大剂量负荷处方策略
IF 2.7 4区 医学
Journal of Pharmaceutical Innovation Pub Date : 2025-10-13 DOI: 10.1007/s12247-025-10101-9
Bushra Kiamoeddin, Arwin Ramcharan, Anouar Ait Hoummad, Niels Ouwerkerk, Fereshteh Shokri
{"title":"Development of 3D-Printed Mexiletine HCl Tablets: Exploring Formulation Strategies for High-Dose Loading","authors":"Bushra Kiamoeddin,&nbsp;Arwin Ramcharan,&nbsp;Anouar Ait Hoummad,&nbsp;Niels Ouwerkerk,&nbsp;Fereshteh Shokri","doi":"10.1007/s12247-025-10101-9","DOIUrl":"10.1007/s12247-025-10101-9","url":null,"abstract":"<div><h3>Objectives</h3><p>3D-printing technology enables the manufacturing of personalised medication tailored to patients’ medical needs. Through semisolid extrusion, 3D-printed tablets can be produced with precise dosages, allowing for customisation across various medications. Achieving this, however, requires careful consideration and optimisation of multiple factors related to 3D printing, including pharmaceutical formulation, printer settings, and tablet dimensions. This research develops 3D-printed Mexiletine HCl tablets for the treatment of Nondystrophic myotonia.</p><h3>Significance</h3><p>Eutectic system-based formulations are introduced to 3D drug printing and employed to develop the first 3D-printed Mexiletine HCl Tablets.</p><h3>Methods</h3><p>Eutectic system-based formulations were designed and further optimised to ensure desired tablet characteristics including hardness, durability, and texture. Tablet size was then adjusted to deliver up to 200 mg per tablet, with High-Performance Liquid Chromatography (HPLC) analysis employed to confirm the active pharmaceutical ingredient (API) content.</p><h3>Results</h3><p>The Mexiletine HCl formulations were developed by combining Monolaurin with either a sugar alcohol (e.g., Sorbitol, Xylitol) or a polymer (e.g., Polyvinyl pyrrolidone (PVP), Polyethylene glycol (PEG) 35,000) and were further optimized with Tween 80 to enhance formulation properties. The incorporation of Tween 80 improved the flow properties of the semisolid formulation, resulting in a higher success rate for tablet printing, and a marked reduction in the required printing temperature. Notably, Xylitol-based formulations yielded robust tablets across different sizes, thanks to the rapid solidification of the material, which maintained the tablets’ shapes.</p><h3>Conclusions</h3><p>Through systematic screening of excipients and printer settings, this study developed eutectic system-based Mexiletine HCl tablets, ensuring process quality and consistency.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145315971","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}
引用次数: 0
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