Journal of Pharmaceutical Innovation最新文献

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Berberine–Carrageenan Complexation: Preparation, Characterization and Employment of the Complex in a Gastric-Floating Matrix 小檗碱-卡拉胶络合物的制备、表征及在胃漂浮基质中的应用
IF 2.7 4区 医学
Journal of Pharmaceutical Innovation Pub Date : 2025-06-19 DOI: 10.1007/s12247-025-10022-7
Rana Z. Al-Sukhun, Ahmad Bani-Jaber
{"title":"Berberine–Carrageenan Complexation: Preparation, Characterization and Employment of the Complex in a Gastric-Floating Matrix","authors":"Rana Z. Al-Sukhun,&nbsp;Ahmad Bani-Jaber","doi":"10.1007/s12247-025-10022-7","DOIUrl":"10.1007/s12247-025-10022-7","url":null,"abstract":"<div><h3>Purpose</h3><p>The efficient clinical utilization of Berberine (BRB), a natural alkaloid, could be hampered by its poor dissolution performance in the gastric fluid and by the intestinal glycoprotein mediated efflux. Therefore, formulations that enhance BRB dissolution with prolonged gastric retention may be beneficial. In this work, we sought to improve the dissolution performance of BRB by its complexation with carrageenan (CRG), a hydrophilic polyelectrolyte.</p><h3>Methods</h3><p>The optimum ratios of the complexation using λ and κ-CRG were studied by viscosity measurements. The release of BRB from the complexes was assessed in simulated gastric fluid (SGF). The complex with enhanced BRB release, namely BRB-κ-CRG complex, was formulated as hydroxypropyl-methylcellulose floating matrix.</p><h3>Results</h3><p>Compared to BRB-λ-CRG complex and neat BRB, BRB-κ-CRG complex showed a higher and faster rate of BRB release in SGF. Relative to that of BRB, the floating matrix of BRB-κ-CRG complex was shown to release twice as much BRB in a sustained-release zero-order pattern throughout the course of 8 h of dissolution in SGF.</p><h3>Conclusion</h3><p>The outcomes of the work are highly beneficial for further investigation of natural alternatives that target gastric related conditions.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 4","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-06-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145167428","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
Statistical Formulation Optimization of Naproxen Microsponges with Eudragit RS100 for Sustained Drug Release 含乌龙茶RS100的萘普生微海绵缓释配方的统计优化
IF 2.7 4区 医学
Journal of Pharmaceutical Innovation Pub Date : 2025-06-19 DOI: 10.1007/s12247-025-09994-3
Sonia Gupta, Himanshu Chopra, Prabhjot Singh bajwa, Dinesh Kumar
{"title":"Statistical Formulation Optimization of Naproxen Microsponges with Eudragit RS100 for Sustained Drug Release","authors":"Sonia Gupta,&nbsp;Himanshu Chopra,&nbsp;Prabhjot Singh bajwa,&nbsp;Dinesh Kumar","doi":"10.1007/s12247-025-09994-3","DOIUrl":"10.1007/s12247-025-09994-3","url":null,"abstract":"<div><h3>Background and Objective</h3><p>This study aims to address the solubility, stability, and bioavailability challenges of Naproxen, a widely used nonsteroidal anti-inflammatory drug (NSAID), by formulating Naproxen-loaded microsponges with controlled release properties. The ultimate objective is to achieve enhanced drug concentration in the bloodstream while ensuring prolonged therapeutic efficacy. Naproxen was specifically chosen for this study due to its frequent clinical use in managing musculoskeletal disorders, arthritis, and inflammatory conditions, along with its poor aqueous solubility (BCS Class II) and gastrointestinal side effects upon oral administration. While other NSAIDs, such as ibuprofen, diclofenac, and celecoxib, face similar biopharmaceutical limitations, Naproxen’s longer half-life and strong anti-inflammatory efficacy make it a suitable candidate for a controlled topical delivery system to enhance localized action, reduce systemic toxicity, and improve patient compliance.</p><h3>Methods</h3><p>Naproxen microsponges were developed using the quasi-emulsion solvent diffusion technique. Eudragit RS100 (ERS100) was employed as the polymer, polyvinyl alcohol (PVA) as the stabilizing emulsifier, and dichloromethane (DCM) as the organic solvent. To systematically optimize the formulation, a Box-Behnken design was utilized, enabling the evaluation of critical formulation and process parameters. The independent variables included ERS100 amount (X₁), PVA concentration (X₂), and stirring speed (X₃). Response factors were defined as particle size, percentage yield, and entrapment efficiency (%EE).</p><h3>Results</h3><p>All prepared microsponge batches demonstrated an initial burst release of more than 40% of Naproxen within the first hour, followed by a sustained drug release profile over 8 h. The optimized batch, identified through desirability-based software optimization, exhibited a particle size of 22.32 µm, a percentage yield of 85.14%, and an entrapment efficiency of 69.11%. Drug release from the optimized formulation (NXMF2) was found to follow the Korsmeyer-Peppas model, indicating a diffusion-controlled release mechanism.</p><p>This study demonstrates the potential of microsponge technology as an effective strategy to enhance the bioavailability and therapeutic performance of Naproxen, with the optimized formulation offering controlled release and improved pharmacokinetic properties.</p><h3>Conclusion</h3><p>The Naproxen-loaded microsponges achieved sustained drug release, improved bioavailability, and enhanced stability, demonstrating their potential for effective controlled drug delivery.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 4","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-06-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145167425","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
Synthesis of Radioiodinated Silica-Coated Magnetic Nanoparticles as SPECT/MR Dual-Modality Probe for Bone Imaging 放射性碘化二氧化硅包覆磁性纳米颗粒作为骨成像SPECT/MR双模探针的合成
IF 2.7 4区 医学
Journal of Pharmaceutical Innovation Pub Date : 2025-06-18 DOI: 10.1007/s12247-025-10011-w
Noha A. Bayoumi
{"title":"Synthesis of Radioiodinated Silica-Coated Magnetic Nanoparticles as SPECT/MR Dual-Modality Probe for Bone Imaging","authors":"Noha A. Bayoumi","doi":"10.1007/s12247-025-10011-w","DOIUrl":"10.1007/s12247-025-10011-w","url":null,"abstract":"<div><h3>Purpose</h3><p>A reliable imaging probe is essential for the accurate diagnosis of diseases and to support effective therapeutic decision-making. Different nanoparticles based multimodal probes have been studied for bone imaging. This work focuses on synthesizing of radiolabeled iron oxide magnetic nanoparticles as a promising dual modality bioprobe (SPECT/MR) for bone imaging.</p><h3>Methods</h3><p>In this work, silica coated magnetic nanoparticles (SiO<sub>2</sub>@MNPs) were synthesized. Radioiodination of SiO<sub>2</sub>@MNPs with iodine − 131 was performed via the Finkelstein reaction to produce a prospective radioiodinated MNPs for bone targeting.</p><h3>Results</h3><p>The radioiodinated NPs were obtained in high radiochemical purity (about 98.5 ± 0.5%) by magnet separation. The aqueous dispersion of the radioiodinated silica coated MNPs (<sup>131</sup>I-SiO<sub>2</sub>@MNPs) exhibited adequate in-vitro stability and biocompatibility. Biodistribution study results after intravenous injection of (<sup>131</sup>I-SiO<sub>2</sub>@MNPs) in normal mice revealed the high bone targeting efficiency of the radiolabeled NPs (C<sub>max</sub>= 6± 0.5% ID/g at t<sub>max</sub>= 2 h post injection). Magnetization properties measurements proved the preservation of the magnetic properties of SiO<sub>2</sub>@MNPs after the iodination process retaining its effectiveness as MRI contrast agent.</p><h3>Conclusion</h3><p>Based on to the results of this study, <sup>131</sup>I-SiO<sub>2</sub>@MNPs could be considered as a promising candidate for SPECT/MR dual bone imaging.</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 4","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s12247-025-10011-w.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145167063","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
A Plant Wide Modelling Framework For The Multistage Processes of The Continuous Manufacturing of Pharmaceutical Tablets 片剂连续生产多阶段过程的全厂范围建模框架
IF 2.7 4区 医学
Journal of Pharmaceutical Innovation Pub Date : 2025-06-17 DOI: 10.1007/s12247-025-10017-4
Motaz Deebes, Mahdi Mahfouf, Chalak Omar, Syed Islam, Ben Morgan
{"title":"A Plant Wide Modelling Framework For The Multistage Processes of The Continuous Manufacturing of Pharmaceutical Tablets","authors":"Motaz Deebes,&nbsp;Mahdi Mahfouf,&nbsp;Chalak Omar,&nbsp;Syed Islam,&nbsp;Ben Morgan","doi":"10.1007/s12247-025-10017-4","DOIUrl":"10.1007/s12247-025-10017-4","url":null,"abstract":"<div><p>Continuous manufacturing can be seen as a promising shift in the pharmaceutical industry, offering benefits such as reduced costs and improved product quality. However, the multistage nature of continuous tablet manufacturing demands a deeper understanding of the complex interactions between process parameters, material attributes, and final product quality. This study aims to address this challenge by developing a novel, data-driven modelling framework to predict key critical quality attributes, including particle size distribution, moisture content, and tablet tensile strength across the processing stages of a pilot-scale continuous tablet manufacturing line. A sequential modelling approach was employed, integrating Random Forest and Gradient Boosting Machines to model each processing stage. These models were sequentially trained and interlinked to holistically capture process–material interactions across granulation, drying, milling, and tabletting stages. To manage error propagation between stages, Gaussian Mixture Models were incorporated for error characterisation and uncertainty reduction. The results showed that the proposed framework captured the non-linear interactions between processing parameters and the quality attributes. The incorporation of GMMs was influential in quantifying uncertainty within each process model, resulting in a final estimation of tablet tensile strength with an <span>( R^2 )</span> value of 0.90 using the integrated Random Forest model. This framework demonstrated considerable improvement in the predictive performance of the continuous manufacturing processes modelling through the integration of machine learning models and an uncertainty-aware strategy. The predictive tool is intended to support the Quality by Design (QbD) concept through systematic design space exploration and process understanding of the pharmaceutical continuous manufacturing.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 4","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-06-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s12247-025-10017-4.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145166097","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
Predicting Skin Permeability of Compounds with Elasticnet, Ridge and Decision Tree Regression Methods 弹性网回归、岭回归和决策树回归预测化合物皮肤渗透性
IF 2.7 4区 医学
Journal of Pharmaceutical Innovation Pub Date : 2025-06-15 DOI: 10.1007/s12247-025-10025-4
Kevin Ita, Pegah Capaul, Pardis Khani
{"title":"Predicting Skin Permeability of Compounds with Elasticnet, Ridge and Decision Tree Regression Methods","authors":"Kevin Ita,&nbsp;Pegah Capaul,&nbsp;Pardis Khani","doi":"10.1007/s12247-025-10025-4","DOIUrl":"10.1007/s12247-025-10025-4","url":null,"abstract":"<div><h3>Purpose</h3><p>The aim of this project was to predict the skin permeability of compounds in three modified datasets (Steinmetz et al., Stevens et al. as well as Wilschut et al.).</p><h3>Methods</h3><p>We employed Elasticnet, Ridge and Decision Tree Regression algorithms to forecast the skin permeability values of these compounds.</p><h3>Results</h3><p>When the Ridge regression technique was applied to the modified Wilschut et al dataset, the mean squared error was 0.20, the mean absolute error was 0.33 and the coefficient of determination (R²) was 0.61. The application of the same technique to the modified Stevens et al. dataset resulted in a mean squared error of 1.04, a mean absolute error of 0.5172 and an R-squared value of 0.18. The utilization of the Ridge regression method on the modified Steinmetz et al. dataset resulted in a mean squared error of 0.65, a mean absolute error of 0.67 and an R-squared Score of 0.48. When the Elasticnet regression approach was used on the modified Wilschut et al, the mean squared error was 0.24 and the coefficient of determination (R²) was 0.60. The utilization of the Elasticnet regression technique on the modified Steinmetz et al dataset led to a mean squared error of 0.88 and the coefficient of determination (R²) of 0.30. In comparison, Elasticnet regression technique on the modified Stevens et al dataset led to a mean squared error of 0.32 and the coefficient of determination (R²) of 0.42. The utilization of the Decision Tree(DT) regression on the modified Wilschut et al. dataset, resulted in the mean squared error of 0.28 and the coefficient of determination (R²) of 0.53. Decision Tree regression technique on the modified Stevens et al. dataset yielded a mean squared error: 0.31 and an R-squared Score :of 0.66. When the DT regression method was used on the Steinmetz et al dataset, the mean squared error was 0.89 and the R-squared Score was 0.14.</p><h3>Conclusion</h3><p>Our comparison analysis utilizing ElasticNet, Ridge, and Decision Tree regression models to forecast skin permeability across three datasets provides significant insights into the relationship between data quality and model efficacy. This finding is consistent with and enhances the advancing field of computer modeling in cutaneous absorption, specifically in medication development, cosmetic safety, and regulatory science.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 3","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-06-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145166124","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
Crosslinked Chitosan-Gellan Gum Nanoparticles for Enhanced Ocular Delivery of Citicoline in Glaucoma Management: Fabrication, Optimization, and Characterization 交联壳聚糖-结冷胶纳米颗粒增强青光眼治疗中胞胆碱的眼部输送:制造、优化和表征
IF 2.7 4区 医学
Journal of Pharmaceutical Innovation Pub Date : 2025-06-14 DOI: 10.1007/s12247-025-10019-2
Gurpreet Kandav, Tamanna Sharma, Akash Chandel
{"title":"Crosslinked Chitosan-Gellan Gum Nanoparticles for Enhanced Ocular Delivery of Citicoline in Glaucoma Management: Fabrication, Optimization, and Characterization","authors":"Gurpreet Kandav,&nbsp;Tamanna Sharma,&nbsp;Akash Chandel","doi":"10.1007/s12247-025-10019-2","DOIUrl":"10.1007/s12247-025-10019-2","url":null,"abstract":"<div><h3>Purpose</h3><p>To overcome the challenges of conventional ocular formulations, such as poor bioavailability and rapid clearance, this study aims to crosslink chitosan (CS) and gellan gum (GG) polymers to develop and optimize citicoline-loaded chitosan-gellan gum nanoparticles (CT-CS-GG<sub>NPs</sub>) for enhanced ocular drug delivery and controlled release, emphasizing glaucoma treatment by protecting neuronal function.</p><h3>Methods</h3><p>CT-CS-GG<sub>NPs</sub> were fabricated by crosslinking CS and GG via the ionic gelation method and were optimized using a central composite design with three levels and two factors to assess the influence of chitosan and gellan gum concentration on % entrapment efficiency (%EE), polydispersity index (PDI), zeta potential (ZP) and particle size (PS). The optimized formulation (CT-CS-GG<sub>NPsopt</sub>) was further examined by FTIR, TEM, DSC, drug release (In-Vitro) &amp; Ex-Vivo including HET CAM and permeation Studies etc.</p><h3>Results</h3><p>The mean values obtained from 13 batches of CT-CS-GG<sub>NPs</sub> for PS, %EE, PDI, and ZP varied within the range of 241.3 to 990.2 nm, 12% to 83.33%, 0.302 to 0.978, and 1.23 to 35.2 mV respectively. CT-CS-GG<sub>NPsopt</sub> demonstrated extended in-vitro drug release, reaching 70.6 ± 1.9% over 12 h. Ex-vivo HET-CAM and permeation studies confirmed the non-irritant nature of CT-CS-GG<sub>NPsopt</sub> and demonstrated a 2.2-fold higher drug uptake by the goat cornea compared to the drug solution.</p><h3>Conclusion</h3><p>CS and GG were successfully crosslinked to prepare CT-CS-GG<sub>NPs</sub>, which exhibit prolonged drug release, potentially enhancing drug absorption and therapeutic effectiveness while showing promise as safe carriers for ocular drug delivery.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 3","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-06-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145165618","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 and Characterization of Leflunomide and Resveratrol Loaded Nanostructured Lipid Carrier Based In-situ Hydrogel System for Effective Management of Rheumatoid Arthritis 来氟米特和白藜芦醇负载的纳米结构脂质载体原位水凝胶系统的开发和表征有效治疗类风湿性关节炎
IF 2.7 4区 医学
Journal of Pharmaceutical Innovation Pub Date : 2025-06-13 DOI: 10.1007/s12247-025-09976-5
Amit Sahu, Sunny Rathee, Shivani Saraf, Sarjana Raikwar, Pooja Das Bidla, Rajesh Singh Pawar, Sanjay K. Jain
{"title":"Development and Characterization of Leflunomide and Resveratrol Loaded Nanostructured Lipid Carrier Based In-situ Hydrogel System for Effective Management of Rheumatoid Arthritis","authors":"Amit Sahu,&nbsp;Sunny Rathee,&nbsp;Shivani Saraf,&nbsp;Sarjana Raikwar,&nbsp;Pooja Das Bidla,&nbsp;Rajesh Singh Pawar,&nbsp;Sanjay K. Jain","doi":"10.1007/s12247-025-09976-5","DOIUrl":"10.1007/s12247-025-09976-5","url":null,"abstract":"<div><h3>Purpose</h3><p>This study aims to improve the therapeutic effect of leflunomide (LEF), an immune-altering drug, and resveratrol (RSV), a polyphenolic compound distributed locally in the body. LEF and RSV were encapsulated in nanostructured lipid carriers (NLCs).</p><h3>Method </h3><p>NLCs were prepared by modified thermal homogenization and melt sonication using compritol ATO 888, oleic acid, Tween 80, and PEG 400. A Box-Behnken design (BBD) was utilized to optimize the formulation. The ideal NLC surface was modified by conjugation with chondroitin sulfate (CHS). Chondroitin sulfate-modified NLCs dispersions (CHS-NLCs) were characterized by particle size, PDI, encapsulation efficiency, and zeta potential. Thermosensitive gel was prepared using Pluronic F-127 (PF-127) and Pluronic F-68 (PF-68). Gels prepared in situ based on CHS-NLCs were characterized by gel time, thermal reversibility, pH, viscosity, injection time, and in vitro release. The effectiveness of the NLC-based in situ hydrogels was tested in an arthritis model.</p><h3>Results </h3><p>The produced CHS-NLCs had a particle size of 188.2 ± 0.85 nm, PDI of 0.396 ± 0.005, zeta potential of -17.16 ± 0.81 mV, LEF and RSV encapsulation efficiency of 92.16 ± 0.41 and 82.82%, respectively. The gel was thermosensitive and released 79.54% and 76.99% of LEF and RSV, respectively, within 144 h. The effectiveness of the proposed method was tested using an arthritis model, and the results showed a reduction in joint pain in mice in 21 days.</p><h3>Conclusion </h3><p>The developed CHS-modified NLC-based in situ hydrogel demonstrated effective, sustained drug release and significant therapeutic benefits in an RA model. This approach holds promise for improved RA management through localized drug delivery.</p><h3>Graphical Abstract</h3><p>Figure: Leflunomide and resveratrol-loaded nanostructured lipid carrier-based in-situ hydrogel system for effective management of Rheumatoid Arthritis</p>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 3","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-06-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145165294","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
Unlocking the Therapeutic Potential of Alisertib in Breast Cancer: An In-Depth Exploration of Molecular Targets Using Network Pharmacology and Gene Expression Network 释放Alisertib治疗乳腺癌的潜力:利用网络药理学和基因表达网络深入探索分子靶点
IF 2.7 4区 医学
Journal of Pharmaceutical Innovation Pub Date : 2025-06-13 DOI: 10.1007/s12247-025-10004-9
Suad A. Alghamdi, Mohammed Alissa, Muhammad Suleman
{"title":"Unlocking the Therapeutic Potential of Alisertib in Breast Cancer: An In-Depth Exploration of Molecular Targets Using Network Pharmacology and Gene Expression Network","authors":"Suad A. Alghamdi,&nbsp;Mohammed Alissa,&nbsp;Muhammad Suleman","doi":"10.1007/s12247-025-10004-9","DOIUrl":"10.1007/s12247-025-10004-9","url":null,"abstract":"<div><h3>Purpose</h3><p>Breast cancer is a prevalent and serious disease marked by uncontrolled cell growth. Alisertib, a small-molecule inhibitor, shows potential in cancer treatment by blocking cell proliferation. This study uses a network pharmacology approach to identify Alisertib's potential targets in breast cancer.</p><h3>Methods</h3><p>We used network pharmacology, molecular dynamic simulation and binding free energies approaches to identify the potential molecular target of Alisertib in Breast Cancer.</p><h3>Results</h3><p>SwissTarget, SuperPred, and CLCpred identified 100, 721, and 327 potential targets for Alisertib, respectively. From DisGeNet, 6,941 markers associated with breast cancer were identified, among which 29 proteins overlapped as both disease-associated genes and drug targets. Furthermore, the CytoHubba identified 10 hub genes from the PPI network of 29 common targets, with FGFR2, FGFR4, and MAPK7 ranked best based on their degree score. Moreover, the docking analysis revealed a docking scores of -8.854 kcal/mol, -7.373 kcal/mol and -7.262 kcal/mol for FGFR2, FGFR4, and MAPK7-Alisertib complexes respectively. The stable interaction of identified targets and Alisertib was further validated by the 200 ns molecular dynamics simulation. Binding free energy calculations using MM/GBSA yielded values of -61.0977 kcal/mol for the FGFR2-alisertib complex, -52.0032 kcal/mol for FGFR4-alisertib, and -47.9903 kcal/mol for MAPK7-alisertib. These results suggest that Alisertib exhibits stronger binding affinity for FGFR2, FGFR4 and MAPK7 compared to the control.</p><h3>Conclusion</h3><p>These findings suggest that Alisertib has a strong binding affinity and favorable pharmacological interactions with FGFR4, FGFR2, and MAPK7, highlighting its potential as a targeted therapeutic for breast cancer. Consequently, Alisertib warrants further investigation in preclinical and clinical settings to evaluate its efficacy in treating malignant neoplasm of the breast.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 3","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-06-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145165296","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
Formulation and Evaluation of Raloxifene Hydrochloride Co-Crystals with Bioenhancer – a Potential Approach for Solubility and Bioavailability Enhancement 含生物增强剂盐酸雷洛昔芬共晶的制备及评价——一种提高溶解度和生物利用度的潜在方法
IF 2.7 4区 医学
Journal of Pharmaceutical Innovation Pub Date : 2025-06-13 DOI: 10.1007/s12247-025-09998-z
Hetal Thakkar, Krishna Modi, Dhvani Shah, Darshana Patel
{"title":"Formulation and Evaluation of Raloxifene Hydrochloride Co-Crystals with Bioenhancer – a Potential Approach for Solubility and Bioavailability Enhancement","authors":"Hetal Thakkar,&nbsp;Krishna Modi,&nbsp;Dhvani Shah,&nbsp;Darshana Patel","doi":"10.1007/s12247-025-09998-z","DOIUrl":"10.1007/s12247-025-09998-z","url":null,"abstract":"<div><h3>Purpose</h3><p>The main purpose of the research work was to formulate cocrystals of Raloxifene Hydrochloride(RXL-HCl) in order to increase its solubility and oral bioavailability. The effect of addition of bioenhancer on the oral bioavailability was also examined.</p><h3>Methods</h3><p>Co-crystals of RXL HCl with tartaric acid as a coformer were successfully formulated with salt to coformer stoichiometric ratio of 1:1 by using solvent evaporation method. Characterization was done by FTIR analysis, SEM, DSC, pXRD, solubility, in- vitro dissolution, and in-vivo pharmacokinetic study.</p><h3>Results</h3><p>Optical microscopy and SEM analysis revealed the formation of plate-shaped crystals. The stretching and bending vibration patterns were different in the FTIR spectra of the developed formulation in comparison to the RXL HCl indicating the formation of the co-crystals. DSC analysis showed a melting endotherm at 235ºC which is less than that of RXL HCl indicating the formation of co-crystals. The pXRD pattern of co-crystals was different compared to that of the RXL HCl. The solubility of co-crystals in aqueous media was found to be 14.1 mg/mL which is almost 80 folds higher compared to RXL HCl. The <i>in-vitro</i> dissolution study of co-crystals showed 82.9%, 57%, and 65% drug dissolution after 120 min in water, acidic media, and alkaline media respectively, which is significantly greater compared to the RXL HCl. The <i>in-vivo</i> pharmacokinetic study showed almost 6 folds higher bioavailability compared to the marketed product.</p><h3>Conclusion</h3><p>Administration of cocrystals of Raloxifene Hydrochloride with Naringin as a bioenhancer led to a significant enhancement in oral bioavailability.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 3","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-06-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145164566","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
Chronotherapeutic Delivery of Lornoxicam Pellets for Rheumatoid Arthritis: Formulation Development and Optimization Using a Randomized Factorial Design 氯诺昔康微丸治疗类风湿性关节炎的时间治疗:使用随机因子设计的配方开发和优化
IF 2.7 4区 医学
Journal of Pharmaceutical Innovation Pub Date : 2025-06-12 DOI: 10.1007/s12247-025-10021-8
Swapnil Jain
{"title":"Chronotherapeutic Delivery of Lornoxicam Pellets for Rheumatoid Arthritis: Formulation Development and Optimization Using a Randomized Factorial Design","authors":"Swapnil Jain","doi":"10.1007/s12247-025-10021-8","DOIUrl":"10.1007/s12247-025-10021-8","url":null,"abstract":"<div><p>Rheumatoid arthritis (RA) is a chronic condition marked by joint pain and stiffness, especially in the morning, necessitating medication for management. This study focused on developing, evaluating, and optimizing coated lornoxicam pellets for targeted colon delivery, utilizing carboxymethyl <i>Caesalpinia spinosa</i> gum to address the chronotherapeutic needs of RA. The pellets were prepared using an extrusion-spheronization technique and subsequently coated in a fluidized bed processor with polymers such as Eudragit<sup>®</sup> S 100 and RL 100. An 11-run, 2-factor, 3-level randomized full factorial design was employed to assess the influence of varying independent factors on the responses, leading to the identification of an optimized formulation. The drug release profiles of the formulation batches showed that at the 4th hour, release in the upper gastrointestinal (GI) tract ranged from 0 to 16.79%, while at the 10th hour, release at colonic pH ranged from 71.95 to 95.64%. Additionally, the optimized formulation demonstrated enhanced drug release in the presence of rat cecal matter, indicating its potential for targeted colonic delivery. In vivo pharmacokinetic studies of the optimized formulation showed a clearance of 0.022 L/hr and a volume of distribution of 0.319 L, indicating slow elimination and limited tissue distribution. The high area under curve values (44.53 and 96.12 µgh/mL) reflected effective absorption and good systemic exposure. The mean residence time of 21.30 h suggested prolonged residence time, supporting sustained therapeutic levels in the colon. These findings suggest that the optimized lornoxicam-coated pellet formulation holds promise for the chronotherapeutic management of early morning RA symptoms.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 3","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-06-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145164875","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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