Journal of Pharmaceutical Innovation最新文献

{"title":"QbD Engineered Paradigm for Development and Validation of Robust RP-HPLC Method for Analysis of Clopidogrel and Rosuvastatin from Solid Oral Dosage Form","authors":"Neela Bhatia,&nbsp;Rupali Waghmare,&nbsp;Rutuja Chougale","doi":"10.1007/s12247-025-10118-0","DOIUrl":"10.1007/s12247-025-10118-0","url":null,"abstract":"<div><p>A robust, accurate, and Quality by Design (QbD)-driven RP-HPLC method was developed and validated for the simultaneous estimation of rosuvastatin calcium and clopidogrel hydrogen sulphate in fixed-dose combination tablets. Method development employed a Box–Behnken design to systematically optimize critical parameters detection wavelength, mobile phase pH, and flow rate targeting key chromatographic responses such as retention time, resolution, theoretical plates, and peak symmetry. The final method used a Prontosil C18 column (250 mm × 4.6 mm, 5 μm) with a mobile phase of methanol: acetonitrile: water (80:10:10 v/v), at a flow rate of 1 mL/min and detection at 225 nm. Retention times were found to be 3.225 min for rosuvastatin and 5.725 min for clopidogrel, with satisfactory resolution of 12.59 and good peak symmetry. The method showed excellent linearity over the range 3.75–300 µg/mL, with correlation coefficients of 0.9975 and 0.9992, respectively. Validation in line with ICH Q2 (R2) guidelines confirmed precision (%RSD &lt; 2), accuracy (recoveries 99.31–100.28%), robustness, and specificity. Limits of detection and quantification were 0.35 µg/mL and 1.09 µg/mL for rosuvastatin, and 0.44 µg/mL and 1.34 µg/mL for clopidogrel, respectively. This risk-based approach established a reliable method for routine quality control, enhancing product quality and patient safety.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145210834","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"“Cogrinding and Microwave-Assisted Cocrystallization of Aceclofenac–Paracetamol: A Dual Approach for the Modification of Physicochemical Properties”","authors":"Ankita Patil,&nbsp;Sujata Jadhav,&nbsp;Amol Shete,&nbsp;Swapnil Patil","doi":"10.1007/s12247-025-10126-0","DOIUrl":"10.1007/s12247-025-10126-0","url":null,"abstract":"<div><h3>Purpose</h3><p>The limited aqueous solubility and poor bioavailability of aceclofenac, a widely prescribed non-steroidal anti-inflammatory drug (NSAID), pose significant formulation challenges. Paracetamol, often co-administered with aceclofenac, also suffers from formulation-related constraints. This study aimed to develop and characterize a novel 1:1 aceclofenac–paracetamol drug–drug cocrystal to overcome these limitations, using a mechanothermal synthesis approach. Molecular docking was employed to predict favourable intermolecular interactions and guide cocrystal design.</p><h3>Methods</h3><p>Molecular docking simulations revealed strong binding interactions between aceclofenac and paracetamol, including hydrogen bonding and π–π stacking, with a binding energy of − 2.4 kcal/mol reflects a weak-to-moderate interaction; still relevant for supramolecular assembly. Cocrystal formation was achieved through cogrinding, microwave irradiation, and a combined mechanothermal method. The resulting solid forms were characterized using Fourier-transform infrared spectroscopy (FTIR), powder X-ray diffraction (PXRD), and differential scanning calorimetry (DSC). Physicochemical properties were evaluated through solubility, dissolution, and in vitro anti-inflammatory activity studies.</p><h3>Results</h3><p>The optimized formulation (Batch G), prepared using sequential cogrinding followed by microwave irradiation, showed significantly enhanced aqueous solubility of aceclofenac (14.50 ± 1.114 µg/mL), improved dissolution rate (49.30 ± 0.24% at 120 min), and potent anti-inflammatory activity (IC₅₀ = 89.96 µg/mL). Structural characterization confirmed the formation of a stable and distinct cocrystalline phase.</p><h3>Conclusion</h3><p>This study demonstrates the effectiveness of integrating molecular modelling with microwave-assisted mechanochemistry for drug–drug cocrystal development. The aceclofenac–paracetamol cocrystal offers a promising strategy to enhance the biopharmaceutical performance of poorly soluble drugs. Further in vivo evaluation and scale-up studies are warranted.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145210835","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Innovative Transdermal Delivery of Synergistic Phytoconstituents from Dalbergia Sissoo and Curcuma Longa: Formulation, Characterization, and Biological Efficacy","authors":"Vishnu Das,&nbsp;Joohee Pradhan","doi":"10.1007/s12247-025-10106-4","DOIUrl":"10.1007/s12247-025-10106-4","url":null,"abstract":"<div><h3>Purpose</h3><p><i>Dalbergia sissoo</i> and <i>Curcuma longa</i> possess established anti-inflammatory and wound-healing properties; however, their key phytoconstituents exhibit poor aqueous solubility and limited membrane permeability, restricting transdermal efficacy. This study aimed to develop and evaluate transdermal ethosomal gels (TEGs) of these extracts to enhance skin penetration, wound repair, and anti-inflammatory activity using a Quality by Design (QbD) approach.</p><h3>Methods</h3><p>Ethosomal formulations of powdered extracts of <i>D. sissoo</i> (PEDS) and <i>C. longa</i> (PECL) were optimized via Box–Behnken Design for particle size and entrapment efficiency. The optimized formulation (F6) was incorporated into three TEGs (G1–G3; pH 7.4, 7.0, and 5.5) and compared with a non-ethosomal gel (NG). Physicochemical characterization, in vitro release (Franz diffusion cell), in vivo wound healing (excision model), and anti-inflammatory activity (carrageenan-induced paw edema) were performed. Molecular docking assessed phytoconstituent interactions with hTNF-α.</p><h3>Results</h3><p>F6 displayed small vesicle sizes (PEDS: 110 ± 4.78 nm; PECL: 100 ± 3.05 nm; PDI &lt; 0.15), high entrapment efficiency (~ 98%), and stable zeta potential (− 50.2 mV). G3 (pH 5.5) showed the highest drug release (PEDS: 96.14%; PECL: 98.64% at 6 h). In vivo, TG3 achieved 98.47 ± 0.82% wound closure by day 8, complete closure by day 12, and the shortest epithelization period (7 days), significantly outperforming NG (<i>p</i> &lt; 0.01). TG3 also exhibited the highest anti-inflammatory effect (69.3% inhibition at 360 min, <i>p</i> &lt; 0.01 vs. NG). Docking studies confirmed strong hTNF-α binding by dalbergin and curcuminoids, correlating with observed biological activity.</p><h3>Conclusion</h3><p>G3 (pH 5.5 TEG) significantly enhances transdermal delivery, wound healing, and anti-inflammatory effects, underscoring its potential as therapeutic candidate for inflammatory skin conditions.</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":"2025-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145210719","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Application of Feedforward Control Strategy to Optimize the Critical Quality Atributes of Solid Dispersion Formulations: A Case Study of Ginkgo Biloba Leaf Dripping Pills","authors":"Xiaoping Wang,&nbsp;Jichen Shen,&nbsp;Sijun Wu,&nbsp;Haibin Qu","doi":"10.1007/s12247-025-10114-4","DOIUrl":"10.1007/s12247-025-10114-4","url":null,"abstract":"<div><h3>Objectives</h3><p>As a solid dispersion formulation, dripping pills exhibit significant advantages in enhancing the solubility and bioavailability of poorly soluble drugs. The quality of dripping pills is intrinsically associated with both the formulation solution and operation parameters. However, the conventional post-production quality assessment methods demonstrate limited effectiveness in achieving robust quality control due to their inherent lack of timely feedback mechanisms. It is essential to develop an appropriate method to improve the product quality.</p><h3>Methods</h3><p>Based on the concept of quality by design (QbD), this research proposed a feed-forward control strategy to explore the association of critical material attributes (CMAs), critical process parameters (CPPs) and critical quality attributes (CQAs) for <i>Ginkgo biloba</i> leaf dripping pills. The viscosity of dispersing liquid was chosen as CMA, and the drop distance and the drop speed were selected as CPPs. Qualified rate, productivity, and an average weight of dripping pills were proposed as CQAs. Several regression models linking CMA and CPPs to CQAs were established, and the design space of CPPs was defined based on these models.</p><h3>Results</h3><p>The coefficients of determination (R²) of all the models were above 0.79. Normal operating ranges were recommended for dispersing liquid viscosity (1.3 ~ 3.1 Pa·s), drop distance (4.5 ~ 6.5 cm), and drop speed (21 ~ 23 d/min). Additionally, the optimized ranges of CPPs can be successfully determined based on the input CMA.</p><h3>Conclusions</h3><p>This case study testified that the feedforward control strategy can be applied successfully to compensate for the quality variation of input CMAs, and it is possible to adjust CPPs to accommodate different CMAs for an acceptable range of CQAs, thus achieving quality control of dripping pills and ultimately contributing to the enhancement of product quality consistency.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145210929","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pharmacognostic, Phytochemical, and Multi-Analytical Profiling of the Leaves and Fruit of Terminalia Catappa L Integrated with In-Silico Docking Studies","authors":"V. A. N. V. Harita,&nbsp;Koustav Dutta,&nbsp;Aishik Banerjee,&nbsp;Sumanta Mondal","doi":"10.1007/s12247-025-10103-7","DOIUrl":"10.1007/s12247-025-10103-7","url":null,"abstract":"&lt;div&gt;&lt;h3&gt;Background&lt;/h3&gt;&lt;p&gt;&lt;i&gt;Terminalia catappa&lt;/i&gt; L (Indian almond), a tropical medicinal tree, has traditionally been used for its therapeutic properties. Despite its ethnopharmacological relevance, comprehensive validation of its bioactive constituents and pharmacological potential remains underexplored.&lt;/p&gt;&lt;h3&gt;Objective&lt;/h3&gt;&lt;p&gt;This study aimed to evaluate the pharmacological, physicochemical, phytochemical, microbial, and metabolomic attributes of &lt;i&gt;T. catappa&lt;/i&gt; leaves and fruits, along with in silico docking, to assess its antiepileptic potential.&lt;/p&gt;&lt;h3&gt;Methods&lt;/h3&gt;&lt;p&gt;Pharmacobotanical studies included macroscopic, microscopic, and physicochemical analyses. Heavy metal and microbial loads were assessed using Atomic Absorption Spectroscopy (AAS). Phytochemical profiling employed Gas Chromatography-Mass Spectrometry (GC-MS), Liquid Chromatography-Mass Spectrometry (LC-MS), and High-Performance Thin Layer Chromatography (HPTLC) to identify bioactive compounds. In silico docking (Schrödinger) targeted epilepsy-related receptors: dopamine (D2), serotonin (5-HT2A), Glutamate- N-methyl-D-aspartate (NMDA), and Gamma-aminobutyric acid (GABA_A).&lt;/p&gt;&lt;h3&gt;Results&lt;/h3&gt;&lt;p&gt;The medicinal potential of leaves and fruits derived from plants was evaluated through a thorough pharmacognostic and phytochemical analysis. Anatomical studies showed unique characteristics including lignified cells and trichomes. Initial analysis of phytochemicals revealed the presence of cardiac glycosides, flavonoids, and tannins. Using sophisticated analytical methods like LC-MS, important bioactive substances such punicalagin, gallic acid, ellagic acid, and quercetin were found. Their presence was further confirmed by HPTLC analysis, which showed minimal methodological deviation (&lt; 10%) and strong spectral correlation (&lt;i&gt;r&lt;/i&gt; = 0.824) for both leaves (ellagic acid: 0.2; gallic acid: 0.881; kaempferol: 0.073; quercetin: 0.3) and fruits (gallic acid: 0.37; ellagic acid: 0.81; rutin: 0.09). The visualisation of phenolic compounds was improved by derivatisation with 1-anilinonaphthalene-8-sulfonic acid (ANS). GC-MS profiling identified 49 phytochemicals in fruits And 42 in leaves, including a variety of terpenoids and phenolics. With the exception of trace amounts of lead (Pb) in fruits, heavy metal analysis verified safety, and microbiological contamination stayed below allowable bounds. According to molecular docking studies, rutin is a strong ligand with a high binding affinity to the NMDA (-6.227 kcal/mol) and dopamine D2 (-8.215 kcal/mol) receptors, suggesting that it has potential antiepileptic properties. The plant’s promise as a source of bioactive chemicals for neurological uses is supported by these findings.&lt;/p&gt;&lt;h3&gt;Conclusion&lt;/h3&gt;&lt;p&gt;A Rich bioactive substances were identified in the leaves and fruits of &lt;i&gt;Terminalia catappa&lt;/i&gt;, with rutin demonstrating great neuroprotective potential by binding to NMDA and dopamine D2. These results provide credence to its applic","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145211041","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development of Naringin Extract from Pomelo Peel Using Natural Deep Eutectic Solvent System as Green Technology for Antidiabetic Purpose: Box-Behnken Design Approach","authors":"Thongtham Suksawat,&nbsp;Natnicha Boonthaworn,&nbsp;Yanisa Junseedeechai,&nbsp;Tharita Kitisripanya,&nbsp;Savita Chewchinda,&nbsp;Chaiwat Aneklaphakij","doi":"10.1007/s12247-025-10084-7","DOIUrl":"10.1007/s12247-025-10084-7","url":null,"abstract":"<div><p>Diabetes remains a critical public health issue, driving demand for safe, affordable, and eco-friendly therapeutic alternatives. Pomelo peel, rich in the flavonoid naringin, shows promising antidiabetic potential. This study introduces a green extraction approach using natural deep eutectic solvents (NADESs), providing a safer alternative to conventional organic solvents. Among six Thai pomelo cultivars, Khao Nam Phueng contained the highest naringin content (4.28% w/w dry weight), significantly exceeding Khao Yai (2.74%w/w DW). Regional variation was observed, with peels from Nakhon Pathom yielding 4.01% DW versus 1.62% DW from Pathum Thani. A seasonal decline was noted, as early-harvest fruit had nearly twice the naringin of late-season samples. Initial NADES screening identified choline chloride: citric acid (1:1) as most effective, extracting 0.19%w/w DW naringin, followed by malic acid (0.18% w/w DW) and oxalic acid (0.13% w/w DW). Box-Behnken optimization improved the yield to 0.28% w/w. The extract exhibited potent <i>α</i>-glucosidase inhibition (IC₅₀=9.99 µg/mL) and strong antioxidant activity, as measured by the ferric reducing antioxidant power (FRAP) assay (192.3 TE/µg DW). Antiglycation activity was moderate (IC₅₀=104.75 µg/mL), lower than naringin standard (IC₅₀=36.77 µg/mL), likely due to solvent-matrix interactions. Predictive response surface models showed high accuracy, and the extract remained chemically stable over six months with minimal degradation (0.24–0.25% w/w DW). In conclusion, this study presents a scalable, green method to valorize pomelo peel waste into bioactive antidiabetic extracts. The findings support broader NADES applications and highlight cultivar and harvest timing as critical to maximizing recovery.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145211020","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Schweinfurthiamide as a Promising Anticancer Agent: Molecular Docking, Dynamics, and ADMET Insights Targeting MTHFD2","authors":"Maram B. Alhawarri","doi":"10.1007/s12247-025-10092-7","DOIUrl":"10.1007/s12247-025-10092-7","url":null,"abstract":"<div><p>Cancer remains a significant global health challenge, necessitating the Discovery of new therapeutic agents to overcome resistance and enhance treatment efficacy. Methylenetetrahydrofolate dehydrogenase 2 (MTHFD2), overexpressed in various cancers, has emerged as a promising molecular target. In this study, the natural alkaloid schweinfurthiamide, isolated from <i>Asparagus flagellaris</i>, was evaluated as a potential MTHFD2 inhibitor using comprehensive in silico techniques. This study provides the first computational evaluation of schweinfurthiamide, focusing on its potential inhibition of MTHFD2 through Molecular docking and 200 ns molecular dynamics (MD) simulations. Molecular docking revealed a binding free energy (Δ<i>G</i>_bind) of − 8.19 kcal/mol for schweinfurthiamide, comparable to DS44960156 (− 8.13 kcal/mol), with key hydrogen bonds formed at ARG43, ASN87, LYS88, and GLY310. 200 ns MD simulations demonstrated the structural stability of the schweinfurthiamide-MTHFD2 complex, supported by RMSD, RMSF, Rg, and hydrogen bond analyses, as well as advanced metrics including radial distribution function (RDF), isotropically distributed ensemble analysis (IDEA), dynamic cross-correlation maps (DCCM), and 3D principal component analysis (3D-PCA). MM-PBSA calculations revealed a binding energy of − 31.51 ± 0.11 kcal/mol, slightly more negative than DS44960156 (− 29.48 ± 0.11 kcal/mol), highlighting robust electrostatic and hydrophobic interactions. Drug-likeness and ADMET predictions confirmed schweinfurthiamide’s compliance with the Lipinski Rule, Pfizer Rule, and Golden Triangle, with favorable plasma protein binding (72.57%), higher fraction unbound (28.66%), and low metabolic liabilities, suggesting strong pharmacokinetic potential. These integrated findings demonstrate that schweinfurthiamide exhibits strong binding affinity, stability, and drug-like properties, supporting its role as a new MTHFD2 inhibitor with potential anticancer efficacy. Further in vitro and in vivo validation is necessary to confirm its therapeutic potential and clinical applicability. </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":"2025-09-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145210694","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"In Situ Evaluation of Drug Release and Water Ingress from 3D Printed Tablets Via Near Infrared and Raman Mapping","authors":"Zoë J Whalley,&nbsp;Tom Mills,&nbsp;Richard Greenwood,&nbsp;Patrick Wray","doi":"10.1007/s12247-025-10068-7","DOIUrl":"10.1007/s12247-025-10068-7","url":null,"abstract":"<div><p>3D printing of pharmaceuticals is an emerging field, which will have many exciting applications in the sphere of personalised medicine. The inherent advantages are that it offers manufacturing flexibility and platform versatility. However, there is limited mechanistic understanding of the dissolution behaviour of these novel dosage forms. In this study, Near Infrared (NIR) and Raman mapping techniques were used in conjunction with a custom dissolution flow cell to gather spatially resolved, real-time dissolution data of two geometries of 3D printed tablets. Caffeine was used as a model drug compound in a polymer filament. Two geometries of tablets were printed using Fused Filament Modelling (FFM); one solid tablet and one with vertical and horizontal channels. Chemical mapping facilitated simultaneous tracking of water ingress and drug distribution. The data obtained from this approach establishes a platform to assess the release mechanisms of many novel formulations and geometries of 3D printed pharmaceuticals to come.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 5","pages":""},"PeriodicalIF":2.7,"publicationDate":"2025-09-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145169986","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"An Innovative Dissolution Method for In-Vitro Release Assessment of Fixed-Dose Combination Tablets of Norfloxacin and Tinidazole","authors":"Pushpendu Gaurav,&nbsp;Sonal Dubey,&nbsp;Prashant Tiwari,&nbsp;Shreeshail Tumbagi","doi":"10.1007/s12247-025-10102-8","DOIUrl":"10.1007/s12247-025-10102-8","url":null,"abstract":"<div><h3>Purpose</h3><p>The fixed-dose combination of Norfloxacin and Tinidazole Tablets is extensively utilized for the treatment of diarrhea and amoebic dysentery in the southern region of the Asian subcontinent, particularly in India. However, the dissolution test procedure for the quality assessment of the finished product has not been documented in any reputable pharmacopoeia, such as USP, BP, Ph. Int.IP, Ph. Eur., and JP, nor has it been reported in any journal. Therefore, the objective of this study was to develop a robust dissolution method for assessing the in vitro release of Norfloxacin and Tinidazole in a fixed-dose combination.</p><h3>Method</h3><p>The dissolution profiles of Norfloxacin and Tinidazole Tablets were determined using four different dissolution media (Water, 0.1 N Hydrochloric Acid, Acetate Buffer pH 4.5, and Phosphate Buffer pH 6.8), two apparatuses (Basket and Paddle), and three different agitation speeds (50, 75, and 100 rpm).</p><h3>Results</h3><p>The method employing a paddle apparatus at 50 rpm in 900 mL of 0.1 N Hydrochloric Acid demonstrated superior hyper-discriminating capability with a Q30 value ≥ 90%. The selected method was successfully validated in accordance with the ICH Q2 (R2) guidelines for AMV, meeting all parameters of analytical method validation. </p><h3>Conclusion</h3><p>An in vitro release assessment method for the determination of Norfloxacin and Tinidazole was successfully developed and validated according to the revised guidelines for analytical method validation (ICH Q2 (R2)). Consequently, the developed method demonstrates robustness and ruggedness and can be employed for the quality assessment of Norfloxacin and Tinidazole Tablets prior to market release.</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":"2025-09-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145170431","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"PEGylated Liposomal Formulation of Alectinib Against Non-Small Cell Lung Cancer: Optimization, Characterization, Stability Assessment, In Vitro Cytotoxicity in A549 Cells and in Vivo Efficacy in C57BL/6 Mice","authors":"Saeem Ahmad,&nbsp;Shahnaj Bano,&nbsp;Nasr A. Emad,&nbsp;Iqra Zai,&nbsp;Shadab Alam,&nbsp;Mohd Aqil,&nbsp;Yasmin Sultana","doi":"10.1007/s12247-025-10098-1","DOIUrl":"10.1007/s12247-025-10098-1","url":null,"abstract":"<div><h3>Purpose</h3><p>Alectinib is a BCS Class IV drug with low solubility and permeability. The high dose of ALB (600 mg) can lead to several adverse effects, making it necessary to address these issues. This study aims to fabricate a PEGylated ALB-loaded liposome to deliver Alectinib through the pulmonary route to treat non-small cell lung cancer (NSCLC).</p><h3>Methods</h3><p>The PEGylated ALB-loaded liposomes were prepared and optimized using the solvent evaporation method and Box-Behnken design (BBD). A mixture of 0.3% (w/w) phosphatidylcholine, 0.175% (w/w) cholesterol, and 1.25% (w/w) PEG 4000 was dissolved in ethanol. Further, the RP-HPLC method was developed to quantify drugs. The formulation was characterized through various parameters: zeta, size and potential, TEM, SEM, %EE, %CDR, MTT, pharmacokinetics, and toxicity studies.</p><h3>Results</h3><p>PEGylated ALB-loaded liposomes had a particle size of 212.8 ± 1.751 nm, a PDI of 0.203 ± 0.034, and an entrapment efficiency of 85%. TEM and SEM images confirmed the morphology of the prepared liposomes. In addition, DSC and FTIR analysis showed drug and excipient compatibility. The drug release was 2.5-fold higher at pH 5.5 and 2.8-fold higher at pH 7.4, compared to drug suspension over 72 h. The IC₅₀ of ALB suspension and PEGylated ALB-loaded liposome were 2.55 ± 0.045 µM and 1.029 ± 0.0251 µM, respectively, by the A549 human lung cell line study. The ex vivo CLSM study showed that ALB penetrated deeper in lung tissue. The pharmacokinetic study showed that ALB from liposomes had higher T_1/2 (1.77 times) and AUC0-t (1.52 times) than ALB suspension in C57BL/6 mice. No significant changes were observed in the biochemical estimations or acute toxicity studies. Additionally, no notable changes were detected during the 6-month stability study.</p><h3>Discussion and Conclusion</h3><p>PEGylated ALB-loaded liposomes showed better drug release, improved cellular uptake, superior pharmacokinetics, good biocompatibility, and stability, showing their promise as an effective inhalational delivery system for ALB in treating NSCLC. Therefore, PEGylated liposomes appear to be a promising carrier for the inhalational delivery of ALB for NSCLC.</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":"2025-09-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145170439","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}