Drug metabolism and bioanalysis最新文献

{"title":"Optimizing Anxiety Management: Comparative Evaluation of Fast-Dissolving Clonazepam Tablets from Multiple Brands.","authors":"Komal Gupta, Tohfa Siddiqui, Vikram Sharma, Priyanka Singh, Manu Sharma","doi":"10.2174/0118723128413699251205181730","DOIUrl":"https://doi.org/10.2174/0118723128413699251205181730","url":null,"abstract":"<p><strong>Introduction: </strong>This study aimed to evaluate and compare the formulation characteristics of four commercially available clonazepam fast-dissolving tablet (FDT) brands in the Indian market and to assess their anxiolytic efficacy using behavioral animal models.</p><p><strong>Methods: </strong>Twenty tablets from each brand were analyzed for weight variation, friability, hardness, and disintegration time in accordance with pharmacopeial standards. Behavioral effects were evaluated in mice subjected to sleep deprivation-induced anxiety using the actophotometer, elevated zero maze, and light/dark box tests.</p><p><strong>Results: </strong>Among the tested brands, Zapiz showed the least weight variation (-0.38% to +0.28%) and the fastest disintegration (24 sec). Lonazep exhibited the lowest friability (0.657%), while Petril had the highest hardness (7.1 kg/cm²). In behavioral tests, all clonazepam FDTs significantly (p < 0.001) reduced anxiety-like behaviors compared with the sleep-deprived group. Zapiz consistently showed superior anxiolytic efficacy, reflected in improved locomotor activity, increased exploration of open quadrants in the elevated zero maze, and greater time spent in the light compartment.</p><p><strong>Discussion: </strong>While all brands met pharmacopeial standards, differences in formulation influenced disintegration and clinical potential. Zapiz demonstrated the most favorable balance of mechanical strength and rapid action, aligning with its superior anxiolytic effects in animal models. These findings emphasize the role of excipient selection and formulation design in optimizing FDT performance.</p><p><strong>Conclusion: </strong>Zapiz emerged as the best-performing brand, offering both pharmaceutical quality and significant anxiolytic benefits. Optimizing FDT formulations with novel superdisintegrants and validating findings through pharmacokinetic and clinical studies may further enhance therapeutic outcomes in anxiety management.</p>","PeriodicalId":521353,"journal":{"name":"Drug metabolism and bioanalysis","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-04-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147725573","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Smart Drug Delivery Solutions for Wound Management: Innovations and Implementation Barriers.","authors":"Priyanka Yadav, Sumit Kumar, Dinesh Kumar","doi":"10.2174/0118723128406161251208194426","DOIUrl":"https://doi.org/10.2174/0118723128406161251208194426","url":null,"abstract":"<p><p>Wound care remains a vital aspect of healthcare, as traditional treatments often struggle to ensure effective healing and prevent complications. Emerging drug delivery systems offer innovative solutions by improving therapeutic efficacy, minimizing side effects, and enabling precise delivery of drugs to the wound site. Techniques such as nanocarriers, hydrogels, microneedles, and bioengineered scaffolds have shown promise in managing chronic wounds, combating infections, and accelerating healing. These advanced approaches enable the integration of antimicrobial agents and stem cells to accelerate tissue regeneration. However, several challenges remain, including achieving biocompatibility, affordability, and scalability, as well as navigating regulatory requirements. This review delves into the progress of wound-targeted drug delivery technologies, emphasizing their transformative potential for wound management and the hurdles that must be addressed for broader clinical implementation.</p>","PeriodicalId":521353,"journal":{"name":"Drug metabolism and bioanalysis","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-03-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149013477","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Validation of a Method for Quantifying Elexacaftor, Elexacaftor-M23, Tezacaftor, Tezacaftor-M1, and Ivacaftor by HPLC-PDA.","authors":"Adriana H Sassone, Andrea S Saulo, Mario Sakson, Alejo G Dominas, Claudio Castaños, Paulo Cáceres Guido","doi":"10.2174/0118723128429458251126072109","DOIUrl":"https://doi.org/10.2174/0118723128429458251126072109","url":null,"abstract":"<p><strong>Introduction/objective: </strong>Cystic fibrosis is a genetic disease primarily treated with pharmacological modulators of the cystic fibrosis transmembrane conductance regulator (CFTR) protein, such as Elexacaftor, Tezacaftor, and Ivacaftor. This study developed and validated a method using Ultra-Fast Liquid Chromatography with Photodiode Array Detection (UFLC/PAD) to simultaneously quantify these three drugs and two of their main pharmacologically active metabolites (Ele-M23, Tez-M1) in plasma.</p><p><strong>Methods: </strong>A Shimadzu UFLC/PAD system was used with a Shim-pack VP-ODS column and an isocratic mobile phase (water:acetonitrile, 35:65). Itraconazole served as the internal standard for plasma calibration curves (0.1-10 μg/ml). Samples were processed by protein precipitation with methanol followed by centrifugation. Linearity, limit of quantification (LQ), precision, and accuracy were validated.</p><p><strong>Results: </strong>The limit of quantification for each calibration curve was 0.1 μg/ml. Intra-day precision (coefficient of variation [CV%]) ranged from 3.8% to 7.2%, and inter-day precision from 8.6% to 16.3%, meeting standard acceptance criteria. Retention times were 2.83 min for Ele-M23, 3.2 min for Elexacaftor, 5.6 min for Tezacaftor, 7.9 min for Tez-M1, 12.8 min for Ivacaftor, and 16.6 min for Itraconazole.</p><p><strong>Discussion/conclusion: </strong>The method is fast, reproducible, and suitable for the simultaneous quantification of CFTR modulators and their main metabolites in plasma. It is applicable in clinical laboratories for the therapeutic monitoring and optimization of cystic fibrosis pharmacotherapy.</p>","PeriodicalId":521353,"journal":{"name":"Drug metabolism and bioanalysis","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2026-01-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149013446","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pharmacokinetic Study: Liquid Chromatographic Assay of Apigenin and Analogues in Rat Plasma after Oral Administration.","authors":"Krishna Radheshyam Gupta, Sujata Bhadang, Ketki Mandawar, Kalyani R Thombre, Monali Dakhole, Milind J Umekar","doi":"10.2174/0118723128392798250807200527","DOIUrl":"https://doi.org/10.2174/0118723128392798250807200527","url":null,"abstract":"<p><strong>Introduction: </strong>Various methods are available for estimating apigenin, but no methods have been applied to the pharmacokinetic study of its prepared analogues, such as polymorphs, co-crystals, and complexes. This study aims to develop a method for the pharmacokinetic assessment of apigenin and its analogues using HPLC-UV.</p><p><strong>Methods: </strong>The internal standardization approach was utilized to analyse apigenin and its derivatives using UV detection at 340 nm, with chromatographic separation achieved under isocratic conditions on a Phenomenex C18 column (250 mm × 4.6 mm id, 5 μm). The optimal mobile phase consisted of a mixture of 0.3% formic acid and methanol (30:70, v/v) at a 1.5 mL/min flow rate. The system demonstrated a significant and well-resolved peak for apigenin and the internal standard quercetin, with retention times of 4.2 and 2.9 minutes, respectively. The calibration curve's linear regression analysis revealed a robust linear relationship over the concentration range of 2-10. 0 μg/mL; R² was determined to be 0.9995.</p><p><strong>Results: </strong>The findings indicated that the limit of quantification (LOQ) and limit of detection (LOD) were 0.0803μg and 0.0265μg, respectively. The pharmacokinetics in rats were evaluated using this approach. Cmax, the plasma concentration of apigenin and its analogs, was reached following an oral dose of 60 mg/kg/rat. The collected data were utilized to calculate all pharmacokinetic parameters.</p><p><strong>Discussion: </strong>The pharmacokinetic study revealed that apigenin analogues (A2-A7 and C1) significantly improved the oral bioavailability of apigenin (AP), as indicated by elevated Cmax and AUC_0-24 values relative to AP alone. Specifically, analogues A6 and A7 reached peak plasma concentrations more swiftly, implying a quicker onset of action, whereas A3 exhibited a delayed Tmax, reflecting slower absorption.</p><p><strong>Conclusion: </strong>Following oral administration of a single dose of apigenin, this method was deemed suitable for quantifying the levels of apigenin and its derivatives in rats. This HPLC methodology could be an effective tool for determining apigenin analogues in plasma due to its excellent sensitivity, accuracy, linearity, and specificity.</p>","PeriodicalId":521353,"journal":{"name":"Drug metabolism and bioanalysis","volume":"19 1","pages":"41-50"},"PeriodicalIF":0.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148564392","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Biomaterial-Based Drug Delivery Systems: Bridging Advances and Applications in Regenerative Medicine.","authors":"Irfan Ansari, Shikha Yadav, Shatrudhan Prajapati","doi":"10.2174/0118723128382078250818143502","DOIUrl":"https://doi.org/10.2174/0118723128382078250818143502","url":null,"abstract":"<p><p>In regenerative medicine, biomaterial-based medication delivery systems are a gamechanger because they allow for the restoration of function and the healing of damaged tissues. This study aims to examine the potential of synthetic and natural biomaterials for the delivery of medications and the regeneration of tissues. Our mission is to highlight the most recent developments in manufacturing techniques, drug delivery systems, and biomaterial design that have enhanced therapeutic benefits. Techniques such as stimuli-responsive carriers, targeted delivery methods, and diffusioncontrolled systems make use of biomaterials including chitosan, PLGA, and collagen. A comprehensive literature evaluation was conducted using search terms such as \"biomaterials AND drug delivery\" and \"regenerative medicine AND nanotechnology\" in PubMed, Scopus, and Web of Science. Microfabrication, lithography, and three-dimensional printing were some of the fabrication techniques covered in the included research. Their versatility has led to their application in the regeneration of many tissues, including skin, cartilage, bone, and nerves. Notable findings have shown that biomaterials can improve therapeutic efficacy by meeting challenges such as biocompatibility, immunogenicity, and stability. This is achieved by controlled drug release and targeted distribution. Biomaterials show great promise for improving tissue regeneration and medication delivery targeting, according to the research. Their treatments are more efficient, have fewer side effects, and promote faster recovery. However, future studies should focus on resolving some difficulties, such as immunological response, material stability, and clinical translation. The field of biomaterial science is having an impact on the future of regenerative medicine with innovations like injectable systems and smart biomaterials. Improved patient outcomes are largely attributable to biomaterials, and recent advances in gene therapy and precision biomaterials point to a future when personalized healthcare solutions are the norm. Research in the future should focus on finding new applications and removing current limitations so that their full therapeutic potential may be realized.</p>","PeriodicalId":521353,"journal":{"name":"Drug metabolism and bioanalysis","volume":"19 2","pages":"119-142"},"PeriodicalIF":0.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149130266","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Solubility Enhancement of Lumefantrine by Co-crystallization Method Using Amino Acids as Potential Coformers.","authors":"Sayani Bhattacharyya, S NagaJyothi, M Venkatesh, B Sarah Priyanka","doi":"10.2174/0118723128407464251028113602","DOIUrl":"10.2174/0118723128407464251028113602","url":null,"abstract":"<p><strong>Introduction: </strong>Lumefantrine, an anti-malarial drug, has a slow onset of action, erratic absorption, and low bioavailability owing to its poor water solubility. The present study explored the possibility of crystal engineering to improve the solubility of lumefantrine.</p><p><strong>Methods: </strong>Solvent drop grinding method was used to prepare the cocrystals of lumefantrine. Seven amino acids were selected as coformers. The best coformer was selected using Dunnett's test on solubility data. Solubility was estimated at pH 1.2, 4.5, and 6.8. The drug dissolution medium was determined based on Gibbs' free energy and the lowest dose-solubility ratio. The best cocrystals were evaluated for compatibility, physical, surface, and thermal properties, and stability studies.</p><p><strong>Results and discussion: </strong>The screening study of coformers revealed that isoleucine and valine were the best. Solubility studies at three different pHs revealed that the valine cocrystals of lumefantrine exhibited significantly greater solubility than the isoleucine-lumefantrine cocrystal. Nuclear magnetic resonance spectroscopy proved the formation of a non-covalent bond between valine and the drug. Surface characterization and thermal analysis revealed the conversion of the drug from crystalline to amorphous form, supporting the observed solubility enhancement of lumefantrine. The cocrystal of lumefantrine and valine in a 1:2 ratio showed the best performance, and its stability was also confirmed.</p><p><strong>Conclusion: </strong>It can be concluded that cocrystals of the drug and valine at a 1:2 stoichiometric ratio can serve as a promising cocrystal of the drug for the development of dosage forms with high bioavailability.</p>","PeriodicalId":521353,"journal":{"name":"Drug metabolism and bioanalysis","volume":" ","pages":"202-212"},"PeriodicalIF":0.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147849392","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Bioanalytical Method for Simultaneous Quantification of Itraconazole and Atorvastatin in Human Plasma.","authors":"Kunjan B Bodiwala, Flora J Pujara, Avinash D Khadela, Shrinivas S Savale","doi":"10.2174/0118723128401590250922065135","DOIUrl":"https://doi.org/10.2174/0118723128401590250922065135","url":null,"abstract":"<p><strong>Introduction: </strong>Drug-drug interactions between statins and azole antifungal agents, due to the inhibition of the CYP3A4 enzyme by antifungals, increase the risk of adverse effects from statins. Thus, a precise bioanalytical method for quantifying Itraconazole and Atorvastatin in human plasma is essential.</p><p><strong>Materials and methods: </strong>A liquid chromatographic method with protein precipitation and liquidliquid extraction was developed. Rosuvastatin calcium served as the internal standard. The method was validated per ICH M10 and USFDA guidelines and used to analyze spiked plasma samples.</p><p><strong>Results: </strong>The method effectively separated Itraconazole, Atorvastatin, and the internal standard without plasma interference. It achieved linear responses for each drug in the 0.1-3.0 μg/mL range with regression coefficients > 0.99. The RSD for within-run and between-run responses was < 5%, and the average recovery exceeded 64%.</p><p><strong>Discussion: </strong>The method accurately and precisely measured each analyte at the LLOQ level (0.1 μg/mL). A sensitive and selective bioanalytical HPLC method was developed, validated, and applied for the simultaneous estimation of Itraconazole and Atorvastatin in human plasma.</p><p><strong>Conclusion: </strong>This method ensures safe and effective co-administration of these medications in clinical practice, benefiting patient care.</p>","PeriodicalId":521353,"journal":{"name":"Drug metabolism and bioanalysis","volume":"19 1","pages":"79-93"},"PeriodicalIF":0.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148564396","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Lipid Nanoparticles: A New Frontier in Diabetes Treatment.","authors":"Bhawna Sharma, Anil Ahuja, Alok Pratap Singh, Amit Kumar Sharma","doi":"10.2174/0118723128404825250930064303","DOIUrl":"https://doi.org/10.2174/0118723128404825250930064303","url":null,"abstract":"<p><p>Lipid-based Nanoparticles (LNPs) have emerged as promising carriers for enhancing the efficacy, safety, and patient adherence of antidiabetic therapies. These systems, including Solid Lipid Nanoparticles (SLNs), Nanostructured Lipid Carriers (NLCs), liposomes, and nanoemulsions, exhibit unique physicochemical and pharmacokinetic advantages. Their biocompatibility, ability to protect labile drugs from degradation, and capacity to improve oral bioavailability make them especially valuable for delivering poorly soluble antidiabetic agents. This review comprehensively evaluates various lipid-based platforms, comparing their structural characteristics, drug loading efficiencies, release profiles, and targeting capabilities. SLNs offer excellent stability and controlled release, while NLCs improve drug loading and flexibility. Liposomes provide versatile encapsulation of both hydrophilic and lipophilic drugs, and nanoemulsions are ideal for enhancing rapid absorption. Collectively, these systems outperform conventional formulations by enhancing therapeutic outcomes and reducing systemic side effects. Current challenges, such as large-scale manufacturing and regulatory complexity, are discussed alongside future directions to inform translational research. Lipid-based nanoparticles represent a transformative strategy in the evolution of antidiabetic drug delivery.</p>","PeriodicalId":521353,"journal":{"name":"Drug metabolism and bioanalysis","volume":"19 1","pages":"29-40"},"PeriodicalIF":0.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148564345","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"<i>In Silico</i> Approaches to Predict Drug Metabolism: Pharmacophore Mapping and Virtual Screening of Heterocyclic Antidiabetic Agents.","authors":"Anuradha Mehra, Amit Mittal, Harmandeep Singh","doi":"10.2174/0118723128355478250711055544","DOIUrl":"https://doi.org/10.2174/0118723128355478250711055544","url":null,"abstract":"&lt;p&gt;&lt;strong&gt;Introduction: &lt;/strong&gt;An emerging impetus has driven the development of various small-molecule compounds for the management of type 2 diabetes. With the advent of novel heterocyclic derivatives, an expansive field of pharmacological endeavors has opened up to stimulate Glucokinase (GK) activation. Recent evidence has validated GK's legitimacy as a potential target for pharmaceutical intervention in diabetes. Glucokinase, an enzyme critical to maintaining blood glucose equilibrium, malfunctions in individuals with type 2 diabetes. A key component of this innovative approach is the use of heterocyclic derivatives to stimulate the GK enzyme, thereby serving as powerful pharmaceutical agents to improve type 2 diabetes management substantially.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Methods: &lt;/strong&gt;Maybridge's digital archive contained 53,000 compounds, known for their efficacy, which were subjected to thorough examination. From this extensive repository, 422 compounds with an indole core were identified. The structures generated by ChemBioDraw Ultra through this method were meticulously docked using AutoDock Vina 1.5.6. Online log P predictions were also made possible by the Swiss ADME algorithm. PKCSM software was used to assess the potential toxicity of the leading compounds.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Results: &lt;/strong&gt;Auto Dock Vina 1.5.6 was used to dock 422 indole derivatives. Compounds with the greatest binding affinity to glucokinase (GK) were found in the majority of the compounds. Based on the superior binding capabilities of the top eight molecules compared to Dorzagliatin (the standard drug) and MRK (the co-crystallized ligand). Following the enhancement of their pharmacokinetic profiles and compliance with Lipinski's rule of five, these eight candidates were further evaluated using ADMET analysis. As a result, AH249 displayed the greatest binding affinity with -11.5 kcal/mol. In contrast to the standard drugs Dorzagliatin (GKA) and MRK (cocrystallized ligand), AH249 showed no skin sensitization, AMES toxicity, or hepatotoxicity using PKCSM.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Discussion: &lt;/strong&gt;This research highlights the importance of in silico techniques in discovering antidiabetic medicines, as AH249 outperformed 421 other indole derivatives in terms of glucokinase affinity. According to SwissADME results, both compounds, AH249 and AH102, are drug-like. Analysis through molecular docking revealed interactions that can be tested and verified using experiments.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Conclusion: &lt;/strong&gt;There are 422 selected lead compounds containing an indole base in the 53,000 compound database that demonstrated the best activation of glucokinase. According to the findings of this computational drug design analysis, the most promising drug candidates deserve consideration for advancement to the in vitro stage, particularly AH249, which exhibits the greatest binding affinity, a favorable pharmacokinetic profile, and negligible toxicity. For a better understanding of the therapeutic im","PeriodicalId":521353,"journal":{"name":"Drug metabolism and bioanalysis","volume":"19 2","pages":"156-177"},"PeriodicalIF":0.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149130254","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Green Ecofriendly RP-HPLC Method for Estimating Bifonazole in Transethosomes: Application of Box Behnken Design.","authors":"Umeshkumar Patel, Vinayak Mastiholimath, Pallavi Chiprikar","doi":"10.2174/0118723128396503250715215742","DOIUrl":"https://doi.org/10.2174/0118723128396503250715215742","url":null,"abstract":"<p><strong>Introduction: </strong>The antifungal drug bifonazole, a substituted imidazole, exhibits broadspectrum in vitro action against Gram-positive bacteria, yeasts, moulds, dermatophytes, and dimorphic fungi.</p><p><strong>Methods: </strong>The analysis was carried out using a C18 reversed-phase column (250 mm × 4.6 mm, 5 μm particle size) maintained at a constant temperature of 25°C. Methanol and 0.1% trifluoroacetic acid were utilized as the mobile phase. Detection was performed at 256 nm with a UV detector, and quantification was achieved using the standard method. The method validation was carried out for various parameters as per ICH guidelines. The developed eco-friendly HPLC method was employed to assess the vesicle size and entrapment efficiency of the transethosomes. The greenness assessment tool was applied to assess the environmental sustainability of the proposed HPLC method.</p><p><strong>Results: </strong>The retention time was under 5 minutes, confirming the method's appropriateness for routine analysis. Linearity was observed in the concentration range of 5 to 25μg/ml, LOD and LOD were 2μg/ml and 8μg/ml respectively. Intraday and interday precision were within ICH limits (<2). The method was successfully used to analyse vesicle size (178nm) and entrapment efficiency (77.6±0.72%.) of the nanoformulation. The greenness assessment tool yielded a value of 0.71.</p><p><strong>Discussion: </strong>The developed method is both analytically sound and eco-friendly, making a significant improvement in the estimation of bifonazole. The developed method's LOD and LOQ values were sufficiently low to facilitate the detection and measurement of bifonazole in pharmaceutical formulations frequently utilized in research applications, thereby supporting its potential utility in analytical and research settings.</p><p><strong>Conclusion: </strong>Overall, this green, eco-friendly HPLC method is well-suited for routine analysis of bifonazole, demonstrating excellent cost-effectiveness, sensitivity, precision, and robustness.</p>","PeriodicalId":521353,"journal":{"name":"Drug metabolism and bioanalysis","volume":"19 2","pages":"178-190"},"PeriodicalIF":0.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149130268","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}