Drug metabolism and bioanalysis letters最新文献

{"title":"Rapid, Simple and Low-Cost Analytical Method Development for Quantification of Eltrombopag Olamine in Tablet dosage by UV Spectroscopy\u0000Method","authors":"Nandan Godani, Sanjay Sharma","doi":"10.2174/0118723128289305240404070703","DOIUrl":"https://doi.org/10.2174/0118723128289305240404070703","url":null,"abstract":"\u0000\u0000Eltrombopag Olamine is a drug used to treat thrombocytopenia, a disorder where blood platelet counts get lower and severe aplastic anemia. It serves as a thrombopoietin receptor agonist, which give rise to platelet production in the bone marrow\u0000\u0000\u0000\u0000The objective of this study is to develop a simple, specific, accurate, precise and\u0000economical Ultraviolet spectroscopy method to estimate the amount of Eltrombopag Olamine in\u0000bulk and tablet dosage form.\u0000\u0000\u0000\u0000The developed method was performed using methanol for identification and physicochemical characterization of the drug. The validation parameters like linearity, precision, accuracy, robustness limits of detection and quantitation, and specificity were assessed as per ICH\u0000Q2 (R2).\u0000\u0000\u0000\u0000The maximum absorbance wavelength (λmax) of the drug was found at 247 nm in\u0000methanol. The linearity was found in the concentration range of 2-14 μg/ml with regression\u0000equation y = 0.0619x - 0.0123 and r² = 0.999. The standard addition method was used to determine the accuracy of the developed method. The result was found in the % recovery range of\u000098-99%. The precision was done on λmax with respect to the parameters such as repeatability,\u0000intraday, and interday. The method was found to be precise as the % RSD value was found to be\u0000<2%. The detection limit value (LOD) and quantitation limit value (LOQ) were 0.0524 µg/ml\u0000and 0.1588 µg/ml, respectively.\u0000\u0000\u0000\u0000The developed method is simple, economical, accurate and selective. The developed method was adaptable for the estimation of Eltrombopag Olamine analysis in pharmaceutical dosage form and routine quality control laboratory.\u0000","PeriodicalId":72844,"journal":{"name":"Drug metabolism and bioanalysis letters","volume":"25 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140695088","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":"Stability Indicating Method Development and Validation for the\u0000Estimation of Bempedoic Acid by RP-HPLC","authors":"Mansi V. Chaudhari, Ujwala Chaudhari, J. K. Sahu, S. Bagade","doi":"10.2174/0118723128278080240404052506","DOIUrl":"https://doi.org/10.2174/0118723128278080240404052506","url":null,"abstract":"\u0000\u0000Bempedoic acid (BEM) belongs to a category of drugs known as\u0000Adenosine triphosphate-citrate Lyase (ACL) inhibitors. It is a prodrug with intracellular activation that is administered orally. Bempedoic acid is used to treat existing atherosclerotic\u0000cardiovascular diseases, mainly hypercholesterolemia.\u0000\u0000\u0000\u0000For the stability-indicating assay, the HPLC method was employed using a Kromasil 100-5-C8 column (100 mm × 4.6 mm), a UV detector set at 230 nm, and a mobile\u0000phase comprising a 70:30 v/v mixture of acetonitrile and 0.1% Orthophosphoric Acid (OPA)\u0000buffer. The method was operated at an ambient temperature with a flow rate of 1 mL/min.\u0000The method developed has been statistically validated according to ICH guidelines.\u0000\u0000\u0000\u0000The stability-indicating method was executed using a Kromasil 100-5-C8 (100 mm\u0000× 4.6 mm) column at a 1.0 mL/min flow rate. A mixture of acetonitrile and 0.1% Orthophosphoric Acid (OPA) buffer in a 70:30 v/v ratio made up the mobile phase. BEM's retention times were discovered to be 1.88 minutes each. The temperature was kept at room temperature. 234 nm was the ideal wavelength for BEM. According to ICH criteria, the approach developed has undergone statistical validation. BEM's % RSD was discovered to be\u00000.6, respectively. For BEM, the % recovery was determined to be 100.0%. Regression models for bempedoic acid yielded LoD and LoQ values of 3.3 and 10.1 g/mL, respectively. The\u0000method showed good reproducibility and recovery with a % RSD less than 2. Studies on\u0000forced degradation confirmed the method's capacity to indicate stability in the presence of\u0000stress conditions, such as acid, basic, peroxide, UV, heat, and humidity. Both the retention\u0000times and the run time were shortened.\u0000\u0000\u0000\u0000In accordance with ICH Q2 (R1) guidelines, this method was successfully tested with HPLC to confirm the chemical structures of newly produced degradation products of\u0000bempedoic acid.\u0000","PeriodicalId":72844,"journal":{"name":"Drug metabolism and bioanalysis letters","volume":"7 17","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140696218","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":"Stimulatory and Inhibitory Effect of Antipsychotic Agents Including Dopaminergic Neuro-depressants on Dopamine Formation from <i>p</i>-tyramine Mediated by Cytochrome P450 2D6.","authors":"Toshiro Niwa, Yuka Yamamoto","doi":"10.2174/2949681016666230914115021","DOIUrl":"10.2174/2949681016666230914115021","url":null,"abstract":"<p><strong>Background and objectives: </strong>The effects of antipsychotic agents, including dopamine D2 receptor blocking agents such as haloperidol, chlorpromazine, and sulpiride, and related compounds such as mirtazapine and sertraline, on dopamine formation from p-tyramine catalyzed by cytochrome P450 (CYP) 2D6.2 (Arg296Cys;Ser486Thr), CYP2D6.10 (Pro34Ser;Ser486Thr), and CYP2D6.39 (Ser486Thr) were compared with those of CYP2D6.1.</p><p><strong>Methods: </strong>Dopamine was determined by high-performance liquid chromatography, and Michaelis constants (K_m), maximal velocity (k_cat) values for dopamine formation, and inhibition constants (Ki) of psychotropic agents were estimated.</p><p><strong>Results: </strong>K_m values for all CYP2D6 variants decreased at lower concentrations, and kcat values for CYP2D6 variants except for CYP2D6.10 gradually increased with increasing haloperidol concentrations up to 5 or 10 μM. The k_cat/K_m values for all CYP2D6 variants increased at under 2.5 μM concentrations. Lower sertraline concentrations decreased K_m values for CYP2D6.10. Chlorpromazine at concentrations under 10 μM competitively inhibited the activities catalyzed by all variants; however, the activities for only CYP2D6.10 were increased by chlorpromazine at concentrations over 250 μM. Mirtazapine and sertraline similarly decreased dopamine formation among all variants except for CYP2D6.10. However, CYP2D6.10 inhibition by mirtazapine was weaker than that of the other variants, and sertraline decreased K_m values for CYP2D6.10.</p><p><strong>Conclusion: </strong>Haloperidol and sertraline, but not sulpiride, decreased the Km and/or increased kcat values for CYP2D6. The present findings suggest that Dopamine D₂ receptor-blocking agents and related compounds may polymorphically affect dopamine formation catalyzed by CYP2D6 in the brain.</p>","PeriodicalId":72844,"journal":{"name":"Drug metabolism and bioanalysis letters","volume":" ","pages":"1-6"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"10234830","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":"Determination of Efinaconazole in Plasma using Validated LC-MS/MS Technique.","authors":"Govindarajan Srinivasan, Asharani Indira Viswambaran","doi":"10.2174/0118723128348675241129100845","DOIUrl":"https://doi.org/10.2174/0118723128348675241129100845","url":null,"abstract":"<p><strong>Background: </strong>Efinaconazole is a topical antifungal medication that is effective against fungal infections of the toenails. In addition, due to its application on the skin, minimal systemic absorption takes place on the epidermic layer, which leads to the availability of lower-level concentration in the bloodstream. Although several reported methods in the literature describe the quantification of Efinaconazole using conventional techniques like HPTLC and HPLC, these methods lack the necessary sensitivity and selectivity to be directly applied for quantification in biological samples.</p><p><strong>Objective: </strong>Current research work aimed to develop a rapid, specific, selective, and sensitive method using plasma as one of the biological samples for quantification of Efinaconazole (EZ) in the presence of Fluconazole (FZ) as an internal standard by tandem mass spectrometry (LC-MS/MS).</p><p><strong>Methods: </strong>Chromatographic separation was achieved with a Thermo Hypersil Gold (100 mm x 2.1 mm, 1.9 μm) UPLC column using a mobile phase composed of 20% formic acid-water (0.1%) and 80% methanol. Liquid-liquid extraction (LLE) was employed for sample preparation. Efinaconazole and the internal standard were detected using the heated electrospray ionization (HESI) technique in parallel reaction monitoring (PRM) mode.</p><p><strong>Results: </strong>The developed method displayed a linearity range of 1 to 2000 pg/mL (0.001-2 ng/mL). Precision and accuracy for the lower limit of quantitation, low, mid, and high-quality control (QC) levels demonstrated a variance of less than 5% and an accuracy of 99 to 103%. Long-term stability was confirmed under various conditions, including storage in an auto-sampler, at room temperature, in a deep freezer, and after freeze-thaw cycles.</p><p><strong>Conclusion: </strong>The validated LC-MS/MS method has exceptional sensitivity, specificity, selectivity, rapid analysis, minimal requirement of sample quantity, wide dynamic range of concentration, robustness, and reproducibility, making it an indispensable tool, especially in fields of <i>in vitro</i> Permeation Testing (IVPT), <i>in vitro</i> Release Testing (IVRT), Pharmacokinetic, Toxicology, Clinical studies, and in drug development program for the quantification of Efinaconazole.</p>","PeriodicalId":72844,"journal":{"name":"Drug metabolism and bioanalysis letters","volume":"17 2","pages":"76-87"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143993688","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":"Evaluating the Influence of St. John's Wort on Naproxen Pharmacokinetics and Pharmacodynamics: A Drug Interaction Assessment.","authors":"Keerthana S Halumane, Sunil Kumar Kadiri","doi":"10.2174/0118723128356859250220063938","DOIUrl":"https://doi.org/10.2174/0118723128356859250220063938","url":null,"abstract":"<p><strong>Introduction: </strong>Rheumatoid arthritis (RA) is a chronic autoimmune disease which leads to pain and disability that may trigger anxiety and sleep disturbances. Naproxen and St. John's Wort concomitant administration in RA and anxiety raises the question of safety due to a potential drug interaction.</p><p><strong>Materials and methods: </strong>Albino Wistar rats were treated with naproxen and St. John's Wort for 30 days. The study involved the evaluation of safety of naproxen when combined with St. John's Wort by estimation of biochemical markers such as SGOT, SGPT, TG's, Creatinine, BUN, the extent of gastromucosal damage and estimation of AUC, t1/2 and Clearance using blood serum analysis with HPLC after 30 days of treatment. Histopathological studies were also conducted to determine the tissue architecture.</p><p><strong>Results: </strong>Elevated levels of hepatic markers SGOT, SGPT, TG, and gastro-mucosal damage with enhanced ulcer index were found in naproxen-St. John's Wort treated rats as compared to only naproxen treated rats. HPLC analysis displayed increased AUC and t1/2 of naproxen with decreased clearance in naproxen-St. John's Wort treated rats. Histopathological findings revealed tissue rupture and mucosal damage supporting the naproxen toxicity.</p><p><strong>Conclusion: </strong>Consulting a healthcare professional before combining St. John's Wort with naproxen is essential to assess potential risks, manage drug interactions, and ensure safety. Personalized advice helps optimize treatment outcomes for both rheumatoid arthritis and mental health.</p>","PeriodicalId":72844,"journal":{"name":"Drug metabolism and bioanalysis letters","volume":"17 3","pages":"137-148"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144047387","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":"Phosphodiesterase Inhibitors: A Therapeutic Approach for Arsenic- Induced Neurotoxicity.","authors":"Sonia Bhatt, Ajay Pal Singh, Sokindra Kumar","doi":"10.2174/0118723128343703250103063848","DOIUrl":"https://doi.org/10.2174/0118723128343703250103063848","url":null,"abstract":"<p><strong>Introduction: </strong>One of the world's most serious health issues is arsenic toxicity. Prolonged consumption of Arsenic contaminated water causes cognitive damage in the developing and adult brain. The present research investigated how sodium arsenite-induced neurotoxicity in SD rats was affected by rolipram, a PDE4 inhibitor, and vinpocetine, a PDE1 inhibitor.</p><p><strong>Methods: </strong>The arsenic concentration was determined, which indicates the accumulation of arsenic in blood. The low weight of the brain indicates the adverse effects on the brain, which was significantly improved by rolipram and vinpocetine. Biochemical markers (MDA, GSH, CAT, and SOD) and protein expression of CREB and P-CREB were studied in the hippocampal region of the brain.</p><p><strong>Results: </strong>The reduced antioxidant activity and elevated levels of inflammation were significantly improved by rolipram and vinpocetine administration. Additionally, rolipram and vinpocetine significantly increased the CREB and P-CREB expression in the hippocampi of rat brains.</p><p><strong>Conclusion: </strong>PDE4 and PDE1 inhibition in arsenic-induced neurotoxicity could be a novel approach and a new drug therapy for arsenic-induced neurotoxicity.</p>","PeriodicalId":72844,"journal":{"name":"Drug metabolism and bioanalysis letters","volume":"17 2","pages":"67-75"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144047483","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":"Interaction Risk: Green Tea Consumption in Patients Taking Alprazolam.","authors":"Darshan Gowda Bharathi Srinivasa, Sunil Kumar Kadiri","doi":"10.2174/0118723128366248250206081121","DOIUrl":"https://doi.org/10.2174/0118723128366248250206081121","url":null,"abstract":"<p><p>developing area of clinical interest is the potential interactions between drugs and herbal products. The potential risk of an interaction between green tea <i>(Camellia sinensis)</i> and alprazolam, a benzodiazepine that is commonly recommended for anxiety disorders, is discussed in this review. Numerous bioactive components included in green tea, such as caffeine and catechins, may alter the pharmacokinetics of alprazolam by altering its metabolism, excretion, or absorption. It has been shown that green tea affects the activity of cytochrome P450 enzymes, particularly CYP3A4, which is involved in alprazolam metabolism. Green tea may increase alprazolam plasma levels and increase the likelihood of adverse effects, such as drowsiness or motor incoordination due to CYP3A4 inhibition, which will be studied from the existing literature and pharmacological evidence. While definitive clinical trials are limited, the aim of the review is to emphasize the necessity for increased awareness among healthcare practitioners and patients regarding potential drug-herb interactions, especially in individuals utilizing anxiolytic drugs along with green tea consumption. Additional clinical investigations are necessary to formulate solid guidelines for the safe consumption of green tea by those using alprazolam.</p>","PeriodicalId":72844,"journal":{"name":"Drug metabolism and bioanalysis letters","volume":"17 3","pages":"104-113"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144047507","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":"Bioactive Formulation and Bulk Allopurinol and Lycopene Estimation by UV Spectroscopy.","authors":"Soumya Mishra, Ranjit K Harwansh, Rupa Mazumder","doi":"10.2174/0118723128322443240919025352","DOIUrl":"https://doi.org/10.2174/0118723128322443240919025352","url":null,"abstract":"<p><strong>Background: </strong>This study developed a UV spectrophotometric method for quantifying allopurinol and lycopene in both bulk and dosage forms, aiming for simplicity and practicality.</p><p><strong>Materials and methods: </strong>The method was developed and validated using methanol and lycopene in phosphate buffer saline at various pH levels (7.4, 6.8, 1.2, 5.5). Validation parameters included linearity, accuracy, precision, limit of quantification (LOQ), and limit of detection (LOD) according to ICH standards.</p><p><strong>Results: </strong>The method demonstrated high sensitivity and linearity over a concentration range of 4-20 μg/ml, adhering to Beer's law. The LOQ and LOD were 2-18 μg/ml and 2-6 μg/ml, respectively. Optimal absorbance wavelengths were 251 nm for lycopene and 471 nm for allopurinol. Calibration curves showed a high correlation coefficient (0.9994), indicating a strong linear relationship.</p><p><strong>Conclusion: </strong>The developed UV spectrophotometric method is effective, interference-free, and suitable for routine quality control, providing reliable measurements for allopurinol and lycopene.</p>","PeriodicalId":72844,"journal":{"name":"Drug metabolism and bioanalysis letters","volume":"17 2","pages":"56-66"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144013803","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":"The Role of Serotonin Modulators in Nicotine Reward and Reinforcement: A Conditioned Place Preference Investigation.","authors":"Rajkumar Tiwari, Bhawna Sharma, Rohit Pandey, Gaurav Kumar, Khushboo Bhardwaj","doi":"10.2174/0118723128348621250207070255","DOIUrl":"https://doi.org/10.2174/0118723128348621250207070255","url":null,"abstract":"<p><strong>Background: </strong>Nicotine addiction remains a significant public health challenge, driving the need for effective treatment strategies. While various pharmacological approaches have been explored, targeting neurotransmitter and neuromodulator systems offers a promising avenue. These systems, particularly those involving dopamine, play a pivotal part in interceding the rewarding effects of nicotine and the development of dependence. Serotonin, a pivotal neuromodulator, exerts a profound influence on dopamine pathways. By interacting with these pathways, serotonin can significantly impact the substantiating effects of nicotine. Understanding the intricate interplay between serotonin and dopamine systems is pivotal for developing new remedial interventions that effectively address the intricacies of nicotine dependence.</p><p><strong>Objective: </strong>The purpose of this research study was to examine the potential roles played by serotonin and its receptors in nicotine addiction by examining the involvement of serotonin modulators in the development of conditioned location preference in mice after exposure to nicotine.</p><p><strong>Methods: </strong>Mice were subjected to conditioned place preference (CPP) training with nicotine. After induction of CPP, the extinction session was given for the disappearance of CPP. There were a total of five groups, each having six animals that participated in the experiments, including group 1 (controls; normal saline), group 2 (nicotine A; 0.25 mg/kg), group 3 (nicotine B; 0.5 mg/kg), group 4 (nicotine C; 0.75 mg/kg), and group 5 (standard drug; fluoxetine). All drugs were given through the subcutaneous route. The treatment of serotonin modulators, i.e., fluoxetine (100 mg/kg), a selective serotonin reuptake inhibitor (SSRI), was given before the priming dose of nicotine, and the effect of the serotonin modulator was observed.</p><p><strong>Results: </strong>On day 17th, the CPP values were 390.16 s, 235.66 s, and 219.16 s, respectively, for nicotine A, nicotine B, and nicotine C in the black compartment groups; however, in the white compartment groups, the CPP values were 347.16 s, 588 s, and 549.66 s, respectively, for nicotine A, nicotine B, and nicotine C.</p><p><strong>Conclusion: </strong>Using the conditioned place preference (CPP) paradigm, we administered both drugs in a context in which their rewarding properties could be measured. Fluoxetine produced a significant but less robust CPP than nicotine. A single injection of fluoxetine was found to reduce nicotine-induced CPP. Moreover, the rewarding properties of nicotine were completely abolished in response to repeated fluoxetine injections. Long-term fluoxetine users may benefit more from the drug than those who have only used it occasionally or in small doses, according to the study.</p>","PeriodicalId":72844,"journal":{"name":"Drug metabolism and bioanalysis letters","volume":"17 3","pages":"114-120"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144051243","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":"Precision Formulation of Ocular Films for Eye Infections using Innovative Quality by Design Optimization.","authors":"Repollu Maddileti, Haranath Chinthaginjala","doi":"10.2174/0118723128364823250130094219","DOIUrl":"10.2174/0118723128364823250130094219","url":null,"abstract":"<p><strong>Aim: </strong>The current study focused on formulating ocular films embedded with levofloxacin for the treatment of conjunctivitis by employing the solvent-casting technique.</p><p><strong>Methods: </strong>These films were formulated with gelatin, Aloe barbadensis leaves mucilage (ABLM), and HPMC K4M to enhance the therapeutic effectiveness of levofloxacin. Various evaluations were carried out to confirm the quality and stability of the films, including assessments of thickness, weight uniformity, uniformity in LFX, % loss of moisture, and permeation. In vitro drug release studies were conducted to simulate ocular environments and analyze the precise release of LFX.</p><p><strong>Results: </strong>The films exhibited uniform thickness (0.15-0.19 mm) and weight (61.85-65.54 mg) with a consistent film area (0.502 cm²). LFX content ranged from 85.66% to 97.03%, with T-6 being the most uniform. Moisture loss was found to be 7.98-9.55%, and absorption (highest in T-6, i.e., 18.05%) increased with gelatin. LFX permeation peaked at 97.03% (T-6) in 24-h diffusion studies. T-8 demonstrated exceptional mucoadhesion (>10 h), and ANOVA confirmed the important influence of gelatin, ABLM, and HPMC K4M on LFX content (F-value: 129.91, p=0.0010).</p><p><strong>Conclusion: </strong>The study concluded that combining ABLM with HPMC K4M enabled consistent, diffusion-controlled release of LFX, offering an effective and sustained formulation for treating conjunctivitis.</p>","PeriodicalId":72844,"journal":{"name":"Drug metabolism and bioanalysis letters","volume":" ","pages":"88-98"},"PeriodicalIF":0.0,"publicationDate":"2024-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143400463","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}