Future Journal of Pharmaceutical Sciences最新文献

{"title":"Cost-effectiveness analysis of denosumab versus alendronate for improving bone mineral density in renal transplant recipients: a comparative study","authors":"Mona Alshahawey,&nbsp;May A Shawki,&nbsp;Sherihan Ahmed Sayed,&nbsp;Ahmad Elseasi,&nbsp;Lamia ElWakeel","doi":"10.1186/s43094-024-00719-w","DOIUrl":"10.1186/s43094-024-00719-w","url":null,"abstract":"<div><h3>Background</h3><p>Denosumab and alendronate had a positive impact on bone mineral density (BMD) preservation after kidney transplantation. However, the cost-effectiveness of these agents in the context of kidney transplantation remains largely unexplored. We have conducted a cost-effectiveness analysis to compare the cost and the clinical outcomes of adding subcutaneous (SC) 60 mg denosumab every 6 months vs. oral weekly 70 mg Alendronate, to the standard care therapy (vitamin D and calcium) in renal transplant recipients (RTRs). The impact of both drugs on BMD t-score improvement and fracture prevention was investigated. A decision-analysis model from a health care payer perspective was applied.</p><h3>Results</h3><p>The cost-effectiveness analysis has shown that alendronate add-on to the standard therapy was the most cost-effective regimen, in terms of BMD improvement and fracture prevention with an incremental cost-effectiveness ratio (ICER) of $154/patient/year. The one-way sensitivity analyses have delineated the change in cost-effectiveness when alendronate retail unit price was increased by 25% and 50%, or when denosumab retail unit price was decreased by 25% and 50%. The model was sensitive to the uncertainties (95% confidence interval) in the probabilities of fracture prevention and the probabilities of attaining the desired outcome.</p><h3>Conclusion</h3><p>The model suggests that oral once weekly alendronate add-on regimen to standard therapy seems to be substantially more cost effective than twice yearly SC denosumab in terms of BMD improvement and fracture prevention in RTRs. Longer time horizon models with longer follow-up periods for fracture risks and adverse events are warranted to validate these data.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-10-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00719-w","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142453099","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Formulation and characterization of 5-fluorouracil and metformin biodegradable nanospheres for treating colon cancer","authors":"K. Bharathi Priya,&nbsp;K. Kulathuran Pillai,&nbsp;C. N. Nalini,&nbsp;Ubaidulla Udhumansha","doi":"10.1186/s43094-024-00713-2","DOIUrl":"10.1186/s43094-024-00713-2","url":null,"abstract":"<div><h3>Background</h3><p>Cancer and diabetes mellitus are quite common diseases found together worldwide. A considerable amount of evidence is available for the rapid development and presentation of various types of cancer in the type 2 diabetes mellitus (DM2) population as compared with the population without diabetes. The objective of the study is to formulate and evaluate 5-fluorouracil (5-FU) and metformin (MET) nanoparticles (NPs) and to establish the characteristic features of the biodegradable NPs. 5-FU and MET NPs with chitosan as a biodegradable polymer were formulated by the ionotropic cross-linking method. 0.25 gm of MET and 0.25 gm of 5-FU were dissolved in 100 ml of distilled water, and stock solution was prepared. 5 ml of stock solution was slowly mixed into the chitosan solution to obtain the mixture of drugs and chitosan. The tripolyphosphate reserve liquid was dripped slowly into the chitosan solution with constant stirring until the opaline appearance was noticed in the mixture, then filtered, and dried. The NPs were evaluated for their physical properties and drug release kinetics. Cell proliferation assay was done using human colorectal carcinoma cell line (HCT 116).</p><h3>Results</h3><p>The formulation composed of 1.5 <i>w</i>/<i>v</i> of chitosan, 0.25 <i>w</i>/<i>v</i> of MET, and 5-FU had an average particle diameter of 198.7 nm. The polydispersity index was 0.757. Thermal and infrared spectroscopy results indicated the drugs and polymers selected for the formulation were unique without any identifiable interaction. The NPs were spherical in appearance, with numerous pours on the surface, which was evident when microscopically examined. Uniformity in drug release was observed, and the formulation demonstrated excellent release kinetics. HTC 116 cell line confirmed that the maximum percentage of cell death and minimum viability of cells were observed while using the combination of MET and 5-FU-NPs as compared to the pure MET or 5-FU alone.</p><h3>Conclusion</h3><p>MET and 5-FU-loaded chitosan NPs were found to have excellent physiochemical properties, particle size, and drug release from the polymer in a controlled manner. Half-maximal inhibitory concentration value (IC₅₀) of MET and 5-FU-NPs was found to be significantly less as compared to MET and 5-FU alone or the combination.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-10-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00713-2","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142452951","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Artesunate-driven autophagy: a shield against liver hypoxia/reoxygenation insult in rats via modulation of GLP1R, the chief metabolic kinase AMPK, mTOR, ULK1, P70S6K, cyclin D1, Akt, and GSK3β","authors":"Mai El-Sayed Ghoneim,&nbsp;Hanan S. El-Abhar,&nbsp;Dalaal M. Abdallah","doi":"10.1186/s43094-024-00704-3","DOIUrl":"10.1186/s43094-024-00704-3","url":null,"abstract":"<div><h3>Background</h3><p>Hepatic hypoxia/reoxygenation (H/R) insult is a critical issue in hepatic transplant and surgeries, profoundly influencing postoperative prognosis. One crucial pathomechanism in this condition is impaired autophagy flux, which disrupts liver homeostasis. Artesunate, an antimalarial drug, has shown potential in providing hepatoprotection against H/R injury; however, whether it can modulate disrupted autophagy to enhance hepatoprotection remains unclear.</p><h3>Purpose of the study</h3><p>Accordingly, we delved into the potential mechanism(s) through which artesunate modulates the autophagy process in a hepatic H/R injury model.</p><h3>Methods and results</h3><p>Rats were categorized into three groups, viz. sham operated, H/R, and artesunate-treated (50 mg/kg, i.p). Disease regression was evaluated microscopically, and molecular alternations were assessed biochemically using ELISA and western blotting techniques. Mechanistic analysis revealed that artesunate administration at reperfusion time significantly upregulated the gene expression of GLP1R protein expression of <i>p</i>-AMPK, accompanied by a downregulation in those of <i>p</i>-mTOR, and its target molecule <i>p</i>-ULK1, presenting the first trail to initiate autophagy. Additionally, artesunate reduced H/R-induced hepatic upregulated protein expression of <i>p</i>-mTOR/P70S6K cue, and cyclin D1 content, which positively correlated with the mTOR/P70S6K axis. Moreover, artesunate sharply upregulated active <i>p</i>-Akt, which in turn phosphorylated/inactivated GSK3β, a cascade that indirectly promotes autophagy. Consequently, artesunate increased the hepatic beclin-1 and LC3-II to further uphold its autophagic capacity. The hepato-therapeutic effectiveness of artesunate was further evidenced by reduced serum ALT and AST levels, along with diminished hepatic histopathological alterations.</p><h3>Conclusion</h3><p>Artesunate protected liver by triggering autophagy partly by modulating the GLP1R/AMPK/mTOR/ULK1, GLP1R/AMPK/mTOR/P70S6K, cyclin D1, and Akt/GSK3β trajectories providing a significant therapeutic potential in managing hepatic H/R insult.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00704-3","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142411382","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"α-Mangostin-phytosomes as a plausible nano-vesicular approach for enhancing cytotoxic activity on SKOV-3 ovarian cancer cells","authors":"Abdulmohsin J. Alamoudi,&nbsp;Shaimaa M. Badr-Eldin,&nbsp;Osama A. A. Ahmed,&nbsp;Serag Eldin I. Elbehairi,&nbsp;Mohammad Y. Alfaifi,&nbsp;Hani Z. Asfour,&nbsp;Gamal A. Mohamed,&nbsp;Sabrin R. M. Ibrahim,&nbsp;Ashraf B. Abdel-Naim,&nbsp;Hossam M. Abdallah","doi":"10.1186/s43094-024-00718-x","DOIUrl":"10.1186/s43094-024-00718-x","url":null,"abstract":"<div><h3>Background</h3><p><i>α</i>-Mangostin is a major xanthone in <i>Garcinia mangostana</i> L. (Clusiaceae) pericarps. It has promising anti-proliferative potential in different cancer cells; however, it has poor oral bioavailability. Phytosomes are used as a novel nano-based drug delivery system. The aim of this research was to enhance the anti-proliferative potency of <i>α</i>-mangostin by formulating it as <i>α</i>-mangostin-phytosome (<i>α</i>-M-PTMs) and assessing its impact on SKOV-3 ovarian cancer cells in comparison to pure <i>α</i>-mangostin.</p><h3>Results</h3><p>The size and entrapment efficiency of the proposed formulation were optimized using Box–Behnken statistics. The optimized formula was characterized using transmission electron microscope. The binding of <i>α</i>-mangostin to phospholipids was confirmed using Fourier-transform infrared (FTIR) spectroscopy. The optimized <i>α</i>-mangostin-phytosomes formula exhibited enhanced anti-proliferative activity with reference to raw <i>α</i>-mangostin. This was further substantiated by assessing the cell cycle phases that indicated an accumulation of SKOV-3 cells in the sub-G1 phase. Annexin-V staining revealed enhanced apoptotic activity in <i>α</i>-mangostin-phytosome-treated cells. This was associated with upregulation of CASP3 (Caspase-3), BAX (BCL2 Associated X, Apoptosis Regulator) and TP53 as well as down-regulation of BCL2 mRNA (B-Cell Leukemia/Lymphoma 2). Moreover, our data indicated enhanced ROS (Reactive oxygen species) production, cytochrome-C release, and disturbed MMP (mitochondrial membrane potential).</p><h3>Conclusion</h3><p>Encapsulation of <i>α</i>-mangostin in a phytosome nano-formula enhances its anti-proliferative effects in SKOV-3 cells via, at least in part, inducing mitochondrial apoptotic cell death.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-10-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00718-x","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142397564","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Effect of crude ethanolic seed extract from Mucuna pruriens on proliferation, apoptosis, and cell cycle arrest in gastric adenocarcinoma (AGS) cells","authors":"Arulvasu Chinnasamy,&nbsp;Vennila Jayaprakash,&nbsp;Deepakrajasekar Padmanaban,&nbsp;Niranjni Sekar,&nbsp;Rajasekar Valayapathi,&nbsp;Aarthi Azhagudurai,&nbsp;Sumathi Ethiraj","doi":"10.1186/s43094-024-00715-0","DOIUrl":"10.1186/s43094-024-00715-0","url":null,"abstract":"<div><h3>Background</h3><p>Gastric cancer is a prevalent form of malignancy among many common carcinoma cases globally. This study was designed to assess the anticancer potential of the crude ethanolic seed extract from <i>Mucuna pruriens</i> against the gastric cancer cell line (AGS). Various assays were employed to assess the anticancer properties, including examinations of cell viability, nuclear morphology, apoptosis using AO/EB staining, changes in mitochondrial membrane potential, lactate dehydrogenase activity, DNA fragmentation, and cell cycle arrest.</p><h3>Results</h3><p>The crude extract exhibited significant anticancer activity against the human gastric cancer cell line (AGS), as determined by the MTT assay, with an inhibition concentration (IC₅₀) of 600 µg/mL at 24 h. Distinct cellular and nuclear morphological changes were observed with different concentrations of crude ethanolic seed extract. The LDH release assay reveals cell death in AGS cells, as evidenced by a significant increase in the release of LDH enzyme. DNA fragmentation analysis and flow cytometry results indicate that the extract induces chromatin condensation, apoptotic cell death, and cell cycle arrest at the G0/G1 phase in the AGS cancer cell line. These results highlight the potential therapeutic advantages of <i>Mucuna pruriens</i> seed extract against gastric cancer cells.</p><h3>Conclusion</h3><p>This study could pave the way for identifying diverse natural bioactive compounds sourced from <i>Mucuna pruriens</i> seed, leading to the development of novel drug with potential anticancer properties.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-10-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00715-0","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142397565","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Simultaneous estimation of nebivolol hydrochloride and amlodipine besylate in human plasma employing an innovative HPLC chromatographic method","authors":"Kaveri T. Vaditake,&nbsp;Atul A. Shirkhedkar","doi":"10.1186/s43094-024-00716-z","DOIUrl":"10.1186/s43094-024-00716-z","url":null,"abstract":"<div><h3>Background</h3><p>This study developed and validated a simple, robust, and cost-effective RP-HPLC bioanalytical method for the determination of nebivolol hydrochloride (NBH) and amlodipine besylate (AMB) in human plasma. Briefly, NBH and AMB were extracted from plasma through protein precipitation using 5% formic acid and acetonitrile. Chromatographic separation was achieved using an Inertsil ODS-3 V column (150 mm × 4.6 mm, 5 μm) with a mobile phase composed of acetonitrile and buffer (40:60, v/v). The analysis was conducted using UV detection at 215 nm.</p><h3>Results</h3><p>The bioanalytical method demonstrated linearity for NBH (4.50–180.12 μg/mL) and AMB (3.50–140.06 μg/mL). It exhibited good selectivity and sensitivity, with LLOQ responses within ≤ 20% of the analyte signal. Accuracy and precision were within acceptable limits. The extraction recovery from human plasma showed a CV (%) of 1.15% for NBH and 1.35% for AMB, indicating consistent recovery rates. Stability studies on drug-spiked human plasma at LQC and HQC levels confirmed the stability of the drugs under various conditions.</p><h3>Conclusion</h3><p>The present bioanalytical method successfully quantified NBH and AMB simultaneously in plasma samples. It demonstrated suitability, supported by high recovery rates and low relative standard deviations. With its proven linearity, accuracy, and precision, this technique is well suited for drug identification in plasma samples.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-10-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00716-z","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142397580","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Assessment of IV albumin and ringer lactate on the acute oral toxicity of acetylsalicylic acid in albino rats","authors":"Inas Harb,&nbsp;Engy Medhat,&nbsp;Mai Samir,&nbsp;Shereen Abdel Fattah,&nbsp;Hend Ahmed Abdallah Badawy,&nbsp;Sarah Mohamoud Gamal,&nbsp;Hayam Ateyya","doi":"10.1186/s43094-024-00714-1","DOIUrl":"10.1186/s43094-024-00714-1","url":null,"abstract":"<div><h3>Background</h3><p>Despite the frequent inclusion of fluid therapy in the treatment of many conditions, there are limited studies available to provide an evidence-based specific recommendation for fluid therapy in acute drug toxicity. Salicylate toxicity is considered one of the common clinical problems. It is commonly associated with fatal complications and even can lead to death. The study was designed to investigate the effects of various IV fluid types as isotonic saline (NaCl 0.9%), Ringer lactate (RL), and albumin and their impact on acetyl salicylic acid (ASA) toxicity outcome in a rat model of acute salicylate toxicity.</p><p>Sixty male Albino rats were divided into 10 groups of 6 rats each. The first four groups were the control, saline, RL, and albumin groups. The fifth group received two doses of ASA solution orally, and the next five groups were treated with IV fluids as follows: saline-ASA, RL-ASA, albumin-ASA, RL + albumin-ASA, and saline + albumin-ASA. Upon completion of the study, spirometry, arterial blood gas analysis (ABG), and serum liver and kidney function tests were done on all groups. Furthermore, quantitative real-time polymerase chain reaction (PCR) was used to assess interleukin-6 (IL6), nuclear factor kappa beta (NF-k<i>β</i>), and beta-actin mRNA gene expression of histopathology and immunohistochemistry assessments were also performed on liver and kidney tissues.</p><h3>Results</h3><p>The results revealed the ASA group showed marked deterioration across all the investigated parameters. The groups that received saline and RL showed improvements in the following: respiratory rates, ABG, liver and kidney function, and histopathological findings.</p><p>The RL + albumin group did not show any improvements. The albumin group and the saline + albumin group showed variable responses, ranging from mild improvement to no improvement.</p><h3>Conclusions</h3><p>The saline and RL groups showed positive results; however, the RL + albumin group showed the worst outcomes. The inclusion of albumin did not appear to provide any extra benefits and produced varying results.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-10-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00714-1","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142383521","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Evaluation of the effect of pentoxifylline on the prevention of paclitaxel‑induced peripheral neuropathy in breast cancer patients: a randomized controlled study","authors":"Sondos S. Saleh,&nbsp;Diaa Eldin Moussa Sherif,&nbsp;Nagwa A. Sabri,&nbsp;May A. Shawki","doi":"10.1186/s43094-024-00691-5","DOIUrl":"10.1186/s43094-024-00691-5","url":null,"abstract":"<div><h3>Background</h3><p>Paclitaxel-induced peripheral neuropathy (PIPN) is one of the most common and debilitating toxicity. Up till now, no treatment or preventive medication is recommended by guidelines. Pentoxifylline has been found to prevent PIPN in animal models. This study aimed to evaluate the tolerability and efficacy of pentoxifylline in preventing PIPN. To our knowledge, this is the first clinical trial to evaluate the potential effect of pentoxifylline on the prevention of PIPN in breast cancer (BC) patients.</p><h3>Results</h3><p>A simple-randomized placebo-controlled study was conducted on 60 BC patients receiving weekly paclitaxel and either pentoxifylline 400 mg twice daily (n = 30) or placebo (n = 30) for 12 weeks. Only 55 patients completed the study. The main objective was the evaluation of the effect of pentoxifylline on the incidence of PIPN which revealed no significant difference between the pentoxifylline group (85%) and the placebo group (100%). Secondary objectives included time to develop grade 2 or 3 (TTG 2/3) PIPN, the patient’s quality of life (QOL), serum tumor necrosis factor-α (TNF-α) and malondialdehyde and the tolerability of pentoxifylline. The median TTG 2/3 PIPN was not reached in the pentoxifylline group compared to 77 days (95% confidence interval of 70.91 to 83.07) in the placebo group. However, the difference did not reach significance. The assessment of the impact of PIPN on QOL was performed at baseline and at weeks 4, 8 and 12 using Functional Assessment of Cancer Therapy/Gynecologic Oncology Group-Neurotoxicity (FACT/GOG-NTX) subscale. The magnitude of the worsening in the QOL was significantly lower in the pentoxifylline group than in the placebo group at weeks 4, 8, and 12 (<i>p</i> values = 0.028, 0.003, and 0.018, respectively). Analysis of the serum TNF-α and malondialdehyde revealed no significant differences between the groups. Pentoxifylline was safe, tolerable and did not affect paclitaxel toxicity.</p><h3>Conclusion</h3><p>Oral pentoxifylline (400 mg twice daily) did not decrease the incidence of PIPN. However, it improved patients’ QOL significantly.</p><p><i>Trial registration</i> Clinical Trials.gov, NCT05189535. Registered 4 October 2021, https://classic.clinicaltrials.gov/ct2/show/NCT05189535.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-10-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00691-5","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142397576","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"AQbD-novel strategy for analytical methods","authors":"Amruta Bairagi,&nbsp;Rutuja Kothrukar,&nbsp;Hemant Chikhale,&nbsp;Sreya Kosanam,&nbsp;Laxmikant Borse","doi":"10.1186/s43094-024-00706-1","DOIUrl":"10.1186/s43094-024-00706-1","url":null,"abstract":"<div><h3>Background</h3><p>Analytical Quality by Design (AQbD) has emerged as a pivotal paradigm in the realm of analytical chemistry, revolutionizing the approach to method development and validation. This innovative strategy integrates principles of Quality by Design (QbD) into analytical procedures, aiming to ensure the quality and robustness of analytical methods. The traditional approach to method development often involves a trial-and-error process, where parameters are adjusted until satisfactory results are obtained. However, this approach can be time-consuming, resource-intensive, and may lack reproducibility. AQbD addresses these challenges by providing a systematic framework for method development that emphasizes understanding the relationship between critical process parameters (CPPs) and critical quality attributes (CQAs).</p><h3>Discussion</h3><p>Analytical Quality by design (AQbD) presents an innovative approach to creating and validating analytical procedures, aimed at achieving quality measurements within the method operable design region (MODR). The QbD approach to analytical development is proactive, methodical, and risk-based significantly helps in acquiring an in-depth knowledge of how critical process parameters (CPPs) affect analytical performances, measured by critical quality attributes (CQAs). Experiment design (DoE) is an essential part of QbD, functioning to carry out the response surface analysis and screening process, and ultimately to enable the definition of the multidimensional region of the successful operating ranges of the CPPs, known as the design space (DS). The purpose of this article is to offer a thorough description of the QbD approach's method development process and its implementation in analytical procedure validation, to produce high-quality output, employing statistical analysis in conjunction with other designing tools.</p><h3>Conclusion</h3><p>Analytical Quality by design (AQbD) offers a systematic and proactive approach to method development in analytical procedures. By focusing on method resilience and incorporating statistical analysis and experiment design (DoE), AQbD enables the production of high-quality outputs, while minimizing out of trend (OOT) and out of specification (OOS) results. This innovative strategy enhances the reliability and reproducibility of analytical methods, ultimately leading to improved outcomes across various industries.</p></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-10-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00706-1","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142377203","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Computational quest, synthesis and anticancer profiling of 3-methyl quinoxaline-2-one-based active hits against the tyrosine kinase","authors":"Priyadarsini Raj,&nbsp;Abiseik Samuel,&nbsp;Anitha Kothandapani","doi":"10.1186/s43094-024-00711-4","DOIUrl":"10.1186/s43094-024-00711-4","url":null,"abstract":"<div><h3>Background</h3><p>Cancer is the predominant cause of mortality and a remarkable obstacle to elevating life anticipation in every nation on globe. Hepatocellular carcinoma (HCC), a hyper-vascular tumour, develops and progresses due to angiogenesis, a key feature of malignancy. HCC exhibits high neoangiogenic activity because of the need to generate new blood vessels for tumour growth.</p><h3>Methods</h3><p>The present work includes the construction of virtual library of ligands, virtual screening using the <i>Dockthor-VS server</i>, <i>ADMET</i> study using the <i>SwissADME</i> and <i>Osiris property explorer</i>. All the synthesized compounds were characterized by UV, IR, NMR and mass spectroscopic techniques. MTT assay was done to find the IC₅₀ of the synthesized compounds against <i>HepG2 cell line</i>. The more active compound found is subjected to the molecular dynamics simulation study.</p><h3>Results</h3><p>The ligands exhibited good docking scores, <i>ADMET</i> profile compared to the reference drugs. The target compounds were obtained with the satisfactory yields of 66–82%. The best activity against the <i>HepG2 cancer cell line</i> is observed with the compound SA-4 with IUPAC name (2-(3-methyl-2-oxoquinoxalin-1(2<i>H</i>)-yl)-<i>N</i>-(5-(3-nitrophenyl)-5<i>H</i>-thiazolo[4,3-<i>b</i>] [1,3,4] thiadiazol-2-yl) acetamide). The experimental results obtained show correlation with the in silico results. MD simulation of the compound SA-4 indicates the moderate stability of the protein-ligand complex in real time environment.</p><h3>Conclusion</h3><p>The results obtained suggest that the compound SA-4 has the potential to be a promising anticancer agent effective against the <i>VEGFR-2</i> and <i>FGFR-4</i>.</p><h3>Graphical abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4,"publicationDate":"2024-10-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00711-4","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142368724","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}