https://www.syncsci.com/journal/JPBR/issue/feedJournal of Pharmaceutical and Biopharmaceutical Research2024-03-14T18:44:03+08:00Snowy Wangsnowy.wang@syncsci.comOpen Journal Systems<p><a title="Registered Journal" href="https://www.reviewercredits.com/user/j-pharm-biopharm-res" target="_blank" rel="noopener"><img class="journalreviewercredits" src="/journal/public/site/images/jasongong/Logo_ReviewerCredits-journal.jpg" alt="ReviewerCredits" align="right"></a><strong>Journal of Pharmaceutical and Biopharmaceutical Research (JPBR)</strong> (ISSN:2630-533X) is an open access, continuously published, international, refereed journal. The aim of the journal is to provide the authors a timely and peer reviewed process for evaluation and publication of their manuscripts. All articles submitted to JPBR will undergo a rigorous double-blind peer review, and all published articles can be downloaded and read for free. JPBR will pay wide attention to the trends in related fields and insist on publishing original research work of highest quality.</p> <p><strong>JPBR</strong> publishes high quality original research work, reviews, and short communications in the following areas:<br><strong>Pharmaceutical Sciences:<br></strong>• Pharmaceutics<br> • Pharmacology and Toxicology<br> • Medicinal Chemistry<br> • Physical Pharmacy<br> • Pharmaceutical Analysis<br> • Chromatography and Hyphenated Techniques<br> • Pharmacognosy and Phytochemistry<br> • Nanotechnology for Pharmaceutical Drug Formulations<br><strong>Biopharmaceutical Sciences:</strong> <br> • Biochemistry<br> • Biotechnology<br> • Molecular Biology<br> • Immunology and Microbiology</p>https://www.syncsci.com/journal/JPBR/article/view/JPBR.2023.01.003A novel role of NK3 receptor signaling in bipolar disorder2024-03-14T18:44:03+08:00Wei Zhang19558916709@163.comLinyao Yuyulinyao98@163.comYaoqin Shisyqly7970202@163.comYingtian Zhangnaitgniy@163.comMin Xuxx13863355194@163.comYang Xuyaoliyangxu@126.comChunmei Lilichunmei@luye.comJingwei Tian17854119865@163.com<p><strong>Objective: </strong>Bipolar disorder (BD) affects more than 1% of the global population with limited therapeutic options. The neurokinin B (NKB)-neurokinin B receptor (NK3R) is involved in a variety of emotional activities. This study explored the role of NK3 receptor signaling in bipolar disorder.<br><strong>Materials and methods: </strong>In this study, a model of intracerebroventricular (ICV) administration of OUA-induced BD was used to investigate the possible role of NK3R signaling in BD. The involvement of NK3R in the expression of OUA-induced BD was assessed by genetically knocking down the NK3R-encoding <em>TACR3</em> gene with shRNA approach in the hippocampus and systemic administration of a NK3R antagonist ESN364,. Biochemical techniques were used to examine the NK3R-associated signaling changes and the oxidative stress parameters in the hippocampus of BD rats.<br><strong>Results: </strong>The NK3R expression level was elevated in the hippocampus BD rats. Both <em>TACR3</em> knockdown in the hippocampus and ESN364 treatment reversed the manic-like and depression-like behaviors in BD rats Inhibition of the NK3R signaling reversed oxidative stress-induced damage via upregulating the BDNF signaling pathway in the hippocampus.<br><strong>Conclusion: </strong>These results demonstrated that NK3R signaling plays a key role in the pathogenesis of BD and that pharmacological antagonist of NK3R such as ESN364 could represent a novel therapeutic strategy for the management of BD.</p>2024-03-14T14:22:47+08:00Copyright (c) 2024 Wei Zhang, Linyao Yu, Yaoqin Shi, Yingtian Zhang, Min Xu, Yang Xu, Chunmei Li, Jingwei Tianhttps://www.syncsci.com/journal/JPBR/article/view/JPBR.2023.01.002Network pharmacology-based prediction for therapeutic mechanism of FuYueKang Lotion on acute eczema2023-11-01T11:53:05+08:00Xiaowen Wenxiao8610@126.comShaokang Cui632016842@qq.comMinzhi Liliminzhi216@163.comYongping Zhengzhengyp_TCM@163.comHaoyou Xuxuhaoyou@gzucm.edu.cn<p><strong>Objective</strong><strong>:</strong> Fuyuekang Lotion (FYKL) is an improved traditional Chinese medicine (TCM) prescription widely used to treat acute eczema (AE). However, the mechanism of action remains unclear. This study aimed to explore the therapeutic mechanism of FYKL in AE.<br><strong>Methods:</strong> We revealed the underlying mechanism by utilizing a network pharmacology approach, molecular docking studies, and in vitro verification. The active compounds in FYKL were identified, and their targets were predicted. These targets were subsequently mapped to a component-target interaction network, with their therapeutic mechanisms predicted through Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses. Molecular docking was used to verify protein-binding efficacy. Potential key targets of FYKL against AE were further confirmed via reverse transcription quantitative polymerase chain reaction (RT-qPCR).<br><strong>Results: </strong>The study identified 59 potential active compounds of FYKL, with quercetin, luteolin, and gallic acid suggested as critical active ingredients. Our findings suggest that these ingredients could exert their effects mainly by modulating the inflammatory immune response and promoting epidermal repair. FYKL was found to be a multi-target, multi-component drug that could potentially regulate the inflammatory immune response in AE through numerous pathways.<br><strong>Conclusions:</strong> The findings from this study provide a scientific basis for further research into the therapeutic effects and mechanisms of FYKL in treating AE, underscoring the potential of TCM in modern therapeutics.</p>2023-11-01T11:53:05+08:00Copyright (c) 2023 Xiaowen Wen, Shaokang Cui, Minzhi Li, Yongping Zheng, Haoyou Xuhttps://www.syncsci.com/journal/JPBR/article/view/JPBR.2023.01.001Exploring the mechanism of three herb pairs for the treatment of atherosclerosis through network pharmacology and molecular modeling2023-04-20T08:22:08+08:00Minjun Wangwangmin4869@126.com<p><strong>Background:</strong> Atherosclerosis (AS) is one of the leading causes of cardiovascular diseases. The traditional China herb pairs such as Huanglian-Gualou, Honghua-Taoren, and Suhexiang-Bingpian showed therapeutic effects on AS by clearing heat and resolving phlegm, invigorating blood and removing blood stasis, as well as aromatic resuscitation, respectively. However, the common and specific mechanisms of these pairs against the same disease are elusive.<br><strong>Objective:</strong> This study aimed to explore the molecular mechanisms of 3 herb pairs treating AS by network pharmacology, molecular modeling and mechanism experiments.<br><strong>Methods:</strong> The components and their corresponding targets of 3 herb pairs, as well as AS-related targets, were collected from multiple databases and literature. Then the protein-protein interaction network was built to identify the key components and targets associated with AS. The pathway enrichment analysis using KEGG was carried out for analyzing the common mechanisms of 3 herb pairs against AS. Finally, the binding modes of the key components and targets were analyzed by molecular docking and molecular dynamic simulation.<br><strong>Results:</strong> The PPI network indicated that the common targets of 3 herb pairs focused on four pathways, including regulated vascular shear stress, TNF, ARE-RAGE, and IL-17 pathways. The molecular docking analysis indicated that the key component quercetin showed highest docking score with PTGS2 in comparison to other targets. Molecular dynamics simulations revealed that quercetin stably anchored to the active pocket of PTGS2 by forming hydrogen bonds with Thr175, Asn351, and Trp356.<br><strong>Conclusion:</strong> The molecular mechanism of Huanglian-Gualou, Honghua-Taoren, and Suhexiang-Bingpian against AS was preliminarily expounded, and we wish to provide a theoretical instruction for clinical treatment of AS.</p>2023-04-19T16:45:35+08:00Copyright (c) 2023 Minjun Wanghttps://www.syncsci.com/journal/JPBR/article/view/JPBR.2022.02.005LPM570065 ameliorates anxiety-like and depressive-like behaviors in CUMS rats through regulating DNA methylation in hippocampus2023-04-17T16:06:01+08:00Shengmin Ji474475908@qq.comChunmei Lilichunmei@luye.comWei Zhang19558916709@163.comLinyao Yuyulinyao98@163.comYue Yangytuyy1203@163.comYaoqin Shisyqly7970202@163.comHongbo Wanghongbowangyt@163.comJingwei TianTianjingwei618@163.com<p><strong>Objective</strong>: This study aims to analyze the effects and underlying mechanisms of LPM570065 on behavioral phenotypes in rats with generalized anxiety disorder (GAD).<br><strong>Methods</strong>: The chronic unpredictable mild stress (CUMS) rats were used to observe the results of LPM570065. Total 72 male Sprague Dawley rats were divided into control, vehicle (0.5% CMC-Na), LPM570065 (32 mg/kg) and diazepam (3 mg/kg) groups, 12 rats in each group. Anxiety-like behaviors of rats were observed by elevated zero maze test and novelty-suppressed feeding test. Depressive-like behaviors of rats were detected by forced swimming test. DNA methylation in hippocampi of rats were measured by reduced representation bisulfite sequencing (RRBS). In hippocampi of rats, expressions of DNA methyltransferase (DNMT) 1 and DNMT3a proteins were measured by western blot, and density of dendritic spines was observed by Golgi staining.<br><strong>Results</strong>: Compared with the control group, the weights of rats were obviously decreased (p < 0.001) and the rats showed anxiety-like and depressive-like behaviors (p < 0.001) in the vehicle group. Compared with the vehicle group, the weights of rats were significantly increased (p < 0.001) and the anxiety-like and depressive-like behaviors were improved (p < 0.001) in the LPM570065 group. The results of RRBS showed that there were 49964 promoters showed hypermethylation in the LPM570065 treatment rats contrasted to the vehicle treatment rats. In addition, these promoters were enriched in signal transduction and immune function. Furthermore, the expressions of DNMT1 and DNMT3a were significantly decreased, the density of dendritic spines was significantly increased in hippocampi of LPM570065 treatment rats compared with the vehicle treatment rats.<br><strong>Conclusions</strong>: LPM570065 ameliorates anxiety-like and depressive-like behaviors in CUMS rats, and its mechanism is possible associated with downregulating DNA methylation in hippocampus.</p>2023-04-17T15:55:48+08:00Copyright (c) 2023 Shengmin Ji, Chunmei Li, Wei Zhang, Linyao Yu, Yue Yang, Yaoqin Shi, Hongbo Wang, Jingwei Tianhttps://www.syncsci.com/journal/JPBR/article/view/JPBR.2022.02.004(E)-2-Benzylidenecyclanones: Part XVII. An LC-MS study of microsomal transformation reactions of (E)-2-[(4'-methoxyphenyl)methylene]-benzosuberon-1-one: A cyclic chalcone analog2023-03-26T21:44:29+08:00Fatemeh Kenarikenari.fatemeh@pte.huSzilárd Molnármolnar.szilard@pte.huZoltán Pintérzoltan.pinter61@gmail.comSobhan Bitarafsobhanbitaraf34@gmail.comPál Perjésipal.perjesi@gytk.pte.hu<p>Biotransformation of the antiproliferative (<em>E</em>)-2-[(4’-methoxyphenyl)methylene]-benzosuberon-1-one (<strong>2c</strong>) was studied using rat liver microsomes. As a result of the CYP-catalyzed transformations, one monooxygenated (<strong>2c+O</strong>) and the demethylated (<strong>2c-CH<sub>2</sub></strong>) metabolites were identified by HPLC-MS. (<em>E</em>)-2-[(4’-methoxyphenyl)methylene]-benzosuberon-1-ol, the expected product of rat liver microsomal carbonyl reductase, was not found in the incubates. Microsomal GST-catalyzed reaction of the compound resulted in formation of diastereomeric GST-conjugates. Under the present HPLC conditions, the diastereomeric adducts were separated into two chromatographic peaks (<strong>2c-GSH-1</strong> and <strong>2c-GSH-2</strong>).</p>2023-03-22T13:53:43+08:00Copyright (c) 2023 Fatemeh Kenari, Szilárd Molnár, Zoltán Pintér, Sobhan Bitaraf, Pál Perjésihttps://www.syncsci.com/journal/JPBR/article/view/JPBR.2022.02.003How antidepressants affect the cerebral ischemic injury and ischemic stroke2023-02-17T14:25:35+08:00Xiaohui Sun1301374138@qq.comTian Wangbluewt2000@163.comLin Zhoujoe199707@163.comYawen Yuyyw0829@163.comZhaofeng Lium17852656495@163.comRunchen Maceltics5920@163.comFenghua Fufenghua@luye.com<p>Ischemic stroke is the main cause of long-term disability and death worldwide. Studies have pointed out that antidepressants not only can be used to treat depression, but also promote nerve regeneration, nerve plasticity, and recovery of nerve function after stroke. Some evidences indicated that antidepressants have beneficial effects on ischemic stroke. At the same time, there are also risks in treatment process. The mechanisms of the effects of antidepressants on ischemic stroke are complicated and rarely reported. This review summarizes the roles of antidepressants in patients and animal models of stroke, the possible mechanisms of antidepressants against brain injury induced by stroke, and the risks and challenges of antidepressants treatment in patients with ischemia.</p>2023-02-17T14:19:00+08:00Copyright (c) 2023 Xiaohui Sun, Tian Wang, Lin Zhou, Yawen Yu, Zhaofeng Liu, Runchen Ma, Fenghua Fuhttps://www.syncsci.com/journal/JPBR/article/view/JPBR.2022.02.002Therapeutic efficacies of nano carriers in delivering drugs2022-10-23T09:55:02+08:00Bailey Kruegereditor@syncsci.comTaylor Fraziereditor@syncsci.comSheila Galbreatheditor@syncsci.comTarun Goswamitarun.goswami@wright.edu<p>The drug release rates of poorly soluble medications such as doxorubicin has been investigated in this paper. Since the drug was fixed, different carriers used to deliver it and their release rates compiled from literature were evaluated in this paper. Even though targeting of drugs is very important in drug delivery, it is not within the scope of this paper. However, functionalization of the carrier may provide this benefit, those constructs are included for comparison in terms of hybrid constructs. Dendrimer, micelles and hybrid constructs used in the delivery of doxorubicin compared in this paper with respect to carrier size and drug loading. Assuming that the dissolution follows a slow release, 40-50% of the drug in the phase I representing a sudden or the burst release, followed by a steady release of 50-60% of the drug in phase II, not all the carriers and their sizes exhibited this behavior. Carriers and hybrid constructs 38nm size were more effective where phases I and II observed, however, as the size decreased to 34 nm or increased above 40nm, minimal release occurred meaning the carriers were too big to penetrate the vasculature permeability. Nano-carriers, dendrimers, micelle, hybrid dendrimers and micelles were found to be effective with the carrier manufacturing, generation, polymer, molecular weight of the carrier and other parameters. The release rate of doxorubicin was found to be effective with dendrimers together with hybrid dendrimer exhibiting a bilinear behavior. Micelles 20nm were more effective representing 60% of release in 10 hours followed by additional 25% in 35 hours exhibiting a bilinear behavior. Size greater than 20nm resulted in slow release reaching less than 10 to 40% of drug. Several drugs exhibited multiple slopes in their kinetics when micelle was used. The therapeutic efficacy of hybrid micelle was superior to other nano-carriers.</p>2022-10-17T12:03:21+08:00Copyright (c) 2022 Bailey Krueger, Taylor Frazier, Sheila Galbreath, Tarun Goswamihttps://www.syncsci.com/journal/JPBR/article/view/JPBR.2022.02.001Effect of experimental hyperglycemia on intestinal elimination and biliary excretion of ibuprofen enantiomers in hyperglycemic rats2022-10-04T13:36:51+08:00Hawsar Othman Mohamedhawsar.mohamed@univsul.edu.iqAttila AlmásiAttila.almasi@aok.pte.huPal Perjesipal.perjesi@gytk.pte.hu<p>Diabetic complications are mostly due to hyperglycemia. Hyperglycemia is reported to be associated with oxidative stress. It can result in changes in the activities of drug-metabolizing enzymes and membrane-integrated transporters, which can modify the fate of drugs and other xenobiotics. An <em>in vivo</em> intestinal perfusion model was used to investigate how experimental hyperglycemia affects intestinal elimination and biliary excretion of ibuprofen enantiomers in the rat. Experimental diabetes was induced by intravenous (i.v.) administration of streptozotocin. The intestinal perfusion medium contained 250 µM racemic ibuprofen. A validated isocratic chiral HPLC method with UV detection was developed to determine the amount of the two enantiomers in the intestinal perfusate and the bile. The results indicated that experimental diabetes doesn’t cause a statistically significant difference in the disappearance of ibuprofen enantiomers from the small intestine. Analysis of the bile samples detected only the (<em>S</em>)-IBP enantiomer. Excretion of the ibuprofen enantiomer to the bile decreased in experimental diabetes. The observed changes can affect the pharmacokinetics of drugs administered in hyperglycemic individuals.</p>2022-10-04T13:34:02+08:00Copyright (c) 2022 Hawsar Othman Mohamed, Attila Almási, Pal Perjesihttps://www.syncsci.com/journal/JPBR/article/view/JPBR.2022.01.004Effectiveness of mesoporous bioglass in drug delivery2022-06-27T14:28:37+08:00Sheila Galbreatheditor@syncsci.comBailey Kruegereditor@syncsci.comTaylor Fraziereditor@syncsci.comTarun Goswamitarun.goswami@wright.edu<p>Since the invention of bioactive glass 50 years ago, it has become a versatile material used in healthcare in a variety of applications and compositions. Bioactive glass has shown superior capabilities of drug delivery compared to traditional carriers. For example, time-released medications are less likely to reach toxic levels, while delivering a specific, therapeutic dose to a localized area. The objective of this paper is to investigate the properties and effectiveness of mesoporous bioglass (MBG) as a drug delivery carrier. A literature review of various polymer coated 45S5 Bioglass<sup>®</sup> loaded with vancomycin was analyzed to determine their drug release response. Since MBG continues to be a preferred carrier with numerous combinations; size, coating, doped with ions, medications, and other physical conditions, there is a need to understand more fully their effectiveness. For a given loading efficiency of 5-15% the burst release % for day 1 remained 15-30% for given surface area, pore volume and pore size of 3.5 to 5 nm. The mechanical properties summarized in this paper are compared with the drug release kinetics. In general, for a given fracture toughness and compressive strength, the ratio of Young’s modulus to bending strength around 250 determined poor apatite mineralization resulting in slow release. As this ratio increased the apatite mineralization and dissolution rate increased. Doping MBG with ions enhanced the drug efficacy to treat a particular condition, for example, silver. Polymer coated MBG exhibited slower dissolution rate than uncoated MBG. Dissolution time increased with the drug loading rate, drying time of the coating, multi-layer coats of drug and polymer for the drug studied in this paper to more than 50%.</p>2022-06-27T14:27:00+08:00Copyright (c) 2022 Sheila Galbreath, Bailey Krueger, Taylor Frazier, Tarun Goswamihttps://www.syncsci.com/journal/JPBR/article/view/JPBR.2022.01.003Transdermal drug delivery systems: Analysis of adhesion failure2022-06-13T14:24:14+08:00Zachary Brookseditor@syncsci.comTushar Goswamieditor@syncsci.comAmy Neidhard-Dolleditor@syncsci.comTarun Goswamitarun.goswami@wright.edu<p>The most critical component of the TDDS is the adhesive, which is responsible for the safety, efficacy and quality of the patch. For drug delivery to successfully occur, the patch must adhere to the surface of the contact area. If a patch has inadequate adhesion, it is likely to fall off before the entire delivery period has been satisfied, leading to risks for the patient and others who may encounter the patch. Despite the critical concerns associated with the adhesive properties of the patches, the adhesion quality and failure mechanisms have not been fully studied. If certain molecules encounter the adhesive, it may cause irreversible altering of its chemical composition, which could render it unsuitable for transdermal applications. In many cases of TDDS failure, sweat is believed to be a culprit responsible for causing adhesive failure. The goal of this project is to investigate the chemical composition of the adhesive layer of a transdermal patch. The patch sample is a Sandoz Estradiol Transdermal System manufactured by Noven Pharmaceuticals, Inc., designed to deliver 0.1mg per day and contains 1.56mg of Estradiol USP, the active ingredient. By analyzing the chemical composition of a patch that has not been worn, versus a patch that has been worn, it may be possible to determine the chemical interaction that causes adhesive failure. Fourier Transform Infra-Red (FTIR) Spectroscopy (OPUS FTIR Spectrometer) was performed on an unused estradiol TDDS patch immediately after opening, and again after 24 hours in ambient air to investigate the potential for oxidation. The IR Spectrum was then analyzed, and the peaks were reviewed. The IR Spectra for the sample left out for 24 hours indicated lengthened peaks corresponding to C=O, C-O, and O-H, a decreased transmittance, and a wider bandwidth in those regions. Based on these results, it can be determined that oxidation does occur on a patch sample that is exposed to ambient air. In future works, additional patch samples will be collected and used for an extensive IR and UV analysis. By comparing the IR and UV Spectrum graphs of “used” patches that did not fail, with “failed” patches, it may be possible to identify a cause for premature patch failure related to sweat interactions.</p>2022-06-13T14:24:14+08:00Copyright (c) 2022 Zachary Brooks, Tushar Goswami, Amy Neidhard-Doll, Tarun Goswami