DARU Journal of Pharmaceutical Sciences最新文献

{"title":"Microbiological acceptance criteria, specifications of herbal drugs and herbal drug preparations in various pharmacopoeias: a global scenario","authors":"Ramesh Munukuntla, Akhilesh Tiwari, Ravi Shankar Yadav, A. Jayanthy, Subhash Chandra Verma, Raman Mohan Singh","doi":"10.1007/s40199-024-00510-5","DOIUrl":"https://doi.org/10.1007/s40199-024-00510-5","url":null,"abstract":"<h3 data-test=\"abstract-sub-heading\">Purpose</h3><p>A pharmacopoeia is a compendium of guidelines and criteria for drug quality. It was established by a national or regional entity and has legal significance. This applies to administration of drugs in a particular nation or region.</p><h3 data-test=\"abstract-sub-heading\">Method</h3><p>In this study, the differences and similarities of microbiological acceptance criteria, specifications for microbial enumeration of herbal drugs and herbal drug preparations in 14 national and international pharmacopeias were investigated.</p><h3 data-test=\"abstract-sub-heading\">Results</h3><p>It was found that 12 pharmacopeias have given separate microbial limits for total aerobic microbial count (TAMC) and total yeast and mold count (TYMC), and a list of specified microorganisms for which acceptance criteria are defined. However, similarities were noticed in Ph.Eur, Ph. Helv and, BP. <i>Salmonella, and Escherichia coli</i> are the most common pathogens specified for herbal preparations in which boiling water is added prior to use and for internal use in all Pharmacopoeias because they serve as indicators of potential contamination.</p><h3 data-test=\"abstract-sub-heading\">Conclusion</h3><p>From this study, it can be concluded that the differences in microbial limit tests and their acceptance criteria as specified in the various pharmacopoeias need to be harmonized. It will become a more convenient option for global drug manufacturers to import/export herbal drugs, and this would also eliminate the burden of performing various analytical methods and comply with different microbial acceptance criteria set by various pharmacopoeias. The comparative data obtained from this study will be used to develop strategies for revisions of pharmacopoeias in a harmonized manner with respect to microbiological acceptance criteria, specifications for microbial enumeration of herbal drugs and herbal drug preparations.</p>","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":"24 1","pages":""},"PeriodicalIF":3.6,"publicationDate":"2024-04-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140601986","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Developing an AI-based prediction model for anaphylactic shock from injection drugs using Japanese real-world data and chemical structure-based analysis","authors":"Tomoyuki Enokiya, Kaito Ozaki","doi":"10.1007/s40199-024-00511-4","DOIUrl":"https://doi.org/10.1007/s40199-024-00511-4","url":null,"abstract":"<h3 data-test=\"abstract-sub-heading\">Background</h3><p>This study aims to develop an AI-based prediction model for injection drugs that cause anaphylactic shock using Japanese Real-World Data (JADER database) and chemical structure-based analysis.</p><h3 data-test=\"abstract-sub-heading\">Methods</h3><p>Data sourced from the JADER database included adverse drug reaction reports from April 2004 to December 2020. Only drugs with an adverse reaction named \"anaphylactic shock\" were selected for analysis. For model building, various models were constructed to predict anaphylactic shock-inducing drugs, such as logistic regression, LASSO, XGBoost, RF, SVM, and NNW. These models used chemical properties and structural similarities as feature variables. Dimension reduction was applied using principal component analysis. The dataset was split into training (80%) and validation (20%) sets. Six different models were trained and optimized through fivefold cross-validation.</p><h3 data-test=\"abstract-sub-heading\">Results</h3><p>From April 2004 to December 2020, 947 drugs with the adverse reaction name \"anaphylactic shock\" were extracted from the JADER database. 320 drugs were excluded due to analytical challenges, and another 400 were removed due to their administration route. 227 drugs were finalized as target medicines. For model validation, the performance of each model was evaluated based on metrics like AUCs of ROC curve, sensitivity, and specificity. Additionally, two ensemble models, constructed from the six models were assessed using bootstrap sampling. Interestingly, it was identified that mepivacaine structural similarity had the highest importance in the final model.</p><h3 data-test=\"abstract-sub-heading\">Conclusions</h3><p>The study successfully developed an AI-based prediction model for anaphylactic shock inducing-injection drugs. The model would offer potential for drug safety evaluation and anaphylactic shock risk assessment.</p><h3 data-test=\"abstract-sub-heading\">Graphical abstract</h3>\u0000","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":"62 1","pages":""},"PeriodicalIF":3.6,"publicationDate":"2024-04-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140585777","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"New amide and diterpene alkaloids with anticholinesterase activity from Delphinium cyphoplectrum roots","authors":"Arash Salehi, Behzad Zolfaghari, Mahmoud Aghaei, Hajar Sirous, Morteza Sadeghi, Mohammad Reza Gholami, Parham Reisi, Mustafa Ghanadian","doi":"10.1007/s40199-024-00509-y","DOIUrl":"https://doi.org/10.1007/s40199-024-00509-y","url":null,"abstract":"&lt;h3 data-test=\"abstract-sub-heading\"&gt;Background&lt;/h3&gt;&lt;p&gt;The cholinergic hypothesis posits a robust correlation between the onset of Alzheimer’s disease and a pronounced deficit in acetylcholine, a pivotal neurotransmitter crucial for the central cholinergic nervous system’s function, pivotal for memory and learning. Diterpene alkaloids exhibit intricate and distinctive chemical structures that facilitate their passage through the blood-brain barrier. Moreover, their potent pharmacological attributes render them promising candidates for addressing central nervous system disorders.&lt;/p&gt;&lt;h3 data-test=\"abstract-sub-heading\"&gt;Objectives&lt;/h3&gt;&lt;p&gt;This investigation aims to scrutinize the alkaloidal composition of &lt;i&gt;Delphinium cyphoplectrum&lt;/i&gt; (Ranunculaceae) roots, further exploring their anticholinesterase inhibitory activity and mode of inhibition.&lt;/p&gt;&lt;h3 data-test=\"abstract-sub-heading\"&gt;Method&lt;/h3&gt;&lt;p&gt;Innovative chromatography techniques were repetitively employed to purify the alkaloids. Acetylcholinesterase (AChE) inhibition assays were conducted using Ellman’s tests. The mode of inhibition was meticulously characterized through Michaelis-Menten, and Lineweaver-Burk plots. Conducting molecular docking studies, we employed the AUTO DOCK 4.2 software package.&lt;/p&gt;&lt;h3 data-test=\"abstract-sub-heading\"&gt;Results&lt;/h3&gt;&lt;p&gt;Eight alkaloids were identified including five C19-diterpene alkaloids (6,14,16,18-tetramethoxy-1,7,8-trihydroxy-4-methylaconitane (&lt;b&gt;1&lt;/b&gt;), 6,16,18-trimethoxy-1,7,8,14-tetrahydroxy-4-methylaconitane (&lt;b&gt;2&lt;/b&gt;), 6,8,16,18-tetramethoxy-1,7,14-trihydroxy-4-methylaconitane (&lt;b&gt;3&lt;/b&gt;), 6,14,16-trimethoxy-1,7,8,18-tetrahydroxy-4-methylaconitane (&lt;b&gt;4&lt;/b&gt;), and 14-&lt;i&gt;O&lt;/i&gt;-acetyl-8,16-dimethoxy-1,6,7,18-tetrahydroxy-4-methylaconitane (&lt;b&gt;5&lt;/b&gt;)), an epoxy C18-diterpene alkaloid (6,8,16-trimethoxy-1,7,14-trihydroxy-3,4-epoxyaconitane (&lt;b&gt;6&lt;/b&gt;)), a known (pyrrolidin-2-one (&lt;b&gt;7&lt;/b&gt;) and an undescribed amide alkaloid (1-(2’-hydroxylethylamine)-3,5,5,-trimethyl-1,5-dihydro-2H-pyrrol-2-one (&lt;b&gt;8&lt;/b&gt;). All diterpene alkaloids underwent assessment for acetylcholinesterase (AChE) inhibition assay and displayed noteworthy AChE activity, surpassing that of the reference drug (with IC&lt;sub&gt;50&lt;/sub&gt; values of 13.7, 21.8, 23.4, 28.2, 40.4, and 23.9 for compounds &lt;b&gt;1&lt;/b&gt;–&lt;b&gt;6&lt;/b&gt;, respectively, in comparison to 98.4 for Rivastigmine). Analysis of Michaelis-Menten and Lineweaver-Burk plots represents an uncompetitive mode of inhibition for compound &lt;b&gt;1&lt;/b&gt; on AChE. Notably, computational docking simulations indicated that all diterpene alkaloids were accommodated within the same enzymatic cleft as the reference ligand, and displaying superior free binding energy values (from − 10.32 to -8.59 Kcal.mol&lt;sup&gt;−1&lt;/sup&gt;) in contrast to Rivastigmine (-6.31 Kcal.mol&lt;sup&gt;−1&lt;/sup&gt;).&lt;/p&gt;&lt;h3 data-test=\"abstract-sub-heading\"&gt;Conclusion&lt;/h3&gt;&lt;p&gt;The phytochemical analysis conducted on the roots of &lt;i&gt;Delphinium cyphoplectrum&lt;/i&gt; yielded the identification of eight alkaloidal co","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":"132 1","pages":""},"PeriodicalIF":3.6,"publicationDate":"2024-03-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140156188","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development of brimonidine niosomes laden contact lenses for extended release and promising delivery system in glaucoma treatment","authors":"Shresthi Tripathi, Khushwant S. Yadav","doi":"10.1007/s40199-023-00500-z","DOIUrl":"https://doi.org/10.1007/s40199-023-00500-z","url":null,"abstract":"<h3 data-test=\"abstract-sub-heading\">Background</h3><p>Increased intraocular pressure is a common symptom of glaucoma. In severe circumstances, it may result in loss of eyesight. Glaucoma treatment is difficult due to ocular physiological barriers that prevent medications from reaching the afflicted area. Traditional formulations (eye drops) have a short residence period and are rapidly drained away via the nasolacrimal duct, resulting in increased adverse drug responses and lower efficacy. The usage of nanoparticles such as niosomes could be one potential answer to these problems. While niosomes improve drug penetration, they have little effect on ocular retention of the medication. Contact lenses containing niosomes can assist to overcome this disadvantage.</p><h3 data-test=\"abstract-sub-heading\">Objective</h3><p>This study aims to prepare and evaluate Brimonidine niosomes laden contact lenses for the treatment of Glaucoma.</p><h3 data-test=\"abstract-sub-heading\">Methods</h3><p>Brimonidine niosomes were prepared using thin film hydration method and evaluated. The contact lenses were soaked in the niosomal formulation at varying intervals (3–10 days). Thereafter, the contact lenses were evaluated for %transmittance, %swelling index, drug quantification and in vitro drug release. The pharmacodynamic studies were conducted to assess the reduction in intraocular pressure (IOP) in albino rabbits. The research compared the results of the reduction in intraocular pressure caused by Brimonidine niosomes laden contact lenses with a marketed preparation of niosomes.</p><h3 data-test=\"abstract-sub-heading\">Results</h3><p>Higher concentration of the drug was loaded in contact lenses loaded with Brimonidine niosomes compared to the marketed formulation, by soaking method. The contact lenses exhibited an optimal %transmittance of 98.02 ± 0.36 and %swelling index of 50.35 ± 0.57. Increase in the soaking time up to 7 days led to an increase in the drug concentration in the contact lenses. However, no further increase was observed after the 7th day due to saturation of the contact lenses. Brimonidine niosomes laden contact lenses provided a reduction in intraocular pressure that was similar to the marketed preparation. Further, the contact lenses provided extended release up to 20 h.</p><h3 data-test=\"abstract-sub-heading\">Conclusion</h3><p>Brimonidine niosomes laden contact lenses exhibited superior drug loading through the soaking method, displaying optimal %transmittance and %swelling index. Soaking for 7 days increased drug concentration in contact lenses with no further increase due to saturation. These lenses reduced intraocular pressure like the marketed formulation, offering extended release for 20 h.</p><h3 data-test=\"abstract-sub-heading\">Graphical abstract</h3>\u0000","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":"132 1","pages":""},"PeriodicalIF":3.6,"publicationDate":"2023-12-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139063358","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Artificial viruses: A nanotechnology based approach","authors":"","doi":"10.1007/s40199-023-00496-6","DOIUrl":"https://doi.org/10.1007/s40199-023-00496-6","url":null,"abstract":"<h3>Abstract</h3> <span> <h3>Objectives</h3> <p>The main objective of this work was to review and summarise the detailed literature available on viral nanoparticle and the strategies utilised for their manufacture along with their applications as therapeutic agents.</p> </span> <span> <h3>Data acquisition</h3> <p>The reported literature related to development and application of virus nanoparticles have been collected from electronic data bases like ScienceDirect, google scholar, PubMed by using key words like “viral nanoparticles”, “targeted drug delivery” and “vaccines” and related combinations.</p> </span> <span> <h3>Result</h3> <p>From the detailed literature survey, virus nanoparticles were identified as carriers for the targeted delivery. Due to the presence of nanostructures in virus nanoparticles, these protect the drugs from the degradation in the gastrointestinal tract and in case of the delivery of gene medicine, they carry the nucleic acids to the target/susceptible host cells. Thus, artificial viruses are utilised for targeted delivery to specific organ in biomedical and biotechnological areas.</p> </span> <span> <h3>Conclusion</h3> <p>Thus, virus nanoparticles can be considered as viable option as drug/gene carrier in various healthcare sectors especially drug delivery and vaccine and can be explored further in future for the development of better drug delivery techniques.</p> </span> <span> <h3>Graphical Abstract</h3> <p> <span> <span> <img alt=\"\" src=\"https://static-content.springer.com/image/MediaObjects/40199_2023_496_Figa_HTML.png\"/> </span> </span></p> </span>","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":"4 1","pages":""},"PeriodicalIF":3.6,"publicationDate":"2023-12-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138717215","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Polymeric nanoparticles delivery circumvents bacterial resistance to ciprofloxacin","authors":"Abdullah A. Ghawanmeh","doi":"10.1007/s40199-023-00498-4","DOIUrl":"https://doi.org/10.1007/s40199-023-00498-4","url":null,"abstract":"<h3 data-test=\"abstract-sub-heading\">Objective</h3><p>The efficient inhibition of bacteria and their by-products from infected root canals is hampered by the limitations of traditional root canal disinfection strategies, bacterial resistance to antibiotic drugs, and regenerative endodontics. Polymeric nanoparticles nanocarrier for controlling antibiotic drug delivery were used to overcome the limitations encountered in endodontics treatment.</p><h3 data-test=\"abstract-sub-heading\">Background</h3><p>Several polymeric nanoparticles have been used for the delivery of ciprofloxacin drug. The application of poly (ethylene glycol) methyl ether-block-poly(lactide-co-glycolide) (PEG-PLGA) nanoparticles has highlighted the clean and safe delivery of ciprofloxacin (CIP) hydrophilic drug for endodontics treatment. PEG/PLGA was prepared using the solid/oil/water method and the CIP was loaded into polymeric nanoparticles via an ion pairing agent.</p><h3 data-test=\"abstract-sub-heading\">Results</h3><p>The CIP-loaded PEG-PLGA nanoparticles have a spherical shape with a 120 ± 0.43 nm size, the CIP encapsulating efficiency was 63.26 ± 9.24% with a loading content of 7.75 ± 1.13%, and sustained release was achieved over 168 h which followed Higuchi model with a non-Fickian mechanism. Moreover, CIP-loaded PEG-PLGA had low cytotoxicity to the stem cells of the apical papilla.</p><h3 data-test=\"abstract-sub-heading\">Conclusion</h3><p>The results conclude invigorating future perspectives of polymeric nanoparticles for a wide range of drug delivery for various disease treatments. It’s anticipated that these polymeric nanoparticles may divert new expectations in the future for topical antibiotic drug delivery with discrete intracellular medicament, and a safe and clean environment.</p><h3 data-test=\"abstract-sub-heading\">Graphical abstract</h3>\u0000","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":"39 1","pages":""},"PeriodicalIF":3.6,"publicationDate":"2023-12-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138682263","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Effectiveness of epigallocatechin gallate nanoparticles on the in-vivo treatment of Alzheimer’s disease in a rat/mouse model: a systematic review","authors":"Maha K. A. Khalifa, Somaia A. Abdel-Sattar, Omnya M. Amin, Neveen A. Kohaf, Heba S. Zaky, Marwa A. Abd El‑Fattah, Kamilia H. A. Mohammed, Noha M. Badawi, Ihab Mansoor, Heba A. Eassa","doi":"10.1007/s40199-023-00494-8","DOIUrl":"https://doi.org/10.1007/s40199-023-00494-8","url":null,"abstract":"<h3 data-test=\"abstract-sub-heading\">Background</h3><p>Alzheimer’s disease (AD) is a neurological disease that causes memory loss over time. Current therapies are limited and frequently inadequate. Epigallocatechin gallate (EGCG), has antioxidant, anti-inflammatory, antifibrosis, anti-remodeling and tissue-protective qualities that may be effective in treatment of different diseases, including AD. Because of nanoparticles’ high surface area, they can enhance solubility, stability, pharmacokinetics and biodistribution, and diminish toxicities. Besides, lipid nanoparticles have a high binding affinity that can enhance the rate of drug transport across BBB. So, EGCG nanoparticles represent a promising treatment for AD.</p><h3 data-test=\"abstract-sub-heading\">Objectives</h3><p>This systematic review sought to assess the efficacy of EGCG nanoparticles against AD in rat/mouse models.</p><h3 data-test=\"abstract-sub-heading\">Methods</h3><p>Study was conducted in accordance with PRISMA guidelines, and the protocol was registered in PROSPERO. Electronic databases were searched to discover relevant studies published up to October 2022.</p><h3 data-test=\"abstract-sub-heading\">Results</h3><p>Two studies met the inclusion criteria out of 1338 and were included in this systematic review. Collectively, the results indicate that EGCG has a significant potential for reducing AD pathology and improving cognitive deficits in rat/mouse models. The formulated particles were in the nanometer range, as indicated by TEM, with good particle size control and stability. EGCG nanoparticles showed superior pharmacokinetic characteristics and improved blood-brain barrier permeability, and increased brain bioavailability compared to free EGCG. Additionally, nanoEGCG were more effective in modulating oxidative stress than free formulation and decreased AChE in the cortex and hippocampus of AlCl3-treated rats.</p><h3 data-test=\"abstract-sub-heading\">Conclusion</h3><p>This systematic analysis of the two studies included showed that EGCG nanoparticles are efficacious as a potential therapeutic intervention for AD in rat/mouse models. However, limited number of studies found indicates insufficient data in this research point that requires further investigation by experimental studies.</p><h3 data-test=\"abstract-sub-heading\">Graphical abstract</h3>\u0000","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":"49 1","pages":""},"PeriodicalIF":3.6,"publicationDate":"2023-12-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138566344","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Multi-functionalization of reduced graphene oxide nanosheets for tumor theragnosis: Synthesis, characterization, enzyme assay, in-silico study, radiolabeling and in vivo targeting evaluation","authors":"Tamer M. Sakr, Mohammed F. Elsabagh, Hend Fayez, Mona O. Sarhan, Yasmin M. Syam, Manal M. Anwar, Mohammed A. Motaleb, Wafaa A. Zaghary","doi":"10.1007/s40199-023-00487-7","DOIUrl":"https://doi.org/10.1007/s40199-023-00487-7","url":null,"abstract":"<h3 data-test=\"abstract-sub-heading\">Background</h3><p>In this study, a combination of nanotechnology, organic synthesis and radiochemistry were utilized in order to design an efficient nano-system conjugated with a suitable radionuclide and an antitumor agent for possible application as tumor theragnostic agent.</p><h3 data-test=\"abstract-sub-heading\">Method</h3><p>Four novel compounds (3 and 4a-c) bearing tetrahydroquinazoline-7-sulfonohydrazide or 1,2,3,4-tetrahydroquinazoline-7-sulfonamide scaffold were designed. Then, docking study predicted that the compounds can be considered as potential inhibitors for PARP-1. Following that; the four compounds were synthesized and properly characterized using ^<i>1</i><i>H</i>NMR, ^<i>13</i><i>C</i>NMR, IR and Mass spectroscopy. The cytotoxic effect of the four compounds was evaluated against breast cancer cell line (MDA-MB-436), where compound 3 showed the most promising cytotoxic effect. The inhibitory effect of the four compounds was evaluated in vitro against PARP-1.</p><h3 data-test=\"abstract-sub-heading\">Result</h3><p>Carboxylated graphene oxide nanosheets (NGO-COOH) were synthesized by a modified Hummer's method and has size of range 40 nm. The NGO-COOH nanosheets were proven to be safe and biocompatible when tested in vitro against normal human lung fibroblast cells (MRC-5). The prepared NGO-COOH nanosheets were conjugated with compound 3 then radiolabeled with ^99mTc to yield ^99mTc-NGO-COOH-3 with a radiochemical yield of 98.5.0 ± 0.5%. ^99mTc-NGO-COOH-3 was injected intravenously in solid tumor bearing mice to study the degree of localization of the nano-system at tumor tissue. The results of the study revealed, excellent localization and retention of the designed nano-system at tumor tissues with targeting ratio of 9.0.</p><h3 data-test=\"abstract-sub-heading\">Conclusion</h3><p>Stirred a new candidate tumor theragnostic agent that is safe, selective and stable.</p><h3 data-test=\"abstract-sub-heading\">Graphical abstract</h3>\u0000","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":"3 4 1","pages":""},"PeriodicalIF":3.6,"publicationDate":"2023-12-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138566855","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Identifying natural products for gastric cancer treatment through pharmacophore creation, 3D QSAR, virtual screening, and molecular dynamics studies.","authors":"Zeinab Jalali, Samad Nejad Ebrahimi, Hassan Rezadoost","doi":"10.1007/s40199-023-00480-0","DOIUrl":"10.1007/s40199-023-00480-0","url":null,"abstract":"<p><strong>Background: </strong>Gastric cancer (GC) is known as the fourth leading cause of cancer-related death and the fifth major cancer in the world, and this is a serious threat to general health all over the world. The lack of early detection markers results in a belated diagnosis, i.e. the final stages, which could be associated with the ineffectiveness of the treatment strategies, and naturally, it leads to poor prognosis. Even though a variety of treatments have been developed, there is a trend of studying traditional medicinal plants, due to the worrying side effect of drugs available in the market.</p><p><strong>Methods: </strong>In this study, pharmacophore generation and 3D-QSAR model were created using 50 compounds with anti-gastric cancer activity (with IC₅₀ had been reported in the previous studies).</p><p><strong>Results: </strong>Based on three of the best pharmacophoric hypotheses, virtual screening was performed to discover the top anti-gastric cancer compounds from a database of 183,885 compounds. The selected compounds were used for molecular docking with three protein receptors 7BKG, 4F5B, and 4ZT1 to investigate the intermolecular interactions between these ligands and receptors. Finally, 21 lead compounds with the highest amount of docking score ranging from - 13.366 to -6.404 kcal/mol were selected, and then the ADME/Tox properties of these compounds were calculated. All these compounds have a fitness score above 1.8, a molecular weight of less than 500 g/mol, hydrogen bond donors up to 3, hydrogen bond acceptors up to 8.50, and logP of 1.013 to 4.174. Finally, molecular dynamic simulations for top-scoring ligand-receptor complexes were investigated.</p><p><strong>Conclusion: </strong>These selected lead compounds have the most anti-gastric cancer effects among the 183,885 compounds in the database. Therefore, lead compounds might be considered for gastric cancer therapy in future studies.</p>","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":" ","pages":"243-258"},"PeriodicalIF":2.5,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10624797/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41111493","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Utilization patterns of cardiovascular medications in patients with diabetes mellitus; a retrospective cross-sectional study, 2013-17.","authors":"Negin Hatami, Mohammad-Reza Malekpour, Farshad Farzadfar, Meysam Seyedifar, Fatemeh Soleymani","doi":"10.1007/s40199-023-00481-z","DOIUrl":"10.1007/s40199-023-00481-z","url":null,"abstract":"<p><strong>Background: </strong>Diabetes Mellitus (DM) is a prominent health care issue worldwide. One of the most prevalent comorbidities of DM is cardiovascular disease (CVD). The objective of this study was to assess the utilization patterns of cardiovascular medications in patients with DM in Iran from 2013 to 2017.</p><p><strong>Methods: </strong>This retrospective cross-sectional study was undertaken using prescription claims data from 2013 to 2017 in Iran. Epidemiological data elements used in this study were obtained from the Global Burden of Disease (GBD) 2019 study. In addition, data on total medication sales were obtained from the national regulatory authority database. The data on medication utilization were analyzed according to the Anatomical Therapeutic Chemical Classification (ATC) /Defined Daily Doses (DDD) international system.</p><p><strong>Results: </strong>Based on the findings, Acetylsalicylic acid was the mainstay of treatment with a utilization rate of 191.7 DDD/ patient/ year in 2017, followed by Atorvastatin with 170.0 and Losartan with 115.1. Although there was an increasing trend in the utilization rate of the medications, the rate of Atenolol and Enalapril was constantly declining during the 2013-17 period. On the other hand, Valsartan and Metoprolol were attracting attention. Almost all medication utilization rates increased from the 30-39 age group up to the 80 + age group. Females had a higher utilization rate in each age group during the whole study period.</p><p><strong>Conclusion: </strong>The present study reflects that medication utilization patterns were rational, according to the standard treatment guidelines. Utilization patterns of medications that are recommended for both prevention and treatment of CVD in diabetes were observed to be the highest. Implementation of further policies is needed to minimize cardiovascular complications of diabetes.</p>","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":" ","pages":"259-266"},"PeriodicalIF":2.5,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10624784/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41233115","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}