{"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}
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
{"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}
Tamer M. Sakr, Mohammed F. Elsabagh, Hend Fayez, Mona O. Sarhan, Yasmin M. Syam, Manal M. Anwar, Mohammed A. Motaleb, Wafaa A. Zaghary
{"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 <sup><i>1</i></sup><i>H</i>NMR, <sup><i>13</i></sup><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 <sup>99m</sup>Tc to yield <sup>99m</sup>Tc-NGO-COOH-3 with a radiochemical yield of 98.5.0 ± 0.5%. <sup>99m</sup>Tc-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 IC<sub>50</sub> 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}
{"title":"Vactosertib potently improves anti-tumor properties of 5-FU for colon cancer.","authors":"Maryam Moradi Binabaj, Fereshteh Asgharzadeh, Farzad Rahmani, Abdulridha Mohammed Al-Asady, Milad Hashemzehi, Atena Soleimani, Amir Avan, Saeedeh Mehraban, Elnaz Ghorbani, Mikhail Ryzhikov, Majid Khazaei, Seyed Mahdi Hassanian","doi":"10.1007/s40199-023-00474-y","DOIUrl":"10.1007/s40199-023-00474-y","url":null,"abstract":"<p><strong>Background: </strong>Several studies have shown that the TGF-β signaling pathway plays a critical role in colorectal cancer (CRC) pathogenesis. The aim of the current study is to investigate the therapeutic potential of Vactosertib (EW-7197), a selective inhibitor of TGF-β receptor type I, either alone or in combination with the standard first-line chemotherapeutic treatment, 5-Fluorouracil (5-FU), in CRC progression in both cellular and animal models.</p><p><strong>Methods: </strong>Real-Time PCR, Zymography, enzyme-linked immunosorbent assay (ELISA), Hematoxylin and Eosin (H&E) tissue staining, and Flow cytometry techniques were applied to determine the anti-tumor properties of this novel TGF-β inhibitor in in vitro (CT-26 cell line) and in vivo (inbred BALB/C mice) samples.</p><p><strong>Results: </strong>Our findings showed that Vactosertib decreased cell proliferation and induced spheroid shrinkage. Moreover, this inhibitor suppressed the cell cycle and its administration either alone or in combination with 5-FU induced apoptosis by regulating the expression of p53 and BAX proteins. It also improved 5-FU anti-cancer effects by decreasing the tumor volume and weight, increasing tumor necrosis, and regulating tumor fibrosis and inflammation in an animal model. Vactosertib also enhanced the inhibitory effect of 5-FU on invasive behavior of CRC cells by upregulating the expression of E-cadherin and inhibiting MMP-9 enzymatic activity.</p><p><strong>Conclusion: </strong>This study demonstrating the potent anti-tumor effects of Vactosertib against CRC progression. Our results clearly suggest that this inhibitor could be a promising agent reducing CRC tumor progression when administered either alone or in combination with standard treatment in CRC patients.</p>","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":" ","pages":"193-203"},"PeriodicalIF":2.5,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10624787/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41101911","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}
Hemant Suryavanshi, Raju D Chaudhari, Vishakha S. Patil, S. Majumdar, S. Debnath, Goutam Biswas
{"title":"Design, synthesis and docking study of Vortioxetine derivatives as a SARS-CoV-2 main protease inhibitor","authors":"Hemant Suryavanshi, Raju D Chaudhari, Vishakha S. Patil, S. Majumdar, S. Debnath, Goutam Biswas","doi":"10.1007/s40199-022-00441-z","DOIUrl":"https://doi.org/10.1007/s40199-022-00441-z","url":null,"abstract":"","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":"9 1","pages":"139 - 152"},"PeriodicalIF":3.6,"publicationDate":"2022-05-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83078621","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":"Facile electrochemical preparation of overoxidizedpolypyrrole/RGO composite for ds-DNA immobilization: a novel signal amplified sensing platform for electrochemical determination of chlorpheniramine","authors":"K. Moulaee, M. Ganjali, P. Norouzi, H. Beitollahi","doi":"10.1007/s40199-019-00314-y","DOIUrl":"https://doi.org/10.1007/s40199-019-00314-y","url":null,"abstract":"","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":"695 1","pages":"57 - 64"},"PeriodicalIF":3.6,"publicationDate":"2019-12-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85320227","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":"The effect of metal salts on aerosol performance of spray dried carrier-free formulations of levofloxacin","authors":"A. Barazesh, K. Gilani, M. Rouini, M. Barghi","doi":"10.1007/s40199-019-00317-9","DOIUrl":"https://doi.org/10.1007/s40199-019-00317-9","url":null,"abstract":"","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":"74 1","pages":"75 - 85"},"PeriodicalIF":3.6,"publicationDate":"2019-12-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74645523","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":"Alpha-mangostin decreased cellular senescence in human umbilical vein endothelial cells","authors":"Hourieh Tousian, B. Razavi, H. Hosseinzadeh","doi":"10.1007/s40199-019-00305-z","DOIUrl":"https://doi.org/10.1007/s40199-019-00305-z","url":null,"abstract":"","PeriodicalId":10888,"journal":{"name":"DARU Journal of Pharmaceutical Sciences","volume":"119 1","pages":"45 - 55"},"PeriodicalIF":3.6,"publicationDate":"2019-12-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77951246","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}