Md.Abu Shyeed , Mahci Al Bashera , Ovijit Sarkar Sazal , Md.Moktar Ali , Md Polok Hossain , Henry Sandip Kumar Mondol , Mohammad Ali Chowdhury , Khan Rajib Hossain , Md Tamzid Hossain Molla
{"title":"Investigation of wound healing and anti-inflammatory activity of Senna occidentalis leaf extract, and in silico screening for both activities","authors":"Md.Abu Shyeed , Mahci Al Bashera , Ovijit Sarkar Sazal , Md.Moktar Ali , Md Polok Hossain , Henry Sandip Kumar Mondol , Mohammad Ali Chowdhury , Khan Rajib Hossain , Md Tamzid Hossain Molla","doi":"10.1016/j.pscia.2023.100016","DOIUrl":"https://doi.org/10.1016/j.pscia.2023.100016","url":null,"abstract":"<div><p>Senna occidentalis, synonym Cassia occidentalis, is a native American pantropical plant species previously classified under the genus Cassia. This study is for testing and to discover new potent phytochemicals from this plant as wound healing and anti-inflammatory agents. The Excision and Assay of Red Blood Cell (RBC) Membrane Stabilization for Anti-Inflammatory Activity Test Method was used to test how well extracts of <em>S. occidentalis</em> leaves from methanol, n-hexane, chloroform, and absolute alcohol helped wounds heal and stopped inflammation. In silico <strong>is another method</strong> for finding potent phytochemicals for both activities. These leaf extracts effectively <strong>cure wound areas and promote re-epithelialization</strong>. The methanol extract exhibited maximum wound healing (95.04%) and anti-inflammation (62.94%) activity compared to their other extracts, standard, and control groups. In silico <strong>molecular docking of Apigenin</strong>, Aloe-emodin with GSK-3B protein, and 1-Methoxynaphthalene, Quinine with COX-2 protein showed binding affinity in <strong>(kj</strong>J<strong>/mol)</strong> of −8.4, −8.6, and −7.3, −7.7, for wound healing and anti-inflammatory activity, respectively, in their binding sites with stability. They support the <strong>\"Lipinski Rule of Five.\"</strong> This plant leaf extract is recommended as a traditional medicine and an alternative, complementary treatment for its continued contribution to drug discovery and development.</p></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"1 2","pages":"Article 100016"},"PeriodicalIF":0.0,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2773216923000144/pdfft?md5=d2a6c0e4ef4496fb0dad488e33ce2598&pid=1-s2.0-S2773216923000144-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"92066690","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":"Flurbiprofen cataplasms: Development and validation of in-vitro dissolution methods and evaluation of multimedia dissolution profiles","authors":"Rathnakar Nathi , Naga Venkata Durga Prasad Ketha , Leela Prasad Kowtarapu , Siva Krishna Muchakayala , Naresh Konduru , Baby Saroja , Arya Lakshmi Marisetti","doi":"10.1016/j.pscia.2023.100018","DOIUrl":"https://doi.org/10.1016/j.pscia.2023.100018","url":null,"abstract":"<div><p>The investigation of the systemic release performance of dosage forms using in vitro tools is a crucial objective in the realm of pharmaceutical development. The dissolution methodology is an effective tool for monitoring batch-to-batch variabilities in quality control and gaining insight into the release mechanisms of pharmaceutical drugs. The majority of the dissolution techniques that have been approved are primarily intended for solid oral dosage forms. Nevertheless, these techniques have also been applied to various other dosage forms, including transdermal drug delivery systems. The administration of medication through cataplasm, a transdermal application, poses challenges in understanding the characteristics of drug release. Flurbiprofen is classified as a class II drug according to the Biopharmaceutics Classification System and is commonly administered in the form of a cataplasm for its analgesic properties. A dissolution method was developed to assess the in vitro release profile of the flurbiprofen transdermal delivery system. This method utilized a United States Pharmacopeia dissolution apparatus V, with a disc assembled over the paddle. Additionally, a method for quantification was developed using liquid chromatography. The discriminatory aspect of the developed method has faced criticism due to substantial alterations in excipient composition. Furthermore, we have developed clearly defined multimedia release profiles within the physiological pH range. The validation of the dissolution and chromatography systems was conducted.</p></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"1 2","pages":"Article 100018"},"PeriodicalIF":0.0,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2773216923000168/pdfft?md5=1770629bbf17febb9b232f33e2aba851&pid=1-s2.0-S2773216923000168-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91986956","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":"Potential therapeutic effect of Salvia coccinea leaf extract in chronic disorders: Myocardial infarction, cataract, and arthritis in rat","authors":"Arun Sundaramoorthy, Narkunaraja Shanmugam","doi":"10.1016/j.pscia.2023.100017","DOIUrl":"https://doi.org/10.1016/j.pscia.2023.100017","url":null,"abstract":"<div><p>Aqueous extract from <em>Salvia coccinea</em> leaf (<em>AESL</em>) has been shown its unique anti-oxidant effect via Nuclear factor (NF)-kappa (κ)B pathway in human monocytic THP-1 cells and pharmacological effect on inflammatory diseases like diabetes in rats. Using <em>AESL,</em> which possess antioxidant activity by scavenging radicals and decreasing oxidative stress, would be a promising strategy for the treatment of other inflammatory disorders like myocardial infarction, arthritis, and cataract. This study was designed to evaluate the ameliorating effects of <em>AESL</em> on isoproterenol (Iso)-induced myocardium infarction (MI), selenite-induced cataractogenesis, and complete Freund's adjuvant-induced arthritis in Wistar rats. In this study, <em>AESL</em> ameliorated pathological changes in Iso-induced MI heart muscles and Electro Cardio Gram pattern, 35–80 % protection of the cataractogenesis, and prevented the apoptosis induced by selenite in the rat lens. Both pre and post-treatment of <em>AESL</em> (600 mg/kg, bw) showed no swelling of the joint and, 35 days treatment showed significant prevention against bony destruction as depicted by less narrowing of joint spaces and soft tissue swelling when compared with control rats. Oral administration of <em>AESL</em> inhibited the Iso-induced increase in serum and myocardial lipid peroxidation, aspartate transaminase, alanine transaminase, creatine kinase, troponin-I, and troponin-T, and lactate dehydrogenase of myocardium infarction rats. Significant increases in the activity of superoxide dismutase, catalase, glutathione peroxidase, and a reduced level of glutathione, were observed in <em>AESL</em> treated cataract rat lens. The results demonstrate that <em>AESL</em> is useful in, in addition to diabetes, controlling myocardium infarction, cataracts, and arthritis.</p></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"1 2","pages":"Article 100017"},"PeriodicalIF":0.0,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2773216923000156/pdfft?md5=8e500d3b1d3b05293dbb64a034e1a5ba&pid=1-s2.0-S2773216923000156-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"92066987","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}
Kriti Shrinet , Ritika K. Singh , Riden Saxena , Avinash K. Chaurasia , Arvind Kumar
{"title":"Ab initio modeling and ligand docking of quercetin and the MC-LR transporter protein Oatp1b2/OATP1B3","authors":"Kriti Shrinet , Ritika K. Singh , Riden Saxena , Avinash K. Chaurasia , Arvind Kumar","doi":"10.1016/j.pscia.2023.100011","DOIUrl":"https://doi.org/10.1016/j.pscia.2023.100011","url":null,"abstract":"<div><p>Trans-membrane proteins (TMPs) play a crucial role in the translocation of organic and inorganic molecules. Unlike other proteins, TMPs are difficult to model structurally because of their location within the amphipathic plasma membrane. In this study, we focused on examining the transport of the cyanotoxin microcystin-LR (MC-LR) through organic ion transporting polypeptides (OATPs) and whether the bioactive phytoconstituent quercetin can function as a barrier to the transportation of MC-LR. To test this hypothesis, we first modeled the transporters OATP1B3 and Oatp1b2 localized in the human and mouse liver, respectively, by <em>ab initio</em> modeling with the Iterative Threading ASSEmbly Refinement server and refined the generated model using the refinement tool of the ModLoop server. Using different tools and servers, the structural quality of the transmembrane helices was validated and found to be an accurate structure of a TMP. Docking analysis was performed with the ligands MC-LR and quercetin with both OATPs using the PatchDock and FireDock online servers. The results, in the form of the global energy of both docked structures, were based on predictions made earlier. The Oatp1b2 global energy for quercetin was −36.4 kcal/mol, compared with the corresponding value at the MC-LR location which was only −5.59 kcal/mol. Similarly, in the case of OATP1B3 with quercetin, the global energy was found to be −39.0 kcal/mol, whereas with MC-LR it was −15.6 kcal/mol. These results clearly show that quercetin competitively inhibits the binding of MC-LR to its respective targets.</p></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"1 2","pages":"Article 100011"},"PeriodicalIF":0.0,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"50190384","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Nanoparticle-enhanced mesalazine therapy for inflammatory bowel disease","authors":"Rajvanshi Sutaria, Zi Hong Mok","doi":"10.1016/j.pscia.2023.100014","DOIUrl":"https://doi.org/10.1016/j.pscia.2023.100014","url":null,"abstract":"<div><p>Inflammatory bowel disease (IBD) is a chronic inflammatory illness that causes ongoing bodily inflammation in the gastrointestinal tract. Drug-targeted delivery of aminosalicylates such as mesalazine at the inflammation sites, to treat ulcerative colitis (UC) and Crohn's disease (CD) has remained a difficulty. Current mesalazine formulations, including tablets, suppositories, and enemas, are typically associated with adverse systemic effects. The use of nanocarriers however has opened the possibility of improved local targeting and pharmacokinetics of loaded mesalazine, based on the new physicochemical properties of the drug vehicle. The innovative nanoencapsulation of mesalazine has demonstrated success in targeting inflammatory regions and treating mild to moderate IBD. The use of nanocarriers, such as lipid-based, polymeric, and inorganic nanocarriers, has demonstrated improved overall solubility, absorption, and bioavailability of mesalazine while minimising the side effects associated with their absorption. This review aims to offer an insight into what is currently known about IBD, and the nanotechnological approaches for the improvement of mesalazine therapy for IBD.</p></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"1 2","pages":"Article 100014"},"PeriodicalIF":0.0,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2773216923000120/pdfft?md5=cce2fa28c0ad0031ff5d2920e9448670&pid=1-s2.0-S2773216923000120-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"92066985","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":"Covalent coating strategy for enhancing the biocompatibility and hemocompatibility of blood-contacting medical materials","authors":"Kangjia Sheng , Yan Gao , Tao Bao , Sicen Wang","doi":"10.1016/j.pscia.2022.100001","DOIUrl":"https://doi.org/10.1016/j.pscia.2022.100001","url":null,"abstract":"<div><p>Blood-contacting medical devices/materials are widely used in the diagnosis and treatment of a variety of diseases. Functional coatings of medical devices are considered one of the core functions in the future, overcoming the limitations of medical devices/materials without modification, including plasma proteins adhesion, platelet activation and coagulation cascade normally result in clotting and thrombosis in clinical use, posing a serious threat to the health and life of patients. In order to improve the anticoagulant properties of material/device surfaces, several surface modified techniques have been developed. Among them, covalent graft method has attracted much attention due to its high stability and excellent hemocompatibility. This review encompasses various covalent modification methods on the surface of blood-contacting medical materials, such as chemical polymers, metallic biomaterials, nylon net membrane, glass slide and etc. Firstly, an overview of the covalent immobilization method for coating is summarized. Secondly, surface coating methods including physical adsorption, electrostatic attachment and layer-by-layer deposition are presented. Finally, the advantages and disadvantages of covalent immobilization method and other methods are compared. Collectively, the information complied should serve as a comprehensively repository in covalent coating strategy for blood-contacting surface, expecting to provide a general retrospect and prospect on the research progress of anticoagulant surface construction and its application in medical devices.</p></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"1 1","pages":"Article 100001"},"PeriodicalIF":0.0,"publicationDate":"2023-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"50189489","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Magic bullets, magic shields, and antimicrobials in between","authors":"Praveen Prathapan","doi":"10.1016/j.pscia.2022.100002","DOIUrl":"https://doi.org/10.1016/j.pscia.2022.100002","url":null,"abstract":"<div><p>There are only two classes of small-molecule drugs for infectious disease: pathogen-directed antimicrobials and host-directed immunomodulators. The former includes antibiotics and antivirals while the latter comprises corticosteroids such as dexamethasone. Here I inaugurate a third class, immunomodulatory antimicrobials (IAs), which considers small-molecule drugs harbouring both pathogen-directed and host-directed pharmacology. I review seven types of IAs, and argue that their high repositionability and network pharmacological ability to counter multiple pathogen types render them more applicable to pandemic-preparedness research than antivirals.</p></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"1 1","pages":"Article 100002"},"PeriodicalIF":0.0,"publicationDate":"2023-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"50189490","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}