Pharmaceutical Science Advances最新文献

{"title":"Corrigendum to “Blockage of HSP90 and IDO1 pathway by α-MSH modified nanoelicitor to dual-facilitate mild photothermal therapy” [Pharmaceut. Sci. Res. 1 (2023) 100009]","authors":"Shunli Fu, Qingping Ma, Jiangnan Li, Yifan Wang, Chunyan Yang, Panpan Gu, Weihan Zhang, Yongjun Liu, Na Zhang","doi":"10.1016/j.pscia.2023.100012","DOIUrl":"https://doi.org/10.1016/j.pscia.2023.100012","url":null,"abstract":"","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"1 2","pages":"Article 100012"},"PeriodicalIF":0.0,"publicationDate":"2023-10-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"50190380","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":"Investigation of wound healing and anti-inflammatory activity of Senna occidentalis leaf extract, and in silico screening for both activities","authors":"Md.Abu Shyeed ,&nbsp;Mahci Al Bashera ,&nbsp;Ovijit Sarkar Sazal ,&nbsp;Md.Moktar Ali ,&nbsp;Md Polok Hossain ,&nbsp;Henry Sandip Kumar Mondol ,&nbsp;Mohammad Ali Chowdhury ,&nbsp;Khan Rajib Hossain ,&nbsp;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":"2023-10-14","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":"Potential application of sucrose acetate isobutyrate, and glyceryl monooleate for nanonization and bioavailability enhancement of rivaroxaban tablets","authors":"Adam A. Al-Shoubki ,&nbsp;Mahmoud H. Teaima ,&nbsp;Rehab Abdelmonem ,&nbsp;Mohamed A. El-Nabarawi ,&nbsp;Sammar Fathy Elhabal","doi":"10.1016/j.pscia.2023.100015","DOIUrl":"https://doi.org/10.1016/j.pscia.2023.100015","url":null,"abstract":"<div><p>This study aimed to investigate the use of Sucrose acetate isobutyrate (SAIB) and Glyceryl monooleate (GMO) as co-formers for creating Cubosomes and SAIB-based nanodispersions of Rivaroxaban (RXB). The process utilized a modified melt dispersion technique with varying polymer: drug ratios (0.5:1, 0.75:1, and 1:1) and a fixed polymer: poloxamer 407 ratio (0.1:1). Particle size (PS), polydispersity index (PDI), zeta potential (ZP), and entrapment efficiency (EE) were measured to determine the optimal formulas. The best-lyophilized formulas were then analyzed using Fourier transform infrared spectroscopy (FT-IR), powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), dissolution testing, and Pharmacokinetic (PK) studies. The results revealed significant correlations between polymer concentrations and various variables in cubosomal and SAIB-based nanodispersions. An increase in GMO concentration led to a decrease in PS, PDI, and ZP but an increase in EE and yield. Maintaining optimal GMO concentration is crucial for consistent nanoparticle formulations. In contrast, increasing SAIB concentration led to a decrease in PS and PDI but an increase in EE and yield. The drug release rates of different preparations were measured during the dissolution test. The best-lyophilized cubosome (L4) and the best-lyophilized SAIB-based nanodispersions (L8) showed significantly improved drug release compared to XARELTO®. L4 displayed the best dissolution rate, and L8 also had a reasonable rate. A PK study demonstrated that L4 and L8 had significantly better bioavailability than XARELTO®, possibly due to their improved solubility. This study suggests that SAIB and GMO can significantly enhance the solubility and bioavailability of RXB in nano preparations, leading to more efficient drug delivery. This new approach can also reduce the required dosage for the desired therapeutic effect. However, further research is needed to fully understand these polymers' potential benefits and limitations.</p></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"2 ","pages":"Article 100015"},"PeriodicalIF":0.0,"publicationDate":"2023-10-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2773216923000132/pdfft?md5=8a41cd1940938eea04f0b2f52f4ba13f&pid=1-s2.0-S2773216923000132-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"92107642","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":"Structure, functions, and recent advances in the development of SIRT2 inhibitors","authors":"Junxin Xue,&nbsp;Xuben Hou,&nbsp;Hao Fang","doi":"10.1016/j.pscia.2023.100010","DOIUrl":"https://doi.org/10.1016/j.pscia.2023.100010","url":null,"abstract":"<div><p>Silent information regulators (sirtuins) are highly evolutionarily conserved and participate in many biological processes in the human body. Unlike classical histone deacetylases, the biological activity of sirtuins depends on nicotinamide adenine dinucleotide (NAD⁺). Among the seven human sirtuins, sirtuin 2 (SIRT2) is one of the most studied and plays important roles in cell aging, energy metabolism, and genome stability. SIRT2 dysregulation is closely associated with the development of cancer and neurodegenerative diseases. In this review, we summarize the structure, function, and recent developments in small-molecule inhibitors of SIRT2. We hope this review will aid the future development of new SIRT2 inhibitors.</p></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"1 2","pages":"Article 100010"},"PeriodicalIF":0.0,"publicationDate":"2023-09-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"50190383","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":"Ab initio modeling and ligand docking of quercetin and the MC-LR transporter protein Oatp1b2/OATP1B3","authors":"Kriti Shrinet ,&nbsp;Ritika K. Singh ,&nbsp;Riden Saxena ,&nbsp;Avinash K. Chaurasia ,&nbsp;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":"2023-09-09","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":"Blockage of HSP90 and IDO1 pathway by α-MSH modified nanoelicitor to dual-facilitate mild photothermal therapy","authors":"Shunli Fu,&nbsp;Qingping Ma,&nbsp;Jiangnan Li,&nbsp;Yifan Wang,&nbsp;Chunyan Yang,&nbsp;Panpan Gu,&nbsp;Weihan Zhang,&nbsp;Yongjun Liu,&nbsp;Na Zhang","doi":"10.1016/j.pscia.2023.100009","DOIUrl":"https://doi.org/10.1016/j.pscia.2023.100009","url":null,"abstract":"<div><p>Mild photothermal therapy (PTT) kills tumors at low temperatures (&lt;45 ​°C) with less non-specific thermal diffusion through adjacent normal tissues, making it a promising antitumor strategy. Although mild PTT can directly convert light energy into heat to kill tumors and indirectly induce immune cell death to prime the immune response, it simultaneously induces negative regulatory factors in the body to resist antitumor functions. In particular, the direct killing effects were reversed by the upregulation of heat shock protein 90 (HSP90) induced by mild PTT. The antitumor effects of T-cell-based immunotherapy counter indoleamine 2,3-dioxygenase1 (IDO1)-catalyzed kynurenine accumulation. Current studies have mainly focused on promoting direct killing effects or utilizing the priming immune response to strengthen the immunotherapy of mild PTT. Therefore, it is necessary to investigate whether the simultaneous promotion of direct killing and indirect immune activation would synergistically maximize mild PTT efficacy. This study reports on the development of a tumor-targeting nanoelicitor, α-<strong>M</strong>SH-<strong>G</strong>A/<strong>I</strong>R780/1-<strong>M</strong>T-<strong>Lip</strong>osome (M-GIM-Lip), by co-loading the photothermal agent IR780, HSP90 inhibitor geldanamycin, and IDO1 inhibitor 1-MT into liposomes with a melanoma-specific target ligand α-MSH modification. After accumulating in the tumor, the M-GIM-Lip could significantly inhibit tumor progress by combinate blockage of HSP90 and IDO1 pathways at 41 ​°C treatment of mild PTT. The study offers an innovative co-regulation strategy for enhancing the antitumor effects of mild PTT.</p></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"1 2","pages":"Article 100009"},"PeriodicalIF":0.0,"publicationDate":"2023-07-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"50190382","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":"Controlled release of bilayer tablet comprising vitamin B6 rapid-release layer and melatonin sustained-release layer","authors":"Yan Wang ,&nbsp;Jiaqi Xu ,&nbsp;Nan Gao ,&nbsp;Hongqian Lv ,&nbsp;Minge Sun ,&nbsp;Peng Zhang","doi":"10.1016/j.pscia.2023.100008","DOIUrl":"https://doi.org/10.1016/j.pscia.2023.100008","url":null,"abstract":"<div><p>Here, the formulation of a novel bilayer tablet comprising a vitamin B₆ rapid-release layer and a melatonin sustained-release layer is described. The effects of viscosity and concentration of the sustained-release matrix material, amount of diluent, and melatonin particle size on the release characteristics of melatonin were examined. In addition, the drug-release behavior of the prepared bilayer tablets was examined in different dissolution media. Further, drug-release kinetics and melatonin behavior in the sustained-release layer were evaluated based on dissolution profiles and changes in tablet weight during dissolution. Furthermore, the stability of the bilayer tablet was established. The <em>in vitro</em> release test revealed that vitamin B₆ was completely released within 10–15 ​min, with melatonin demonstrating ∼90% cumulative release within 8 ​h. Based on kinetic model fitting results, melatonin release was well fitted to the Ritger-Peppas model; the release mechanism was non-Fick diffusion with both diffusion and erosion. The drug-release study confirmed that the melatonin sustained-release layer predominantly underwent polymer swelling rather than polymer erosion. The stability test results showed that the bilayer tablets had good stability under high temperature, high humidity, and light conditions. The bilayer tablets offer an alternative for the controlled-release oral administration of melatonin, although their <em>in vivo</em> effects need to be investigated in human studies.</p></div>","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"1 2","pages":"Article 100008"},"PeriodicalIF":0.0,"publicationDate":"2023-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"50190387","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":"The inaugural editorial of pharmaceutical science advances","authors":"","doi":"10.1016/j.pscia.2023.100003","DOIUrl":"https://doi.org/10.1016/j.pscia.2023.100003","url":null,"abstract":"","PeriodicalId":101012,"journal":{"name":"Pharmaceutical Science Advances","volume":"1 1","pages":"Article 100003"},"PeriodicalIF":0.0,"publicationDate":"2023-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"50189054","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":"Covalent coating strategy for enhancing the biocompatibility and hemocompatibility of blood-contacting medical materials","authors":"Kangjia Sheng ,&nbsp;Yan Gao ,&nbsp;Tao Bao ,&nbsp;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}