Pharmaceutical Science Advances最新文献

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Flurbiprofen cataplasms: Development and validation of in-vitro dissolution methods and evaluation of multimedia dissolution profiles 氟比洛芬膏剂:体外溶出方法的开发和验证以及多媒体溶出谱的评价
Pharmaceutical Science Advances Pub Date : 2023-10-16 DOI: 10.1016/j.pscia.2023.100018
Rathnakar Nathi , Naga Venkata Durga Prasad Ketha , Leela Prasad Kowtarapu , Siva Krishna Muchakayala , Naresh Konduru , Baby Saroja , Arya Lakshmi Marisetti
{"title":"Flurbiprofen cataplasms: Development and validation of in-vitro dissolution methods and evaluation of multimedia dissolution profiles","authors":"Rathnakar Nathi ,&nbsp;Naga Venkata Durga Prasad Ketha ,&nbsp;Leela Prasad Kowtarapu ,&nbsp;Siva Krishna Muchakayala ,&nbsp;Naresh Konduru ,&nbsp;Baby Saroja ,&nbsp;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":"2023-10-16","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}
引用次数: 0
Potential therapeutic effect of Salvia coccinea leaf extract in chronic disorders: Myocardial infarction, cataract, and arthritis in rat 鼠尾草叶提取物对大鼠慢性疾病:心肌梗死、白内障、关节炎的潜在治疗作用
Pharmaceutical Science Advances Pub Date : 2023-10-16 DOI: 10.1016/j.pscia.2023.100017
Arun Sundaramoorthy, Narkunaraja Shanmugam
{"title":"Potential therapeutic effect of Salvia coccinea leaf extract in chronic disorders: Myocardial infarction, cataract, and arthritis in rat","authors":"Arun Sundaramoorthy,&nbsp;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":"2023-10-16","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}
引用次数: 0
Nanoparticle-enhanced mesalazine therapy for inflammatory bowel disease 纳米颗粒增强美沙拉嗪治疗炎症性肠病
Pharmaceutical Science Advances Pub Date : 2023-10-16 DOI: 10.1016/j.pscia.2023.100014
Rajvanshi Sutaria, Zi Hong Mok
{"title":"Nanoparticle-enhanced mesalazine therapy for inflammatory bowel disease","authors":"Rajvanshi Sutaria,&nbsp;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":"2023-10-16","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}
引用次数: 0
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] “α-MSH修饰的纳米激发子阻断HSP90和IDO1通路以双重促进温和光热治疗”的更正[Pharmaceut.Sci.Res.1(2023)100009]
Pharmaceutical Science Advances Pub Date : 2023-10-16 DOI: 10.1016/j.pscia.2023.100012
Shunli Fu, Qingping Ma, Jiangnan Li, Yifan Wang, Chunyan Yang, Panpan Gu, Weihan Zhang, Yongjun Liu, Na Zhang
{"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,&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.2023.100012","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}
引用次数: 0
Investigation of wound healing and anti-inflammatory activity of Senna occidentalis leaf extract, and in silico screening for both activities 西泻叶提取物创面愈合和抗炎活性的研究,并对其进行了计算机筛选
Pharmaceutical Science Advances Pub Date : 2023-10-14 DOI: 10.1016/j.pscia.2023.100016
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 ,&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}
引用次数: 0
Potential application of sucrose acetate isobutyrate, and glyceryl monooleate for nanonization and bioavailability enhancement of rivaroxaban tablets 醋酸异丁酸蔗糖和单油酸甘油在利伐沙班片纳米化和提高生物利用度方面的潜在应用
Pharmaceutical Science Advances Pub Date : 2023-10-14 DOI: 10.1016/j.pscia.2023.100015
Adam A. Al-Shoubki , Mahmoud H. Teaima , Rehab Abdelmonem , Mohamed A. El-Nabarawi , Sammar Fathy Elhabal
{"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}
引用次数: 0
Structure, functions, and recent advances in the development of SIRT2 inhibitors SIRT2抑制剂的结构、功能及开发进展
Pharmaceutical Science Advances Pub Date : 2023-09-09 DOI: 10.1016/j.pscia.2023.100010
Junxin Xue, Xuben Hou, Hao Fang
{"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<sup>+</sup>). 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}
引用次数: 0
Ab initio modeling and ligand docking of quercetin and the MC-LR transporter protein Oatp1b2/OATP1B3 槲皮素与MC-LR转运蛋白Oatp1b2/OATP1B3的从头算建模及配体对接
Pharmaceutical Science Advances Pub Date : 2023-09-09 DOI: 10.1016/j.pscia.2023.100011
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 ,&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}
引用次数: 0
Blockage of HSP90 and IDO1 pathway by α-MSH modified nanoelicitor to dual-facilitate mild photothermal therapy α-MSH修饰的纳米激发子阻断HSP90和IDO1通路双重促进温和光热治疗
Pharmaceutical Science Advances Pub Date : 2023-07-22 DOI: 10.1016/j.pscia.2023.100009
Shunli Fu, Qingping Ma, Jiangnan Li, Yifan Wang, Chunyan Yang, Panpan Gu, Weihan Zhang, Yongjun Liu, Na Zhang
{"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}
引用次数: 0
Controlled release of bilayer tablet comprising vitamin B6 rapid-release layer and melatonin sustained-release layer 含有维生素B6快速释放层和褪黑素缓释层的双层片剂的控释
Pharmaceutical Science Advances Pub Date : 2023-05-15 DOI: 10.1016/j.pscia.2023.100008
Yan Wang , Jiaqi Xu , Nan Gao , Hongqian Lv , Minge Sun , Peng Zhang
{"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 B<sub>6</sub> 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 B<sub>6</sub> 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}
引用次数: 0
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