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Effect of Surface Modification with Na Lauryl Sulfate on The Water-Uptake and Release Properties of Na Tripolyphosphate-Cross Linked Chitosan Beads 十二烷基硫酸钠表面改性对三磷酸钠交联壳聚糖微珠吸水和释放性能的影响
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-07-24 DOI: 10.35516/jjps.v16i2.1543
Wasan Alwahsh, Mai Jaber, Suha Al Muhaissen, Bashar Al-khalidi, S. Sahudin, Hatim S Alkhatib
In this study we evaluated the effect of Na Lauryl sulfate (SLS) on the water-uptake and release properties of Na Tripolyphosphate (TPP)-cross linked chitosan beads. Chitosan beads were prepared by dropping riboflavin-loaded, chitosan (CS) solution into a curing medium composed of either an aqueous solution of TPP, SLS or a combination of these solutes. The resultant beads were characterized in terms of their size, drug encapsulation efficiency, water uptake properties by gravimetry and image analysis. Drug release properties of the prepared beads were studied using USP Apparatus 1 in media with different pH and ionic strength. Composites (CS/TPP, CS/SLS, and CS/TPP/SLS) were also evaluated using DSC, FTIR and contact angle measurements. Encapsulation efficiency was found to be 93%, 93.2% and 93.1% for CS/TPP, CS/SLS, and CS/TPP/SLS beads respectively and did not show any dependence on the composition of the curing medium for riboflavin. FTIR data suggested the presence of electrostatic interactions between positively charged amine group of CS and the negatively charged TPP and SLS. Drug release from the prepared beads was prolonged with CS/SLS beads releasing the drug faster than CS/TPP beads. The slowest drug release was observed in the case of CS/TPP/SLS beads. Drug release from the different types of beads was pH-dependent with the fastest release observed in 0.1 N HCl. Gravimetric water uptake was highest for CS/SLS beads followed by CS/TPP and CS/TPP/SLS respectively. Swelling study using image analysis showed a similar trend to the gravimetric water uptake results. The drug release and water uptake results could be explained by the effect of SLS on the wettability of the beads and the ability of the release medium to hydrate them which was confirmed by the high contact angle between water and CS/TPP/SLS composites.
研究了十二烷基硫酸钠(SLS)对三聚磷酸钠(TPP)交联壳聚糖微球吸水和释水性能的影响。将装载核黄素的壳聚糖(CS)溶液滴入由TPP、SLS水溶液或这些溶质的组合组成的固化介质中,制备壳聚糖微球。用重量法和图像分析对所得微球的粒径、包封率、吸水性能等进行了表征。用USP仪器1研究了制备的微球在不同pH和离子强度介质中的释药性能。复合材料(CS/TPP、CS/SLS和CS/TPP/SLS)也通过DSC、FTIR和接触角测量进行了评估。CS/TPP、CS/SLS和CS/TPP/SLS微球的包封率分别为93%、93.2%和93.1%,与核黄素固化介质的组成无关。FTIR数据表明,CS中带正电的胺基与带负电的TPP和SLS之间存在静电相互作用。CS/SLS微球的释药速度比CS/TPP微球快,延长了微球的释药时间。CS/TPP/SLS微珠的释药速度最慢。不同类型微球的药物释放呈ph依赖性,在0.1 N HCl中释放最快。CS/SLS的吸水率最高,其次是CS/TPP和CS/TPP/SLS。使用图像分析的溶胀研究显示了与重力吸水结果相似的趋势。水与CS/TPP/SLS复合材料的高接触角证实了SLS对微珠润湿性的影响和释放介质对微珠的水化作用。
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引用次数: 0
Investigations of Lipid Droplets Role in Attenuating Chemotherapeutic Responses to 5-FU in Cancer Cells in vitro 脂滴在减轻癌症细胞对5-FU化疗反应中的作用研究
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-07-24 DOI: 10.35516/jjps.v16i2.1509
Duaa Sabbah
Cancer has been considered as a main cause of death worldwide. Despite the effectiveness of traditional anticancer therapies such as 5-Flurouracil (5-FU), poor therapeutic outcomes are reported in many cases, due to tumor recurrence and chemoresistance. Intracellular lipid accumulation as lipid droplets (LDs) is now a well-recognized hallmark of cancer. However, the influence of LDs accumulation in cancer progression and treatment remains to be elucidated. Adjuvant use of non-chemotherapeutic drugs (e.g. NSAIDs and corticosteroids) with anticancer drugs to manage cancer related symptoms, may though serve as factors modulating the therapeutic response to anticancer agents via LDs related mechanisms. The aim of this study is to evaluate possible strategies influencing chemoresistance by attenuating LDs biogenesis and function. LDs levels in eight human cancer cell lines were measured. The existence of correlation between the cellular levels of LDs and cytotoxicity of ten chemotherapeutic agents was evaluated. A moderate correlation between basal LDs levels and the half inhibitory concentration (IC50) values of 5-FU on selected cell lines was established (r2= 0.5235). Nevertheless, LDs levels were significantly elevated following exposure to 5-FU. A549 human lung cancer cells showed the highest increase in LD accumulation (***P >0.001) compared to their basal levels of LDs. LDs levels were also assessed following exposure to 5-FU in the presence of sub-lethal doses of celecoxib (CXB), dexamethasone (DEX), and simvastatin (SMV). Interestingly, CXB and DEX exposure to 5-FUtreated cells resulted in an alleviation in the antiproliferative activities of 5-FU in MDA-MB-468 and HCT116 but not in A549 cells. While, SMV exposure to 5-FU-treated cells resulted in reduced antiproliferative activities of 5-FU in MDA-MB-468 only. These results strongly suggest that increased LDs levels caused by CXB, DEX, and SMV may contribute in the development of a resistance mechanism exist only in some cancer types, which therefore, attenuates responses to 5- FU. The inhibition of phospholipid metabolism by DEX, as well as the inhibition of 3-hydroxy-3- methylglutaryl-CoA reductase (HMGCR) by SMV were expected to result in the up regulation of triacylglycerol (TAG), leading to LDs accumulation. This study highlights the importance of assessing drug-drug interaction before designing integrated therapy regimens for cancer patients receiving 5-FU treatment. Further studies are needed to discover the role of TAG inhibition on the sensitivity of cancer cells against 5-FU.
癌症一直被认为是世界范围内死亡的主要原因。尽管5-氟尿嘧啶(5-FU)等传统抗癌疗法有效,但由于肿瘤复发和化疗耐药,许多病例的治疗效果不佳。细胞内脂质以脂滴(ld)的形式积聚是目前公认的癌症的标志。然而,LDs积累对癌症进展和治疗的影响仍有待阐明。辅助使用非化疗药物(如非甾体抗炎药和皮质类固醇)与抗癌药物来控制癌症相关症状,可能通过ld相关机制调节抗癌药物的治疗反应。本研究的目的是评估可能影响化疗耐药的策略,通过降低lld的生物发生和功能。测定了8种人类癌细胞系的ld水平。对10种化疗药物的细胞毒性与LDs细胞水平之间是否存在相关性进行了评价。在选定的细胞株上,5-FU的半数抑制浓度(IC50)值与基础LDs水平呈中等相关性(r2= 0.5235)。然而,暴露于5-FU后,ld水平显著升高。与基础LD水平相比,A549人肺癌细胞的LD积累增加最多(***P < 0.001)。在亚致死剂量塞来昔布(CXB)、地塞米松(DEX)和辛伐他汀(SMV)存在的情况下暴露于5-FU后,还评估了ld水平。有趣的是,CXB和DEX暴露于5- fu处理的细胞导致5-FU在MDA-MB-468和HCT116中的抗增殖活性减轻,但在A549细胞中没有。然而,SMV暴露于5-FU处理的细胞只导致MDA-MB-468中5-FU的抗增殖活性降低。这些结果强烈提示,CXB、DEX和SMV引起的LDs水平升高可能促进了抗性机制的发展,这种机制仅存在于某些癌症类型中,因此减弱了对5- FU的反应。DEX对磷脂代谢的抑制,以及SMV对3-羟基-3-甲基戊二酰辅酶a还原酶(HMGCR)的抑制,预计会导致三酰甘油(TAG)的上调,导致ld的积累。这项研究强调了在为接受5-FU治疗的癌症患者设计综合治疗方案之前评估药物-药物相互作用的重要性。TAG抑制癌细胞对5-FU敏感性的作用有待进一步研究。
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引用次数: 0
Knowledge and Attitudes towards Antibiotic Usage 对抗生素使用的认识和态度
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-07-24 DOI: 10.35516/jjps.v16i2.1486
H. Hejaz
Background: Antibiotic resistance is a global problem, and the World Health Organization (WHO) has made this problem one of its priorities for solving. Repeated and improper use of antibiotics is the main reason for the bacteria's resistance to the drugs. Objectives: This study aimed to evaluate the knowledge, and attitudes of Palestinians regarding antibiotic usage and awareness about resistance. Methods: This was a cross-sectional study that targeted Palestinians from different cities. We used an online questionnaire which distributed randomly for data collection. The questionnaire consists of 52 questions to measure the knowledge, attitudes, and awareness of antibiotic use and resistance. Statistical Package for the Social Sciences (SPSS) version 25 was used to analyze the data collected. Results: A total of 744 participated in the study and completed the questionnaire, and the majority of them (60.5 %; n= 450 out of 744) were from the Hebron Governorate. The major of the respondents also were females (n= 653, 87.8%) and their age between 20-35 years old (n= 498, 66.9%) with a bachelor degree (n= 502, 67.5%). The majority of them (75.5%, n= 560) think that antibiotics should be given only by prescription, and about half of the people (52%= n= 387) believe that antibiotics are not safe. Most participants relied on the physician for dispensing the antibiotic (60.1%, n= 455) but the same percentage of them use leftover antibiotics that have been used previously. Four hundred eighty-three (65%, n= 483) who completed the questionnaire heard about the antibiotic resistance term from medical staff, and their main primary sources of information about antibiotics and medicines were from health staff too (50%, n= 371), then internet (25%, n= 185). Some people (16%, n= 119) mentioned that pharmacists have a role in educating them and providing all the necessary information, or advice about the use of medicines and the dangers of medication misuse. Most of the participants obtained the antibiotics by prescription from a doctor (n= 339, 45.6%), then from the Pharmacist (n= 91, 12.2%), and 63 persons (8.5%) purchases them on their own. Quite a high number of participants (n= 348, 46.8%) stop taking antibiotics when they start feeling better. According to the results obtained, social media was the primary source of information regarding antibiotic resistance. Conclusions: Higher education, younger age, gender, profession, and a high monthly income were associated significantly with good knowledge and a positive attitude toward antibiotic use. Educational interventions for appropriate antibiotic use are needed all the time and enforcing antibiotics regulations should be also considered to reduce antibiotic resistance.
背景:抗生素耐药性是一个全球性问题,世界卫生组织(WHO)已将这一问题列为其优先解决的问题之一。反复和不当使用抗生素是细菌耐药的主要原因。目的:本研究旨在评估巴勒斯坦人对抗生素使用和耐药性认识的知识和态度。方法:这是一项针对来自不同城市的巴勒斯坦人的横断面研究。我们采用随机分布的在线问卷进行数据收集。问卷包括52个问题,用于衡量对抗生素使用和耐药性的知识、态度和意识。使用SPSS (Statistical Package for the Social Sciences)第25版对收集到的数据进行分析。结果:共有744人参与研究并完成问卷调查,其中绝大多数(60.5%;744人中有450人来自希布伦省。受访者的专业也以女性为主(n= 653, 87.8%),年龄在20-35岁之间(n= 498, 66.9%),本科学历(n= 502, 67.5%)。其中大多数人(75.5%,n= 560)认为抗生素只能凭处方使用,约一半的人(52%= n= 387)认为抗生素不安全。大多数参与者依赖医生分配抗生素(60.1%,n= 455),但他们使用以前使用过的剩余抗生素的比例相同。483人(65%,n= 483)从医务人员那里听说了抗生素耐药术语,其抗生素和药物信息的主要来源也是医务人员(50%,n= 371),其次是互联网(25%,n= 185)。一些人(16%,n= 119)提到,药剂师在教育他们和提供所有必要的信息或关于药物使用和药物滥用危险的建议方面发挥着作用。其中,通过医生处方获得抗生素者最多(339人,占45.6%),其次是药剂师(91人,占12.2%),自行购买者63人(8.5%)。相当多的参与者(n= 348, 46.8%)在感觉好转后停止服用抗生素。根据获得的结果,社交媒体是有关抗生素耐药性的主要信息来源。结论:高学历、年龄、性别、职业和高月收入与抗菌药物使用知识和积极态度显著相关。始终需要适当使用抗生素的教育干预措施,还应考虑执行抗生素法规以减少抗生素耐药性。
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引用次数: 0
QCARxE: Qatar-based cardiovascular risk assessment using the English/Arabic version of the EPI·RxISK™ mobile application QCARxE:基于卡塔尔的心血管风险评估,使用EPI·RxISK™移动应用程序的英语/阿拉伯语版本
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-07-24 DOI: 10.35516/jjps.v16i2.1534
Lana Kattan
Background: Cardiovascular disease (CVD) is the leading cause of death worldwide, accounting for almost one-third of the total global deaths. Early CVD risk assessment and management (RAM) has demonstrated to be effective in decreasing CVD-related burden. However, CVDRAM services face many challenges and barriers in the community. Mobile technology has been advocated to facilitate access to CVDRAM for both healthcare providers and patients to overcome these barriers. Nevertheless, there is limited availability and use of CVDRAM-related mobile technology in the Middle East region. Objectives: To develop and implement an English and Arabic version of a mobile and a web application for CVDRAM in both, community pharmacies and selected primary care centres in Qatar. Methodology: This study was conducted in two phases. In Phase 1, translation of the EPI·RxISK™ CV risk calculator (ERC) into the Arabic language was conducted based on guidelines developed by the International Society for Pharmacoeconomics and Outcomes Research. The English/Arabic version of the ERC was pilot tested by potential end users, consisting of a sample of community pharmacists (CRxs) and members of the public (MOP) accessing community pharmacy services. Semi-structured interviews were conducted based on the constructs of the Mobile Application Rating Scale (MARS) and data were analyzed using deductive content analysis. In Phase 2, a prospective observational study (QCARxE) is underway to explore the feasibility of using the ERC in patients accessing primary health care services for CVDRAM, including community pharmacies and primary health care centers (PHCC). Results: In Phase 1, a total of 10 CRxs and 5 MOP were interviewed. The data derived from the interviews indicate that the ERC web and mobile application were overall, positively perceived as having quality engagement, functionality, aesthetics, information and subjective quality attributes. To date, a total of 36 patients have enrolled in the QCARxE study (20 from PHCC and 16 from community pharmacies). At their initial CVD risk assessment visit, the mean CVD risk score for these patients was 28.3%, and the most prevalent risk factor was obesity (mean BMI = 30.2 kg/m²). Conclusion: The themes derived from the interviews indicate that the ERC was overall, positively perceived. Preliminary data derived from the QCARxE study indicated a significant proportion of patients accessing primary health care services are at high CVD risk. It is speculated that the use of the ERC will enable patients to become better aware of their CVD risk and improve access to risk factor interventions.
背景:心血管疾病(CVD)是世界范围内死亡的主要原因,几乎占全球总死亡人数的三分之一。早期心血管疾病风险评估和管理(RAM)已被证明在减少心血管疾病相关负担方面是有效的。然而,CVDRAM服务在社区中面临着许多挑战和障碍。移动技术已被提倡,以促进访问CVDRAM为医疗保健提供者和患者克服这些障碍。然而,在中东地区,与cvdram相关的移动技术的可用性和使用有限。目标:在卡塔尔的社区药房和选定的初级保健中心开发和实施CVDRAM移动和网络应用程序的英语和阿拉伯语版本。方法:本研究分为两个阶段进行。在第一阶段,EPI·RxISK™CV风险计算器(ERC)翻译成阿拉伯语是根据国际药物经济学和结果研究协会制定的指南进行的。ERC的英文/阿拉伯语版本在潜在最终用户中进行了试点测试,这些最终用户包括社区药剂师(CRxs)和使用社区药房服务的公众(MOP)。基于移动应用评级量表(MARS)的结构进行半结构化访谈,并使用演绎内容分析对数据进行分析。在第二阶段,一项前瞻性观察性研究(QCARxE)正在进行中,以探索在获得CVDRAM初级卫生保健服务的患者中使用ERC的可行性,包括社区药房和初级卫生保健中心(PHCC)。结果:在第一阶段,共采访了10名CRxs和5名MOP。从访谈中获得的数据表明,ERC网络和移动应用程序总体上被积极地认为具有质量粘性、功能、美学、信息和主观质量属性。迄今为止,共有36名患者参加了QCARxE研究(20名来自PHCC, 16名来自社区药房)。在他们最初的心血管疾病风险评估访问中,这些患者的平均心血管疾病风险评分为28.3%,最普遍的危险因素是肥胖(平均BMI = 30.2 kg/m²)。结论:从访谈中得出的主题表明,ERC总体上是积极的。来自QCARxE研究的初步数据表明,获得初级卫生保健服务的患者中有很大一部分是心血管疾病高风险人群。据推测,ERC的使用将使患者更好地意识到他们的心血管疾病风险,并改善获得风险因素干预的机会。
{"title":"QCARxE: Qatar-based cardiovascular risk assessment using the English/Arabic version of the EPI·RxISK™ mobile application","authors":"Lana Kattan","doi":"10.35516/jjps.v16i2.1534","DOIUrl":"https://doi.org/10.35516/jjps.v16i2.1534","url":null,"abstract":"Background: Cardiovascular disease (CVD) is the leading cause of death worldwide, accounting for almost one-third of the total global deaths. Early CVD risk assessment and management (RAM) has demonstrated to be effective in decreasing CVD-related burden. However, CVDRAM services face many challenges and barriers in the community. Mobile technology has been advocated to facilitate access to CVDRAM for both healthcare providers and patients to overcome these barriers. Nevertheless, there is limited availability and use of CVDRAM-related mobile technology in the Middle East region. \u0000Objectives: To develop and implement an English and Arabic version of a mobile and a web application for CVDRAM in both, community pharmacies and selected primary care centres in Qatar. \u0000Methodology: This study was conducted in two phases. In Phase 1, translation of the EPI·RxISK™ CV risk calculator (ERC) into the Arabic language was conducted based on guidelines developed by the International Society for Pharmacoeconomics and Outcomes Research. The English/Arabic version of the ERC was pilot tested by potential end users, consisting of a sample of community pharmacists (CRxs) and members of the public (MOP) accessing community pharmacy services. Semi-structured interviews were conducted based on the constructs of the Mobile Application Rating Scale (MARS) and data were analyzed using deductive content analysis. In Phase 2, a prospective observational study (QCARxE) is underway to explore the feasibility of using the ERC in patients accessing primary health care services for CVDRAM, including community pharmacies and primary health care centers (PHCC). \u0000Results: In Phase 1, a total of 10 CRxs and 5 MOP were interviewed. The data derived from the interviews indicate that the ERC web and mobile application were overall, positively perceived as having quality engagement, functionality, aesthetics, information and subjective quality attributes. To date, a total of 36 patients have enrolled in the QCARxE study (20 from PHCC and 16 from community pharmacies). At their initial CVD risk assessment visit, the mean CVD risk score for these patients was 28.3%, and the most prevalent risk factor was obesity (mean BMI = 30.2 kg/m²). \u0000Conclusion: The themes derived from the interviews indicate that the ERC was overall, positively perceived. Preliminary data derived from the QCARxE study indicated a significant proportion of patients accessing primary health care services are at high CVD risk. It is speculated that the use of the ERC will enable patients to become better aware of their CVD risk and improve access to risk factor interventions.","PeriodicalId":14719,"journal":{"name":"Jordan Journal of Pharmaceutical Sciences","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45976532","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
Planar Waveguide NMR Gradients (B0 and B1) for spatiotemporal Investigations of Anticancer Drug Concentration in 3D Cancer Cell Cultures 平面波导NMR梯度(B0和B1)用于三维癌症细胞培养物中抗癌药物浓度的时空研究
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-07-24 DOI: 10.35516/jjps.v16i2.1487
A. Telfah, Nour Sharar, Hanan Jafar, R. Hergenröder
Despite the progression in cancer therapeutic approaches, cancer is still the leading cause of death worldwide with a steadily increasing incidence rate. In Jordan, CRC is the most common type of cancer among men and the second most common among women, while being one of the most accruing cancers in Germany. The difficulties in cancer treatments arise from the poor correlation between in vivo and in in vitro anti-cancer drug testing results and cancer cells resistance to chemotherapy, which are attributed to the heterogeneity of cancer cells, and the interaction of cancer cells with non-cancerous cells in the tumor microenvironment (TME). In addition to, the several mechanisms, that governs DNA damages repair, epigenetics, epithelial to mesenchymal transition (EMT). Cell culture techniques have been developed to construct in vitro multicellular cancer spheroids (MTCS) that mimic cell-cells interaction and the cellular organization in the TME. They also illustrate the proliferation gradient of solid tumors, and the nutrition and gas supply to cancer cells at different depth in the spheroid. Therefore, they are considered an excellent in vitro cancer model to study the efficiency and to investigate the penetration depth of the anti-cancer materials. Nuclear Magnetic Resonance (NMR) spectroscopy is a reliable analytical method that gives comprehensive and rich chemical information, along with high speciation performance. It is one of the major noninvasive tools for metabolomics, therefore it has been utilized to study the metabolic profiling of freshly isolated- non-destructed tissues, and living in vitro cellular models. A micro-imaging technique for real-time NMR investigations is developed to study the penetration depth, rate, and effective diffusion coefficients of anti-cancer materials through cancer spheroids. This technique is based on our patented invention of planar waveguide micro slot NMR detector with on board thermal regulator integrated and a microfluidic device. Based on this innovative development, we are able to perform real-time magnetic resonance spectroscopic imaging (MRSI) on a living synthetic tissue constructed in micrometer scale to monitor drug penetration and diffusion, while providing spectroscopic information about the production and degradation of metabolites in picomoles concentrations.
尽管癌症治疗方法取得了进展,但癌症仍然是全球死亡的主要原因,发病率稳步上升。在约旦,结直肠癌是男性中最常见的癌症类型,女性中第二常见,同时也是德国发病率最高的癌症之一。癌症治疗的困难源于体内和体外抗癌药物测试结果与癌症细胞对化疗的耐药性之间的相关性差,这归因于癌症细胞的异质性,以及癌症细胞与肿瘤微环境(TME)中的非癌细胞的相互作用。此外,控制DNA损伤修复、表观遗传学、上皮-间充质转化(EMT)的几种机制。已经开发了细胞培养技术来构建体外多细胞癌症球体(MTCS),其模拟TME中的细胞-细胞相互作用和细胞组织。它们还说明了实体瘤的增殖梯度,以及球体中不同深度癌症细胞的营养和气体供应。因此,它们被认为是研究抗癌材料的有效性和渗透深度的一种优秀的癌症体外模型。核磁共振(NMR)光谱是一种可靠的分析方法,它能提供全面而丰富的化学信息,并具有高的物种形成性能。它是代谢组学的主要非侵入性工具之一,因此它已被用于研究新分离的未破坏组织的代谢谱和体外活细胞模型。开发了一种用于实时NMR研究的微成像技术,以研究抗癌材料通过癌症球体的穿透深度、速率和有效扩散系数。这项技术是基于我们的专利发明平面波导微槽核磁共振检测器,集成了板载热调节器和微流体设备。基于这一创新发展,我们能够在微米级构建的活体合成组织上进行实时磁共振波谱成像(MRSI),以监测药物渗透和扩散,同时提供有关皮摩尔浓度代谢物产生和降解的光谱信息。
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引用次数: 0
Implication of Nanotechnology for Pulmonary Delivery of Docetaxel 纳米技术在多西他赛肺部给药中的应用
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-07-24 DOI: 10.35516/jjps.v16i2.1527
Alaa Abudayah
Docetaxel (Taxotere®) is a taxoid antineoplastic agent used in the treatment of various cancers. Docetaxel belongs to class IV drugs in the Biopharmaceutics Classification System (BCS), and their clinical use is limited due to their extreme hydrophobicity, low water solubility, low bioavailability, and high toxicity. This study aims to prepare nanoparticles for pulmonary delivery of Docetaxel with enhanced solubility and dissolution targeting pulmonary tissues. Accordingly, PLGA-Docetaxel nanoparticles (NPs) were prepared by nanoprecipitation method and coated with Carboxymethyl chitosan to investigate its effectiveness as inhaled anticancer therapy. Four formulations had been prepared to reach the highest loading capacity (LC%) and encapsulation efficiency (EE%) and to study the effect of the amount of Carboxymethyl chitosan on the drug release. The sizes, charges, homogeneity, surface morphology, LC% and EE% of the NPs were determined. The NPs were characterized using FTIR and XRD. In vitro release profiles of Docetaxel from PLGA NPs, at pH 5.5, 6.5, and 7.4 were determined. The sizes of the four formulations ranged between 227.7± 9.5 and 306.4 ± 27.4. All prepared formulations showed acceptable monodispersity with positive charges. The EE% was above 99% and the LC% ranged between 31-63%. The in vitro release of Docetaxel show an inverse relation to the amounts of Carboxymethyl chitosan used and the pH of the dissolution medium. In conclusion, coating PLGA NPs with Carboxymethyl chitosan may be used as a good carrier for pulmonary delivery of Docetaxel
多西他赛(Taxotere®)是一种用于治疗各种癌症的类taxetaxel抗肿瘤药物。多西紫杉醇在生物制药分类系统(BCS)中属于IV类药物,由于其极疏水性、低水溶性、低生物利用度和高毒性,其临床应用受到限制。本研究旨在制备多西紫杉醇肺递送纳米颗粒,增强其溶解度和溶出性,靶向肺组织。为此,采用纳米沉淀法制备了plga -多西紫杉醇纳米颗粒(NPs),并以羧甲基壳聚糖包被,研究其吸入抗癌效果。以羧甲基壳聚糖的最高载药量(LC%)和包封率(EE%)为目标,研究了羧甲基壳聚糖用量对药物释放的影响。测定了NPs的尺寸、电荷、均匀性、表面形貌、LC%和EE%。用FTIR和XRD对NPs进行了表征。测定多西他赛在pH为5.5、6.5和7.4时在PLGA NPs中的体外释放谱。四种剂型的大小范围为227.7±9.5 ~ 306.4±27.4。所有制备的配方均表现出可接受的带正电荷的单分散性。EE%在99%以上,LC%在31 ~ 63%之间。多西紫杉醇的体外释放量与羧甲基壳聚糖的用量和溶出介质的pH值成反比。综上所述,羧甲基壳聚糖包覆PLGA NPs可作为多西紫杉醇肺给药的良好载体
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引用次数: 0
Preparation of Semi-Solid Dosage Forms Containing Psidium Guava Leaves Extract as Antimicrobial Preservative 番石榴叶提取物抗菌防腐剂半固体剂型的制备
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-07-24 DOI: 10.35516/jjps.v16i2.1499
F. Al-Rimawi, Mohammad A. Atieh
Guava leaves extract has several medicinal activities as antimicrobial, antioxidant, anti-cancer and anti-inflammatory. Several studies have been proposed to use guava leaves extract in several preparations. However, applying guava leaves extract as a preservative in a pharmaceutical product has not been studied previously. In the present work, Guava leaves extract was used as natural preservative instead of chemical ones (methyl and propyl paraben). Guava leaves were extracted with ethanol 95% as extraction solvent with a percentage yield of 20%. This extract was tested by HPLC; several phenolic compounds were detected. To determine the ability to use this extract as a preservative, antimicrobial effectiveness test (preservative efficacy test) was conducted for extracted powder in purified water at different concentrations (0.5, 1.0, 1.5, and 2.0 % w/w), against three bacteria, one gram-positive (S. aureus), two gram-negative (P. aeruginosa, E. coli) and two fungi: one yeast (Candida albicans) and one mold (Aspergillus (Niger) brasiliensis). Results showed that 2% was effective and passed the test of preservative effectiveness test; this concentration was used in semi-solid pharmaceutical products. For this purpose, six different preparations (Ketoconazole shampoo, Clotrimazole Cream, Permethrin Cream, Gentamycin Cream, Ibuprofen gel, Indomethacin emulgel) were used. Chemical preservative was replaced by natural one (guava leaves extract powder) to serve as a preservative. Three out of the six preparations (Ketoconazole shampoo, Clotrimazole Cream, Ibuprofen gel,) passed preservative efficacy test. These preparations were fully checked-up by chemical (drug content,) physical (odor, physical appearance) and biological test (total count test) for three months at accelerated conditions. These results confirmed that these pharmaceutical preparations were stable and effective. As a conclusion Guava leaves extract can be used at 2% as natural preservative instead of chemical ones which have adverse side effects on human health.
番石榴叶提取物具有抗菌、抗氧化、抗癌、抗炎等多种药用活性。一些研究建议在几种制剂中使用番石榴叶提取物。然而,将番石榴叶提取物作为防腐剂应用于医药产品中还没有研究。本研究采用番石榴叶提取物作为天然防腐剂代替化学防腐剂(对羟基苯甲酸甲酯和丙酯)。以95%乙醇为提取溶剂提取番石榴叶,提取率为20%。采用高效液相色谱法测定提取物;检测到几种酚类化合物。为了确定该提取物作为防腐剂的使用能力,对提取粉末在不同浓度(0.5、1.0、1.5和2.0% w/w)的纯净水中进行了抗菌效果试验(防腐效果试验),对三种细菌,一种革兰氏阳性(金黄色葡萄球菌),两种革兰氏阴性(铜绿假单胞菌、大肠杆菌)和两种真菌:一种酵母菌(白色念珠菌)和一种霉菌(巴西曲霉)进行了抗菌效果试验。结果表明,2%有效,通过了保鲜性试验;该浓度用于半固体药品。采用6种不同的制剂(酮康唑洗发水、氯霉唑乳膏、氯菊酯乳膏、庆大霉素乳膏、布洛芬凝胶、吲哚美辛乳膏)。用天然防腐剂(番石榴叶提取物粉末)代替化学防腐剂作为防腐剂。酮康唑洗发水、克曲霉唑乳膏、布洛芬凝胶等6种制剂中有3种通过了防腐效果试验。这些制剂在加速条件下进行了三个月的化学(药物含量),物理(气味,物理外观)和生物试验(总数试验)的全面检查。这些结果证实了这些药物制剂是稳定有效的。结论番石榴叶提取物可作为天然防腐剂,以2%的浓度代替对人体健康有不良影响的化学防腐剂。
{"title":"Preparation of Semi-Solid Dosage Forms Containing Psidium Guava Leaves Extract as Antimicrobial Preservative","authors":"F. Al-Rimawi, Mohammad A. Atieh","doi":"10.35516/jjps.v16i2.1499","DOIUrl":"https://doi.org/10.35516/jjps.v16i2.1499","url":null,"abstract":"Guava leaves extract has several medicinal activities as antimicrobial, antioxidant, anti-cancer and anti-inflammatory. Several studies have been proposed to use guava leaves extract in several preparations. However, applying guava leaves extract as a preservative in a pharmaceutical product has not been studied previously. In the present work, Guava leaves extract was used as natural preservative instead of chemical ones (methyl and propyl paraben). Guava leaves were extracted with ethanol 95% as extraction solvent with a percentage yield of 20%. This extract was tested by HPLC; several phenolic compounds were detected. To determine the ability to use this extract as a preservative, antimicrobial effectiveness test (preservative efficacy test) was conducted for extracted powder in purified water at different concentrations (0.5, 1.0, 1.5, and 2.0 % w/w), against three bacteria, one gram-positive (S. aureus), two gram-negative (P. aeruginosa, E. coli) and two fungi: one yeast (Candida albicans) and one mold (Aspergillus (Niger) brasiliensis). Results showed that 2% was effective and passed the test of preservative effectiveness test; this concentration was used in semi-solid pharmaceutical products. For this purpose, six different preparations (Ketoconazole shampoo, Clotrimazole Cream, Permethrin Cream, Gentamycin Cream, Ibuprofen gel, Indomethacin emulgel) were used. Chemical preservative was replaced by natural one (guava leaves extract powder) to serve as a preservative. Three out of the six preparations (Ketoconazole shampoo, Clotrimazole Cream, Ibuprofen gel,) passed preservative efficacy test. These preparations were fully checked-up by chemical (drug content,) physical (odor, physical appearance) and biological test (total count test) for three months at accelerated conditions. These results confirmed that these pharmaceutical preparations were stable and effective. As a conclusion Guava leaves extract can be used at 2% as natural preservative instead of chemical ones which have adverse side effects on human health.","PeriodicalId":14719,"journal":{"name":"Jordan Journal of Pharmaceutical Sciences","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-07-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42877078","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
Nuclear Magnetic Resonance for Targeted Metabolomics and Biochemical Sensor 核磁共振用于靶向代谢组学和生化传感器
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-07-24 DOI: 10.35516/jjps.v16i2.1519
Ahmed Bahti, A. Telfah, Nour Sharar, Hanan Jafar, R. Hergenröder
NMR spectroscopy is quantitative, highly reproducible, non-selective and non-destructive. However, NMR costs and complexity hinder a use as point-of-care and biochemical sensor instrumentation. Low field NMR (LF-NMR) is an inexpensive and low footprint technique to obtain physical, chemical, electronic and structural information on small molecules, but suffers from poor spectral dispersion, especially when applied to the analysis of mixtures. Subspectral editing employing optimal control pulses is a suitable approach to cope with the severe signal superpositions in complex mixture spectra at low field. We have calculated the optimal control pulse shapes at 0.5 T NMR frequency using the Krotov algorithm. Downsizing the complexity of the algorithm from exponential to polynomial is shown to be possible by using a system approach with each system corresponding to a (small) molecule. In this way compound selective excitation pulses can be calculated. The signals of substructures of the cyclopentenone molecule were excited using optimal control pulses calculated by the Krotov algorithm demonstrating the feasibility of subspectral editing. Likewise, for a mixture of benzoic acid and alanine, editing of the signals of either benzoic acid or alanine employing optimal control pulses was shown to be possible. The obtained results are promising and can be extended to the targeted analysis of complex mixtures such as biofluids or metabolic samples at low field strengths opening access for benchtop NMR to point of care settings. Moreover, the LF-NMR was improved to allow a unique detection and reliable quantification of metabolites in biofluids like blood, urine, cerebrospinal fluid, or even tissue. In contrast to standard large scale NMR equipment the portable LF-NMR allows for an analysis of the chemical composition of biofluid samples directly at the patient (point-of-care). LF-NMR can be freely programmable for detecting and detecting and sensing sets of small molecules which deliver information on the health status of a person. Such an analytical tool would be useful for the prediction, diagnosis, monitoring and prognosis of diseases, and for supervision of therapeutic interventions.
核磁共振光谱是定量的,高重复性的,非选择性和非破坏性的。然而,核磁共振的成本和复杂性阻碍了它作为即时护理和生化传感器仪器的使用。低场核磁共振(LF-NMR)是一种廉价、低足迹的技术,可获得小分子的物理、化学、电子和结构信息,但其光谱色散较差,特别是在用于分析混合物时。采用最优控制脉冲进行子谱编辑是处理低场复杂混合光谱中严重信号叠加的有效方法。我们利用Krotov算法计算了0.5 T核磁共振频率下的最优控制脉冲形状。通过使用系统方法,每个系统对应一个(小)分子,可以将算法的复杂性从指数级降低到多项式级。用这种方法可以计算复合选择性激励脉冲。利用Krotov算法计算的最优控制脉冲激发环戊酮分子的子结构信号,证明了子谱编辑的可行性。同样,对于苯甲酸和丙氨酸的混合物,使用最优控制脉冲编辑苯甲酸或丙氨酸的信号被证明是可能的。所获得的结果是有希望的,可以扩展到复杂混合物的目标分析,如生物流体或代谢样品在低场强打开访问台式核磁共振到护理点设置。此外,LF-NMR经过改进,可以对血液、尿液、脑脊液甚至组织等生物体液中的代谢物进行独特的检测和可靠的定量。与标准的大型核磁共振设备相比,便携式LF-NMR允许直接在患者(护理点)分析生物流体样品的化学成分。LF-NMR可以自由编程,用于检测、检测和传感小分子集,这些小分子集可以传递关于人的健康状况的信息。这种分析工具将有助于疾病的预测、诊断、监测和预后,以及对治疗干预措施的监督。
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引用次数: 0
A Comparative Study of in Vitro Lipoxygenase Inhibition and DPPH (1, 1-Diphenyl-2-Picrylhydrazyl) Free Radical Scavenging Activity of Silybum marianum and [Notobasis syriaca (L.) Cass.] Fruits and Linum usitatisimum Seeds 水飞蓟和丁香对体外脂氧合酶抑制及清除DPPH(1,1 -二苯基-2-苦酰肼基)自由基活性的比较研究卡斯。果实和亚麻种子
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-07-24 DOI: 10.35516/jjps.v16i2.1500
M. Alshieka, R. Jandali, Mohammad Isam Hasan Agha
Silybum marianum and Notobasis Syriaca belong to the most widespread thorny plants in the Middle East, the Mediterranean, and large areas of Asia. Both plants are derived from the Asteraceae family, while Flax seed (Linum usitatissmum L.) is belong to the family of Linaceae. The aim of this study was to compare the scavenging activity of free radicals, and to evaluate the anti-inflammatory activity of the fruit in vitro compared with flax seed. Methanol and ethanol extracts were prepared and the activity of scavenging free radicals was studied using DPPH, and the anti-inflammatory activity was investigated in-vitro using soybean lipoxygenase, in comparison with quercetin and Lignin as standards. The fruit extract from Notobasis Syriaca has the highest capacity to scavenge free radical DPPH (IC50=22.1 μg/ml), and it has higher ability to inhibit soybean lipoxygenase in-vitro (IC50= 2.7 μg/ml) than fruit extract from Silybum marianum (IC50= 9.8 μg/ml). This study showed that Silybum marianum and Notobasis Syriaca have a high ability to scavenge free radicals; and that both plants possess anti-inflammatory properties, while the scavenging potential of free radicals expressed in terms of IC50 (μg/ml) of flax seed showed extraction with a mixture of equal volumes of diethyl ether and ethyl acetate after direct acid hydrolysis exhibited higher antioxidant capacity (IC50=22.257±0.095 μg/ml). The median inhibitory concentration (IC50) was calculated according to the LOX enzyme inhibitory method. The IC50 value of a mixture of equal volumes of diethyl ether and ethyl acetate after direct acid hydrolysis extract of flaxseeds is 73.689±0.585 μg/ml. As final conclusion it was found that flax seed extract has the highest anti-inflammatory activity.
水飞蓟和叙利亚水飞蓟是中东、地中海和亚洲大部分地区分布最广的多刺植物。这两种植物都来自菊科,而亚麻籽(Linum usitatissmum L.)属于亚麻科。本研究的目的是比较其对自由基的清除能力,并评价其与亚麻籽的体外抗炎活性。制备甲醇和乙醇提取物,用DPPH法研究其清除自由基的活性,用大豆脂氧合酶法研究其体外抗炎活性,并以槲皮素和木质素为对照。丁香果提取物对自由基DPPH的清除能力最高(IC50=22.1 μg/ml),对大豆脂氧合酶的体外抑制能力(IC50= 2.7 μg/ml)高于水飞蓟果提取物(IC50= 9.8 μg/ml)。研究表明,水飞蓟和叙利亚香具有较强的自由基清除能力;两种植物均具有抗炎作用,而以亚麻籽IC50 (μg/ml)表示的自由基清除电位表明,直接酸水解后,等体积乙醚和乙酸乙酯混合提取物具有更高的抗氧化能力(IC50=22.257±0.095 μg/ml)。根据LOX酶抑制法计算中位抑制浓度(IC50)。亚麻籽直接酸水解提取液经等体积乙醚与乙酸乙酯混合后的IC50值为73.689±0.585 μg/ml。最后得出结论,亚麻籽提取物具有最高的抗炎活性。
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引用次数: 0
Compliance with Antimicrobial Prophylaxis Guidelines in Endourological Procedures: Frequency and Related Outcomes 尿内外科手术中抗菌药物预防指南的依从性:频率和相关结果
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2023-07-24 DOI: 10.35516/jjps.v16i2.1541
Sondos Abdaljaleel, M. Abdeljalil, O. Awwad, Ghazi Al Edwan, M. Amaireh, Manar Hamdan, A. Khattab, Tasneem Al-Hourani
Introduction: Surgical antimicrobial prophylaxis (SAP), when used appropriately based on evidence-based guidelines, reduces the rate of infectious complications following endourological procedures without compromising patient outcomes. Aims: to audit the appropriateness of the current SAP used in endourological surgeries based on international guidelines and report their associated outcomes (urinary tract infection (UTI) and bloodstream infection (BSI)). Methodology: The adherence to international guidelines recommendations; AUA 2019 and EAU 2020, regarding indication, duration, choice, and dose of the antibiotics used in endourological procedures were assessed in two medical centers in Amman/Jordan. Also, patients were asked to conduct laboratory urine test to determine the rate of infectious complications within one-month post-procedure. Results: Three hundred sixty-one patients were recruited for the study. The adherence rate to guidelines regarding indication, choice, and dose of pre-operative antibiotics was 90.3%, 2.8%, and 77.8% respectively. The duration was concordant with guidelines in only 3.4% of participants. A total of 41.8% of patients completed follow-up. Among those, 4.6% developed bacterial UTIs, and 0.7% developed BSI. Conclusion: Adherence to SAP guidelines in endourological procedures is far from optimal, especially by an inappropriate selection of broad-spectrum antibiotics as the agent of choice and prolonged use of antibiotics after the procedure in the absence of any documented infectious complication.
引言:如果根据循证指南适当使用外科抗菌药物预防(SAP),可以在不影响患者预后的情况下降低泌尿外科手术后感染性并发症的发生率。目的:根据国际指南,审计目前在泌尿外科手术中使用SAP的适当性,并报告其相关结果(尿路感染(UTI)和血流感染(BSI))。方法:遵守国际准则的建议;在安曼/约旦的两个医疗中心评估了2019年AUA和2020年EAU在泌尿外科手术中使用的抗生素的适应症、持续时间、选择和剂量。此外,患者被要求在手术后一个月内进行实验室尿液测试,以确定感染性并发症的发生率。结果:本研究共招募了361名患者。术前抗生素的适应症、选择和剂量对指南的依从率分别为90.3%、2.8%和77.8%。只有3.4%的参与者的持续时间与指南一致。共有41.8%的患者完成了随访。其中,4.6%发生细菌性尿路感染,0.7%发生BSI。结论:在腔内泌尿外科手术中遵守SAP指南远不是最佳的,尤其是不适当地选择广谱抗生素作为首选药物,以及在没有任何感染并发症的情况下在手术后长期使用抗生素。
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引用次数: 0
期刊
Jordan Journal of Pharmaceutical Sciences
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