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Safety Profile of Molnupiravir with Significant Effect on COVID-19: A Review 莫努匹拉韦对COVID-19疗效显著的安全性综述
IF 0.6 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-24 DOI: 10.2174/1574885518666230124123054
A. Pattnaik, Tuhin Mukherjee, Payel Mal, Abhay Kumar Upadhyay, Satyajit Mohanty, Nikita Nayak, Ravi Pratap Singh, Tanisha Das, Sourav Basak
As the COVID era unfolds, researchers reveal that rapid changes in viral genetic material allow viruses to circumvent challenges triggered by the host immune system and resist anti-viral drugs, potentially leading to persistent viral manifestations in host cells. Molnupiravir (RNA-dependent RNA polymerase inhibitor) is a novel anti-viral medicine promising a vital role in coming setbacks.This review aims to clarify the safety and efficacy of the molnupiravir molecule in light of existing case studies. As a result, it is intended to explore and discuss the molecular structure, mechanism of action, discovery and development process, preclinical research, clinical investigations, and other subtopics.A total of 75 publications were searched using multiple engines, such as Google Scholar, PubMed, Web of Science, Embase, Cochrane Library, ClinicalTrials.gov, and others, with a constraint applied to exclude publications published over 11 years ago. Molnupiravir, safety, efficacy, COVID-19, RdRp, PK-PD, and clinical study were utilized as keywords.Clinical results on molnupiravir are supported by investigations that were recently disclosed in a study on both sex volunteers (male and female) with an age restriction of 19 to 60 years, followed by a Phase-3 Clinical Trial (NCT04575584) with 775 randomly assigned participants and no fatalities reported due to treatment.Molnupiravir proved a high level of safety, allowing it to be tested further. This review supports the safety and efficacy of this molecule based on the established evidence, which claims the most anticipated employment of molnupiravir in COVID protocol.
随着新冠肺炎时代的展开,研究人员揭示,病毒遗传物质的快速变化使病毒能够绕过宿主免疫系统引发的挑战,抵抗抗病毒药物,从而可能导致病毒在宿主细胞中持续表现。Molnupiravir(RNA依赖性RNA聚合酶抑制剂)是一种新型抗病毒药物,有望在未来的挫折中发挥重要作用。本综述旨在根据现有的病例研究阐明莫努匹拉韦分子的安全性和有效性。因此,它旨在探索和讨论分子结构、作用机制、发现和发展过程、临床前研究、临床研究和其他子主题。使用谷歌学者、PubMed、Web of Science、Embase、Cochrane Library、ClinicalTrials.gov等多个引擎共搜索了75篇出版物,并对11年前出版的出版物进行了限制。莫努匹拉韦、安全性、有效性、新冠肺炎、RdRp、PK-PD和临床研究被用作关键词。莫努匹拉韦的临床结果得到了最近在一项针对年龄限制为19至60岁的两性志愿者(男性和女性)的研究中披露的调查的支持,随后进行了一项3期临床试验(NCT04575584),随机分配了775名参与者,没有因治疗而死亡的报告。Molnupiravir被证明具有很高的安全性,可以进行进一步的测试。这篇综述基于既定证据支持该分子的安全性和有效性,该证据声称莫努匹拉韦在新冠肺炎方案中最受期待。
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引用次数: 0
Yellow fever vaccination in hemodialysis patients: A systematic review 血液透析患者接种黄热病疫苗:一项系统综述
IF 0.6 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-23 DOI: 10.2174/1574885518666230123160533
M. Rodrigues Bacci, Emery Ciana Figueiredo Vidal, Glaucia Luciano da Veiga, Eglidia Carla Figueiredo Vidal, Beatriz da C. Aguiar Alves, T. Gascón, F. L. Affonso Fonseca
Yellow fever is an infectious disease endemic to Africa, and Central andSouth America with a significant impact on public health, causing outbreaks and epidemics. Clinicalmanifestations can vary from asymptomatic to more severe and lethal disease outcomes. The primaryprevention of yellow fever occurs through the vaccination of individuals, which confers immunity forlife. Patients with chronic kidney disease, especially those undergoing dialysis, have low vaccinationand seroconversion rates. As mentioned above, this research aimed to perform a systematic review ofthe yellow fever vaccination protocol in hemodialysis patientsA systematic review on vaccination against yellow fever in hemodialysis patients using databases, PubMed and Biblioteca Virtual em Saúde (BVS), was performed. For data collection, combinations were made using the following descriptors: protocols, vaccination, yellow fever, kidney dialysis, chronic kidney failure, chronic kidney disease, and group risk included in the title and abstract description. Articles with no subject related to the search were excluded and also if they were duplicated.In this review, 90 scientific articles were identified in both databases. After applying exclusion criteria, a total of 3 articles were selected.We recommend carefully assessing the risk-benefit and contraindications for the patient,emphasizing the risk groups. There is an evident lack of studies on the subject, and there is a need tobroaden investigations related toimmunization for patients on dialysis. The review is registered in thePROSPERO system with the number 323550.
黄热病是一种流行于非洲、中美洲和南美洲的传染病,对公共卫生产生重大影响,引起疫情和流行。临床表现可以从无症状到更严重和致命的疾病结局。黄热病的初级预防是通过个人接种疫苗实现的,这种疫苗可提供终身免疫。慢性肾脏疾病患者,尤其是透析患者,疫苗接种率和血清转换率较低。如上所述,本研究旨在对血液透析患者的黄热病疫苗接种方案进行系统评价。利用PubMed和Biblioteca Virtual em Saúde (BVS)数据库对血液透析患者的黄热病疫苗接种进行系统评价。为了收集数据,使用以下描述符进行组合:方案、疫苗接种、黄热病、肾透析、慢性肾衰竭、慢性肾脏疾病和标题和摘要描述中包含的群体风险。与检索主题无关的文章被排除在外,如果它们被重复,也被排除在外。在本综述中,在两个数据库中确定了90篇科学论文。应用排除标准后,共筛选出3篇文章。我们建议仔细评估患者的风险-收益和禁忌症,强调风险群体。这方面的研究明显缺乏,有必要扩大透析患者免疫相关的研究。该审查已在prospero系统中注册,编号为323550。
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引用次数: 0
Quality by Design Enabled Systematic Optimization of Calcineurin Inhibitor-loaded Polymeric Nanoparticles for Sustained Topical Delivery in Psoriasis 质量设计使得钙调磷酸酶抑制剂负载的聚合纳米颗粒用于银屑病局部持续递送的系统优化
IF 0.6 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-20 DOI: 10.2174/1574885518666230120151823
Asha Patel, P. Ahlawat, Shruti Patel, Abhay Dharmasi
The present work describes the systematic development and optimization of cyclosporine-A loaded biodegradable polymeric nanoparticulate system using quality by design paradigm, to achieve an effective and sustained release of the cyclosporine-A to the targeted lesion of plaque psoriasis.The polymeric nanoparticles were formulated using the solvent emulsification method using Polycaprolactone and Hyaluronic acid as polymers. An Ishikawa fishbone diagram was constructed for risk assessment and to describe various plausible product and process variables influencing the quality target product profile. Critical process and product parameters were further optimized by Response surface methodology using Central Composite Design by Minitab 19 Software. The development and optimization of cyclosporine-A loaded biodegradable polymeric nanoparticles were further carried out by developing the relationship of independent variables viz. amount of polymers polycaprolactone and hyaluronic acid on dependent variables viz. particle size, zeta potential, and entrapment efficiency and exploring their interactions. Validation of the model was done by checkpoint analysis method.The particle size, zeta potential, and Entrapment efficiency of the optimized polymeric nanoparticles were found to be 317.2 ± 1.271, -0.249 ± 0.903 mV and 83.33 ± 1.124%, respectively. SEM images of the lyophilized nanoparticles showed spherical particles. In-vitro drug release study showed a slow and sustained release of 88.52 ± 1.10% of drugs up to 14 days.The nanoparticulate system would also help in overcoming the problem associated with poor water solubility and low permeability of the drug and will explore drug loaded biodegradable polymeric nanoparticles as a novel platform for effective therapy of psoriasis.
本工作描述了使用设计质量范式系统开发和优化负载环孢菌素-A的可生物降解聚合物纳米颗粒系统,以实现环孢霉素-A向斑块型银屑病靶向病变的有效和持续释放。使用溶剂乳化法,使用聚己内酯和透明质酸作为聚合物来配制聚合物纳米颗粒。石川鱼骨图用于风险评估,并描述影响质量目标产品概况的各种合理的产品和过程变量。使用Minitab 19软件的Central Composite Design,通过响应面方法进一步优化了关键工艺和产品参数。通过开发自变量(即聚合物聚己内酯和透明质酸的量)与因变量(即粒径、ζ电位和包封效率)的关系,并探索它们的相互作用,进一步开发和优化了负载环孢菌素-A的可生物降解聚合物纳米颗粒。通过检查点分析方法对模型进行了验证。优化的聚合物纳米颗粒的粒径、ζ电位和截留率分别为317.2±1.271、-0.249±0.903mV和83.33±1.124%。冻干纳米颗粒的SEM图像显示为球形颗粒。体外药物释放研究显示,药物在14天内缓慢持续释放88.52±1.10%。纳米颗粒系统还将有助于克服与药物的水溶性差和渗透性低相关的问题,并将探索负载药物的可生物降解聚合物纳米颗粒作为有效治疗银屑病的新平台。
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引用次数: 0
Development and optimization of Guggul extract loaded ultra-deformable vesicles using central composite design for improving anti-oxidant potential 利用中心复合设计开发和优化Guggul提取物负载的超变形囊泡以提高抗氧化能力
IF 0.6 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-16 DOI: 10.2174/1574885518666230116103000
Vineet Mittal, Neha Dhankar, R. Verma, Manish Kumar, Anil Hooda, Deepak Kaushik
After almost 30 years of study, it is a scientific fact that inflammation is the root cause of arthritis.Guggul has a beneficial role in arthritis because of its ability to neutralize the NF-kappa factor. A topical drug delivery system is beneficial to overcome the problems associated with oral drug delivery and offers several potential advantages. Ultra-deformable vesicles (UDVs) are a special type of liposome made up of phospholipids and surfactants, and they are highly flexible.Guggul has a beneficial role in arthritis because of its ability to neutralize the NF-kappa factor. A topical drug delivery system is beneficial to overcome the problems associated with oral drug delivery and offers several potential advantages. Ultra-deformable vesicles (UDVs) are a special type of liposome made up of phospholipids and surfactants, and they are highly flexible.In the present investigation, 20 formulations were suggested by Design Expert® 10 software (Central Composite Design) which were prepared using film hydration method with lecithin (70-90 mg), tween 80 (10–30 mg), Guggul extract (3 mg) and sonicated for 5–15 minutes. The formulation was optimized based on particle size (R₁) and maximum entrapment efficiency (R2).The optimized formulation consists of 78.92 mg soya phosphatidyl choline (lecithin), 22.08 mg Tween 80, and 3 mg Guggul with a sonication time of 12.74 minutes that resulted in a particle size of 375.5 ±15.1 nm and entrapment efficiency of 80.3 ± 3.1%. Guggul UDVs showed more antioxidant activity compared to Guggul extract, control and standard. The same results were obtained in the case of anti-arthritic activity, which was measured by egg albumin denaturation, bovine serum albumin denaturation, proteinase inhibitory action, and anti-lipoxygenase activity. The data of both activities were analyzed using an unpaired t-test to determine significant values (p < 0.05).These results demonstrate the potential of UDVs in the treatment of all arthritis diseases.
经过近30年的研究,炎症是关节炎的根本原因是一个科学事实。Guggul在关节炎中具有有益的作用,因为它能够中和NF-κ因子。局部给药系统有利于克服与口服给药相关的问题,并提供了几个潜在的优点。超变形囊泡(UDVs)是一种由磷脂和表面活性剂组成的特殊类型的脂质体,具有高度的柔韧性。Guggul在关节炎中具有有益的作用,因为它能够中和NF-κ因子。局部给药系统有利于克服与口服给药相关的问题,并提供了几个潜在的优点。超变形囊泡(UDVs)是一种由磷脂和表面活性剂组成的特殊类型的脂质体,具有高度的柔韧性。在本研究中,Design Expert®10软件(Central Composite Design)提出了20种配方,这些配方使用卵磷脂(70-90 mg)、吐温80(10-30 mg)、古古尔提取物(3 mg)的膜水合法制备,并超声处理5-15分钟。配方基于颗粒大小(R₁) 和最大包封效率(R2)。优化的配方由78.92 mg大豆磷脂酰胆碱(卵磷脂)、22.08 mg吐温80和3 mg谷朊组成,超声处理时间为12.74分钟,粒径为375.5±15.1 nm,包封效率为80.3±3.1%。与谷朊提取物、对照品和标准品相比,谷朊UDVs表现出更高的抗氧化活性。在抗关节炎活性的情况下获得了相同的结果,其通过鸡蛋白蛋白变性、牛血清白蛋白变性、蛋白酶抑制作用和抗脂氧合酶活性来测量。使用非配对t检验对两种活性的数据进行分析,以确定显著值(p<0.05)。这些结果证明了UDVs在治疗所有关节炎疾病中的潜力。
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引用次数: 0
Protective Effects of Momordica charantia (Bitter Melon) against Methotrexate-induced Kidney Damage 苦瓜对甲氨蝶呤所致肾损伤的保护作用
IF 0.6 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-12 DOI: 10.2174/1574885518666230112110246
G. Şener, Ç. Macit, D. Ozbeyli, O. Cevik, Melisa Cetin, Sevil Özkan
Methotrexate is a cytotoxic chemotherapeutic agent. However, it has severe side effects, such as nephrotoxicity. Momordica charantia is a bright yellow-orange fruity plant that has been shown to have antioxidant, antidiabetic, and, anti-inflammatory properties.This study scrutinized the protective effects of Momordica charantia extract against methotrexate-induced nephrotoxicity.24 Sprague Dawley rats were divided into three experimental groups (8 rats in each): Control (C); Methotrexate (MTX); and Methotrexate plus Momordica charantia (MTX+MC). All rats were fed ad libitum and tap water. Methotrexate was administered at 20 mg/kg intraperitoneally as a single dose. In the MTX+MC group, MC was administered at a dose of 50mg/kg for 5 days orally. At the end of the 5th. day, the rats were decapitated and kidney samples were taken to analyze glutathione (GSH), malondialdehyde (MDA), myeloperoxidase (MPO), 8-hydroxy-2'-deoxyguanosine (8-OHdG) and caspase-3 activity. Data was analyzed with GraphPad Prism 5.0.Findings showed that while there was a significant increase in MDA, MPO, 8-OHdG levels, and an essential reduction in GSH levels in the MTX-treated group when compared with the control group, bitter melon treatment significantly reversed MDA, MPO, and 8-OHdG levels (p< 0.001). GSH level elevation was observed in the MTX-MC group when compared to the MTX-treated group (p< 0.001).This study showed that bitter melon is thought to have a protective effect against kidney damage caused by methotrexate. With future studies, we believe that the use of bitter melon extract as a protective agent in kidney damage caused by drug-induced oxidative damage will bring an innovative approach to treatment.
甲氨蝶呤是一种细胞毒性化疗药物。然而,它有严重的副作用,如肾毒性。苦瓜(Momordica charantia)是一种明亮的黄橙色果状植物,已被证明具有抗氧化、抗糖尿病和抗炎的特性。本研究考察了苦瓜提取物对甲氨蝶呤引起的肾毒性的保护作用将Sprague Dawley大鼠分为3个实验组,每组8只:Control (C);氨甲叶酸(简称MTX);甲氨蝶呤加苦瓜(MTX+MC)。所有的大鼠都被随意喂食和自来水。甲氨蝶呤按20 mg/kg腹腔单次给药。在MTX+MC组中,MC以50mg/kg的剂量口服5天。在第五大道的尽头。d,处死大鼠,取肾脏标本测定谷胱甘肽(GSH)、丙二醛(MDA)、髓过氧化物酶(MPO)、8-羟基-2′-脱氧鸟苷(8-OHdG)和caspase-3活性。使用GraphPad Prism 5.0对数据进行分析。研究结果显示,与对照组相比,mtx治疗组MDA、MPO、8-OHdG水平显著增加,GSH水平显著降低,而苦瓜治疗组显著逆转了MDA、MPO和8-OHdG水平(p< 0.001)。与mtx治疗组相比,MTX-MC组观察到GSH水平升高(p< 0.001)。这项研究表明,苦瓜被认为对甲氨蝶呤引起的肾脏损伤有保护作用。在未来的研究中,我们相信使用苦瓜提取物作为药物性氧化损伤肾损伤的保护剂,将为治疗药物性氧化损伤带来创新的途径。
{"title":"Protective Effects of Momordica charantia (Bitter Melon) against Methotrexate-induced Kidney Damage","authors":"G. Şener, Ç. Macit, D. Ozbeyli, O. Cevik, Melisa Cetin, Sevil Özkan","doi":"10.2174/1574885518666230112110246","DOIUrl":"https://doi.org/10.2174/1574885518666230112110246","url":null,"abstract":"\u0000\u0000Methotrexate is a cytotoxic chemotherapeutic agent. However, it has severe side effects, such as nephrotoxicity. Momordica charantia is a bright yellow-orange fruity plant that has been shown to have antioxidant, antidiabetic, and, anti-inflammatory properties.\u0000\u0000\u0000\u0000This study scrutinized the protective effects of Momordica charantia extract against methotrexate-induced nephrotoxicity.\u0000\u0000\u0000\u000024 Sprague Dawley rats were divided into three experimental groups (8 rats in each): Control (C); Methotrexate (MTX); and Methotrexate plus Momordica charantia (MTX+MC). All rats were fed ad libitum and tap water. Methotrexate was administered at 20 mg/kg intraperitoneally as a single dose. In the MTX+MC group, MC was administered at a dose of 50mg/kg for 5 days orally. At the end of the 5th. day, the rats were decapitated and kidney samples were taken to analyze glutathione (GSH), malondialdehyde (MDA), myeloperoxidase (MPO), 8-hydroxy-2'-deoxyguanosine (8-OHdG) and caspase-3 activity. Data was analyzed with GraphPad Prism 5.0.\u0000\u0000\u0000\u0000Findings showed that while there was a significant increase in MDA, MPO, 8-OHdG levels, and an essential reduction in GSH levels in the MTX-treated group when compared with the control group, bitter melon treatment significantly reversed MDA, MPO, and 8-OHdG levels (p< 0.001). GSH level elevation was observed in the MTX-MC group when compared to the MTX-treated group (p< 0.001).\u0000\u0000\u0000\u0000This study showed that bitter melon is thought to have a protective effect against kidney damage caused by methotrexate. With future studies, we believe that the use of bitter melon extract as a protective agent in kidney damage caused by drug-induced oxidative damage will bring an innovative approach to treatment.\u0000","PeriodicalId":11004,"journal":{"name":"Current Drug Therapy","volume":" ","pages":""},"PeriodicalIF":0.6,"publicationDate":"2023-01-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46880251","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
Evaluation of Microbiological Culture and Antibiogram of the Patient with Corneal Ulcer due to Exposure Keratitis in the Intensive Care Unit in Sina Farshchian Hospital (2019-2020) 新发医院重症监护室暴露性角膜炎角膜溃疡患者微生物培养及抗生素谱评价(2019-2020)
IF 0.6 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-05 DOI: 10.2174/1574885518666230105115229
Anahita Eslami-Ghayour, A. Taher, F. Eslami, H. Ghasemibasir, A. Irani, Arash Eslami -Ghayour
Since patients admitted to the intensive care unit have a compromised immune system and are more prone to infection than other patients, timely diagnosis and treatment of corneal ulcers among this group of patients can prevent vision loss. Therefore, it is necessary to treat eye infections and corneal ulcers promptly and economize prohibitive costs.Appropriate treatment with the most effective antibiotic before the answer is available to prevent corneal ulcer complications and blindness.This study was conducted from November 2019 to November 2020 and after approval by the ethics committee of Hamedan University of Medical Sciences with the code of ethics: IR.UMSHA.REC.1398.716. First, the corneal secretions of 121 patients admitted to the intensive care unit of Sina Hospital are prepared by an ophthalmologist (after anesthetizing the cornea with tetracaine drops and sterile swabs) and culture in four growth mediums (blood agar, chocolate agar, thioglycolate, and EMB). Microbial cultures are examined after 48 hours and a fungal culture is examined one week later. Disc diffusions are placed in positive microbial cultures. Antibiotic susceptibility or resistance of the antibiogram was recorded. Other demographic data, including patients' age and sex, are extracted from ICU files. Also, test results and patient identifications are recorded in a checklist designed for this purpose.Of all the antibiotics used against common bacteria, vancomycin (84%), colistin (80.43%), cefazolin (80%), and levofloxacin (60%) had the highest sensitivity and gentamicin (93.75%), ceftazidime (86.42 %) Erythromycin (85%) had the highest resistance against isolated bacteria.The data obtained from this study showed that the most common microorganisms in the age group under the age of 30 years were Acinetobacter Baumannii, in the group of 30-60 years old was Klebsiella pneumonia, and age group over 61 years old was Staphylococcus aureus, and the most sensitive antibiotics in the age group under 30 years were vancomycin and levofloxacin and the age group30-60 were colistin and vancomycin and in the age group over 61 years were vancomycin and cefazolin.
由于重症监护病房的患者免疫系统受损,比其他患者更容易感染,因此及时诊断和治疗这组患者的角膜溃疡可以预防视力丧失。因此,有必要及时治疗眼部感染和角膜溃疡,以节省高昂的费用。在得到答案之前,用最有效的抗生素进行适当的治疗,以防止角膜溃疡并发症和失明。本研究于2019年11月至2020年11月进行,经哈马丹医科大学伦理委员会批准,伦理准则为:IR.UMSHA.REC.1398.716。首先,新浪医院重症监护室121例患者的角膜分泌物由眼科医生(用丁卡因滴液和无菌拭子麻醉角膜后)制备,并在四种生长培养基(血琼脂、巧克力琼脂、氨基乙酸酯和EMB)中培养。48小时后检查微生物培养,一周后检查真菌培养。圆盘扩散放置在阳性微生物培养物中。记录抗生素的药敏或耐药情况。其他人口统计数据,包括患者的年龄和性别,都是从ICU的文件中提取的。此外,测试结果和患者身份也记录在为此目的设计的检查表中。在常用抗菌药物中,万古霉素(84%)、粘菌素(80.43%)、头孢唑林(80%)、左氧氟沙星(60%)对分离菌的敏感性最高,庆大霉素(93.75%)、头孢他啶(86.42%)、红霉素(85%)对分离菌的耐药性最高。从这项研究中获得的数据显示,最常见的微生物在30年的岁以下年龄组鲍曼不动杆菌,群30 - 60岁的克雷伯氏菌肺炎,年龄超过61岁的是金黄色葡萄球菌,和最敏感的抗生素年龄30岁以下是万古霉素、左氧氟沙星和group30-60粘菌素、万古霉素和年龄组61多年是万古霉素和头孢唑林。
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引用次数: 0
Formulation Development and Evaluation of Apremilast Nanoemulgel for Enhancing Permeability 阿普雷米司特增透纳米凝胶的配方研制及性能评价
IF 0.6 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-03 DOI: 10.2174/1574885518666230103152130
Neelam Patel, S. Chaudhary, Ankit Chaudhary
Oral apremilast, a selective phosphodiesterase-4 inhibitor, is ef-fective in the treatment of moderate to severe plaque psoriasis and acute pso-riatic arthritic disease. According to BCS categorization, it is a class IV medi-cation, which denotes low solubility and lesser permeability through the skin.The objective of the research is to develop a nanoemulsion that will increase apremilast’s skin permeability. Utilizing a simplex lattice design, an optimised nanoemulsion has been developed, and then transformed into a gel form and created as a nanoemulgel.The nanoemulsion was developed by selecting the oil, surfactant, co-surfactant, and co-solvent, in that order, based on the solubility study, and was then evaluated based on various criteria. Different grades and concentra-tions of carbopol polymer were used to make nanoemulgel, which was then tested for physicochemical parameters like pH, viscosity, spreadability, ex-trudability, percentage of drug content, percentage of drug diffusion, skin permeation, and skin retention. For skin irritancy tests, male Wistar albino rats weighing between 200 and 250 g were used to find out how likely it was that apremilast-loaded nanoemulgel would cause skin irritation.The nanoemulsion formulation A5 containing 10% Captex 355 and 40% Smix in a 3:1 ratio of Cremophore RH 40: Labrafil showed the smallest particle size and greatest drug diffusion. In comparison to other formulations of emulgel, the 0.75 % concentration of carbopol 940 produced the best re-sults.A stable nanoemulgel system with apremilast loaded was creat-ed, and a number of process factors were assessed. The optimised batch pro-duced repeatable results when evaluated, exhibited no skin irritation, and was shown to be stable after three months at ambient conditions of temperature and humidity.
口服阿普雷米司特是一种选择性磷酸二酯酶-4抑制剂,可有效治疗中度至重度斑块性银屑病和急性银屑病关节炎。根据BCS分类,它是IV类药物,这意味着低溶解度和通过皮肤的渗透性较低。这项研究的目的是开发一种纳米乳液,可以增加阿普雷米司特的皮肤渗透性。利用单纯形晶格设计,开发了一种优化的纳米乳液,然后将其转化为凝胶形式并制成纳米乳液。在溶解度研究的基础上,依次选择油、表面活性剂、助表面活性剂和助溶剂制备纳米乳,并根据各种标准对纳米乳进行评价。采用不同等级和浓度的卡波醇聚合物制备纳米乳液,并对其进行pH、粘度、展布性、可挤出性、药物含量百分比、药物扩散百分比、透皮率和皮肤保留率等理化参数的测试。在皮肤刺激试验中,体重在200到250克之间的雄性Wistar白化大鼠被用来研究装载阿普雷米ast的纳米凝胶引起皮肤刺激的可能性。以10% Captex 355和40% Smix为原料,Cremophore RH 40: Labrafil比例为3:1的纳米乳配方A5粒径最小,药物扩散最大。与其他配方相比,0.75%浓度的卡波醇940效果最佳。建立了一种负载阿普雷米司特的稳定纳米凝胶体系,并对许多工艺因素进行了评估。优化后的批次在评估时产生了可重复的结果,没有皮肤刺激,并且在温度和湿度的环境条件下显示出三个月后的稳定性。
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引用次数: 1
Silymarin: A Phytoconstituent with Significant Therapeutic Potential - A Narrative Review 水飞蓟素:一种具有显著治疗潜力的植物成分
IF 0.6 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2022-12-27 DOI: 10.2174/1574885518666221227100052
Pravin Kumar, Sahil Sharma, M. Ashawat, V. Pandit, Chandrapal Verma, Dinesh Kumar Sharma
Silymarin, is a phytoactive constituent isolated from the fruits and seeds of Silybum marianum L Gaetn.), also called milk thistle belonging to the family of Asteracease. The phytoactive has been used to treat several physiological disorders.The objective of this manuscript was to review the therapeutic prospective of silymarin due to its ability to treatseveral physiological disorders.The databases such as Pubmed, Elsevier, and Google Scholar were reviewed for the investigations or reviews published related to the title.The discussion is focused on the immunomodulatory, chemopreventive, and anti-inflammatory mechanisms of silymarin in various metabolic and dermatological disorders. In addition, the review discusses the different therapeutic potentials of silymarin such as the management of the liver disorder, skin carcinogenesis, cardiovascular disorders, diabetes mellitus, neurodegenerative disorders, and several dermatological disorders such as melasma, anti-aging, acne, rosacea, atopic dermatitis, and psoriasis. Silymarin is safe even with a dose higher than the therapeutic dose.Silymarin had good potential for the safe and effective treatment of numerous metabolic and dermatological disorders.
水飞蓟素是从水飞蓟的果实和种子中分离的植物活性成分),也被称为乳蓟,属于菊科。这种植物活性物质已被用于治疗几种生理疾病。本文的目的是综述水飞蓟素的治疗前景,因为它能够治疗几种生理疾病。Pubmed、Elsevier和Google Scholar等数据库被审查了与该标题相关的调查或评论。讨论的重点是水飞蓟素在各种代谢和皮肤病中的免疫调节、化学预防和抗炎机制。此外,该综述还讨论了水飞蓟素的不同治疗潜力,如治疗肝病、皮肤癌变、心血管疾病、糖尿病、神经退行性疾病和几种皮肤病,如黄褐斑、抗衰老、痤疮、酒渣鼻、特应性皮炎和牛皮癣。水飞蓟素即使剂量高于治疗剂量也是安全的。水飞蓟素在安全有效治疗多种代谢和皮肤病方面具有良好的潜力。
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引用次数: 0
Comparison of the Efficacy of Honey and Clotrimazole Cream in the Vulvovaginal Candidiasis treatment: a systematic review and meta-analysis 蜂蜜和克曲唑乳膏治疗外阴阴道念珠菌感染的疗效比较:系统综述和荟萃分析
IF 0.6 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2022-12-21 DOI: 10.2174/1574885518666221221085942
M. Mirghafourvand, Zahra Mollazadeh-Narestan, Parisa Yavarikia, Sepideh Mashayekh-Amiri, P. Gholizadeh
Vulvovaginal candidiasis (VVC) is a common fungal infection of the vaginal area affecting 75% of women at least once in their lifetime. However, there is no clear evidence helping to choose the most effective treatment method to improve the symptoms of VVC.The objective of this study was to compare the effect of using honey with clotrimazole on the treatment of symptoms of VVC.All databases in English (Embase, MEDLINE, ProQuest, Google Scholar, Scopus, Cochrane Library, and Web of Science) and Persian (Irandoc, SID, and Magiran) were searched without time limitation. Evaluation of studies in terms of bias was performed using the Cochrane handbook. Four clinical trials were included in the present systematic review; however, only three of them were included in the meta-analysis.The results of the meta-analysis demonstrated that the rate of positive culture after treatment (RR: 2.35; 95%CI: 1.45 to 3.82) was significantly higher in the honey group than in the clotrimazole one. The frequency of itching after treatment (RR: 0.25, 95%CI: 0.12 to 0.49) was significantly lower in the honey-receiving group than in the clotrimazole one. However, there was no statistically significant difference in the incidence of other symptoms of VVC, including vaginal discharge (RR: 0.26, 95%CI: 0.02 to 2.75), vaginal burning (RR: 0.35, 95%CI: 0.03 to 3.80) and dyspareunia (RR: 0.64, 95%CI: 0.27 to 1.50) between groups.Due to the low quality of the studies, more clinical trial studies with stronger designs in this field are needed to clearly identify the therapeutic effects of honey on improving the symptoms of VVC.
外阴阴道念珠菌感染(VVC)是一种常见的阴道真菌感染,75%的女性一生中至少感染一次。然而没有明确的证据可以帮助选择最有效的治疗方法来改善VVC的症状。本研究的目的是比较蜂蜜和克霉唑对VVC症状的治疗效果。所有英文数据库(Embase、MEDLINE、ProQuest、Google Scholar、Scopus、Cochrane Library和Web of Science)和波斯语数据库(Irandoc、SID和Magiran)在没有时间限制的情况下进行搜索。使用Cochrane手册对研究的偏倚进行评估。本系统综述包括四项临床试验;荟萃分析结果表明,蜂蜜组治疗后培养阳性率(RR:2.35;95%CI:1.45~3.82)显著高于克霉唑组。蜂蜜接受组治疗后瘙痒的频率(RR:0.25,95%CI:0.12-0.49)显著低于克霉唑组。然而,VVC的其他症状,包括阴道分泌物(RR:0.26,95%CI:0.02至2.75)、阴道灼热(RR:0.35,95%CI:0.03至3.80)和性交困难(RR:0.64,95%CI:0.27至1.50)的发生率在各组之间没有统计学上的显著差异。由于研究质量低,需要在该领域进行更多设计更强的临床试验研究,以明确蜂蜜对改善VVC症状的治疗效果。
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引用次数: 0
Hepatoprotective Potential Of Phytoconstituents And Vitamins Against Antitubercular Drugs Induced Hepatotoxicity In Albino Rats 植物成分和维生素对抗结核药物诱导的白化大鼠肝毒性的保护作用
IF 0.6 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2022-12-16 DOI: 10.2174/1574885518666221216100311
B. Kumari, T. Kumar, D. Kumar, Aninda Sen
This study aims to develop a new hepatoprotective drug from common plants and vitamins that are potent, nontoxic, and cost-effective. The literature search found that Curcuma longa, Zingiber officinale, Terminalia, chebula, and Vitamin A (Vitamin C + Vitamin E) provide hepatoprotective action against drugs-induced hepatotoxicity. A major side effect of antitubercular drugs (ATD) is liver toxicity, which reduces their effectiveness.In this study, Vitamins and Phytoconstituents (Combined extract) were evaluated for their potential hepatoprotective effects against hepatotoxicity induced by antitubercular drugs in Wistar albino rats of either sex.In the study, ethanolic extract of rhizomes of Curcuma longa and Zingiber officinale, fruits of Terminalia chebula, and vitamins C and E were used. As a standard drug, silymarin was also used. For 30 days, albino rats received 7.5 mg/kg isoniazid, 10 mg/kg rifampicin, and 35 mg/kg pyrazinamide orally as a suspension in distilled water.A combined extract plus vitamins (500mg/kg) treatment significantly reduced the hepatic toxicity caused by antitubercular drugs (P<0.05-P<0.001). A combination of extracts + vitamins (500mg/kg) eliminates hepatotoxicity, and the results are close to those of Silymarin, a standard drug.As a result of this study, extracts+vitamins provide protection against liver injury attributed to their hepatoprotective activity, which supports their traditional use.
本研究旨在从常见植物和维生素中开发一种有效、无毒、经济的新型保肝药物。文献检索发现,姜黄、生姜、天竺葵、天竺葵和维生素A(维生素C +维生素E)对药物性肝毒性具有保护肝脏的作用。抗结核药物(ATD)的一个主要副作用是肝毒性,这降低了它们的有效性。在本研究中,我们评价了维生素和植物成分(联合提取物)对抗结核药物引起的Wistar白化大鼠肝毒性的潜在保护作用。以姜黄根茎、生姜根茎、chebula果实乙醇提取物和维生素C、E为主要成分。作为标准药物,水飞蓟素也被使用。白化大鼠口服7.5 mg/kg异烟肼、10 mg/kg利福平、35 mg/kg吡嗪酰胺作为悬浮液溶于蒸馏水中30 d。500mg/kg复合提取物加维生素可显著降低抗结核药物引起的肝毒性(P<0.05 ~ P<0.001)。提取物+维生素的组合(500mg/kg)消除了肝毒性,其效果接近标准药物水飞蓟素。这项研究的结果是,提取物+维生素可以保护肝脏免受肝损伤,这归功于它们的肝保护活性,这支持了它们的传统用途。
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引用次数: 0
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Current Drug Therapy
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