Current Drug Therapy最新文献

{"title":"Enhanced Solubility and Increased Bioavailability with Engineered Nanocrystals","authors":"Reetika Sood, D. Tomar, Peeyush Kaushik, Prerna Sharma, N. Rani, Kumar Guarve, Sanchit Dhankar, Nitika Garg","doi":"10.2174/0115748855269071231113070552","DOIUrl":"https://doi.org/10.2174/0115748855269071231113070552","url":null,"abstract":"The exploration of nanocrystal technology is currently receiving significant attention in various fields, including therapeutic formulation, clinical formulation, in-vivo and in-vitro correlation research, and related investigations. The domain of nanocrystals in pharmaceutical delivery has received significant interest as a potential solution for the difficulties associated with medications that have low solubility. The nanocrystals demonstrate promise in improving solubility and bioavailability, presenting a potential resolution to significant challenges. Significantly, nanocrystals have exhibited efficacy in the context of oral administration, showcasing prompt absorption due to their quick breakdown, hence fitting with the requirements of medications that necessitate fast commencement of action. In addition, the adaptability of drug nanocrystals encompasses several methods of administration, including oral, parenteral, ophthalmic, cutaneous, pulmonary, and targeted delivery modalities. The observed consistency can be ascribed to the increased solubility of nanocrystals of the medicine, which effectively counteracts the influence of food on the absorption of the drug. Surface modification tactics have a significant influence on insoluble medicines by enhancing hydrophilicity and reducing plasma protein adsorption on the crystal surface. The surface properties of nanocrystals are modified through the utilization of specific surfactants and polymers, which are subsequently incorporated into polymer solutions via high-pressure homogenization procedures. This article encompasses an examination of the drug distribution mechanism, the nanocrystal formulation technology, the therapeutic applications, the potential future developments, and the challenges associated with the solubility and bioavailability of tailored nanocrystals, as discussed in this article. Consequently, it possesses the capacity to provide guidance for future investigations pertaining to nanocrystal technology.","PeriodicalId":11004,"journal":{"name":"Current Drug Therapy","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-11-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139268210","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"QSAR Studies on Thienopyrimidines as Potential Antimicrobial Agents","authors":"Pranali A. Jadhav, Pratiksha Jadhav","doi":"10.2174/0115748855266001231026063520","DOIUrl":"https://doi.org/10.2174/0115748855266001231026063520","url":null,"abstract":"Background: Recent research has revealed promising antibacterial action for thienopyrimidines. To comprehend the underlying molecular features underlying their antibacterial potency, a thorough quantitative structure-activity relationship (QSAR) investigation is required. Objective: In order to clarify the structural parameters for effective antibacterial activity, we conducted QSAR analyses on a variety of thienopyrimidines in this work. Methods: Through the analysis of physicochemical properties and molecular descriptors, we aimed to develop predictive models that can guide the design of novel thienopyrimidine derivatives with enhanced antimicrobial potential. Result: It was discovered through the descriptor importance analysis that specific physicochemical characteristics, including lipophilicity, electronic distribution, and steric effects, significantly influenced the antibacterial efficacy of these drugs. Conclusion: The identified molecular characteristics and descriptors can be used to guide the development of new thienopyrimidine derivatives with higher antibacterial activity.","PeriodicalId":11004,"journal":{"name":"Current Drug Therapy","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-11-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135136671","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Melatonin Alleviates High Glucose-induced Oxidative Stress and Mitochondrial Dysfunction in Chondrocytes","authors":"Saeed Mehrzadi, Shokoufeh Hassani, Azam Hosseinzadeh","doi":"10.2174/0115748855270821231030043727","DOIUrl":"https://doi.org/10.2174/0115748855270821231030043727","url":null,"abstract":"Background:: Hyperglycemia triggers mitochondrial dysfunction in chondrocytes, potentially contributing to cell damage and the onset of osteoarthritis. Objective:: This study is undertaken with the objective of examining the protective properties of melatonin against toxicity induced by high glucose in C28I2 human chondrocytes. Methods:: To determine non-cytotoxic concentrations of melatonin, various concentrations (10, 25, 50, 75, 100, 500, and 1000 μM) were assessed over different time periods (24, 48, and 72 hours) for their impact on C28I2 cell viability. Following this, cells underwent a pretreatment with melatonin (10 and 100 μM) for 6 hours. This was followed by subjecting the cells to a high concentration of glucose (75 mM) for 48 hours. Oxidative stress markers, including reactive oxygen species (ROS) and malondialdehyde (MDA), alongside the enzymatic activities of glutathione peroxidase, superoxide dismutase, and catalase were quantitatively assessed. To assess mitochondrial function, we evaluated the adenosine diphosphate (ADP)/adenosine triphosphate (ATP) ratio and measured the mitochondrial membrane potential (MMP). Results:: Elevated glucose levels significantly increased ROS and MDA levels, accompanied by reduced MMP, an elevated ADP/ATP ratio, and altered antioxidant enzyme activity. Pretreatment with melatonin effectively reversed the mitochondrial toxicity induced by high glucose (75 mM). Conclusion:: These results indicate that melatonin exhibits a protective influence against hyperglycemia- induced toxicity in chondrocyte mitochondria.","PeriodicalId":11004,"journal":{"name":"Current Drug Therapy","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-11-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135684931","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Biological Potential of a Bibenzyl Compound ‘Gigantol’ for the Treatment of Human Disorders: Pharmacological Activities and Analytical Aspects of an Active Phytochemical Isolated from Orchid","authors":"K. Patel, Gireesh Singh, G. M. Husain, Satyendra K Prasad, D. Patel","doi":"10.2174/0115748855254948231024112016","DOIUrl":"https://doi.org/10.2174/0115748855254948231024112016","url":null,"abstract":"Dendrobium chrysotoxum Lindl. is an important medicinal plant of the genus Dendrobium from the Orchidaceae family. Gigantol is one of the key bioactive phytochemicals found in Dendrobium plants. Gigantol is reported to have diverse pharmacological activities. This narrative review explores the analytical aspects along with pharmacological activities of gigantol as reported in different scientific publications. To find appropriate information related to Dendrobium plants and gigantol, extensive data extraction was done using ScienceDirect, Google, PubMed, and Scopus databases, and diverse facts were collected, arranged and analyzed to know the therapeutic potential of gigantol. Analytical aspects of gigantol were also discussed in the present work. Gigantol has a wide distribution in the Dendrobium officinale, Dendrobium chrysanthum, Dendrobium crystallinum, Dendrobium aphyllum, and Dendrobium devonianum. Available data indicates diverse pharmacological activities of gigantol. Preclinical studies have shown its effectiveness in the treatment of cataractogenesis, liver injury, leishmaniasis, nephrotoxicity, spasm, and skin disorders. Gigantol has been found to control hepatocellular cancer, lung cancer, breast cancer, bladder cancer, and cervical cancer. The neuroprotective, antinociceptive, anti-inflammatory, antioxidant, vasorelaxant, immune modulatory effect, antimalarial, and anti-herpetic properties of gigantol have also been observed. Applications of different analytical techniques for the isolation and characterization of gigantol were also discussed in detail. Gigantol has significant and diverse pharmacological activities that must be explored in clinical setup to develop therapeutic leads for different diseases and health conditions.","PeriodicalId":11004,"journal":{"name":"Current Drug Therapy","volume":null,"pages":null},"PeriodicalIF":0.6,"publicationDate":"2023-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139290555","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A Critical Assessment of Remdesivir","authors":"Subhash Chandra, Alka N Choudhary, Santwana Palai, Abdur Rauf, Hassan Y. Aboul-Enein","doi":"10.2174/0115748855255004231001182927","DOIUrl":"https://doi.org/10.2174/0115748855255004231001182927","url":null,"abstract":"Abstract: The COVID-19 pandemic that originated in Wuhan city, China, has affected every village in India. This has killed millions of people. This disease involves symptomatic and asymptomatic mutations. The purpose of this review was to assess the effectiveness of remdesivir particularly against SAR-CoV-2 (Coronaviridae family). The relevant works have been studied with respect to the drug's chemistry, mechanism of action, pharmacokinetics, pharmacodynamics, clinical data, and side effects. Remdesivir has been used in many cases of coronavirus-infected patients because it has been proven to possess beneficial effects; however, significant adverse effects have also been reported. Remdesivir has been reported to help in lowering the disease's high fatality rate. However, the WHO has warned against using the medicine because there is no clinical data to support its therapeutic efficacy.","PeriodicalId":11004,"journal":{"name":"Current Drug Therapy","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135929588","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Pharmacological Potential of Sulindac and Its Active Metabolite: A Comprehensive Review","authors":"Shraddha Manish Gupta, Ashok Behera, Siddharth Singh","doi":"10.2174/0115748855264953231020142004","DOIUrl":"https://doi.org/10.2174/0115748855264953231020142004","url":null,"abstract":"Abstract: In this review, we describe and discuss the pharmaceutical aspects, pharmacokinetic profile, and preclinical and clinical studies of sulindac and its active metabolite and emphasise their potential activity not only in anti-inflammation strategies but also as chemoprevention drug candidates. Though they are widely validated through in vitro and in vivo models, to date, no efforts have been made to compile in a single review on their pharmacologically potential, pharmacokinetics and toxicity profiles. Key databases such as PubMed, Science Direct, Scopus, and Google Scholar, among others, were probed for a systematic search using keywords to retrieve relevant publications. An exhaustive electronic survey of the related literature on the pharmacologically potential activity and the pharmacokinetic and toxicity profiles of sulindac resulted in around 200 articles (1975 and 2023) being included. The studies conducted on sulindac sulphide and sulindac sulfone metabolites reported a varied range of biological effects deployed in this review. The review concluded that there is scope for repurposing sulindac using computer-aided drug design and biological study to find out possible new targets for strengthening the potency and selectivity of the metabolites.","PeriodicalId":11004,"journal":{"name":"Current Drug Therapy","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135315920","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Optimal Weight-Based Dosing of Intravenous Immunoglobulin (IVIG) among Overweight and Obese Patients","authors":"shima Heidari, Bita Shahrami, Kourosh Sadeghi","doi":"10.2174/0115748855258149231001142811","DOIUrl":"https://doi.org/10.2174/0115748855258149231001142811","url":null,"abstract":"Intravenous immunoglobulin (IVIG), as an expensive medication under a national shortage, has been widely used for the treatment of several autoimmune diseases and immunodeficiency syndromes. Although conducting studies on therapeutic indications of IVIG has increased significantly, a limited number of researches have investigated individualized dosing in terms of the drug, disease state, and some patient-specific factors like obesity. The objective of the review was to describe the impact of various weight-based dosing regimens on the pharmacokinetics parameters, efficacy, safety, and cost of IVIG and to choose the best dosing approach for obese patients. Thirteen of the total 128 manuscripts collected, reviewed, and analyzed were found from Scopus, PubMed, and Google scholar. The evidence suggests that obesity may have an impact on IVIG pharmacokinetics, safety, and efficacy. The logical approach is to initial the dose based on the ideal or adjusted body weight and then modify the maintenance dose according to the patient's clinical response.","PeriodicalId":11004,"journal":{"name":"Current Drug Therapy","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136357467","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"An Outlook of Substantial Progress in Nanotechnology Emerged in Treatment Approaches for Rheumatoid Arthritis","authors":"Amana Parveen, Pranay Wal, Awani Kumar Rai, Ankita Wal","doi":"10.2174/0115748855238869231002073717","DOIUrl":"https://doi.org/10.2174/0115748855238869231002073717","url":null,"abstract":"Background: Rheumatoid arthritis affects roughly 5 out of every 1000 persons, rheumatoid arthritis is a persistent anarchic ailment with complicated pathophysiology a well-known cause of arthritis-related stinging apropos nexus, degradation of synovium, the creation of pannus, damage to bones, and loss of the cartilage. Thus, it is imperative to diagnose and treat rheumatoid arthritis. Due to rheumatoid arthritis's complexity, early diagnosis is difficult, which makes the treatment difficult. Moreover, anti- rheumatoid arthritis drugs taken on a long-term basis can damage patients' organs as well. Due to this, these anti- rheumatoid arthritis medications may cause severe side effects in extra-articular tissues since they cannot selectively target the affected zone. There has been substantial progress in the discovery of this disease's pathophysiology and treatment strategy over the past few years, as well as in developing effective diagnostic methods, early detection, and efficient treatment strategies. In the rheumatoid arthritis, nanotechnology has come to the fore as a game-changer in effectively managing many diseases. Various nanotechnology approaches are promising for designing formulations that can deliver drugs to bone and cartilage in targeted and non-targeted ways like Targeting receptors on inflammation-related cells (CD44, Scavengers receptors, etc.) Conclusion: Nanotechnology is used to treat Rheumatoid arthritis, improve implants and prostheses, and develop new diagnostic and treatment methods in orthopedic medicine. Many chronic orthopedic diseases exist, but rheumatoid arthritis is the most common. Several research studies have found that nanotechnology could deliver targeted drugs, reduce adverse effects on non-target organs, increase drug concentration in synovial tissues, and slow the progression of immune-mediated rheumatoid diseases such as rheumatoid arthritis. This review examines how nanotechnology can be used to diagnose and treat rheumatoid arthritis.","PeriodicalId":11004,"journal":{"name":"Current Drug Therapy","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136358108","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The Use of Daflon Tablets in Treating Hemorrhoids and Alleviating Symptoms","authors":"Leila Hajimaghsoudi, Mojtaba Ahmadinejad, Mohsen Karimian, Mohammad Hadi Bahri, Ali Karbalaeikhani, Izadmehr Ahmadinejad","doi":"10.2174/0115748855260887230925095817","DOIUrl":"https://doi.org/10.2174/0115748855260887230925095817","url":null,"abstract":"Background: Varicose-like bulging veins that occur in the anus and lower rectum are known as hemorrhoids. Depending on their degree of prolapse, they can cause symptoms such as bleeding, discomfort, mucous discharge, perianal irritation, and burning. The aim of the study was to investigate the impact of Daflon pills on the treatment of hemorrhoids and their associated symptoms, as well as the duration of hospitalization and the likelihood of recurrence. Methods: A randomized clinical trial was used in this investigation. Patients who had been referred to the surgical clinic of the Madani Hospital in 2021 with hemorrhoid complaints were participants in a random selection process. Participants were separated into control groups (getting non-invasive regular treatments) and the intervention group after being informed and given ethical approval (Receiving Daflon 500 mg twice daily for 4 weeks). Patients' symptoms, potential sequelae, and illness recurrence were assessed in both chosen groups at each visit, and data was gathered until the desired sample size was reached. Results: This study was performed on 200 patients who received Daflon 500 mg (intervention, N = 100) or placebo (control, N = 100). The number of visits required to achieve therapeutic goals did not differ statistically significantly between the intervention and control groups (P >0.05). The mean recovery time was 56.5 ± 12.53 days for the intervention group and 61.04 ± 13.63 days for the control group, which is considered statistically significant (P<0.05). A total of 56 patients (28.0%) relapsed and 144 patients (72.0%) recovered. This rate in the intervention group included 78 (78.0%) recovery and 22 (22.0%) relapsed and in the control group 66 (66.0%) recovered and 34 (34.0%) relapsed, clinically it suggests that treatment Daflon can prevent relapse of the disease, although the statistical results of this study do not support this hypothesis (P = 0.059). Conclusion: The study's findings demonstrated that Daflon therapy is a superior and more effective treatment option for all grades of hemorrhoids. Moreover, the medication's side effects are manageable, making it a well-tolerated choice.","PeriodicalId":11004,"journal":{"name":"Current Drug Therapy","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136357990","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A Comprehensive Review of Preclinical Models for Polycystic Ovary Syndrome","authors":"G. SANTHANA KUMAR, KRITIKA GARG, Arun Soni, MITTAL DALAL","doi":"10.2174/0115748855248659230922111800","DOIUrl":"https://doi.org/10.2174/0115748855248659230922111800","url":null,"abstract":"Background:: Polycystic ovary syndrome (PCOS) is a reproductive, metabolic, and endocrine disorder with unclear aetiology. PCOS, the most common cause of female reproductive and metabolic disorders, is known to affect more than one in ten women globally. PCOS and associated clinical manifestations are probably underdiagnosed despite their high occurrence. Objective:: Alternative animal models have been employed to investigate the causes of PCOS or assess potential treatments. In light of this piece of information, it is challenging to create an animal model that accurately captures all components of this condition; nonetheless, the resemblance of an animal model's biology and/or biochemical characteristics to the phenotypes of PCOS in humans may boost its applicability. Result:: The key characteristics of these models are closer to human situations when compared to women with PCOS, as shown by this comparison. The creation and testing of drugs for the treatment of PCOS are necessary Conclusion:: The overview of PCOS, current preclinical models, and appropriate models chosen in different studies to mimic various phenotypes in PCOS studies are all covered in this review paper. Additionally, we have outlined the benefits and drawbacks of PCOS animal models.","PeriodicalId":11004,"journal":{"name":"Current Drug Therapy","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135546205","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}