Current Drug Therapy - Volume 19, Issue 6, 2024

Numerous herbal-based Ayurvedic and Chinese medications contain a variety of phytochemicals that may have a neuroprotective impact and help treat a variety of neurodegenerative diseases. The natural medicinal drug has long been used to treat neural signs and symptoms. There has been an enormous public and clinical interest in the use of Phytoconstituents for neuroprotection or the prevention of neurodegenerative illnesses. Various compounds, isolated from exclusive natural sources with multiple objectives seem as a capacity and promising class of therapeutics for the remedy of illnesses associated with neuro-related issues. It is vitally important to identify and create novel therapeutic strategies. The possibility for safe, naturally occurring secondary metabolites with neuroprotective characteristics is present in plants and other natural products. This review intends to take a closer look at some specific elements of natural phytoactives that are thought to be significant for the treatment of neuro-related illnesses.

Background: Depression is a prevalent global illness, impacting 280 million people worldwide, and Major Depressive Disorder (MDD) is ranked as the third leading cause of disease burden globally. People previously diagnosed with depression are more likely to develop Alzheimer's disease (AD). The recent approval of Auvelity by the FDA has made a remarkable breakthrough in drug development, offering a multi-dimensional approach for managing multiple diseases. Objective: The main objective of this study is to investigate the role of Auvelity, a new drug, in treating MDD and its potential to manage agitation in individuals with Alzheimer's disease (AD). Methodology: Data on Auvelity was collected from various sources, including accessdata.fda.gov, PubMed, and Scopus, and compiled for analysis. Discussion: Auvelity is the first oral medication to demonstrate the rapid onset of action, with statistically significant antidepressant efficacy observed as early as one week compared to a placebo. It contains a combination of dextromethorphan (45 mg) and bupropion (105 mg). The drug's mechanism of action involves a combination of NMDA receptor blockade and agonism of the sigma-1 receptor, resulting in the antagonization of the glutamatergic neurotransmitter pathway. Due to the similarity in the mechanism of action with AD medications like Memantine, there is a hypothesis that Auvelity could effectively reduce symptoms of AD. Conclusion: The approval of Auvelity marks a significant advancement in depression treatment with its unique NMDA antagonist mechanism, rapid onset of action, and low-risk profile.

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.

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.

The creation of innovative drug delivery systems to enhance therapeutic effectiveness, safety, and patient compliance has resulted in considerable developments in pharmaceutics in recent years. The most recent formulation techniques and technologies are reviewed in this article to improve medication distribution and accomplish specific therapeutic goals. This article thoroughly summarizes the most recent formulation techniques and technologies used to enhance medication delivery and provide specific therapeutic effects. It discusses the variety of medication delivery methods, including nanoparticles, liposomes, micelles, and dendrimers, and explores the application of nanotechnology and biotechnology in drug delivery. Additionally, the paper emphasizes the significance of targeted drug delivery systems and their capacity to cross biological barriers including the blood-brain barrier and tumor microenvironment. The review also addresses the challenges faced in developing and commercializing drug delivery systems and suggests potential solutions to overcome them. Furthermore, the article emphasizes the role of computational modeling and simulation in designing and optimizing drug delivery systems. Overall, this review paper offers insightful information for pharmaceutics researchers, scientists, and practitioners that will help in the creation of novel drug delivery systems that improve patient outcomes and quality of life.

Medicinal and culinary uses of plants date back centuries. Projects on a global scale are conducting laboratory research to identify plants with therapeutic properties, with the ultimate goal of developing such compounds into medicines with acceptable drug delivery mechanisms and bringing them to market. Non-synthetic medications derived from plant or herbal sources have attracted a lot of interest because of their high tolerability and low likelihood of adverse medication reactions. All diseases, the theory goes, can be cured by something found in nature. Medicines can be taken in a wide variety of forms, including tablets, capsules, powders, semi-liquid extracts, tinctures, decoctions, medicinal teas, solutions, and more. Longer release, patient adherence, and other objectives necessitate adjustments to herbal medications. Researchers into novel drug delivery systems had hitherto overlooked herbal remedies due to a lack of scientific validation and the challenges inherent in processing, standardizing, extracting, and identifying them. Transdisciplinary research and cuttingedge isolation, purification, and identification techniques have led to the development of novel herbal compositions. Bioactive plant extracts and phytoconstituents are used in a wide variety of Nano- Emulsions, microspheres, transferosomes, implants, and ethosomes. Compared to herbal remedies, novel formulations fared better. Among these advantages are increased solubility, bioavailability, toxicity, pharmacological activity, stability, delivery duration, and resistance to physical and chemical degradation. As a result, the pharmacokinetic and pharmacodynamic properties of herbal medications can be enhanced by the use of novel drug delivery systems, making them safer and more effective. This article aims to provide a concise description of the many new drug delivery techniques that have been created for the administration of herbal medications. The ultimate goal is to increase the efficacy of therapies and to learn more about their significance and worldwide appeal.

Background: As a developed technology, microfluidics now offers a great toolkit for handling and manipulating suspended samples, fluid samples, and particles. A regular chip is different from a microfluidic chip. A microfluidic chip is made of a series of grooves or microchannels carved on various materials. This arrangement of microchannels contained within the microfluidic chip is connected to the outside by inputs and outputs passing through the chip. Objectives: This review includes the current progress in the field of microfluidic chips, their advantages and their biomedical applications in diagnosis. Methods: The various manuscripts were collected in the field of microfluidic chip that have biomedical applications from the different sources like Pubmed,Science direct and Google Scholar, out of which some were relevant and considered for the present manuscript. Results: Microfluidic channels inside the chip allow for the processing of the fluid, such as blending and physicochemical reactions. Aside from its practical, technological, and physical benefits, microscale fluidic circuits also improve researchers' capacity to do more accurate quantitative measurements while researching biological systems. Microfluidic chips, a developing type of biochip, were primarily focused on miniaturising analytical procedures, especially to enhance analyte separation. Since then, the procedures for device construction and operation have gotten much simpler. Conclusion: For bioanalytical operations, microfluidic technology has many advantages. As originally intended, a micro total analysis system might be built using microfluidic devices to integrate various functional modules (or operational units) onto a single platform. More researchers were able to design, produce, and use microfluidic devices because of increased accessibility, which quickly demonstrated the probability of wide-ranging applicability in all branches of biology.

Background: Nitophyllum marginale holds potential for medical applications due to its bioactive compounds, making it promising for developing new therapeutic interventions. Our study aims to evaluate the bioactivity of Nitophyllum marginale extracts obtained using methanol and chloroform solvents. We focus on analyzing the phytochemical profile, antioxidant activity, and antidiabetic potential of seaweed extract in this study. By examining the medicinal properties of Nitophyllum marginale, we aim to explore the therapeutic bioactivity potentiality and its prime role in improvising and searching for potential alternatives for seizing Diabetes mellitus. Materials and Methods: The antioxidant activity of Nitophyllum marginale was evaluated using ABTS, DPPH, nitric oxide, lipid peroxidation, and hydrogen peroxide assays. Additionally, alphaglucosidase inhibition tests were conducted to evaluate the potential as an antidiabetic agent. Results: The study revealed that extracts from Nitophyllum marginale contain antioxidants that protect cells from oxidative stress. These extracts also contain bioactive compounds like alkaloids, flavonoids, phenols, saponins, and carbohydrates. These compounds work together to provide antioxidant benefits. Additionally, the extracts showed activity against alpha-glucosidase, which is vital for managing blood sugar levels. Conclusion: These results emphasize the existence of bioactive metabolites exhibiting phytochemicals, antioxidants, and antidiabetic activities obtained from the extract using chloroform and methanol solvents. These findings suggest the potential of Nitophyllum marginale extracts as a natural reservoir of antioxidants and antidiabetic agents.

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.

Background: The current research aimed to create and analyze a new long-acting Brexpiprazole (BRX) injectable for successful anti-psychotic drug therapy in order to decrease dosage frequency and increase patient compliance. Systems for drug transport to particular body sites or regulating release rates with accuracy are known as drug delivery systems (DDS). By affixing the drug to a carrier particle like liposomes, nanoparticles, microspheres, etc., which modifies the drug's absorption and release properties, using carrier technology, drugs may be delivered in an intelligent manner. Methods: Utilizing Resomer RG 502 H and RESOMER^® RG 752 H extended-release Polymer, Using a quasi-emulsion solvent diffusion, microspheres were made, and emulsification and solvent evaporation process. Results: The produced microspheres were assessed for stability tests, in vitro drug release, flow characteristics, and drug entrapment efficiency. FTIR experiments were used to establish how well the drug excipients worked together. The acarbose microspheres that were created had an 89.9 to 96.1 percent drug entrapment efficiency. The impact of factors like polymer content on medication release was studied. The Stability study of the formulation was carried out under different conditions, and data were established. Comparative pharmacokinetic studies between marketed oral formulation and Brexpirazole microsphere test formulations in Wistar/SD Rats were carried out and concluded. Conclusion: Brexpiprazole (BRX) novel long-acting injectable formulation, could be used effectively for the treatment of mentally challenged anti-psychotic patients worldwide.

Background: Bacillus species create several kinds of metabolites, which contain cyclic lipopeptide-type antibiotics, consisting of three major families: fengycin, surfactin, and iturin. Iturin demonstrates powerful biocontrol characteristics and can restrain the growth of a diversity of plant fungal pathogens. Objective: The current study investigates the identification of iturin A from Bacillus atrophaeus using HPLC and Mass spectrometry analysis and evaluate its antifungal effects. Materials and Methods: In this study, the lipopeptide antibiotics were isolated by HPLC and characterized by MS. Then, the lipopeptides were examined for their ability to antagonize the growth of different pathogenic fungi. Antifungal performance of the lipopeptides was determined against Fusarium oxysporum, Aspergillus niger, Penicillium chrysogenum, and Mucor hiemalis according to well diffusion and percentage of growth inhibition. Results: Bacillus atrophaeus HNSQJYH170, isolated from Isfahan soil, offered strong fungicidal activity by producing cyclic lipopeptide-type antibiotics. Inhibition zones were 17.55, 17, 18.50, and 20.99 mm, and the percentages of growth inhibition were 78.54, 62.55, 83.11, and 84/95 for Fusarium oxysporum, Penicillium chrysogenum, Mucor hiemalis and Aspergillus niger, respectively. The spectrum represented the iturins family in retention times of 32.423–33.893 min. MS demonstrated molecular ion peaks (M+H) + for iturin at m/z 1029.55, 1043.60, 1051.55, 1065.60, 1079.60 and 1093.65. The inhibition rate against all fungi on the seventh day of incubation was higher than 80%. Among them, Aspergillus niger was the most sensitive fungal species with an average of 84.95% inhibition. Conclusion: According to the results, Bacillus atrophaeus HNSQJYH170 could operate as a biocontrol agent against a wide spectrum of pathogenic fungi.

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. Objectives: 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. Results: 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.