Research Work Research Articles

Formulation and Optimization of Solid Lipid Nanoparticle-based Gel for Dermal Delivery of Linezolid Using Taguchi Design.

Linezolid (LNZ) is a synthetic oxazolidinone antibiotic approved for the treatment of uncomplicated and complicated skin and soft tissue infections caused by gram-positive bacteria. Typically, LNZ is administered orally or intravenously in most cases. However, prolonged therapy is associated with various side effects and life threatening complications. Cutaneous application of LNZ will assist in reducing the dose, hence minimizing the unwanted side/adverse effects associated with oral administration. Dermal delivery provides an alternative route of administration, facilitating a local and sustained concentration of the antimicrobial at the site of infection. The current research work aimed to formulate solid lipid nanoparticles (SLNs) based gel for dermal delivery of LNZ in the management of uncomplicated skin and soft tissue infections to maximise its benefits and minimise the side effects. SLNs were prepared by high-shear homogenisation and ultrasound method using Dynasan 114 as solid lipid and Pluronic F-68 as surfactant. The effect of surfactant concentration, drug-to-lipid ratio, and sonication time was investigated on particle size, zeta potential, and entrapment efficiency using the Taguchi design. The main effect plot of means and signal-to-noise ratio were generated to determine the optimized formulation. The optimized batch was formulated into a gel, and ex-vivo permeation study, in-vitro and in-vivo antibacterial activity were conducted. The optimised process parameters to achieve results were 2% surfactant concentration, a drug-to-lipid ratio of 1:2, and 360 s of sonication time. The optimized batch was 206.3± 0.17nm in size with a surface charge of -24.4± 4.67mV and entrapment efficiency of 80.90 ± 0.45%. SLN-based gel demonstrated anomalous transport with an 85.43% in vitro drug release. The gel showed a 5 cm zone of inhibition while evaluated for in vitro antibacterial activity against Staphylococcus aureus. Ex-vivo skin permeation studies demonstrated 20.308% drug permeation and 54.96% cutaneous deposition. In-vivo results showed a significant reduction in colony-forming units in the group treated with LNZ SLN-based gel. Ex-vivo studies ascertain the presence of the drug at the desired site and improve therapy. In-vivo results demonstrated the ability of SLN-based gel to significantly reduce the number of bacteria in the stripped infection model. The utilization of SLN as an LNZ carrier holds significant promise in dermal delivery.

Biological Potential and Therapeutic Effectiveness of Artemetin from Traditional to Modern Medicine: An Update on Pharmacological Activities and Analytical Aspects.

Plant products derived from natural sources have been used in medicine as a raw material and newer kinds of drug molecules in pharmaceuticals and other allied health sectors. Phytochemicals have numerous medicinal potentials, including anti- ageing, anti-carcinogenic, anti-microbial, anti-oxidant, and anti-inflammatory activity in medicine. Development and biological application of herbal products in modern medicine signified the value of traditional medicinal plants in health care systems. The objective of the present study was to explore the scientific knowledge of the medicinal importance and therapeutic potential of artemetin in medicine. However, scientific investigations for their pharmacological activities in medicine have been done through scientific data analysis of different scientific research work collected from PubMed, Google, Science Direct and Google Scholar in order to know the biological importance of artemetin in medicine. Moreover, analytical data of artemetin have also been discussed in the present work. The present work and scientific data signified the biological potential of artemetin in medicine. Artemetin has been derived from numerous medicinal plants and dietary herbs, including Artemisia absinthium, Artemisia argyi, Achillea millefolium, and Vitex trifolia. Artemetin has anti-malarial, anti-oxidant, anti-apoptotic, anti-microbial, antitumoral, anti-atherosclerotic, anti-inflammatory, hypotensive and hepatoprotective effects. Further, the biological role of artemetin on lipid oxidation, cytokine production, lipoxygenase, and estrogen-like effects was also investigated in the present work. Analytical data on artemetin in the present paper signified their important role in the isolation, separation, and identification of different classes of pure phytochemicals, including artemetin in medicine. Scientific data analysis of artemetin signified its therapeutic potential in medicine for the development of newer scientific approaches for different human disorders.

A Rationalized Approach to Design and Discover Novel Non-steroidal Derivatives through Computational Aid for the Treatment of Prostate Cancer.

Prostate cancer is one of the most prevalent cancers in men, leading to the second most common cause of death in men. Despite the availability of multiple treatments, the prevalence of prostate cancer remains high. Steroidal antagonists are associated with poor bioavailability and side effects, while non-steroidal antagonists show serious side effects, such as gynecomastia. Therefore, there is a need for a potential candidate for the treatment of prostate cancer with better bioavailability, good therapeutic effects, and minimal side effects. This current research work focused on identifying a novel non-steroidal androgen receptor antagonist through computational tools, such as docking and in silico ADMET analysis. Molecules were designed based on a literature survey, followed by molecular docking of all designed compounds and ADMET analysis of the hit compounds. A library of 600 non-steroidal derivatives (cis and trans) was designed, and molecular docking was performed in the active site of the androgen receptor (PDBID: 1Z95) using Auto- Dock Vina 1.5.6. Docking studies resulted in 15 potent hits, which were then subjected to ADME analysis using SwissADME. ADME analysis predicted three compounds (SK-79, SK-109, and SK-169) with the best ADME profile and better bioavailability. Toxicity studies using Protox-II were performed on the three best compounds (SK-79, SK-109, and SK-169), which predicted ideal toxicity for these lead compounds. This research work will provide ample opportunities to explore medicinal and computational research areas. It will facilitate the development of novel androgen receptor antagonists in future experimental studies.

Architectural Design for Data Security in Cloud-based Big Data Systems

التصميم المعماري للنظام هو عملية إبداعية بعد كل شيء. المتطلبات غير الوظيفية وبنية البرامج لها علاقة قوية. يعد أمن النظام أحد الشواغل الكبيرة وهو حاجة ومتطلب غير وظيفي. يجب أن يعتمد الأسلوب والهيكل المعماري المختاران للنظام على متطلبات النظام غير الوظيفية. تُستخدم تقنيات البيانات الضخمة لتخزين كميات هائلة من البيانات التشغيلية في المجال العام. تم اقتراح مخططات هيكل وسلوك النظام التي تستخدم تصميمًا معماريًا آمنًا لنظام يعمل عبر السحابة. تم التحقيق في مكونات مختلفة من البيانات الضخمة في هذا العمل البحثي نظرًا لخطورة القضايا الأمنية التي تركز على الخصوصية والسرية. يعد تأمين البيانات عبر السحابة التي يتم الاستعانة بمصادر خارجية لها مصدر قلق متزايد. هناك مسؤولو قواعد بيانات ضارة من الخارج ومن الداخل يمكنهم الوصول إلى البيانات الخاصة والحساسة وتعديلها ، وبالتالي يمكن أن يكون مزود خدمة قاعدة البيانات مخادعًا. آليات الأمان مطلوبة بالضرورة لحماية البيانات الحساسة الموجودة على السحابات العامة. على مستوى التطبيق ، يضمن الحل المقترح خصوصية وسرية البيانات الموجودة على السحابة. تم إجراء اختبارات مكثفة ، وكانت نتائج هذا البحث كما يلي: كشفت النتائج المسجلة عن اختلافات ذات دلالة إحصائية في النص العادي ومحتويات الوسائط المتعددة (أي الصوت والفيديو) مع قياس الوقت بالمللي ثانية لمجموعات البيانات الصغيرة والمتوسطة والكبيرة.

Investigations on Cylindrical Surrounding Double-Gate (CSDG) MOSFET using AlxGa1-xAs/InP: Pt with La2O3 oxide layer for fabrication.

The Cylindrical Surrounding Double-Gate MOSFET has been designed using Aluminium Gallium Arsenide in its arbitrary alloy form alongside Indium Phosphide with Lanthanum Dioxide as a high-ƙ dielectric material. The heterostructure based on the AlxGa1-xAs/InP: Pt has been used in the design and implementation of the MOSFET for RF applications. Platinum serves as the gate material, which has higher electronic immunity toward the Short Channel Effect and highlights semiconductor properties. The charge buildup is the main concern in the field of MOSFET design when two different materials are considered for fabrication. The usage of 2 Dimensional Electron Gas has been outstanding in recent years to help the electron buildup and charge carrier accumulation in the MOSFETs regime. Device simulation used for the smart integral systems is an electronic simulator that uses the physical robustness and the mathematical modeling of semiconductor heterostructures. In this research work, the fabrication method of Cylindrical Surrounding Double Gate MOSFET has been discussed and realized. The scaling down of the devices is essential to reduce the area of the chip and heat generation. By using these cylindrical structures, the area of contact with the circuit platform is reduced since the cylinder can be laid down horizontally. The coulomb scattering rate is observed to be 18.3 % lower than the drain terminal when compared to the source terminal. Also, at x = 0.125 nm, the rate is 23.9 %, which makes it the lowest along the length of the channel; at x = 1 nm, the rate is 1.4 % lesser than that of the drain terminal. A 1.4 A/mm2 high current density had been achieved in the channel of the device, which is significantly larger than comparable transistors. The conventional transistor occupies a larger area than the proposed cylindrical structures transistor and is also efficient in RF applications.

Biodegradation as More-Than-Human Unmaking

In this work, we introduce biodegradation as a process of more-than-human unmaking. We begin by positioning biodegradation amongst related works in design research before presenting a circular process of making and unmaking biomaterials and living organisms through biodegradation. To exemplify this process, we detail two existing works—ReClaym and Biomenstrual—that exemplify how biodegradability can be explored in design through different biomaterials, methods, and contexts. By diffractively reading these projects through one another, we identify six themes and corresponding suggestions for researchers engaging with biodegradation. Lastly, we discuss the broader design implications and limitations, as well as the more-than-human values that emerge from designing for biodegradation via biomaterials. Through this, we aim to provide design researchers with practical tools and insights for engaging with biodegradation to unmake anthropocentric hierarchies between humans, non-humans, and biomaterials, which in turn can promote environmental sustainability and support more-than-human collaboration and care.

Software for Bioprinting.

The bioprinting of heterogeneous organs is a crucial issue. To reach the complexity of such organs, there is a need for highly specialized software that will meet all requirements such as accuracy, complexity, and others. The primary objective of this review is to consider various software tools that are used in bioprinting and to reveal their capabilities. The sub-objective was to consider different approaches for the model creation using these software tools. Related articles on this topic were analyzed. Software tools are classified based on control tools, general computer-aided design (CAD) tools, tools to convert medical data to CAD formats, and a few highly specialized research-project tools. Different geometry representations are considered, and their advantages and disadvantages are considered applicable to heterogeneous volume modeling and bioprinting. The primary factor for the analysis is suitability of the software for heterogeneous volume modeling and bioprinting or multimaterial three-dimensional printing due to the commonality of these technologies. A shortage of specialized suitable software tools is revealed. There is a need to develop a new application area such as computer science for bioprinting which can contribute significantly in future research work.

Herbal Medicines Genkwadaphnin as Therapeutic Agent for Cancers and Other Human Disorders: A Review of Pharmacological Activities through Scientific Evidence

Backgrounds: Daphnane-type diterpenes are an important class of phytochemicals found to be present in the family Euphorbiaceae and Thymelaeaceae. It has anti-leukaemic, antihyperglycaemic, and anti-fertility activities in medicine. Daphne genkwa is indigenous to the Yangtze River and Yellow River of China. Daphne genkwa contains significant amounts of daphnane- type diterpenes. Phytochemical analysis of Daphne genkwa led to the isolation of flavonoids, lignins, coumarins, caffeotannic acids, and genkwadaphnin. Methods: Present review highlighted the biological potential of genkwadaphnin in medicine. All the scientific data of Daphne genkwa, and genkwadaphnin were collected from Google, Google Scholar, Science Direct, Scopus, and PubMed and analyzed in the present work to know the therapeutic potential of genkwadaphnin in medicine. Detailed pharmacological activities of genkwadaphnin were analyzed in the present work through scientific data analysis of various research works. Results: Genkwadaphnin is a daphnane diterpene ester molecule mainly isolated from the Daphne genkwa, Dendrostellera lessertii, Daphne odorata, Gnidia latifolia, and Gnidia glaucus. Genkwadaphnin has been reported to exert therapeutic potential against hepatocellular carcinoma, human colon cancer, squamous cell carcinoma, and leukemia. Further, it has a significant role in innate immunity, melanogenesis, skeletal diseases, inflammatory cytokines, and natural killer cell. However, pharmacokinetics and metabolomics aspects of genkwadaphnin were also discussed in the present work. Further, more scientific data on human clinical trials is needed to ensure the safety and efficacy of genkwadaphnin in medicine. Conclusion: In the present work, a successful review had been achieved by the above-mentioned scientific data, which signified the therapeutic potential of genkwadaphnin in medicine.

Nanomaterials used in Flexible Electronics: Recent Trends and Future Approaches

Abstract: The latest research in soft electronics reveals a substantial demand for devices that can fold, bend and stretch to suit the requirements of technological advances. Cellulose, silk, and elastomers are employed in making biodegradable, environmentally benign substrates that accommodate nanofibers, nanoparticles, nanotubes, graphene, and biomaterials in their nano-form. Flexible materials can hold circuits and sensors and can substitute conventional substrates. Transient electronics, e-skin, and biosensors are the most sought-after in medical technology, sensors, energy storage devices, and wearables. These stretchable materials lead the way for developing eco-friendly and sustainable technology to attain sustainable development goals. This research work discusses nano species imbibed in printable and flexible electronics. An analysis of the documents extracted from the Scopus database using VOSviewer and patents in the domain of flexible electronics are presented along with altmetrics.

Restraint of Starch-hydrolyzing Enzyme in the Management of Postprandial Blood Glucose Level: An Alternative Approach

Background: Diabetes is a multifaceted metabolic condition defined by postprandial hyperglycemia with perturbances in the majority of the metabolic systems in the human body. α-amylase is a key enzyme present in pancreatic juice and saliva that converts one of the common food sources i.e., starch molecules into absorbable molecules and raises plasma glucose levels. Reducing starch digestion by the inhibitors of starch hydrolyzing enzymes could be an intriguing strategy for improved postprandial hyperglycemia management. Objective: The present research work was undertaken to evaluate the inhibition potential of natural inhibitors of α-amylase from Trichosanthes dioica (pointed gourd) and Moringa oleifera (moringa leaves) extracts in vitro. Furthermore, in vivo cytotoxicity assessment was also conducted through brine shrimp lethality bioassay. Methods: Different organic solvents (namely acetone, ethanol, and methanol) were used to isolate plant extracts. DNS (3,5-dinitrosalicylic acid) was used to conduct the α-amylase inhibition assay. The safety of the natural inhibitors was determined by the most common technique i.e, brine shrimp lethality bioassay. Results: Among all the different organic solvent extracts, pointed gourd and its peel exhibited the highest α-amylase inhibition activity (64.03 ± 7.33–69.40 ± 9.38%) which is very close to standard α-amylase inhibitor acarbose (72.34 ± 4.23%) whereas moringa leaves showed moderate inhibition activities (59.10 ± 5.25–62.03 ± 1.77%). The cytotoxicity of pointed gourd and its peel was higher while moringa leaves demonstrated lower toxicity. Conclusion: Considering the inhibition rate and cytotoxicity, pointed gourd ethanol extract (Inhibition: 67.43 ± 11.80%; Cytotoxicity: 209.98 μg/mL) would be the best candidate for managing postprandial hyperglycemia.

Naturally Occurring Cholinesterase Inhibitors from Plants, Fungi, Algae, and Animals: A Review of the Most Effective Inhibitors Reported in 2012-2022.

Since the development of the "cholinergic hypothesis" as an important therapeutic approach in the treatment of Alzheimer's disease (AD), the scientific community has made a remarkable effort to discover new and effective molecules with the ability to inhibit the enzyme acetylcholinesterase (AChE). The natural function of this enzyme is to catalyze the hydrolysis of the neurotransmitter acetylcholine in the brain. Thus, its inhibition increases the levels of this neurochemical and improves the cholinergic functions in patients with AD alleviating the symptoms of this neurological disorder. In recent years, attention has also been focused on the role of another enzyme, butyrylcholinesterase (BChE), mainly in the advanced stages of AD, transforming this enzyme into another target of interest in the search for new anticholinesterase agents. Over the past decades, Nature has proven to be a rich source of bioactive compounds relevant to the discovery of new molecules with potential applications in AD therapy. Bioprospecting of new cholinesterase inhibitors among natural products has led to the discovery of an important number of new AChE and BChE inhibitors that became potential lead compounds for the development of anti-AD drugs. This review summarizes a total of 260 active compounds from 142 studies which correspond to the most relevant (IC50 ≤ 15 μM) research work published during 2012-2022 on plant-derived anticholinesterase compounds, as well as several potent inhibitors obtained from other sources like fungi, algae, and animals.

Additively Manufactured Porous Metallic Implants and Their Surface Modification for Biomedical Applications: A Review

The evolution of three dimensional (3D) printed porous metallic biomaterials and their clinical applications are currently receiving much consideration. Many research works have been focused on the shaping by 3D printing of lightweight metal implants with improved mechanical properties. In the same way, the effect of surface finishes on roughness and porosity distribution on biological properties is still debated. Therefore, several factors need to be addressed and revisited in this context. This review focuses on the importance of porous metallic implant design and its relationship with biological and mechanical properties. First, the additive manufacturing (AM) techniques for bio-inert metals and alloys will be discussed. The review will then introduce the most efficient surface treatments and coating approaches for biomedical porous metals to enhance bone tissue regeneration, prevent corrosion, reduce revision surgery and improve implant lifetime. A critical study of the various parameters impacting the biological properties will also be carried out in this review.

Multilevel Thresholding-based Medical Image Segmentation using Hybrid Particle Cuckoo Swarm Optimization

Background: The most important aspect of medical image processing and analysis is image segmentation. Fundamentally, the outcomes of segmentation have an impact on all subsequent image testing methods, including object representation and characterization, measuring of features, and even higher-level procedures. The problem with image segmentation is recognition and perceptual completion while segmenting the image. However, these issues can be resolved by multilevel optimization techniques. However, multilevel thresholding will become more computationally intensive with increasing thresholds. Optimization algorithms can resolve these issues. Therefore, hybrid optimization is used for image segmentation in this research work. Methods: The researchers propose a Multilevel Thresholding-based Segmentation using a Hybrid Optimization approach with an adaptive bilateral filter to resolve the optimization challenges in medical image segmentation. The proposed model utilizes Kapur's entropy as the objective function in the nature-inspired optimization algorithm. Results: The result is evaluated using parameters such as the Peak Signal-to-Noise Ratio (PSNR), Structural Similarity Index (SSIM), and Feature Similarity Index (FSIM). The researchers perform result analysis with variable thresholding levels on KAU-BCMD and mini-MIAS datasets. The highest PSNR, SSIM, and FSIM achieved were 31.9672, 0.9501, and 0.9728 respectively. The results of the hybrid model are compared with state-of-the-art models, demonstrating its efficiency. Conclusion: The research concludes that the proposed Multilevel thresholding-based segmentation using a Hybrid Optimization approach effectively solves optimization challenges in medical image segmentation. The results indicate its efficiency compared to existing models. The research work highlights the potential of the proposed hybrid model for improving image processing and analysis in the medical field.

A DRL-Based Reactive Scheduling Policy for Flexible Job Shops With Random Job Arrivals

In real-life production systems, arrivals of jobs are usually unpredictable, which makes it necessary to develop solid reactive scheduling policies to meet delivery requirements. Deep reinforcement learning (DRL) based scheduling methods are capable of quickly responding to dynamic events by learning from the training data. However, most of policy networks in DRL algorithms are trained to choose priority dispatching rules (PDR), thus, to some extent, the efficiency of obtained scheduling plans is limited by the performance of PDRs. This paper investigates a dynamic flexible job shop scheduling problem with random job arrivals for the total tardiness minimization. A DRL-based reactive scheduling method, proximal policy optimization with attention-based policy network (PPO-APN), is proposed to make real-time decisions for the dynamic scheduling environment, where the attention-based policy network (APN) is able to directly select pending jobs distinguished from the action space that consists of PDRs. Additionally, a global/local reward function (GLRF) is designed to address the reward sparsity issue during training processes. The proposed PPO-APN is tested on randomly generated instances with different production configurations, and is compared with frequently-used PDRs and DRL-based methods. Numerical experimental results indicate that APN and GLRF components significantly improve the training efficiency, and the PPO-APN shows better overall performance compared with other methods. <italic xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">Note to Practitioners</i> —This work is motivated by a typical production scenario in discrete manufacturing systems, where orders randomly arrive at the shop floor and require to be scheduled in a short time to ensure the on-time delivery. Previous research work tends to apply DRL algorithms to choose suitable dispatching rules for the ease of implementation. Nevertheless, the jobs that can be selected by dispatching rules are rather limited, thus many possible high-quality scheduling plans are ignored. This work first sorts all the unscheduled jobs by a heuristic algorithm, and puts some of top-ranked jobs to a pool. When a machine becomes available, it will directly choose a job from the pool as the next processing task. The job selection policy is represented by a novel attention-based network, and is trained by a powerful DRL algorithm. The aforementioned process is repeatedly executed in a simulation environment to collect the training data. Therefore, after being trained for a certain period of time, the policy will become smarter and can be applied to make right decisions in real-time. The proposed reactive scheduling method has been proved to be more efficient than dispatching rules and DRL-based approaches, and is effective in the production scheduling for a wide variety of discrete manufacturing scenarios, such as automobile and electronics industries. Moreover, the proposed method can be further extended to address dynamic scheduling problems with some production characteristics via adding constraints for the job selection or re-defining calculations for the completion time of operations accordingly.

Richard Maack's Vilyui expedition in the study of avifauna and gallinaceous birds (Gallinaceae) of Eastern Siberia

The article is dedicated to the 170th anniversary of the Vilyuisk (Yakutia) expedition organised by the Siberian (Irkutsk) branch of the Imperial Russian Geographical Society (1853-1885). It was led by Richard Karlovich Maack (Germ. Richard Otto Maack), a Russian naturalist of German origin and explorer of Siberia and the Far East. It also contains some information on the Pribaikalia and Transbaikalia, taken along the way during the subsequent Amur (1855-1856) and Ussuri (1859-1960) expeditions. The route, dates, and composition of the expedition are described and the contribution of the scientist to various fields of natural science and, above all, to the study of vertebrates of the region is evaluated. Scientists have identified the habitat of amphibians and reptiles (4 species), birds (121), mammals (34), which is relatively large against the background of regional studies conducted in Eastern Siberia at that time. According to the lists of bird species published in the fundamental work of the scientist "Vilyuisky district of the Yakut region" [1883-1887], the distribution of 5 species of Gallinaceous birds (Gallinaceae) in the middle of the XIX century was revealed – Hazel Grouse, Western and Black-billied Capercaillies, Black Grouse, Willow Ptarmigan. For Transbaikalia and Pribaikalia, the habitat of two more species is noted - Gray and Bearded Partridges. The Common Pheasant was accounted for by R. K. Maack only in the Amur region and the Amur region (Far East). In general, over the century and a half of the history of studying Gallinaceous birds, their species composition has practically not changed in the researcher's work area. In Yakutia, it was replenished with species from the eastern and southern regions, living there Rock Partridge and Siberian Grouse. On the scale of Eastern Siberia, only the Pheasant is currently supplementing the Gallinaceous birds list as a new species in the region, documented in the south of Eastern Siberia – in the Eastern Sayan bordering the Baikal region and in some places of Transbaikalia (not yet precisely confirmed).

Percepción de la violencia en el noviazgo entre universitarios: ¿control o amor?

La violencia en el noviazgo es tema central de múltiples trabajos de investigación, en este estudio en particular, se analizó la percepción de la violencia en el noviazgo por parte de jóvenes universitarios. Entre los resultados más importantes se encontró que la violencia psicológica y emocional que consiste en mantener el control y en utilizar apodos para humillar, resulta ser la más común. Ambos sexos coinciden en que tanto hombres como mujeres, son agresores y receptores de este tipo de violencia.

Review on Diabetes Mellitus: An Insight into the Current Scenarios, the Challenges of Therapy, and Application of Traditional Drugs

Abstract: Diabetes mellitus, an epidemic of the 21st century, is listed as one of the top ten causes of death around the world by the World Health Organization and is a complicated disease to deal with. Medically, a metabolic disorder characterized by elevated blood glucose levels and altered metabolism of biological macromolecules, mainly carbohydrates. Diabetes mellitus has a worldwide prevalence, and populations of all high, middle, as well as low-income countries, are affected by it. More than 400 million persons are currently living with diabetes. Many risk factors, such as lack of exercise, irregular diet, drinking, and smoking habits, as well as genetic factors, also contribute to the increased incidence of diabetes mellitus in the modern era. The conventional therapies for diabetes are based on insulin, insulin analogues, peptides, and oral hypoglycemics. The primary objective is to lower the elevated blood glucose levels and manage the distress to enhance the quality of life of the patient. The management of diabetes is very crucial to avoid complications having serious consequences such as the extra economic burden due to these complications. Conventional drug therapy has its own adverse effects, and its timely availability and cost are still an issue in many low and middle-income countries. Diabetes mellitus has been reported in various ancient kinds of literature along with various natural remedies (plants/herbals) useful in it. These plant-based remedies offer the benefits of lesser or no adverse effects, easy availability due to natural abundance, and low cost. Therefore, extensive research work is carried out in the past few decades to identify and understand the underlying principles of plant-based/herbal medicines to develop new potential lead molecules and a relatively safer, easily available and more economical alternative treatment therapy for diabetes mellitus.

Flavonoid and Chalcone Scaffolds as Inhibitors of BACE1: Recent Updates.

Flavonoids and chalcones are two major classes of chemical moieties that have a vast background of pharmacological activities. Chalcone is a subclass of flavonoids whose therapeutic potential has been implicated due to an array of bioactivities. A lot of research works have shown interest in investigating the neuroprotective effect of these molecules, and have revealed them to be much more potent molecules that can be used to treat neurodegenerative disorders. Beta-site APP cleaving enzyme (BACE1), which is majorly found in the brain, is one of the reasons behind the development of Alzheimer's disease (AD). Flavonoids and chalcones have proven clinical data that they inhibit the production of Aβ plaques that are involved in the progression of AD. In this article, we have provided a detailed chronological review of the research work on the BACE1 inhibiting potency of both flavonoids and chalcones. Almost all the flavonoids and chalcones mentioned in this article have shown very good in vitro and in vivo BACE1 inhibiting activity. The docking studies and the structural importance of some BACE1-inhibiting flavonoids, as well as chalcones, are also mentioned here.

D-Optimal Mixture Design Enabled Development of Lyophilized Nanoemulsifying Drug Delivery System of Paliperidone

Background: Schizophrenia is a chronic disease with acute psychotic symptoms, which is having frequent recurrence. Paliperidone palmitate (PP) is a second-generation antipsy-chotic drug to treat schizophrenia. Aims: The aim of the study was to prepare lyophilized nanoemulsifying drug delivery system (NEDDS) of paliperidone (PD). Objective: The primary objective of the current research work was to develop a lyophilized nanoemulsifying drug delivery system (NEDDS) of paliperidone (PD) to improve its oral bioa-vailability and stability. Methods: Optimization using D-Optimal Mixture Design DMD) was conducted, and optimized NEDDS was further lyophilized to improve stability. The lyophilized optimized NEDDS was fur-ther evaluated for biopharmaceutical evaluation. Result: A saturation solubility study revealed Peceol, Tween 80, and Plurol Olique CC497 as suitable candidates for oil, surfactant, and co-surfactant, respectively. Optimized NEDDS of PD showed mean globule size (MGS) of 185 nm, PDI of 0.27 and cumulative % drug release within 15 min Q15 of 86.6%. Lyophilized optimized NEDDS was found to have no significant change in quality attributes within the stability study period. A pharmacokinetic study revealed more than two-fold increases in bioavailability for lyophilized optimized NEDDS. Conclusion: Hence, lyophilized NEDDS of PD can be used as an effective approach for the im-provement of oral bioavailability and stability.

Sida cordifolia L.: Ethnobotany, Phytochemistry, Phytonanotechnology, and Commercial Application.

After a period of prolonged indifference, where synthetic drugs were preferred, interest in the biological aspects and bioactive ingredients of plants accountable for therapeutic potential has been explored eminently. Sida cordifolia L. is a perennial herb that has been widely utilized in Indian (Ayurveda, Unani, and Siddha), American, and Chinese folk medicine and herbalism practice for curing a wide range of ailments in human beings. The goal of this review is to elucidate indigenous knowledge parallelly with the pharmacotherapeutics potential of Sida cordifolia L. against various diseases. It is also intended to display pertinent information related to nanoparticle profiling. In the current comprehensive study, web-based searches were performed by using several databases, such as Google Scholar, PubMed, ResearchGate, Science Direct, and Scopus, to figure out relevant research work and data published in academic journals from 1930 to July, 2023 using single or combination of keywords listed herewith. More than 50 chemical constituents, including quinazoline and phenethylamine alkaloids, flavones, flavonol, phytosterol, fatty acids, etc., were reported to be found in different parts of healthy plants. Apart from traditional claims and pharmacological aspects, several marketed herbal formulations and granted patents were also described. Several in-vitro and in-vivo studies validated the usage of S. cordifolia as antiinflammatory, antibacterial, antifungal, antiprotozoal, anthelmintic, anticancer, antiulcer, cardioprotective, hypoglycemic, etc. agent. Few patents are also related to S. cordifolia, and more research work needs to be carried out for its potential granted to use as an antiviral agent and other new drug discovery molecules.