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Hyperuricemia is characterized by higher-than-normal levels of uric acid in the bloodstream. This condition can increase the likelihood of developing gout, a form of arthritis triggered by the deposition of urate crystals in the joints, leading to inflammation and pain. An essential part of purine metabolism is played by the enzyme xanthine oxidase (XO), which transforms xanthine and hypoxanthine into uric acid. Despite its vital role, diseases such as gout have been associated with elevated uric acid levels, which are linked to increased XO activity. To manage hyperuricemia, this study focuses on potential nitrogen based heterocyclic compounds that may serve as XO inhibitors which may lower uric acid levels and prevent hyperuricemia. Xanthine oxidase inhibitors are a class of medications used to treat conditions like gout by reducing the production of uric acid. The present study demonstrates numerous compounds, particularly nitrogen containing heterocyclic compounds including their synthesis, structure–activity relationship, and molecular docking studies. This paper also contains drugs undergoing clinical studies and the xanthine oxidase inhibitors that have been approved by the FDA.

Most of the new drug candidates and present ones are lipophilic, which leads to low bioavailability. Self-emulsifying drug delivery systems (SEDDS) have emerged as promising formulation system for poorly water-soluble drug candidates. Over the last two decades, various such drug compounds were used by researchers for the development of SEDDS. At present, many SEDDS formulations are also available in the market. Though SEDDS offer many advantages but drawbacks like low drug loading, few dosage form choices, difficulty in handling and storage led to the solidification of this system by various methods. Solidification by spray drying technique offers a lot of advantages like scalability and stability. This particular method is the focus of this review. Adsorbent carriers have the most significant role in the fate of this formulation and its compatibility with the drug candidate. This review addresses the advantages, method of development, spray drying specifications, and characterization of S-SEDDS in detail. Furthermore, the prospect of turning spray-dried SEDDS into tablets by punching which offers potential advantages of increased bioavailability and stability has also been discussed.

The synthesis of biogenic nanoparticles from readily available natural resources may have large demand in numerous fields including pharmaceuticals and medicine. The biogenic nanoparticles catch the attention of the scientific community due to their low cytotoxicity and biocompatibility. Chemical, physical, and greener methods are used for the synthesis of biogenic nanoparticles. Researchers used eco-friendly and nontoxic approaches in the synthesis of this nanoparticle. This nanomaterial-based medicine plays a vital role in the management of public health, including earlier detection of disease, therapeutics candidates in the treatment of cancer. Biogenic nanocomposites are environmentally benign candidates that include fabrication of various composites, detoxification, and act as a catalyst in the biodegradation process. In this review article, we emphasize the recently reported methods used for synthesis, summarizing their biomedical applications and commercial and environmentally benign applications. Synthetic strategies include greener, chemical, physical, and biogenic methods and their role in surface modifiers involves various biomedical, commercial, and environmental-related applications. Moreover, we glimpse existing status, key contests, and future perspectives.

Dysregulated actin cytoskeleton gives rise to aberrant cell motility and metastatic spread of tumor cells. This study evaluates the effect of overexpression of wild-type versus functional mutants of MRTF-A on migration and invasion of breast cancer (BC) cells. Our studies indicate that SRF's interaction is critical for MRTF-A-induced promotion of both two-dimensional and three-dimensional cell migration, while the SAP-domain function is important selectively for three-dimensional cell migration. Increased MRTF-A activity is associated with more effective membrane protrusion, a phenotype that is attributed predominantly to SRF's interaction with MRTF. We demonstrate formin-family protein mDia2 as an important mediator of MRTF-stimulated actin polymerization at the leading edge and cell migration. Multiplexed quantitative immunohistochemistry and transcriptome analyses of clinical BC specimens further demonstrate a positive correlation between nuclear localization of MRTF with malignant traits of cancer cells and enrichment of MRTF–SRF gene signature in pair-matched distant metastases versus primary tumors. In conclusion, this study establishes a novel mechanism of MRTF-dependent regulation of cell migration and provides evidence for the association between MRTF activity and increased malignancy in human BC, justifying future development of specific small molecule inhibitors of the MRTF-SRF transcriptional complex as potential therapeutic agents in BC.

Background: This study aimed to formulate solid self-nanoemulsifying drug delivery systems (SNEDDS) for nimodipine (NIM). The selection of Cremophor RH 40, Lipoxol 300, and PEG 400 as oil, surfactant, and co-surfactant was based on solubility and self-emulsification assessments. A ternary phase diagram determined the optimal oil to Smix (surfactant/co-surfactant) ratio (40:60). By utilizing liquid SNEDDS (NIM-SNEDDS) as an adsorbate and chitosan EDTA microparticles, developed through spray drying (SD-CHEM) and solvent evaporation (SE-CHEM) as adsorbents, the solid SNEDDS were created (NIM-SD-SSNEDDS and NIM-SE-SSNEDDS, respectively). Results: Both solid formulations exhibited favourable drug loading (NIM-SD-SSNEDDS = 79.67 ± 2.97%, NIM-SE-SSNEDDS = 77.76 ± 4.29%), excellent flowability, and drug amorphization as per XRD and DSC analysis. Scanning electron microscopy revealed smoothening and filling of adsorbent surfaces by adsorbate (with size range NIM-SD-SSNEDDS = 10–15 μm, NIM-SE-SSNEDDS = 20–25 μm). FTIR confirmed no interaction of drug and excipients. Stability studies demonstrated the physical and thermodynamic stability of reconstituted nanoemulsions with droplet size, PDI, zeta potential, emulsification time, % transmittance and cloud temperature for NIM-SD-SSNEDDS as 247.1 nm, PDI 0.620, 1.353 mV, 38–41 s, 94.64%, 54 °C and for NIM-SE-SSNEDDS as 399.6 nm, PDI 0.821, 1.351 mV, 40–48 s, 92.96%, 49 °C, respectively. FE-SEM images showed globules formed with small sizes, and there was no coalescence evidence, implying the reconstituted nanoemulsions' stability. In vitro dissolution studies revealed a fourfold increase in drug dissolution for NIM-SD-SSNEDDS (84.43%) and NIM-SE-SSNEDDS (76.68%) compared to pure drug (28%). Ex vivo permeation studies indicated almost similar profiles for NIM-SD-SSNEDDS (22.61%) and NIM-SE-SSNEDDS (21.93%) compared to NIM-SNEDDS (25.02%). Conclusion: NIM-SD-SSNEDDS exhibited superior performance compared to NIM-SE-SSNEDDS, highlighting the efficacy of microparticles developed by the spray drying method (SD-CHEM) as adsorbents for solidification. These results suggest enhanced dissolution and permeation for nimodipine in both the solid SNEDDS.

Background: The present study focused on developing a superior adsorbent carrier (microparticles) to solidify the self-emulsifying drug delivery system. The two approaches, solvent evaporation and spray drying, were explored to synthesize the microparticles using chitosan (CH) and EDTA disodium. The 32full factorial design was applied to optimize the microparticle process produced by both methods. Results: The various characterization evaluations of the microparticles revealed amide linkages between the CH and EDTA disodium, and XRD results showed that microparticles were amorphous. The SE-CHEM (C2) and SD-CHEM (Y1) optimized microparticles were free-flowing and had percentage yield (%), 96 ± 1.2 and 58 ± 1.1, zeta potential (mV), 9 ± 0.44 and 4 ± 0.13, and particle size (μm), 3 ± 0.57 and 2 ± 0.4, respectively. SEM images showed uneven surfaces with wide void spaces and flaky texture for optimized microparticles Y1and C2, respectively. The SE-CHEM (C2) had an oil adsorption capacity (OAC %) of 46 ± 0.54 and 60 ± 0.77, and oil desorption capacity (ODC %), 38 ± 0.65 and 56 ± 0.86, for Labrafac and Cremophor RH 40, respectively. The SD-CHEM (Y1) had an oil adsorption capacity (OAC %) of 59 ± 0.71 and 68 ± 0.39, and oil desorption capacity (ODC %), 54 ± 0.11 and 65 ± 0.74, for Labrafac and Cremophor RH 40, respectively. In the surface free energy components analysis, the SE-CHEM (C2) had an enhanced dispersive component [γLW(mJ/m2)] of 32 ± 0.68 and 37 ± 0.47 for Labrafac and Cremophor RH 40, respectively. The SD-CHEM (Y1) had an enhanced dispersive component [γLW(mJ/m2)] of 48 ± 0.7 and 52 ± 0.41 for Labrafac and Cremophor RH 40, respectively. The SE-CHEM (C2) had enhanced dynamic advancing contact angles [θa(°)] of 75 ± 0.19 and 78 ± 0.75 for Labrafac and Cremophor RH 40, respectively. The SD-CHEM (Y1) had enhanced dynamic advancing contact angles [θa(°)] of 74 ± 0.6 and 80 ± 0.21 for Labrafac and Cremophor RH 40, respectively. Conclusion: All the findings indicate that the microparticles have superior characteristics to serve as the adsorbent base for solid self-emulsifying drug delivery systems.

Background: Prostate cancer is considered the second most diagnosed cancer, and one of the most commoncauses of death from cancer in men. Apalutamide is an effective, safe, and well-tolerated agent used for the treatmentof men with non-metastatic Castration-Resistant Prostate Cancer (nmCRPC) and metastatic Hormone-Naive ProstateCancer (mHNPC). Androgen receptor signaling is a leading factor that drives these prostate tumors. USFDA has approvedapalutamide on 14 February 2018 as an agent that targets androgen receptor signaling through inhibition causingsignificant improvement in metastasis-free survival in patients with prostate cancer. Objective: In this review, various aspects related to apalutamide have been summarized which involve the mechanismof action, chemistry, synthesis, pharmacokinetics, pharmacodynamics, adverse reactions, and safety parameters. Methods: The literature was thoroughly searched in the relevant databases to identify studies published in this fieldduring recent years. Special attention has been given to apalutamide clinical trials phases and its promising future asone of the first-line agents for the treatment of patients with advanced prostate cancer. Results: Ongoing trials are progressing for apalutamide monotherapy and also for its combinations in other diseasesettings. The expected results of such trials will shape the future scenario of prostate cancer therapy. Conclusion: This review article has highlighted different aspects of Apalutamide like its mechanism of action, adverseeffects, pharmacokinetics, pharmacodynamics, clinical trials among others. The contents of this article should make anexcellent read for prospective researchers in this field.

Background: The platinum (II) complexes as anticancer agents have been well explored for the developmentof novel analogs. Yet, none of them achieved clinical importance in oncology. At present, anticancer compoundscontaining platinum (II) complexes have been employed in the treatment of colorectal, lung, and genitourinary tumors.Among the platinum-based anticancer drugs, Cisplatin (cis-diamine dichloroplatinum (II), cis-[Pt(NH3)2Cl2]) is one ofthe most potent components of cancer chemotherapy. The nephrotoxicity, neurotoxicity and ototoxicity, and platinumcompounds associated resistant cancer are some major disadvantages. Objective: With the rapidly growing interest in platinum (II) complexes in tumor chemotherapy, researchers havesynthesized many new platinum analogs as anticancer agents that show better cytotoxicity, and less off-target effectswith less cellular resistance. This follows the introduction of oxaliplatin, water-soluble carboplatin, multinuclear platinumand newly synthesized complexes, etc. Methods: This review emphasizes recent advancements in drug design and development, the mechanism of platinum(II) complexes, their stereochemistry, current updates, and biomedical applications of platinum-based anticancer agents. Conclusion: In the last few decades, the popularity of platinum complexes as potent anti-cancer agents has risen asscientists have synthesized many new platinum complexes that exhibit better cytotoxicity coupled with less off-targeteffects.

Background: Lurbinectedin was approved on June 15, 2020 by the Food and Drug Administration with thebrand name ZEPZELCA as the first systematic approved therapy for patients having Small Cell Lung Cancer (SCLC). Objectives: In this review, an attempt is made to summarize different aspects of Lurbinectedin, including the pathophysiology,chemistry, chemical synthesis, mechanism of action, adverse reactions, and pharmacokinetics. Specialattention is given to various reported clinical trials of lurbinectedin. Methods: A comprehensive literature search was conducted in the relevant databases like ScienceDirect, PubMed,ResearchGate and Google Scholar to identify studies. After a thorough study of these reports, significant findings/datawere collected and compiled under suitable headings. Important findings related to clinical trials have been tabulated. Conclusion: Lurbinectedin is known to act by inhibiting the active transcription of encoding genes, thereby suppressingtumor-related macrophages with an impact on tumour atmosphere. Lurbinectedin has emerged as a potential drugcandidate for the treatment of Small-Cell Lung Cancer (SCLC).

Background: Neurodegenerative disorders belong to different classes of progressive/chronic conditions that affect the peripheral/central nervous system. It has been shownthrough studies that athletes who play sports involving repeated head trauma and sub-concussiveimpacts are more likely to experience neurological impairments and neurodegenerative disorders inthe long run Aims: The aim of the current narrative review article is to provide a summary of various nutraceuticalsthat offer promise in the prevention or management of sports-related injuries, especially concussionsand mild traumatic brain injuries. Methods: This article reviews the various potential nutraceutical agents and their possible mechanismsin providing a beneficial effect in the injury recovery process. A thorough survey of the literaturewas carried out in the relevant databases to identify studies published in recent years. In thepresent article, we have also highlighted the major neurological disorders along with the associatednutraceutical(s) therapy in the management of disorders. Results: The exact pathological mechanism behind neurodegenerative conditions is complex aswell as idiopathic. However, mitochondrial dysfunction, oxidative stress as well as intracellular calciumoverload are some common reasons responsible for the progression of these neurodegenerativedisorders. Owing to the multifaceted effects of nutraceuticals (complementary medicine), thesesupplements have gained importance as neuroprotective. These diet-based approaches inhibit differentpathways in a physiological manner without eliciting adverse effects. Food habits and lifestyleof an individual also affect neurodegeneration. Conclusion: Studies have shown nutraceuticals (such as resveratrol, omega-3-fatty acids) to be efficaciousin terms of their neuroprotection against several neurodegenerative disorders and to beused as supplements in the management of traumatic brain injuries. Protection prior to injuries isneeded since concussions or sub-concussive impacts may trigger several pathophysiological responsesor cascades that can lead to long-term complications associated with CNS. Thus, the use ofnutraceuticals as prophylactic treatment for neurological interventions has been proposed.

Background: Nowadays, biomedical research has been focusing on the design and development of new drug delivery systems that provide efficient drug targeting. The molecularly imprinted polymers (MIPs) have attracted wide interest and play an indispensable role as a drug carrier. Drug delivery systems based on MIPs have been frequently cited in the literature. They are cross-linked polymers that contain binding sites according to the complementary structure of the template molecules. They possess distinctive features of structure predictability and site recognition specificity. Versatile applications of MIPs include purification, biosensing, bioseparation, artificial antibodies, and drug delivery. An ideal MIPs should include features such as biocompatibility, biodegradability, and stability. Objective: In this article, we elaborate on the historic growth, synthesis, and preparation of different MIPs and present an updated summary of recent advances in the development of new drug delivery systems which are based on this technique. Their potential to deliver drugs in a controlled and targeted manner will also be discussed. Conclusion: MIPs possess unique advantages, such as lower toxicity, fewer side effects, and good therapeutic potential. They offer administration of drugs by different routes, i.e., oral, ocular or transdermal. Despite several advantages, biomedical companies are hesitant to invest in MIPs based drug delivery systems due to the limited availability of chemical compounds.

Today, antibacterial drug resistance has turned into a significant public health issue. Repeatedintake, suboptimal and/or unnecessary use of antibiotics, and, additionally, the transfer of resistancegenes are the critical elements that make microorganisms resistant to conventional antibiotics.A substantial number of antibacterials that were successfully utilized earlier for prophylaxis and therapeuticpurposes have been rendered inadequate due to this phenomenon. Therefore, the explorationof new molecules has become a continuous endeavour. Many such molecules are at various stages ofthe investigation. A surprisingly high number of new molecules are currently in the stage of phase 3clinical trials. A few new agents have been commercialized in the last decade. These include solithromycin,plazomicin, lefamulin, omadacycline, eravacycline, delafloxacin, zabofloxacin, finafloxacin,nemonoxacin, gepotidacin, zoliflodacin, cefiderocol, BAL30072, avycaz, zerbaxa, vabomere,relebactam, tedizolid, cadazolid, sutezolid, triclosan, and afabiacin. This article aims to review theinvestigational and recently approved antibacterials with a focus on their structure, mechanisms ofaction/resistance, and spectrum of activity. Delving deep, their success or otherwise in various phasesof clinical trials is also discussed while attributing the same to various causal factors.

Nanotechnology is thriving these days and plays a great role in the expansion of biosensors. A range of nanomaterials is used in the growth of biosensors in order to boost the performance and sensitivity of biosensors. Nanomaterials like nanowire, nanoparticles, carbon nanotubes, quantum dots, etc., are helpful in increasing different properties like enzyme loading capacity, bioanalyte loading, good absorption as well as immobilization of enzymes. The skill of nanobiosensors becomes extra accurate and reliable as it allows quick selection of diverse analytes at little cost. The main target for nanobiosensor research includes the development of novel technologies in order to make improvements in the field of marker detection of human and animal disease, identification and study of therapeutic compounds, characterization of nano and bio-materials and the development of biocatalysts. This paper has reviewed basic principles and various nano-structure based biosensors along with their applications in different areas such as biomedical and forensic, environmental, agricultural and the food sector and recent advancements.

The pyrazolines give the reactions of aliphatic derivatives, resembling unsaturated compounds in their behavior towards permanganate and nascent hydrogen. This nucleus has been associated with various biological activities, including inflammatory action. Thiazolinone is a heterocyclic compound that contains both sulfur and nitrogen atom with a carbonyl group in their structure. Thiazolinone and their derivatives have attracted continuing interest because of their various biological activities, such as anti-inflammatory, antimicrobial, anti-proliferative, antiviral, anticonvulsant, etc. The aim of the research was to club pyrazoline nucleus with thiazolinone in order to have a significant anti-inflammatory activity. The synthesized compounds were chemically characterized for the establishment of their chemical structures and to evaluate it as an anti-inflammatory agent. In the present work, eight derivatives of substituted pyrazoline (PT1-PT8) were synthesized by a threestep reaction. The compounds were subjected to spectral analysis by Infrared, Mass, and Nuclear magnetic resonance spectroscopy and elemental analysis data. All the synthesized derivatives were evaluated for their in vivo anti-inflammatory activity. The synthesized derivatives were evaluated for their affinity towards target COX-1 and COX-2, using indomethacin as the reference compound molecular docking visualization through AutoDock Vina. Compounds PT-1, PT-3, PT-4, and PT-8 exhibited significant anti-inflammatory activity at 3rd hour, being 50.7%, 54.3%, 52.3%, and 57%, respectively, closer to that of the standard drug indomethacin (61.9%). From selected anti-inflammatory targets, the synthesized derivatives exhibited better interaction with COX-1 and COX-2 receptor, where indomethacin showed a docking score of -6.5 kJ/mol, compound PT-1 exhibited the highest docking score of -9.1 kJ/mol for COX-1 and compound PT-8 had a docking score of 9.4 kJ/mol for COX-2. It was concluded that synthesized derivatives have more interaction with COX-2 receptors in comparison to the COX-1 receptors because the docking score with COX-2 receptors was very good. It is concluded that the synthesized derivatives (PT-1 to PT-8) are potent COX-2 inhibitors.

Background: Tenosynovial giant cell tumor refers to a group of rarely occurring tumors that are formed in the joints, which are characterized by pain, swelling, and limitation of movement of the joint. Surgery is the main treatment strategy, but the tumor is likely to recur, especially in pigmented villonodular synovitis, which is the diffuse-type giant cell tumor. Pexidartinib was approved in August 2019 by the Food and Drug Administration (FDA) with a brand name TURALIO as the first systemic approved therapy for patients having Tenosynovial Giant Cell Tumors (TGCT). Objective: In this review, different aspects pertaining to pexidartinib have been summarized, including the pathophysiology of TGCT, chemistry, pharmacokinetics and pharmacodynamics of pexidartinib. Special attention is given to various reported clinical trials of pexidartinib. Methods: A comprehensive literature search was conducted in the relevant databases to identify studies published in this field during recent years. Conclusion: Pexidartinib acts by inhibiting the Colony-Stimulating Factor (CSF1)/CSF1 receptor pathway, which leads to the inhibition of the cell lines proliferation and promotes the autophosphorylation process of the ligand-induced CSF1 receptor. Pexidartinib emerged as a potential drug candidate for the treatment of TGCT.

A sizeable proportion of currently marketed drugs come from heterocycles. The heterocyclic moiety 5-pyrazolone is well known five-membered ring containing nitrogen. Derivatives of this wonder nucleus have exhibited activities as diverse as antimicrobial, anti-inflammatory, analgesic, antidepressant, anticonvulsant, antidiabetic, antihyperlipidemic, antiviral, antitubercular, antioxidant, anticancer and antiviral, including action against severe acute respiratory syndrome (SARS) or 3C protease inhibitor. A number of drugs based on this motif have already made it to the market. Standard texts and literature on medicinal chemistry cite different approaches for the synthesis of 5- pyrazolones. The present review provides an insight view to 5-pyrazolone synthesis, their biological profile and structure-activity relationship studies.

Over the years, the branch of oncology has reached a mature stage, and substantial development and advancement have been achieved in this dimension of medical science. The synthesis and isolation of numerous novel anticancer agents of natural and synthetic origins have been reported. Thiazole and 4-thiazolidinone containing heterocyclic compounds, having a broad spectrum of pharmaceutical activities, represent a significant class of medicinal chemistry. Thiazole and 4-thiazolidinone are five-membered unique heterocyclic motifs containing S and N atoms as an essential core scaffold and have commendable medicinal significance. Thiazoles and 4-thiazolidinones containing heterocyclic compounds are used as building blocks for the next generation of pharmaceuticals. Thiazole precursors have been frequently used due to their capabilities to bind to numerous cancer-specific protein targets. Suitably, thiazole motifs have a biological suit via inhibition of different signaling pathways involved in cancer causes. The scientific community has always tried to synthesize novel thiazole-based heterocycles by carrying out different replacements of functional groups or skeleton around thiazole moiety. Herein, we report the current trend of research and development in anticancer activities of thiazoles and 4-thiazolidinones containing scaffolds. In the current study, we have also highlighted some other significant biological properties of thiazole, novel protocols of synthesis for the synthesis of the new candidates, along with a significant broad spectrum of the anticancer activities of thiazole containing scaffolds. This study facilitates the development of novel thiazole and 4-thiazolidinone containing candidates with potent, efficient anticancer activity and less cytotoxic property.

Flavonoids are polyphenolic compounds that are mainly derived from fruits and vegetables and constitute an essential part of plant-derived beverages such as green tea, wine and cocoa-based products. They have been shown to possess anticancer effects via different mechanisms such as carcinogen inactivation, antiproliferation, cell cycle arrest, induction of apoptosis and differentiation, inhibition of angiogenesis, anti-oxidation and reversal of multidrug resistance or a combination of any two or more of these mechanisms. The present review summarizes the chemistry, biosynthesis and anticancer evaluation of flavonoids in both animal and human studies. A special emphasis has been placed on the flavonoids that are being screened in different phases of clinical trials for chemoprotective action against various cancers.

Background: Having various limitations in conventional drug delivery system, it is importantto focus on the target-specific drug delivery system where we can deliver the drug withoutany degradation. Among various challenges that are thrown to a formulation scientist, deliveringthe drug to its right site, in its right dose, is also an important aim. A focused drug transport aims toextend, localize, target and have a safe drug interaction with the diseased tissue. Objective: The aim of targeted drug delivery is to make the required amount of the drug availableat its desired site of action. Drug targeting can be accomplished in a number of ways that includeenzyme mediation, pH-dependent release, use of special vehicles, receptor targeting, among othermechanisms. Intelligently designed targeted drug delivery systems also offer the advantages of alow dose of the drug along with reduced side effects which ultimately improves patient compliance.Incidences of dose dumping and dosage form failure are negligible. A focused drug transportaims to have a safe drug interaction with the diseased tissue. Conclusion: This review focuses on the available targeting techniques from experiment to perfectionfor delivery to the colon, brain, and other sites of interest. Overall, the article should make anexcellent read for the researchers in this area. Newer drug targets may be identified and exploitedfor successful drug targeting.

Background: Olanzapine belongs to a new class of dual spectrum antipsychotic agents. It is known to show promise in managing both the positive and negative symptoms of schizophrenia. Drug delivery systems based on nanostructured lipid carriers (NLC) are expected to provide rapid nose-to-brain transport of this drug and improved distribution into and within the brain. Objective: The present study deals with the preparation and evaluation of olanzapine loaded NLC via the intranasal route for schizophrenia. Methods: Olanzapine-NLC were formulated through the solvent injection method using isopropyl alcohol as the solvent, stearic acid as solid lipid, and oleic acid as liquid lipid, chitosan as a coating agent, and Poloxamer 407 as a surfactant. NLC were characterized for particle size, polydispersity index, entrapment efficiency, pH, viscosity, X-ray diffraction studies, in-vitro mucoadhesion study, in- vitro release and ex-vivo permeation studies. The shape and surface morphology of the prepared NLC was determined through transmission electron microscopy. To detect the interaction of the drug with carriers, compatibility studies were also carried out. Results: Average size and polydispersity index of developed formulation S6 was 227.0±6.3 nm and 0.460, respectively. The encapsulation efficiency of formulation S6 was found to be 87.25%. The pH, viscosity, in-vitro mucoadhesion study, and in- vitro release of optimized olanzapine loaded NLC were recorded as 5.7 ± 0.05, 78 centipoise, 15±2 min, and 91.96%, respectively. In ex-vivo permeation studies, the percent drug permeated after 210 min was found to be 84.03%. Conclusion: These results reveal the potential application of novel olanzapine-NLC in intranasal drug delivery system for the treatment of Schizophrenia.

Background: An upsurge in the number of antibiotic-resistant microbial infections has warranted the discovery and development of new antibiotics. This is a matter of great concern for effective therapy for a search of novel antimicrobial agents. Literature has a number of reports of involvement of oxidative stress due to an imbalance between the generation and neutralization of free radicals in many diseases. Heterocyclic compounds have been involved in the treatment of various disorders. Benzothiazole is one such heterocyclic nucleus having benzene ring merged with the thiazole ring. Among the various substitutions possible in this nucleus, substitutions at position-2 have already been reported with potential bioactivities. Thus, different substituted compounds have been synthesized which could serve as antimicrobials and antioxidants. Methods: Benzothiazole derivatives (B1-B7) were synthesized by two-step reactions and the structures were confirmed through infrared, mass and NMR spectroscopy. The compounds were evaluated for in vitro antioxidant and antimicrobial activities using standard methods. Results: The results of antibacterial and antifungal activity showed that compound B4exhibited maximum activity against all the tested strains of microorganisms with the zone of inhibition 17.1-18.5 mm and MIC value 1.1-1.5 μg/mL. Compound B5exhibited potent antioxidant activity. Conclusion: The compounds substituted with halogen on the aryl ring showed increased antimicrobial activity as seen in the case of compound B4(6-fluoro). The compounds substituted with a hydroxyl group (B5) exhibited good antioxidant activity.

Thiazolidine-2, 4-diones and their derivatives are a well-established chemical class of compounds that express their pharmacological actions through insulin sensitization and enhanced glucose utilization in peripheral tissues. In the current research different approaches have been employed to synthesize thiazolidine-2, 4-dione derivatives and these synthesized compounds were chemically characterized for the establishment of their chemical structures. A series of thiazolidine-2, 4-dione (TZD) derivatives, Scheme 1 (3A-3V) 22 compounds, were synthesized and characterized by FT-IR, 1H NMR and mass spectral analysis. The title compounds were screened for their in vitro and in vivo antidiabetic, antioxidant, and cytotoxicity studies. In vivo antihyperglycemic effect was assessed by measuring plasma glucose (PG) levels in alloxan-induced type II diabetic rat models. The synthesized TZD derivatives were evaluated for hepatotoxicity and pancreatic tissue integrity. Antioxidant activity was evaluated by the DPPH method and H2O2 method. Thiazolidinedione derivatives were subjected to predict free energy of binding towards target PPARγ, using rosiglitazone as the reference compound for molecular docking visualization through the FlexX docking program. Molecular docking studies are also performed for understanding the binding of a ligand to a receptor. The compound 3V 4-(5- (naphthalen-1-ylmethylene)-2, 4-dioxothiazolidin-3-yl) benzoic acid exhibited better blood glucoselowering activity than that of the standard drug rosiglitazone. Compound 3T and 3U exhibited potent antioxidant activity. Among the tested compounds for cytotoxicity using an MTT assay, compound 3H 5-(4-chlorobenzylidene)-2, 4-dioxothiazolidin-3-yl) benzoic acid exhibited better viability and cytotoxicity activity. From selected anti-diabetic targets, the proposed derivatives exhibited better interaction with PPARγ receptor, for example, while rosiglitazone showed a docking score of -19.891 kJ/mol, compound 3V exhibited highest docking score of -31.6617 kJ/mol. Computational molecular docking study demonstrated the selectivity and provided a binding model for the further refinement of this chemotype. Therefore, this series of thiazolidine-2, 4-diones derivatives (3A-3V) have considerable importance for development as a potential antihyperglycemic and hypolipidemic agents.

Lymphoma refers to a specialized category of blood cancers, which is characterized by lymph node enlargement, reduced body weight, prolonged tiredness, and fever associated with sweats. Traditional treatment strategies involve chemotherapy, radiation therapy, targeted therapy, and surgery. Copanlisib has emerged as a very potent drug which acts through inhibiting PI3K enzyme. The FDA has approved it for specific treatment of follicular Lymphoma in September 2017. Copanlisib induces tumor cell death along with the prevention of proliferation of dominant malignant β-cells. Copanlisib has a large volume of distribution i.e., 871L (%CV 47.4), plasma protein binding up to 15.8%, plasma half-life(t1/2) of 39.1h and the mean systemic plasma clearance 18.9 L/h (%CV 51.2). In the present review, various aspects related to Copanlisib have been summarized, which include pathophysiology, synthetic strategy, pharmacokinetics, pharmacodynamics and clinical studies. A special emphasis is paid on various reported adverse effects and in silico/in vivo studies conducted on Copanlisib.

In the present research work, ten novel thiazolidine-2,4-dione-coumarin adducts were synthesized using three step reaction procedure. Firstly, benzylidene thiazolidinediones (II) were synthesized by facile Knoevenagel condensation reaction using various substituted aldehydes, thiourea and chloroacetic acid. Further, 3-bromoacetyl coumarins (IV) were synthesized using salicylaldehyde and ethylacetoacetate in the presence of piperidine as a catalyst forming 3-acetylcoumarin (III) which was brominated to form 3- bromoacetyl coumarin. Finally, both these compounds i.e., (II) and (IV) were condensed in the presence of dimethyl formamide and potassium carbonate leading to the formation of novel thiazolidine-2,4-dione-coumarin adducts. The synthesized compounds were screened for different biological activities. Antioxidant activity was performed in-vitro by three different methods namely FRAP (Ferric ion reducing antioxidant power) method, DPPH (1,1-diphenyl-2-picrylhydrazyl) method and hydrogen peroxide scavenging assay method using ascorbic acid as a standard. Among the synthesized compounds, FP10 and FP9 emerged as breakthrough antioxidant agents. Furthermore, the compounds were checked for their anti-inflammatory and antidiabetic activity in which compounds FP7 and FP1 showed promising anti-inflammatory and antidiabetic potential in-vivo, and may be used as lead compound for future studies.

Hydrogels are the biomaterials comprising network of natural or synthetic polymers capable of absorbing large amount of water. Hydrogels are “Smart Gels” or “Intelligent Gels” which can be made to respond to the various environmental conditions like temperature, pH, magnetic/electric field, ionic strength, inflammation, external stress etc. There are numerous potential applications of hydrogels in modern day life ranging from a diaper to gene delivery. This review succinctly describes the classification, properties and preparation methods along with numerous diverse applications of hydrogels like agricultural hydrogels, hydrogel for drug delivery, sensing, dental adhesives, wound healing and tissue regeneration, diet aid and gastric retention and in tissue engineering etc. Hydrogels can be regarded as highly valuable biomaterials for human-beings.

Two series of novel 1-(4-substitutedbenzoyl)-3-((2-oxoimidazolin-1-yl)methyl)-1H-pyrazol-5(4H)-one, 1- methyl-3-((1-(4-substitutedbenzoyl)-5-oxo-4,5-dihydro-1H-pyrazol-3-yl)methyl)urea,1-((1-(4-substitutedbenzoyl)-5-oxo- 4,5-dihydro-1H-pyrazol-3-yl)methyl) thio urea and 1-((1-(4-substitutedbenzoyl)-5-oxo-4,5-dihydro-1H-pyrazol-3- yl)methyl)-3-phenyl thiourea were synthesized and characterized by IR, mass, 1HNMR spectroscopic techniques. The synthesized compounds were evaluated for anticonvulsant activity by using maximal electroshock seizure (MES) model. Among the newly synthesized compounds, most of the compounds showed significant activity and 1C2 emerged as the most active analogue.

Fullerenes, the third carbon allotrope, have emerged as agents which could revolutionize the treatment of many diseases. Fullerenes possess different biological applications like neuroprotective agents, antioxidants, anti-HIV activity, enzyme inhibition, antiapoptotic activity and the list is ever increasing. Moreover, they are being utilized as drug carrier systems and also for many non-biological applications like superconductors, catalysis and so on. Their size has made them promising agents for nanotechnology. This article aims at outlining the chemistry, properties and non-biological applications of fullerenes and their evolution to biological applications, thereby traversing their evolution from simple carbon allotropes to present day nano-medicinal agents.