Liposomes: An Emerging Strategy for the Effective Treatment of Rheumatoid Arthritis.

BACKGROUND: A Liposomal delivery system is a novel and distinguishing way of organized medicine administration. The advancements in liposomal technology allow for controlled drug distribution to treat rheumatoid arthritis effectively. Liposomes are microscopic lipid-based vesicles that have shown promise in transporting substances, such as superoxide dismutase, hemoglobin, erythrocyte interleukin-2, gamma interferon, and smaller compounds. OBJECTIVE: Liposomes are biocompatible, nontoxic, biodegradable, non-immunogenic, and flexible, with sizes ranging from 0.025 to 2.5 micrometers. LDS is normally employed to distribute drugs through topical conduits, but fresh investigation has shown that it offers promise for oral, ocular, and parenteral administration. Our major objective is to gather information about liposomes, focusing on their applicability in rheumatoid arthritis treatment. METHODS: In the current review, we have tried to cover the preparation techniques, clinical trials, patents, marketed formulations, vesicle types, formulations used to treat rheumatoid arthritis and other ailments, and layered liposomal formulations with improved characteristics. CONCLUSION: Research has established LDS as a biocompatible, sustainable, non-toxic, adaptable material. Researchers working on LDS technology in rheumatoid arthritis will find this review particularly useful as it may unclutter novel ways for therapeutic intercessions in treating the disease.

Marine-Derived Compounds: A Powerful Platform for the Treatment of Alzheimer's Disease.

Alzheimer's disease (AD) is a debilitating form of dementia that primarily affects cholinergic neurons in the brain, significantly reducing an individual's capacity for learning and creative skills and ultimately resulting in an inability to carry out even basic daily tasks. As the elderly population is exponentially increasing, the disease has become a significant concern for society. Therefore, neuroprotective substances have garnered considerable interest in addressing this universal issue. Studies have shown that oxidative damage to neurons contributes to the pathophysiological processes underlying AD progression. In AD, tau phosphorylation and glutamate excitotoxicity may play essential roles, but no permanent cure for AD is available. The existing therapies only manage the early symptoms of AD and often come with numerous side effects and toxicities. To address these challenges, researchers have turned to nature and explored various sources such as plants, animals, and marine organisms. Many historic holy books from different cultures emphasize that adding marine compounds to the regular diet enhances brain function and mitigates its decline. Consequently, researchers have devoted significant time to identifying potentially active neuroprotective substances from marine sources. Marine-derived compounds are gaining recognition due to their abundant supply of diverse chemical compounds with biological and pharmacological potential and unique mechanisms of action. Several studies have reported that plants exhibit multitarget potential in treating AD. In light of this, the current study focuses on marine-derived components with excellent potential for treating this neurodegenerative disease.

Decoding Therapeutic Applications of Quercetin: Recent Advancements in Nanotechnological Strategies.

For centuries, people have used herbal medicine to treat a diversity of health complications and as a natural substance, they have a favourable effect on our health. Herbal ingredients can be utilized as lead molecules in the innovation and development of a new drug. Flavonoids are a class of chemical compounds with diverse phenolic structures, and they are found in a wide variety of foods, including fruits, vegetables, cereals, bark, roots, stems, flowers, tea, and wine. Quercetin is the most prevalent polyphenolic bioflavonoid or flavonoid. Quercetin is found in many food products and has demonstrated a wide range of pharmacological activities, including the treatment of allergies, ocular diseases, metabolic ailments, inflammatory illnesses, cardiovascular ailments and arthritis. Quercetin has attracted interest as an emerging pharmacophore with the potential to significantly advance research and the development of novel therapeutic medicines for a variety of diseases. Despite having a huge therapeutic potential, these flavonoids have unfavourable pharmacokinetic characteristics, low bioavailability, and poor solubility, limiting their application in therapeutics. The objective of the current study is to present a new update on the major therapeutic uses of quercetin and other types of nanocarriers that contain quercetin to treat various ailments.

Therapeutic Potential and Clinical Effectiveness of Quercetin: A Dietary Supplement.

Fruits and vegetables (like apples, citrus, grapes, onions, parsley, etc.) are the primary dietary sources of quercetin. In addition, isolated quercetin is also available on the market as a dietary supplement with a daily dose of up to 1000 mg/d. The objective of the present study is to explore the therapeutic potential and clinical efficacy of quercetin as a dietary supplement. The present paper highlights the safety parameters and clinical trial studies with several targets reviewed from the data available on PubMed, Science Direct, ClinicalTrails. gov, and from many reputed foundations. The results of the studies prove the unique position of quercetin in the treatment of various disorders and the possibility of using phytochemicals such as quercetin for an efficient cure. As evidenced by the numerous published reports on human interventions, it has been concluded that quercetin intake significantly improves disease conditions with minimal adverse effects.

A Profound Insight into the Structure-activity Relationship of Ubiquitous Scaffold Piperazine: An Explicative Review.

Despite extensive research in the field of drug discovery and development, still there is a need to develop novel molecular entities. Literature reveals a substantial heterocyclic nucleus named, piperazine, which shows an immense therapeutic voyage. For several decades, molecules having the piperazine nucleus have entered the market as a drug exhibiting biological potential. It was known to possess antipsychotic, antihistamine, antianginal, antidepressant, anticancer, antiviral, cardioprotective, and anti-inflammatory activity with a specific basis for structural activity relationship. Thus, it is regarded as a key structural feature in most of the already available therapeutic drugs in the market. Reports also suggest that the extensive utilization of these currently available drugs having a piperazine nucleus shows increasing tolerance significantly day by day. In addition to this, various other factors like solubility, low bioavailability, cost-effectiveness, and imbalance between pharmacokinetics and pharmacodynamics profile limit their utilization. Focusing on that issues, various structural modification studies were performed on the piperazine moiety to develop new derivatives/analogs to overcome the problems associated with available marketed drugs. Thus, this review article aims to gain insight into the number of structural modifications at the N-1 and N-4 positions of the piperazine scaffold. This SAR approach may prove to be the best way to overcome the above-discussed drawbacks and lead to the design of drug molecules with better efficacy and affinity. Hence, there is an urgent need to focus on the structural features of this scaffold which paves further work for deeper exploration and may help medicinal chemists as well as pharmaceutical industries.

A Review on Novel Applications of Nanotechnology in the Management of Prostate Cancer.

BACKGROUND: Prostate cancer continues to be a serious danger to men's health, despite advances in the field of cancer nanotechnology. Although different types of cancer have been studied using nanomaterials and theranostic systems derived from nanomaterials, they have not yet reached their full potential for prostate cancer due to issues with in vivo biologic compatibility, immune reaction responses, accurate targetability, as well as a therapeutic outcome related to the nano-structured mechanism. METHOD: The ultimate motive of this article is to understand the theranostic nanotechnology-based scheme for treating prostate cancer. The categorization of diverse nanomaterials in accordance with biofunctionalization tactics and biomolecule sources has been emphasized in this review so that they might potentially be used in clinical contexts and future advances. These opportunities can enhance the direct visualization of prostate tumors, early identification of prostate cancer-associated biomarkers at extremely low detection limits, and finally, the therapy for prostate cancer. RESULT: In December 2022, a thorough examination of the scientific literature was carried out utilizing the Web of Science, PubMed, and Medline databases. The goal was to analyze novel applications of nanotechnology in the treatment of prostate cancer, together with their structural layouts and functionalities. CONCLUSION: The various treatments and the reported revolutionary nanotechnology-based systems appear to be precise, safe, and generally successful; as a result, this might open up a new avenue for the detection and eradication of prostate cancer.

Quercetin-based Nanoformulation: A Potential Approach for Cancer Treatment.

Nanoformulations derived from natural products are gaining popularity as a treatment option for several human diseases, including cancer, as they offer a viable alternative to conventional cancer therapies, which are often associated with numerous side effects and complications. Quercetin (Que), a plant-derived phenolic molecule, has demonstrated potential as a chemotherapeutic agent for different types of cancer. However, Que's low water solubility, instability towards antioxidants, low bioavailability, and severe biotransformation constraints make it challenging to use in vivo. Nanoparticles have emerged as a promising technology for the precise targeting of tumor cells, leading to improved efficacy and specificity in cancer therapies. In this review, the impact of flavonoid nanoformulations on enhancing the safety, therapeutic potential, and bioavailability of Que in cancer treatment is highlighted. A variety of nanoparticle types have been developed, including polymeric micelles, liposomes, PLGA nanoparticles, coencapsulation, chitosan NPs, lipid carriers, silver and gold NPs, inorganic NPs, organic metal frameworks, and biomacromolecule- based NPs, all aimed at improving the antineoplastic efficacy of Que. These nanoparticles offer several advantages, including prolonged circulation time, tumor-specific biodistribution, high encapsulation efficiency, enhanced therapeutic efficacy, and controlled release. This review provides fresh insights into the arena of drug discovery for tumor therapies by focusing on the influence of flavonoid nanoformulations on the enhancement of their safety, therapeutic, and bioavailability characteristics.

1,3-thiazole Derivatives: A Scaffold with Considerable Potential in the Treatment of Neurodegenerative Diseases.

1,3-thiazoles, which contain nitrogen and a sulfur atom is an unsaturated five-membered heterocyclic ring, have achieved a unique significant place in drug design and development because of their versatile structure and a variety of pharmacological activities, viz. anticancer, antiviral, antimicrobial, anticonvulsant, antioxidant, antidiabetic, etc. They have inspired researchers to design novel thiazole with different biological activities. The presence of the thiazole moiety has resulted in a large number of clinically useful drugs with a wide range of activities, such as Ritonavir (antiviral), Sulfathiazole (antimicrobial antibiotic), Abafungin, Ravuconazole (antifungal), Meloxicam (NSAID), etc., that further verify this statement. The prevalence of neurodegenerative diseases like Alzheimer's, Parkinson's, and Huntington's is increasing at a rapid pace but existing treatments mainly provide symptomatic relief and are associated with undesired effects. Consequently, designing novel compounds with more effectiveness and reduced toxicity are required. 1,3-thiazole derivatives have emerged as excellent candidate in this regard and have an important role for the treatment of neurodegenerative diseases. In the current review, we have gathered all the appropriate literature which demonstrate the remarkable role of 1,3-thiazole and its derivatives in these diseases that may help design new compounds with more desired characteristics. The literature was assessed through worldwide scientific databases like GOOGLE, SCOPUS, and PUBMED using different keywords, and only relevant information published in English was evaluated.

An Update on Herbal Products for the Management of Inflammatory Bowel Disease.

Inflammatory Bowel Disease (IBD), including Ulcerative Colitis (UC) and Crohn's Disease (CD), is a continuously increasing healthcare problem mainly characterized by chronic relapsing intestinal inflammation. The common symptoms of UC and CD include inflammation, diarrhea, abdominal pain, bleeding, and weight loss. IBD is generally caused by an interaction between genetic and environmental or microbial factors that influence the body's immune response and is responsible for digestive disorders and inflammation of the intestinal tract. However, a complete understanding of the pathophysiology and work-up of IBD is necessary to ensure appropriate treatment for the management of this complex disease. This review enlightens herbal therapeutics and drug delivery systems for the management of IBD, and thus provides new insights into this field and facilitates access to new treatments.

In silico docking based screening of constituents from Persian shallot as modulators of human glucokinase.

Purpose: Small molecule glucokinase (GK) modulators not only decrease fasting and basal plasma sugar contents but also progress glucose tolerance. The hydro-ethanolic extract of the Persian shallot (Allium hirtifolium Boiss.) decreased blood glucose, improved plasma insulin and amplified GK action. The present study was proposed to screen phytoconstituents from Persian shallot as human GK activators using in silico docking studies. Methods: A total of 91 phytoconstituents reported in Persian shallot (A. hirtifolium Boiss.) were assessed in silico for the prediction of drug-like properties and molecular docking investigations were carried out with human GK using AutoDock vina with the aim of exploring the binding interactions between the phytoconstituents and GK enzyme followed by in silico prediction of toxicity. Results: Almost all the phytoconstituents tested showed good pharmacokinetic parameters for oral bioavailability and drug-likeness. In the docking analysis, cinnamic acid, methyl 3,4,5-trimethoxy benzoate, quercetin, kaempferol, kaempferol 3-O-ß-D-glucopyranosyl-(1- > 4)-glucopyranoside, 5-hydroxy-methyl furfural, ethyl N-(O-anisyl) formimidate, 2-pyridinethione and ascorbic acid showed appreciable hydrogen bond and hydrophobic type interactions with the allosteric site residues of the GK enzyme. Conclusion: These screened phytoconstituents may serve as promising hit molecules for further development of clinically beneficial and safe allosteric activators of the human GK enzyme.

Hemorrhoid Disease: A Review on Treatment, Clinical Research and Patent Data.

BACKGROUND: Hemorrhoid disease (HD) is an anal-rectal ailment that is commonly painful or may be painless and causes rectal bleeding with or without prolapsing anal tissue. It is generally associated with bleeding, prolapse, pruritus, and discomfort, which results in a diminished quality of life and well-being. OBJECTIVE: To highlight the recent developments in terms of safety, clinical efficacy, and marketed formulation for the effective management of hemorrhoids. METHOD: Reported literature available on Scopus, PubMed, Science Direct, Clinicaltrails.gov, and from many reputed foundations has been studied to summarize the recent development and clinical studies for the management of hemorrhoids. RESULTS AND CONCLUSION: The high incidence of hemorrhoids obliges the development of new molecules; therefore, safe and efficient drugs to confer protection against hemorrhoids are urgently needed. This review article mainly focuses on the newer molecules to overcome hemorrhoids and also emphasizes various studies carried out in the past.

Development and Validation of Robust, Highly Sensitive and Stability-Indicating RP-HPLC Method for Estimation of Deferasirox and its Degradation Products.

A rapid, simple and highly sensitive stability-indicating reverse-phase high-performance liquid chromatographic technique, coupled with a photodiode array detector, was developed and validated for the estimation of Deferasirox (DFS). The chromatographic separation was achieved using a C-18 (250 × 4.6 mm, 5 µm) stationary phase and a mobile phase composed of 0.1% orthophosphoric acid and acetonitrile at a flow rate of 1 mL/min. The detection was carried out at a wavelength of 245 nm with a constant injection volume of 10 µL throughout the analysis. With an R2 value of 0.9996, the calibration curve was determined to be linear over an appropriate concentration range of 50-500 ng/mL. According to the International Conference on Harmonization (ICH) Q1 (R2) guideline, DFS was evaluated under stress conditions that included hydrolytic (acid, alkali and neutral), oxidative and thermal degradation. The findings demonstrated that significant degradation was observed in acidic degradation conditions, whereas drug substance was found to be stable when exposed to neutral, basic, oxidative and thermal degradation. The developed method was validated as per ICH guidelines. The developed method was employed successfully to estimate the amount of DFS in bulk and pharmaceutical formulation.

Therapeutic and Health Promoting Potential of Bakuchiol from Psoralea corylifolia: A Comprehensive Review.

Bakuchiol, is a principal bioactive component present in seeds of Psoralea corylifolia. It is one of the important monoterpene phenols and has been reported to possess extensive pharmacological properties like antioxidant, anti-inflammatory, anticancer, and hepatoprotective. Bakuchiol also plays a significant role in mental disorders. With an aim to explore the pharmacological potential of plant Psoralea corylifolia and its bioactive constituent, Bakuchiol; which may act as a lead to develop new molecular entities as drugs. A substantial literature survey was performed by scientific search engines like PubMed, Scopus,Web of Science, Science Direct, etc., and were reviewed with particular emphasis on their scientific impact and novelty. The study concludes that both Psoralea and bakuchiol possess innumerable pharmacological potentials to treat multiple disorders. Altogether, the promising pharmacological activities of bakuchiol may open new probes for therapeutic invention in the management of numerous ailments. Thus, the present review gives the erudition of bakuchiol as d foundation for further studies on the molecular mechanisms of BXXXD in the treatment of T2DM.

Rationally designed donepezil-based hydroxamates modulate Sig-1R and HDAC isoforms to exert anti-glioblastoma effects.

The pursuit of activating the HDAC inhibitory template towards additional mechanisms spurred us to design dual modulators (Sig-1R agonist - HDAC inhibitor) via utilization of the core structural unit of donepezil (an FDA-approved anti-Alzheimer's agent) as a surface recognition part. Literature precedents coupled with our experience rendered us with several insights that led to the inclusion of chemically diverse linkers and hydroxamic acid (zinc-binding motif) as the other components of HDAC inhibitory pharmacophore. With this envisionment and clarity, donepezil-based HDAC inhibitory adducts were furnished and exhaustively explored for their anti-GBM efficacy. Resultantly, a magnificently potent HDAC inhibitor 10 [IC50 (HDAC6) = 2.7 nM, IC50 (HDAC2) = 0.71 µM] was pinpointed that was endowed with the ability to: i) exert cell growth inhibitory effects against Human U87MG GBM cells ii) cause death in TMZ-resistant GBM cells iii) induce subG1 arrest in GBM cells iv) prolong the survival of TMZ-resistant U87MG inoculated orthotopic mice (in-vivo studies) v) induce GBM cell apoptosis via binding to Sig-1R. Collectively, the results led to the identification of compound 10 as a tractable anti-GBM agent that deserves detailed investigation for the accomplishment of its candidature as a GBM therapeutic.

Bakuchiol: A Potential Anticancer Compound from Psoralea corylifolia Linn.

BACKGROUND: Bakuchiol is a monoterpene phenol isolated from the seeds of Psoralea corylifolia Linn. It is used traditionally in Indian and Chinese medicine and has been reported to possess extensive pharmacological potential against a variety of ailments. A recent study enumerates the anticancer potential of bakuchiol. OBJECTIVE: The objective of the present review study is to explore the anticancer potential of bakuchiol which provides insight into the design and develop novel molecular entities against various disorders. METHODS: Current prose and patents emphasizing the anticancer potential of bakuchiol have been identified and reviewed with particular emphasis on their scientific impact and novelty. An extensive literature survey was performed and compiled via the search engine, PubMed, Science Direct, and from many reputed foundations. RESULTS: The study's findings suggested and verified the anticancer potential that Psoralea and bakuchiol against a variety of cancer. Both Psoralea and bakuchiol also portrayed synergistic or potentiating effects when given in combination with other anticancer drugs or natural compounds. CONCLUSION: Altogether, the promising anticancer potential of bakuchiol may open new probes for therapeutic invention in various types of tumors. Thus, the present review gives the erudition of bakuchiol and Psoralea as anticancer which paves the way for further work in exploring their potential.

A Review of Clinical Studies Assessing the Therapeutic Efficacy of Escitalopram: A Step Towards Development.

BACKGROUND: Major depression is a debilitating, sometimes fatal disorder, deteriorating the quality of life and well-being. Escitalopram showed highly selective and dose-dependent inhibitory activity on human serotonin transport. Selective serotonin reuptake inhibitors (SSRIs) are the first-line drugs to manage major depressive disorder (MDD). OBJECTIVE: The objective of this study is to explore the therapeutic potential of escitalopram, a clinically approved drug to manage MDD and panic disorders. METHODS: It emphasizes comparative and clinical trial studies with several pharmacological targets reviewed from the data available on PubMed, Science Direct, Clinicaltrails.gov, and from many reputed foundations. RESULTS: To highlight the clinical efficacy, safety, recent development, and stable formulation of escitalopram with an increased bioavailability profile. Evidence-based on the available clinical and pharmacoeconomic data, escitalopram represents an effective first-line treatment option for MDD patients. CONCLUSION: The present review highlights the placebo-controlled clinical studies and the recent development that can be helpful for further research perspectives.

Hesperidin: A Potential Therapeutic Agent against COVID-19.

COVID-19, aka Coronavirus Disease 2019, triggered by new severe acute respiratory syndrome coronavirus-2 or SARS-CoV-2, is now a public health emergency due to its rapid spread, high transmission efficiency, and severe viral pandemic that is significantly increasing the number of patients and associated deaths. Currently, no specific treatment is available for this highly contagious virus. The unavailability of effective and specific treatments and the severity of this epidemic situation potentiate medicinal chemists' in supporting new prophylactic or therapeutic interventions against COVID-19. This study discusses the therapeutic potential of hesperidin, a traditionally used herbal medicine with an exceptional safety profile. Recent studies on hesperidin advocate its promising potential in the prevention and management of COVID-19. This paper also discusses the recent clinical studies based on the previously documented antiviral activity of hesperidin. Herein, we propose the detailed preclinical and clinical manifestations of hesperidin based on its multifaceted bioactivities to develop a novel anti-COVID-19 lead.

Pulegone: An Emerging Oxygenated Cyclic Monoterpene Ketone Scaffold Delineating Synthesis, Chemical Reactivity, and Biological potential.

Pulegone ((R)-5-Methyl-2-(1-methylethylidine) cyclohexanone) is a pharmacologically active, natural monoterpene ketone obtained from leaves and flowering tops of the mint family (Lamiaceae). The aim is to comprise the physicochemical and biological aspects of pulegone. All significant databases were collected via electronic search using Pubmed, Scopus, Web of Science, and Science Direct and were compiled. This review presents the occurrence, chemistry, and modifications of pulegone structure and its effect on the biological system. Pulegone represents various pharmacological properties, i.e., antioxidant, antimicrobial, anti-feeding, antifungal, antiviral, and pesticide activities, and has a significant role as an abortifacient and emmenagogue. Thus, this present review concludes the knowledgeable erudition on pulegone that paves the way for further work.

Synergistic Effect of Piperine and its Derivatives: A Comprehensive Review.

Piperine is a fascinating substance since it can be used as a biomarker in combination with other bioactive compounds or their analogues, as well as therapeutic molecules used for the healing of a variety of diseases. It displays a plentiful therapeutic potential and various health benefits when administered alone or in combination with several other drugs and/or phytochemicals. It has also been used to enhance the pharmacokinetic profile of many nutraceutical compounds like curcumin, resveratrol, quercetin, beta-carotene, barbiturates, propranolol, metformin, theophylline etc. The present review discloses the synergistic effect of piperine and its derivatives, clinical studies, and patent studies of piperine.

Formulation, Development, and in-vitro Evaluation of Escitalopram Fast Dissolving Tablets.

BACKGROUND: Escitalopram, a selective serotonin reuptake inhibitor (SSRI), acts by increasing the serotonin level in the brain and is used widely for the management of depression and anxiety disorders. However, the poor dissolution rate of escitalopram due to less water solubility is a consequential problem confronting the pharmaceutical industry in developing pharmaceutical dosage forms for oral delivery systems. OBJECTIVE: The present work aims to deliver a novel formulation for improving the dissolution profile and, thus, the bioavailability of escitalopram. METHODS: Fast Dissolving Tablets (FDT) are expected to enable quick drug release, which will improve the drug's dissolving profile, allowing for the initial increase in plasma concentration mandatory in an acute depression attack. The use of co-processed excipients in tablets has been shown to increase the compressibility and disintegration properties of the tablets, resulting in improved in-vitro drug release and bioavailability. As co-processed excipients, a mixture of banana powder (a natural super disintegrant with nutritional value) and microcrystalline cellulose (a highly compressible substance with good wicking and absorption capacity) was used. RESULTS: The tablets were made using a response surface, randomised central composite design, and a direct compression technique. The manufactured tablets were found to be released more than 95% of the drug within 10 minutes and showed an improved drug release profile than the available marketed formulation. CONCLUSION: After confirming in-vivo potential, the fast release formulation exhibited impressive in-vitro findings and may prove to be a boon in treating acute depression attacks.