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Molecular Docking Aided Study of Transient Metal Inclusion and Tertiary Complexation of Fenofibrate: Effect on Solubility
Available online: 16 May 2025More LessBackgroundFenofibrate, a widely used lipid-lowering agent, exhibits limited bioavailability due to its BCS Class II status and poor aqueous solubility. Enhancing its solubility is crucial to improving therapeutic efficacy.
MethodsThis study explored solubility enhancement via molecular docking-guided screening of transition metal complexes and inclusion complexes with beta-cyclodextrin (β-CD). Transition complexes of fenofibrate with copper acetate were synthesized at a 1:1 molar ratio in a methanol-water mixture (2:1). Additionally, inclusion complexes of these metal complexes with β-CD were prepared in a 1:1 molar ratio and dried. Physicochemical characterization was performed using FTIR, XRD, and SEM analyses. Molecular docking identified potential interactions and conformational stability of the complexes.
ResultsThe aqueous solubility of fenofibrate increased significantly, 17-fold in the transition metal complex and 25-fold in the β-CD inclusion complex compared to the pure drug. The complexes demonstrated structural changes, including amorphization, which likely contributed to enhanced solubility. Molecular docking revealed strong interactions between fenofibrate, copper acetate, and β-CD, supporting the formation of stable complexes.
ConclusionThe results indicate that fenofibrate’s solubility can be markedly enhanced through complexation with transition metals and β-CD. These approaches, particularly the β-CD inclusion complexes, hold the potential for improving fenofibrate's bioavailability and therapeutic outcomes, offering a promising strategy for addressing solubility challenges in poorly water-soluble drugs.
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Silk Sericin: A Promising Sustainable Natural Biopolymer for Pharmaceutical and Biomedical Applications
Available online: 21 April 2025More LessSilk Sericin, a natural biopolymer, has gained increasing attention for its diverse applications in pharmaceuticals and biomedicine. This is an organic biomaterial derived from the Silkworm cocoon (silkworm Bombyx mori), by the degumming process, which exhibits remarkable biocompatibility, biodegradability, making it a promising candidate for various therapeutic and regenerative approaches. Sericinhas an excellent property that makes it a potential candidate for wound healing, skin care, and drug delivery applications. This hydrophilic protein is recognized as an anti-inflammatory, antioxidant, and anti-cancer agent. The high molecular weight and granular protein composition of sericin give it a sticky consistency and gelatin-like quality. The presence of many hydroxyl groups absorbs significant water from the skin, providing a natural moisturizing effect. Silk sericin presents a sustainable alternative to synthetic polymers, boasting exceptional characteristics, including minimal immune response, excellent moisture retention, and versatility in forming various structures such as films, fibers, and hydrogels. The sustained release of sericin from wound dressings can also be efficacious in providing a prolonged healing effect during the treatment of pressure ulcers. This can contribute to a more favourable environment for faster and effective wound healing. This review aims to provide a comprehensive overview of silksericin, highlighting its unique characteristics, extraction methods, and recent advancements in its utilization for pharmaceutical and biomedical purposes, along with emphasizing the significant potential of this protein as a versatile biopolymer for advanced healthcare solutions.
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Polyurethane Foam-based Wound Dressings and their Potential Applications and Challenges in Wound Healing
Authors: Sindhu Abraham and Sri CharanAvailable online: 16 April 2025More LessWound healing is an intricate biological process that is supported by well-coordinated cellular activities along with the influence of various factors, such as infection at the site of the wound, comorbidities, and lifestyle habits. Non-healing wounds pose a significant global health concern, with a substantial impact on healthcare resources and patient well-being. Wound dressings play a crucial role in creating an optimal microenvironment for healing, and the selection of an appropriate dressing is imperative to ensure faster healing and improved patient outcomes. Polyurethane (PU) foam based wound dressings have gained considerable attention owing to their versatile properties and potential applications in wound care. PU foam dressings are known for their high absorbency in managing moderate to heavy exudate, ability to maintain a moist wound environment, comfort, flexibility, and non-adherent properties. PU is the preferred substrate material for dressings because of its customizable mechanical properties, excellent biocompatibility, and low toxicity. Several studies have explored the use of polyurethane foam-based wound dressings and have highlighted their potential benefits and limitations. Despite the promising results of previous studies, there is still a lack of comprehensive understanding of the applications and challenges of PU foam-based wound dressings in wound healing. This review aims to address the knowledge gap by providing an update on the current state of research on polyurethane foam based wound dressings and their potential applications and challenges in wound healing.
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Unlocking the Potential of Ethosomes in Dermatological Treatments
Authors: Shreyasi Katari, Priyanti Halder, Pratibha Bhowmick and Mithun BhowmickAvailable online: 14 April 2025More LessIn recent times, Ethosome has become a new promising pharmaceutical nano-carrier for the development of innovative dermal and transdermal therapies that help in the treatment of various skin diseases like skin allergies, urticaria, melisma, eczema, melanoma, and other skin disease. Ethosome is a non-invasive, modified phospholipid-based elastic, soft vesicular nano-carrier with high ethanol content. Ethanol in this formulation facilitates rapid penetration of the drug into the skin accelerating cell membrane lipid fluidity. After permeation into the skin, those get fused with the cell membrane lipids and release the loaded drug. BCS III & IV drugs, having low permeability, can be developed with ethosomal systems. Histamine is one of the responsible biogenic factors for itching, skin wheals, allergies, other skin disorders, etc., so incorporation of low permeable antihistaminic drugs in ethosome is an emerging prospect in the field of dermatology and cosmetology. Ethosomes reflect positive insights to overcome side effects associated with conventional oral therapy, quick onset of action, and targeted drug delivery to inflamed skin. The concept of ethosome is considered advantageous over liposome to be more penetrable to the skin. Besides the need for further pharmacokinetic and pharmacodynamics studies on ethosome, it seems to significantly hold a great contemplation for the delivery of medicaments in the skin through different pathways.
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Novel Approach and Recent Advancement In-Situ Gel as Smart Carriers for Controlled Drug Delivery via Ophthalmic Route
Authors: Smita Singh, Sumita Singh, Vishal Khandelwal, Atul Pratap Singh, Kapil Sachan and Pranjal Kumar SinghAvailable online: 24 March 2025More LessResearch in ocular delivery of medication has both challenging and promising opportunities for the pharmaceutical sector. Present ocular delivery methods of drugs, including ointments, solutions, and suspensions, have a number of limitations, such as rapid elimination from the precorneal area, high variation in efficacy, and the risk of blurred vision. These disadvantages underscore the need for the introduction of more effective drug delivery systems. Research on ocular drug delivery has increased significantly in the past years, resulting in the use of numerous standard formulation forms, such as ointments and eye drops. One big drawback of the two formulations is the fast expulsion of the deposited dose through the action of blinking eyelids as well as the excretion of tear fluid. To counter this, in situ, gelling systems have been created that minimize drainage and prolong the period of contact with the ocular tissues and cornea. The formulations in these systems go through a sol-to-gel change due to conditions in the environment, for example, temperature, ionic strength, and pH. The transitions are usually triggered by the common polymers sodium alginate and high-performance methylcellulose. These preparations can be tested for any one of a number of properties, such as but not limited to clarity, ocular irritancy, texture, isotonicity, sterility, gel strength, gelling capacity, gelling time, ex-vivo release, in vitro drug release, stability, in vivo retention, and absorption.
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Unlocking the Role of pH-sensitive Nanoparticles in the Targeted Management of Different Types of Ulcers
Authors: Tahreen Taj, Venishaa Sethumadhavan, Prashant Kumar, Tinku Kumar, Sumel Ashique and Mayank SharmaAvailable online: 19 March 2025More LessThe pH-sensitive drug delivery systems (PSDDS) are attracting significant attention as these systems transport the drug at a specific time as per the pathophysiological need of the disease, leading to improved patient therapeutic effectiveness and compliance. The pH-sensitive nanoparticles are a favorable alternative to treat ulcers, especially gastrointestinal ulcers comprising peptic ulcers and mouth ulcers. These nanoparticles can be intended to release medication in a meticulous way at specific pH levels of the ulcer site, which can improve therapeutic effectiveness and decrease side effects. It is significant to note that the use of pH-sensitive nanoparticles for ulcer management is an evolving field of research, and the specific applications and formulations may vary based on the type and location of the ulcer. Additionally, regulatory approvals and clinical trials may be necessary before such treatments become widely available to patients.
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Advances in Green Synthesis of Zinc Oxide Nanoparticles: A Promising Nanotechnology Approach for Diabetes Mellitus Management
Authors: Rashi Banchhor, Alka Patel, Mukesh Kumar Sharma, Ajazuddin3, Parag Jain, Sanjay Kumar Gupta and Kushagra NagoriAvailable online: 19 March 2025More LessDiabetes mellitus (DM) is a major global health concern, with a growing patient population and associated complications. Traditional treatments often fall short due to the complex nature of the disease. Recent advances in nanotechnology, particularly the use of zinc oxide nanoparticles (ZnO NPs), offer promising solutions. This review aims to highlight the eco-friendly, economical, and biocompatible characteristics of ZnO NPs, with a focus on green synthesis techniques for their production.
It also explores the green synthesis of ZnO NPs using natural resources, such as microorganisms and plant extracts, which act as stabilizing and reducing agents. It examines the potential of these nanoparticles in improving medicinal properties, particularly through their antibacterial, antidiabetic, and antioxidant activities. The possibility of combining ZnO NPs with other nanomaterials is also investigated, with an emphasis on applications in biosensing, therapeutics, and diagnostics.
ZnO NPs synthesized through green methods demonstrate significant potential in enhancing insulin sensitivity, glucose management, and preventing diabetes-related complications. Their improved medicinal properties, including antibacterial, antidiabetic, and antioxidant activities, are highlighted. This review also identifies opportunities for the development of combination products and discusses the transition from laboratory-scale research to industrial-scale production.
Extensive safety and clinical studies are required to confirm the safety and efficacy of ZnO NPs, paving the way for regulatory approval and wider adoption in medical applications. This review underscores the importance of medicinal plants and biogenic approaches for the synthesis of zinc oxide nanoparticles and calls for further research to explore the full potential of ZnO NPs in diabetes management and beyond.
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Renoprotective Effects of Eugenol-Loaded Chitosan Nanoparticles on Septic Rats
Available online: 04 February 2025More LessBackgroundSepsis is a severe medical disorder that poses a significant risk to life, leading to elevated rates of sickness and mortality globally, reaching 11 million annually. It is distinguished by an imbalanced immune response to infection, which subsequently causes failure in several organs. Eugenol is obtained from clove oil and possesses various beneficial properties, such as antifungal, anti-inflammatory, antiviral, antioxidant, anticancer, and antibacterial effects.
AimThe present study aimed to assess the effectiveness of eugenol-loaded chitosan nanoparticles (EC-NPs) in protecting against kidney damage caused by sepsis using the cecal ligation and puncture (CLP) model.
MethodsThirty rats were divided into five groups: sham, sepsis, and septic rats treated with chitosan, eugenol, or EC-NPs.
ResultsAdministration of EC-NPs dramatically enhanced renal function, as evidenced by the reduced urea, creatinine, and uric acid concentrations. Moreover, EC-NPs caused an elevation in glutathione reductase (GSH), glutathione-S-transferase (GST), superoxide dismutase (SOD), glutathione peroxidase (GPx), and catalase (CAT) in addition to decreasing the production of malondialdehyde (MDA) and nitric oxide (NO). EC-NPs administration reduced the DNA damage in septic rats and partially restored the aberrant structure of renal tissues in septic rats. Furthermore, the immunohistochemical examination showed a marked decrease in tumor necrosis factor-alpha (TNF-α) and interleukin-1 beta (IL-1β) expression.
ConclusionIn conclusion, EC-NPs attenuated renal injury in septic rats through their anti-oxidant and anti-inflammatory activities and protection of DNA.
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Pleiotropic Leukemia Inhibitory Factor Encapsulated in DODAB:MO Liposomes for Multiple Biomedical Applications
Available online: 14 January 2025More LessIntroductionThe development of novel drug carriers is invaluable to maximize therapeutic efficiency and improve specificity. Dioctadecyl-dimethylammonium bromide (DODAB): monoolein (MO) (1:2) liposomes exhibit non-lamellar phases in their core that improve the encapsulation ability of both hydrophobic and hydrophilic molecules. This study explores the use of this nanosystem for the therapeutic delivery of cytokines, specifically of leukemia inhibitory factor (LIF). Nanocarriers can overcome the drawbacks of direct cytokine administration, like poor bioavailability.
MethodsDODAB:MO (1:2) liposomes were produced by lipid film hydration, followed by extrusion, and used for encapsulating 0.125 and 0.25 µM LIF. The produced nanoparticles were characterized in terms of size and zeta potential, FTIR and STEM. LIF was quantified with an optimized Bradford method to determine encapsulation efficiencies, drug loading, and release profile. Cytotoxicity was assessed by hemolysis, and mouse myoblasts were used to validate bioactivity in vitro.
ResultsNeither the extrusion nor the protein incorporation steps promoted significant alterations in cytokine structure. LIF-containing liposomes DODAB (1:2) nanosystem were small (~200-300nm), positively charged (~50-60mV), non-toxic, and stable at physiological pH. Biophysical characterization identified liposomal formulation of 200 µM DODAB:MO (1:2) at 0.25 µM as the most efficient system. The bioactivity analysis showed an increase of ~20% in cell proliferation after 48h of incubation when compared to free mLIF. Also, the LIF-containing DODAB:MO (1:2) liposomal formulation, when exposed to serum, revealed a capacity to protect its cargo for up to 6 h.
ConclusionThe DODAB:MO (1:2) nanosystem was found to be efficient for cytokine delivery, stabilizing mLIF, and promoting its bioactivity with multiple applications.
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Inulin: A Versatile Biopolymer for Pharmaceutical Application
Available online: 13 December 2024More LessFor many years, inulin has been a versatile oligosaccharide that is mainly utilized in food. When compared to other biodegradable polysaccharides, inulin's unique and flexible structure, protective/stabilizing properties, along with organ-targeting abilities make it an ideal drug delivery vehicle. Inulin has drawn a lot of attention as a promising multifunctional natural biopolymer with a wide range of uses in drug delivery, prebiotics, and therapies. The three hydroxyl groups on each fructose unit present in inulin enable chemical modifications like (Esterification, Conjugation, crosslinking, Oxidation, or Reduction), allowing it to be tailored for drug delivery applications. Thus, therapeutics and biomolecules can be released in a sustained and controlled manner, increasing their bioavailability and cellular absorption at the targeted site. It clarifies the complex interactions between the host and inulin, microbiota, and medicinal drugs, exposing a multidimensional biopolymer with transformative potential. They are excellent carriers in healthcare and biomedicine due to their flexible structure, biocompatibility, remarkable target ability, innate ability to govern release behaviour, customizable degradation kinetics, and protective capacity. Drug targeting is the process of delivering a medication to the desired site of action. One of the advantages of drug targeting is that the medicinal molecule is released at a consistent and regulated rate, preventing overdose. The potential of inulin as an encapsulating material was examined in terms of its enzymatic degradability and drug-release characteristics. Inulin has a wide range of therapeutic applications. These include use as a dietary fibre with extra health benefits, as a diagnostic and analytical tool, and as a carrier in a drug delivery system. Inulin has been the subject of extensive research as a drug delivery carrier for colon-specific drug administration. Inulin has a wide range of applications in the pharmaceutical industry overall, and research on it is still ongoing, especially concerning chemically modified inulin. Therefore, it's conceivable that this flexible oligosaccharide will find even more uses.
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Nanotheranostic Approach for Targeting Tauopathies in Alzheimer's Disease: Mechanistic Insight and Recent Advances
Authors: Kantrol Kumar Sahu, Ruchi Chaudhary, Mohd. Asad Farooqi and Monika KauravAvailable online: 26 November 2024More LessThe most prevalent type of dementia, Alzheimer's disease (AD), is typified by the presence of intracellular tau protein neurofibrillary tangles and extracellular amyloid plaques. There are currently about 50 million people who have dementia, and by 2030, that number is predicted to rise to 75 million, placing a significant financial strain on the nation's healthcare system. Novel disease-modifying treatments are desperately needed to combat this illness, given the consequences on patients' quality of life and the mounting financial strain. There are currently no disease-modifying medications available; instead, the majority of available therapies are symptomatic ones such as cholinesterase inhibitors and N-methyl-D-aspartate receptor blockers. The primary focus of therapeutic research against AD has shifted to tau-targeting strategies following multiple unsuccessful attempts to create medications against amyloidopathy. This article first provides an introduction to tauopathy in AD before summarizing current research on the creation of tau-oriented multi-target directed ligands and small compounds as therapies that target tau alteration, aggregation, and degradation. The overall goal of this work is to present a thorough and critical review of small compounds that are being investigated as potential treatment candidates for AD tauopathy.
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Advanced Technologies in Rectal Drug Delivery Systems: A Comprehensive Review of Recent Innovations and Future Prospects
Available online: 31 October 2024More LessRectal Drug Delivery System (RDDS) emerges as an alternative administration route due to the rectum's small surface area and limited enzyme activity, which contribute to efficient drug absorption. RDDS offers various advantages, such as reduced first-pass metabolism, rapid absorption of low molecular weight drugs, and the ability to accommodate large retention volumes and facilitate absorption via the lymphatic system. Moreover, RDDS is preferable for drugs with low stability, solubility, and permeability via oral administration, as well as effectively addressing concerns related to gastric irritation or degradation. This review delves into the factors influencing drug absorption in RDDS, including drug properties, formulation types, and physiological and pathology-associated considerations. It further explores conventional RDDS, including enemas, suppositories, tablets, gels, sprays, ointments, and creams, as well as novel approaches involving nanoparticles, liposomes, microspheres, and solid lipid nanoparticles (SLNs) in rectal dosage forms. Furthermore, the challenges and prospects of RDDS in treating rectal diseases are discussed. This review provides valuable insights into the potential of RDDS, highlighting the importance of continuous research and development in enhancing patient outcomes and advancing healthcare practices.
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3D and 4D Technology for Pharmaceutical Drug Delivery: A Detailed Insight
Authors: Shashank Soni, Vivek Yadav, Dhananjay Kumar and Sandeep Kumar TiwariAvailable online: 17 October 2024More Less3D Printing, sometimes referred to as additive manufacturing, has made the concept of personalized medicine a reality. The primary objective of 3D and 4D printing is to produce intricate, customized pharmaceuticals at a reasonable cost. With improvements in materials, resolution, and speed, 3D printing technology is quickly developing. It includes faster construction, cost efficiency through reduced waste, design flexibility for complex structures, and sustainability through optimized material usage. An extensive literature survey was done on 3D and 4D printing of pharmaceuticals using PubMed, Elsevier, ScienceDirect, and Springer. The results were then filtered based on the titles, abstracts, and accessibility of the complete texts. The search engine Google Scholar was accessed for literature data mining. From the data mining, it was found that from the year 2009 to 2024 the number of research publications surged more than 200 times on the current topic. Even though 3-D and 4-D printing technologies have advanced significantly in a short amount of time, the most often used ones are still stereolithography, nozzle-based deposition, inkjet, and selective laser sintering. Their use has been modified for the production of nanoparticles, polypills, tablets, and implants, etc. Pharma's aspirations for tailored medications are being revolutionized by 3D printing, but cost, flexibility, and bioequivalence still need to be investigated. The present review offers a thorough analysis of various 3D and 4D printing methods and emphasizes the major advantages and disadvantages and major key challenges of 3D and 4D printing related to pharmaceuticals. Compared to 3D Printing, 4D printing offers better quality, efficacy, and functionality.
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