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- Volume 15, Issue 1, 2023
Current Drug Research Reviews - Volume 15, Issue 1, 2023
Volume 15, Issue 1, 2023
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Role of Nanotechnology in Taste Masking: Recent Updates
Authors: Vivekanand Vishvakarma, Malkiet Kaur, Manju Nagpal and Sandeep AroraOne of the important parameters in the case of dosage form is taste. Most of the drugs available in oral dosage form have an unpleasant taste which leads to patient incompliance and affects the success ratio of products in the market. Geriatric and paediatric patients suffer more with the bitter taste of medicines. According to the studies reported, it is found that 50% of the population have the problem swallowing tablets, especially the pediatric and geriatric population. Masking the taste of bitter drugs has become necessary in the pharmaceutical field and increasing interest of researchers to develop various methods for masking the bitter taste of drugs. Five major tastes, felt by our tongue are salt, sour, sweet, bitter, and umami. When the drug dissolves with saliva, drug molecules interact with taste receptors present on the tongue and give taste sensations. Although, many solid oral dosage forms like pills, and tablets have an additional advantage of masking and encapsulation of bitter taste drugs; however, they might not be effective for children because they may or may not swallow pills or tablets. There are various other methods that mask the bitter taste of drugs such as the addition of sweeteners and flavouring agents, granulation, coating, inclusion complexes, extrusion method, ion-exchange resins, etc, discussed in the first section of the article. The second part of this article consists of various nanotechnology-based drug delivery systems that were fabricated by researchers to mask the bitter taste of drugs. A brief of recent literature on various nanocarriers that were fabricated or developed for taste masking has been discussed in this part. A better understanding of these methods will help researchers and pharmaceutical industries to develop novel drug delivery systems with improved taste masking properties.
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Nanocarriers Based Ocular Therapeutics: Updates, Challenges and Future Prospectives
Authors: Udesh Kaushal, Malkiet Kaur, Manju Nagpal, Madhusmita Bhuyan and Kailasam P. GounderBackground: Ocular disorders mainly affect patient’s eyesight and quality of life. Formulation scientists encounter a hurdle in drug distribution to ocular tissues. Anatomical barriers (static and dynamic) and physiological barriers, such as nasolacrimal drainage system, blinking action of eye, and metabolic barriers and efflux pumps, are the principal obstacles to medication delivery to the posterior and anterior parts. Over the last twenty years, ophthalmic research has evolved rapidly for the development of innovative, safe, and patient friendly formulations and drug delivery devices or techniques that may get over these obstacles and sustain drug levels in tissues. Methods: Literature from the past ten years has been collected using various search engines, such as ScienceDirect, J-Gate, Google Scholar, Pubmed, Sci-Hub, etc., and research data have been compiled according to various novel carrier systems. Results: Nanocarriers have been shown to be helpful in overcoming the drawbacks of traditional ocular dosing forms. Modification of standard topical solutions by both permeability and viscosity imparters has resulted in breakthroughs in anterior segment medication delivery. Various nanocarriers, including liposomes, implants, dendrimers, nanosuspensions, nanoparticles, solid lipid nanocarriers, niosomes and proniosomes have been studied for enhanced penetration and the successful targeted drug administration to various ocular locations. Conclusion: Recently developed nanocarriers for ocular delivery have proved to be cost-effective, efficacious, safe, and sustained-release carriers, which can be incorporated in suitable dosage forms. In this review, the authors have discussed various challenges in ocular drug administration. Various research reports on advancements in ocular drug delivery based on modified drug delivery carriers have been analyzed and included. Additionally, marketed formulations and patent literature on ocular drug delivery have been added as a part to support the review content.
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Are Herbal-peptides Effective as Adjunctive Therapy in Coronavirus Disease COVID-19?
More LessBackground: Plant antiviral peptides (AVP) are macromolecules that can inhibit the pathogenesis of viruses by affecting their pathogenic mechanism, but most of these peptides can bind to cell membranes, inhibit viral receptors, and prevent viruses. Recently, due to the coronavirus pandemic, the availability of appropriate drugs with low side effects is needed. In this article, the importance of plant peptides in viral inhibition, especially viral inhibition of the coronavirus family, will be discussed. Methods: By searching the databases of PubMed, Scopus, Web of Science, the latest articles on plant peptides effective on the COVID-19 virus were collected and reviewed. Results: Some proteins can act against the COVID-19 virus by blocking sensitive receptors in COVID-19, such as angiotensin-converting enzyme 2 (ACE2). The 23bp sequence of the ACE2 alpha receptor chain can be considered as a target for therapeutic peptides. Protease and RNAP inhibitors and other important receptors that are active against COVID-19 should also be considered. Conclusion: Herbal medicines with AVP, especially those with a long history of antiviral effects, might be a good choice in complement therapy against the COVID-19 virus.
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Carbapenem Antibiotics: Recent Update on Synthesis and Pharmacological Activities
Authors: Abhishek Tiwari, Varsha Tiwari, Biswa M. Sahoo, Bimal Krishna Banik, Manish Kumar and Navneet VermaRight from the breakthrough of carbapenems since 1976, many schemes on synthesis, structure-activity relationship (SAR), and biological activities have been carried out, and several carbapenems have been developed, including parentally active carbapenems like imipenem, doripenem, biapenem, meropenem, ertapenem, panipenem, razupenem, tomopenem, and cilastatin, whereas orally active carbapenems like GV-118819, GV-104326, CS-834, L-084, DZ-2640, CL 191, 121, L-646, 591, S-4661, ER-35768, MK-826. Prodrugs of carbapenem with increased bioavailability include temopenem, tebipenem, sanfetrinem, LK-157, and CP 5484. Merck, Glaxo Welcome Research Group, Johnson & Johnson, Sankyo Group and Dai-ichi Group, and Wyeth-Ayerst Group were among the businesses that produced carbapenems. In this review Witting reaction, Mitsunobu reaction, Dieckmann reaction, palladium-catalyzed hydrogenolysis, E. coli-based cloned synthesis, as well as biosynthetic enzymes such as carbapenem synthetase (carA), carboxymethylproline synthase (carB), carbapenem synthase (carC) are included. Carbapenems are biologically mainly active in the infections like urinary tract infections, bloodstream infections, tuberculosis, intra-abdominal infections, and pathogens like anaerobes, gram-positive and gram-negative bacteria.
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Toxicological Analysis of Drugs in Human Mummified Bodies and Proposed Guidelines
More LessFrom palaeopathology to forensic taphonomy, mummified human bodies constitute biological archives of paramount importance. Toxicology analysis of endobiotics and xenobiotics has already shown value to archaeological mummies research with detecting heavy metals, sedative-hypnotic drugs, and stimulants. Thanks to the large window of drug detection in hair and nails, the information from such studies has increased the scientific community’s knowledge regarding past populations’ lifestyles. Still, few bibliographic references exist regarding toxicology reports in mummified bodies from forensic settings. Here, the authors aim to draw attention to the valuable contribution of toxicology analysis, taking into account previously conducted studies and their findings. Given that sample collection on mummified bodies from forensic scenarios may not always happen in laboratories or autopsy rooms, the authors also suggest guidelines for in situ sampling of forensic mummies. It is expected that the present technical note will encourage experts to perform toxicology analysis in mummified bodies and publish their case reports more often.
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Phytochemical and in-vitro Biological Investigation of Indian Traditional Medicinal Plants for their Cytotoxicity and Hepatoprotective Potential
Objective: This study aimed to select 16 medicinal plants based on their folklore remedy for treating various diseases like inflammation, cancer, etc., and scientifically validate their potency. Methods: Five among them, namely Centella asiatica (CA), Myristica fragrans (MF), Trichosanthes palmata (TP), Woodfordia fruticosa (WF), and Curculigo orchioides (CO), were scientifically confirmed through the extraction and in-vitro cytotoxic and hepatoprotective evaluation. Based on the cytotoxic and hepatoprotective results, the various fractions of CO were chosen for an in-depth phytochemical study to isolate and characterize active compounds by GC-MS. Results: The results showed promising cytotoxic activity (i.e., IC50=<100 μg/ml) against HeLa cell lines and significant hepatoprotective activity in a dose-dependent manner on CCl4 intoxicated isolated hepatocyte cells. Conclusion: The present study confirmed the scientific evidence regarding the effectiveness of selected medicinal plants in HeLa and hepatocyte cells. Furthermore, a detailed study on their mechanism of action and clinical application is suggested.
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An In-silico Approach: Design, Homology Modeling, Molecular Docking, MM/GBSA Simulations, and ADMET Screening of Novel 1,3,4-oxadiazoles as PLK1inhibitors
Background: Breast cancer is the most commonly diagnosed and major cause of cancer-related deaths in women worldwide. Disruption of the normal regulation of cell cycle progression and proliferation are the major events leading to cancer. Human Polo-like Kinase 1 (PLK1) plays an important role in the regulation of cellular division. High PLK1 expression is observed in various types of cancer including breast cancer. 1,3,4-oxadiazoles are the fivemembered heterocycles, that serve as versatile lead molecules for designing novel anticancer agents and they mainly act by inhibiting various enzymes and kinases. Objective: A novel series of 1,3,4-oxadiazole derivatives (A1-A26) were designed and subjected to an in-silico analysis against PLK1 enzyme (PDB ID:1q4k), targeting breast cancer. Methods: The chemical structure of each compound (A1-26) was drawn using ChemDraw software. The 3D structure model of protein target (PDB ID:1q4k) was built using the SWISSMODEL server. Molecular docking simulation was performed to determine the designed compound’s probable binding mode and affinity towards the protein target (PDB ID:1q4k). The designed compounds were subjected to ADME screening, as well as Prime MM/GBSA simulations using Schrodinger suite 2020-4. Furthermore, the safety profile of compounds was examined through the OSIRIS property explorer program and the results were compared with the standard drugs, 5-fluorouracil and cyclophosphamide. Results: Based on the binding affinity scores, the compounds were found selective to target protein 1q4k through hydrogen bonding and hydrophobic interactions. The compounds A11, A12, and A13 were found to have higher G scores and binding free energy values. The ADME screening results were also found to be within the acceptable range. Moreover, the in-silico toxicity prediction assessments suggest that all designed compounds have a low risk of toxicity, and have higher efficiency for the target receptor. Conclusion: The study showed that the substitution of electron-donating groups at the various position of the aromatic ring, which is bonded at the second position of the substituted 1,3,4- oxadiazole nucleus resulted in compounds with good binding energy and G score compared to the standard drugs, and hence, they can be further developed as potent PLK1 enzyme inhibitors.
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