Search

C-Glucosyl Xanthone derivatives were assessed to inhibit the JNK3 mediated Caspase pathway in Almal (Aluminum Maltolate) induced neurotoxicity in SHSY-5Y cells. Mangiferin was selected among 200 C-Glucosyl Xanthones based on molecular interaction, docking score (−10.22 kcal/mol), binding free energy (−71.12 kcal/mol), ADME/tox properties and by molecular dynamic studies. Further, it was noticed that glycone moiety of Mangiferin forms H-bond with ASN 194, SER 193, GLY 76, and OH group in the first position of the aglycone moiety shows interaction at Met 149 which is exceptionally crucial for JNK3 inhibitory activity. Mangiferin (0.5, 1, 10, 20 and 30 µM) and standard SP600125 (20 µM) treatment increased the cell survival rate against Almal 200 µM, with EC50 of Mangiferin (8 µM) and standard SP600125 (4.9 µM) respectively. Mangiferin significantly impedes kinase activation, indicating suppression of JNK3 signaling with IC50 (98.26 nM). Mangiferin (10 and 15 µM) dose-dependently inhibits the caspase 3, 8, and 9 enzyme activation in comparison to Almal group. Mangiferin demonstrated neuroprotection in SHSY-5Y cells against apoptosis induced by Almal by adapting the architecture of the neurons and increasing their density. Among all Xanthone derivatives, Mangiferin could improve neuronal toxicity by inhibiting JNK3 and down-regulating the Caspase activation. [ABSTRACT FROM AUTHOR]

Recent advancements in drug delivery technologies paved a way for improving cancer therapeutics. Nanotechnology emerged as a potential tool in the field of drug delivery, overcoming the challenges of conventional drug delivery systems. In the field of nanotechnology, solid lipid nanoparticles (SLNs) play a vital role with a wide range of diverse applications, namely drug delivery, clinical medicine, and cancer therapeutics. SLNs establish a significant role owing to their ability to encapsulate hydrophilic and hydrophobic compounds, biocompatibility, ease of surface modification, scale-up feasibility, and possibilities of both active and passive targeting to various organs. In cancer therapy, SLNs have emerged as imminent nanocarriers for overcoming physiological barriers and multidrug resistance pathways. However, there is a need for special attention to be paid to further improving the conceptual understanding of the biological responses of SLNs in cancer therapeutics. Hence, further research exploration needs to be focused on the determination of the structure and strength of SLNs at the cellular level, both in vitro and in vivo, to develop potential therapeutics with reduced side effects. The present review addresses the various modalities of SLN development, SLN mechanisms in cancer therapeutics, and the scale-up potential and regulatory considerations of SLN technology. The review extensively focuses on the applications of SLNs in cancer treatment. [ABSTRACT FROM AUTHOR]

Ionic liquids are a potent class of organic compounds exhibiting unique physico-chemical properties and structural compositions that are different from the classical dipolar organic liquids. These molecules have found diverse applications in different chemical, biochemical, biophysical fields, and a number of industrial usages. The ionic liquids-based products and procedural applications are being developed for a number of newer industrial purposes, and academic uses in nanotechnology related procedures, processes, and products, especially in nanobiotechnology and nanomedicine. The current article overviews their uses in different fields, including applications, functions, and as parts of products and processes at primary and advanced levels. The application and product examples, and prospects in various fields of nanotechnology, domains of nanosystem syntheses, nano-scale product development, the process of membrane filtering, biofilm formation, and bio-separations are prominently discussed. The applications in carbon nanotubes; quantum dots; and drug, gene, and other payload delivery vehicle developments in the nanobiotechnology field are also covered. The broader scopes of applications of ionic liquids, future developmental possibilities in chemistry and different bio-aspects, promises in the newer genres of nanobiotechnology products, certain bioprocesses controls, and toxicity, together with emerging trends, challenges, and prospects are also elaborated. [ABSTRACT FROM AUTHOR]

Nanoparticles are widely used in different technological fields, one of which is in medicine because of their antibacterial properties. Copper nanoparicles (CuNPs) are used in several types of wound dressing for the treatment of wounds. Mafenide acetate (MFA) is an antibiotic that is also widely used for treatment of wounds. In this research work, we have studied the antibacterial activity of MFA loaded in Copper (Cu) nanocomposite for enhanced antibacterial activity through the development of dosage form cream. Antibacterial effect of MFA loaded CuNPs against microbes such as Staphylococcus aureus, Salmonella typhi, Escherichia coli, Klebsiella pneumonia, and Pseudomonas aeruginosa were observed. Minimum inhibitory concentration for MFA-CuNPs was achieved in the concentration of 12.25 µg/ml but for MFA without CuNPs, the MIC was 50 µg/ml. Among the Cu nanocomposite dosage forms, cream CF2 has the maximum zone of inhibition. [ABSTRACT FROM AUTHOR]

Background: Combined plant extracts of Phyllanthus niruri, Croton tiglium, and Zingiber officinale are reported to have potential pharmacological applications. Ethosomes have a unique ability of encapsulating drugs or plant extracts with varying hydrophobicities in the phospholipid bilayer. Aim: To explore cytotoxicity of the combined plant extracts and ethosome loaded combined plant extracts for topical delivery. To study effect of ethosomes loaded combined plant extracts using HaCaT cells model treated with testosterone. Methods: Dried powder of plant was extracted with ethanol using Soxhlet and cold macerations. Total phenolic and flavonoid contents were also determined using established methods. The combined extract loaded ethosome formulation was prepared by solvent dispersion method. Results: The plant extracts loaded ethosomes formulation with a vesicle size range 1524.6‐167.7 nm was prepared. HaCaT cells treated with testosterone negative control showed an IC50 value of 27 ± 1.0. Thw standard marketed topical minoxidil (1% solution) treated cells with testosterone showed an IC50 value 33 ± 1.0 and the combined plant extracts loaded ethosomes with testosterone showed an IC50 value 30 ± 1.0. Morphological alterations of rat skin exposed to the combined plant extract loaded ethosomes solution were assessed and compared with untreated skin and negative control. Conclusion: The preclinical safety was investigated employing an in vitro cytotoxicity and histopathological study. The cell line study results confirmed that the combined plant extracts loaded ethosomes inhibits testosterone and increase cell viability closer to that of standard drug minoxidil. According to our histopathological study, the combined plant extract loaded ethosomal formulations did not cause any damage to the rat skin layer. [ABSTRACT FROM AUTHOR]

The aim of the present research work was to prepare and evaluate in situ gel forming ophthalmic drug delivery system loaded with brimonidine tartarate (BT). In this work, carbopol and hydroxy propyl methyl cellulose (HPMC), ophthalmic gel-forming mucoadhesive polymers, which gets converted to gel in the lachrymal fluid were used as in the preparation of pH t riggered in situ gel formulation. The formulations were then autoclaved at 121°C for 15 min and evaluated for pH, clarity, gelling capacity, drug content, viscosity, and in vitro release. The developed formulations exhibited extended release of drug over a period of 8 hours in in vitro studies and therefore it could increase the residence time in eye. The optimized formulations were finally tested for its ability to cause irritation in male albino rabbits. The results indicated that the formulations did not irritate or damage the cornea, iris and conjunctiva. [ABSTRACT FROM AUTHOR]

Introduction: The objective of the present study was to improve the anti-inflammatory and antibacterial activities of mastic gum resin (MGR). MGR was loaded into a phospholipid nanocarrier with or without partially hydrolyzed ginsenoside, followed by dispersion into distilled water., Method: The phospholipid nanocarrier dispersion showed significantly enhanced in-vitro release, porcine skin/ intestine permeation, and retention. When the ratio of the MGR versus partially hydrogenated ginsenoside reached 1:1 w/w in the nanocarrier composition, the in-vitro release increased 54.8-fold compared to the MGR powder suspended in the release media., Results: Permeation of the nanocarrier dispersion through the porcine skin and intestine increased 160-fold and 42-fold, respectively, compared to permeation of the MGR powder suspension. Furthermore, the nanocarrier dispersion reduced NO production and iNOS mRNA expression in the LPS-stimulated RAW264.7 cells. MIC and MBC of the nanocarrier dispersion against P. gingivalis were 4.11 ± 1.17 and 8.22 ± 2.35 μg/mL, respectively., Conclusion: In conclusion, the anti-inflammatory and antibacterial activities of MGR were remarkably enhanced when the MGR was loaded into the nanocarrier with partially hydrolyzed ginsenoside., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Metallic nanoparticles (MNPs) have been widely used for diagnostic and therapeutic purposes in clinical practice. A number of MNP formulations are being investigated in clinical trials for various applications. This increase in the use of NPs results in higher exposure to humans, leading to toxicity issues. Hence, it is necessary to determine the possible undesirable effects of the MNPs after in-vivo application and exposure. One of the main reasons for the toxicity of MNPs is the release of their respective metallic ions throughout the body. Many research studies are in progress investigating the various strategies to reduce the toxicity of MNPs. These research studies aim to change the size, dose, agglomeration, release, and excretion rates of MNPs. In this perspective review, we discussed the possible strategies to improve the therapeutic effects of MNPs through various processes, with lessons learned from the studies involving silver nanoparticles (AgNPs). We also discussed the ways to manage the toxicity of MNPs by purification, surface functionalization, synergistic effect, and targeted therapy approach. All these strategies could reduce the dose of the MNPs without compromising their therapeutic benefits, which could decrease the toxicity of MNPs. Additionally, we briefly discussed the market and toxicology testing for FDA-regulated MNPs., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Background: Silver nanoparticles (AgNPs) have attracted considerable interest in the medical industry due to their physicochemical properties, small size, and surface plasmon behavior. Their smaller particle size and instability in blood circulation leads to toxicity due to its aggregation as Ag+ ions and accumulation at the deepseated organ. In the present study, we aimed at reducing the toxicity of AgNPs by conjugation with an anticancer drug GEM and to improve their internalization through folate receptors-mediated endocytosis by capping the nanoparticles with folic acid (FA)., Methods: One-pot facile synthesis of FA capped silver nanoparticles (FA-AgNPs) has been achieved by using FA as a reducing agent. FA-AgNPs were mixed with Gemcitabine (GEM) to obtain tethered FA-GEM-AgNPs. Nanoparticles were characterized by Dynamic Light Scattering (DLS), UV-Visible spectroscopy, Transmission Electron Microscopy (TEM), Energy Dispersive X-ray Analysis (EDAX), Selected Area Electron Diffraction (SAED), and Atomic Absorption Spectroscopy (AAS). The 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was carried out to determine the cytotoxic effect of the prepared nanoformulations. The apoptotic cell death induced by FA-GEM-AgNPs in breast cancer cells were monitored with Acridine orange (AO)/Ethidium Bromide (EtBr) staining., Conclusion: Compared to GEM and AgNPs, FA-GEM-AgNPs showed enhanced cytotoxic effect and internalization in MDA-MB-453 breast cancer cell line. FA-GEM-AgNPs could be an ideal candidate for targeting cancer cells via folate receptor-mediated endocytosis., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)