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Due to various limitations in conventional drug delivery system, it is important to focus on the target-specific drug delivery system where we can deliver the drug without any degradation. Among various challenges faced by a formulation scientist, delivering the drug to its right site, in its right dose, is also an important aim. A focused drug transport aims to extend, localize, target and have a safe drug interaction with the diseased tissue.
The aim of targeted drug delivery is to make the required amount of the drug available at its desired site of action. Drug targeting can be accomplished in a number ways that include enzyme mediation, pH-dependent release, use of special vehicles, receptor targeting among other mechanisms. Intelligently designed targeted drug delivery systems also offer the advantages of a low 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 transport aims to have a safe drug interaction with the diseased tissue.
This review focuses on the available targeting techniques for delivery to the colon, brain and other sites of interest. Overall, the article should make an excellent read for the researchers in this area. Newer drug targets may be identified and exploited for successful drug targeting.
This review focuses on the available targeting techniques for delivery to the colon, brain and other sites of interest. Overall, the article should make an excellent read for the researchers in this area. Newer drug targets may be identified and exploited for successful drug targeting.Clays have been used in various health care products, including drug delivery systems. Advanced formulations have been investigated to take full advantage of clays or clay-based materials. The remarkable properties of clays, such as high adsorption, high surface area, and high ion exchange capacities, provide an ideal system for the delivery of poorly water-soluble drugs. There is currently limited information on the classification and discussion of clay-based formulations for poorly water-soluble drugs. This review aims to describe efficient delivery systems that use clay as the main excipient in formulations. More details about the strategies of using clays in formulations as well as fabrication methods will be discussed. Moreover, combinations with other excipients in hybrid formulations will also be mentioned in evaluating the efficacy of these systems. The highlighted recent studies on clay-based formulations for poorly water-soluble drugs could provide fundamental approaches and prospects to apply them in drug development.
Various phenolics show inhibitory activity towards xanthine oxidase (XO), an enzyme that generates reactive oxygen species which cause oxidative damage.
This study investigated the XO inhibitory activity of Euphorbia peplus phenolics.
The dried powdered aerial parts of E. peplus were extracted, fractioned and phenolics were isolated and identified. The XO inhibitory activity of E. peplus extract (EPE) and the isolated phenolics was investigated in vitro and in vivo.
Three phenolics were isolated from the ethyl acetate fraction of E. peplus. All isolated compounds and the EPE showed inhibitory activity towards XO in vitro. In hyperuricemic rats, EPE and the isolated phenolics decreased uric acid and XO activity. Molecular docking showed the binding modes of isolated phenolics with XO, depicting significant interactions with the active site amino acid residues. GSK-3 inhibitor Molecular dynamics simulation trajectories confirmed the interaction of isolated phenolics with XO by forming hydrogen bonds with the active site residues. Also, the root mean square (RMS) deviations of XO and phenolics-XO complexes achieved equilibrium and fluctuated during the 10 ns MD simulations. The radius of gyration and solvent accessible surface area investigations showed that different systems were stabilized at ≈ 2500 ps. The RMS fluctuations profile depicted that the drug binding site exhibited a rigidity behavior during the simulation.
In vitro, in vivo and computational investigations showed the XO inhibitory activity of E. peplus phenolics. These phenolics might represent promising candidates for the development of XO inhibitors.
In vitro, in vivo and computational investigations showed the XO inhibitory activity of E. peplus phenolics. These phenolics might represent promising candidates for the development of XO inhibitors.Objective Exercise is an essential rehabilitative strategy after stroke butits implementation is limited as its very early use can exacerbate damage and is restricted by patient disability. Remote Ischemic Conditioning (RIC) is a safe alternative for post-stroke neuroprotetion. The present study investigated the neurorehabilitative benefits of early RIC followed by exercise (RICE) therapy.Methods 48 adult male Sprague-Dawley rats were divided into groups 1) sham, 2) stroke, 3) stroke with RICE at day 3 (RIC 6 hours after reperfusion followed by exercise days 3 to 28), 4) stroke with exercise at day 3 (exercise days 3 to 28), and 5) stroke with RICE at day 1 (RIC 6 hours after reperfusion followed by exercise days 1 to 28), 6) stroke with exercise at day 1 (exercise days 1 to 28 after reperfusion). Long-term functional outcomes were determined by grid walk, rota-rod, adhesive tape touch, and Morris water maze. Levels of mRNA and proteins of neuroplasticity, synaptogenesis, and angiogenesis, were determined.Results As compared to exercise only, animals that underwent RICE had significant improvements in functional outcomes after stroke. These improvements were most significant in groups that had the later initiation of exercise. In addition, all treatment groups showed significant increases in mRNA and protein expression of the target molecules for neuroplasticity, synaptogenesis, and angiogenesis, while further significant increases were observed after RICE following ischemic stroke.Conclusions RICE, a novel therapy that supplements RIC prior to exercise, is superiorly effective in inducing rehabilitation after stroke as compared to the traditional exercise monotherapy rehabilitation in rats with ischemic brain injury.
My Website: https://www.selleckchem.com/GSK-3.html
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