Posted by admin on Jan 31, 2021 in |
Nanosuspension is a biphasic system consisting of drug particles dispersed in an aqueous surfactant or polymeric solution with a particle size between 10 to 1000 nm. Nanosuspension offers the unique advantage of increasing solubility of the pure drug resulting into faster drug absorption and hence achieving faster maximum plasma concentration. Hence, the aim of this research work was to formulate and characterize surfactants/polymer-stabilized nanosuspensions of diosmin (DSN), a phytomedicine, to surpass its poor physicochemical properties and low oral bioavailability. Nanosuspensions were prepared by probe sonication with varying concentrations of different surfactants and polymers such as PVP K 25, poloxamer 188, Tween 80, and PEG 400. Nanosuspension prepared with 3% w/v PEG 400 and 3% w/v DSN, exhibited the lowest size of 203.9 nm, PDI of 0.219, and adequate zeta potential of -27.26 mV, which was subjected to solubility and in-vitro drug release study. The highest solubilizing capacity of DSN was manifested in orthophosphate buffer pH 12. Approximately five times increase in saturation solubility of lyophilized nanosuspension was observed than...
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Posted by admin on Jan 31, 2021 in |
The present research work involves the use of exclusively and commercially available indole-3-carbaldehyde as a starting material to synthesize novel pyrimidine analogues. The synthesis of series of indole and pyrimidine containing N-substituted-4-(1H-indol-3-yl)-6-methyl-2-oxo-1, 2, 3, 4-tetrahydro-pyrimidine-5-carbohydrazide U(1-10) has been done by using principle of Biginelli condensation reaction.Indole-3-carbaldehyde was prepared by formylation of indole (Vilsmeier Haack reaction) using dimethylformamide and phosphorus oxychloride (1). The intermediate indole dihydropyrimidines was synthesized from a mixture of indole-3-carbaldehyde, urea and ethyl acetoacetate in the presence of zinc chloride as acid catalyst (2). The intermediate compound then refluxed with hydrazine hydrate by the addition of catalytic amount of conc. sulphuric acid, led to formation of parent compound 4-(1H-indol-3-yl)-6-methyl-2-oxo-1, 2, 3, 4-tetrahydropyrimidine-5-carbohydrazide(3). The parent compound 3 was used for synthesis of N’-substituted-4-(1H-indol-3-yl)-6-methyl-2-oxo- 1, 2, 3, 4-tetrahydropyrimidine-5-carbohydrazide and substituted aldehydes U (1-10), and/or Schiff bases of N’-substituted-4-(1H-indol- 3- yl)- 6- methyl- 2- oxo- 1, 2, 3, 4-tetrahydropyrimidine-5-carbohydrazide. Elemental analysis, FT-IR, 1H-NMR, and Mass spectral data supports the structures of synthesized compounds. The selected synthesized compounds were screened for...
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Posted by admin on Jan 31, 2021 in |
Dengue is a fatal disease connected to the environment that spreads rapidly. As there is currently no effective vaccine against dengue and no exact treatment for the disease, controlling and preventing dengue fever outbreaks are essential steps for keeping people healthy. Dengue viruses are a member of the Flaviviridae family, mosquito-borne, and causative agents for dengue fever. Bioactive compounds obtained from natural products, including medicinal plants, are a potentially good target to control infections. Thus the current study was designed to find potential phytochemical inhibitors against the Dengue virus NS2B/NS3 protease, which can inhibit the viral replication and control the dengue vector Aedes aegypti. Larvicidal, functional group analysis (FTIR), and molecular docking studies results revealed that the bioactive compounds from the medicinal plant flower extract Cassia auriculata showed high inhibitory activity against the dengue protease enzyme NS2B-NS3 and Aedes aegypti vector. Out of fifteen compounds identified from GCMS, five compounds showed high inhibitory activity against the protease 2FOM in the docking analysis. The main antiviral approach of plant compounds...
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Posted by admin on Jan 31, 2021 in |
Hydroxychloroquine, widely used to treat certain autoimmune diseases and inflammatory conditions, has been repositioned as a new lead against the COVID-19 pandemic. Preliminary studies have suggested that hydroxychloroquine inhibits the entry of the SARS-CoV2 virus mediated by the ACE2 receptor and is a particularly interesting anti-inflammatory and immunomodulatory action in the cytokine storm during COVID-19 infection. Furthermore, cardiovascular effects have been reported in hypertensive patients. These last are thought to result from the inhibition of cyclooxygenase 2. Our results reveal for the first time in atomic detail how hydroxychloroquine, one of the most controversial drugs, has an affinity for a new molecular target (COX2) with a docking score: -7.6 (kcal/mol) and a root mean square deviation (RMSD = 2.542). Hydroxychloroquine binds to cyclo-oxygenase 2 via two hydrogen bonds (H-GLY136 and H-GLY45) and four hydrophobic bonds: Cl -CYS36, 0 -CYS36, 0 -CYS47 and 0 -PRO154). This mechanism has never been elucidated. Hydroxychloroquine proved to be promiscuous. Its structure, which differs from that of non-steroidal anti-inflammatory drugs , tends to show...
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Posted by admin on Jan 31, 2021 in |
Dengue is the most rapidly spreading mosquito-borne viral disease in the world. Patients with dengue fever are treated symptomatically. There is no specific allopathic treatment for dengue fever. Traditional medicinal plants have been reported to be useful in the treatment of dengue fever. The development of new anti-dengue products from bioactive compounds is necessary to find an effective treatment for dengue. The present work aims at formulation development and evaluation of herbal IR tablets with faster disintegration and good mechanical strength for the treatment of Dengue. Tablets are stable solid dosage forms and are favorable for formulation derived from herbal extracts. The Carica papaya Linn and Boswellia serrata having anti-thrombocytopenic effect, anti-viral and antipyretic effect were used for the development of the nutraceutical tablet. Simple direct compression method was used for the formulation of an immediate release tablet. The effect of various superdisintegrant and diluents was explored. The compressed formulations were evaluated on various pre-compression and post-compression parameters. The tablets were coated with hydroxyl propyl methylcellulose (HPMC) 5 cps...
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