A Novel Smart Biomucoadhesent from Phoenix Sylvestris Fruit Pulp

Phoenix . Sylvestrise belongs to Arecaceae family is also known as the date palm. It is widely available in India. The aim of our research work was to isolate a novel biomucoadhesent from phoenix sylvestris (PS) fruit pulp. The fruit of the plant have potential nutraceuticals and fibers to be used as a food supplements for nutrition. The fruit pulp is rich of minerals. acid, flavanoids, vitamins etc. The fruit pulp was isolated by a simplified. economic process and was evaluated for its various physicochemical properties like solubility, Particle si7e, viscosity, angle of repose, Carrs index, Hausner’s ratio, color, texture, nature, Thin layer chromatography. chemical tests and lR spectral study. The mucaddhesivity of the biomaterial was determined by shear stress method, Park & Robinson method, rotating cylinder method and the results were compared with standard polymers like NaCMC, Carbopol-934. Xanthan gum and Guar gum. The research study revealed that the biomaterial from Phoenix sylvestrise fruit pulp exhibits promising inbuilt mucoadhesion and good mucoretentability. TLC reveals the presence of galactose type polysaccharide. In conclusion, it was drawn that the biomaterial can serve as promising mucoadhesent for formulating the various transmucosal drug delivery systems

Histological and mucoadhesion studies on transpalatal mucoadhesive disks of Rosiglitazone maleate

The present research is aimed to develop a mucoadhesive drug delivery system exhibiting a unique combination of mucoadhesion and controlled drug release in systemic manner to prolong residence in the soft palatal mucosa using rosiglitazone maleate as a model drug. In this study, a mucoadhesive disks formulation for palatal delivery were designed using a simplex lattice design with a mixture of various mucoadhesive polymers (Cp, SCMC, or HPMC, Guar gum and DPP), followed by optimization of the evaluation parameters was employed to get final optimized formulation. In vitro mucoadhesion and mucoretentability property of the formulated disks were examined and histological study was carried out to examine an ex-vivo interaction between the disks and tissue. The optimized F-11 composition showed a force of adhesion  (N)  > 3   and a mucoadhesion time >12 hours with zero order release profile as best fit model closer to the target release profile and followed  anomalous  mediated release of rosiglitazone maleate .The different concentration of mucoadhesive polymer significantly affects the drug release rate, force of adhesion and mucoretentability characteristics of the disks. No more histological changes were observed in the excised palatal mucosa after 12 h contact with the disks  Conclusion: This kind of disks extends the residence time of a dosage form at a particular site and controlling the release of drug in systemic manner from the dosage form and  useful especially for achieving controlled plasma level of the drug as well as improving bioavailability with  reduced side effects

Antioxidant, antiinflammatory and antiinvasive activities of biopolyphenolics

A large number of polyphenolic and heterocyclic compounds, i.e. 4-methylcoumarins, 4-methylthionocoumarins, xanthones, pyrazoles, pyrazolylacrylonitriles, flavones and isoflavones have been tested for their antioxidant activity towards NADPH-catalysed liver-microsomal lipid peroxidation with a view to establish their structure-activity relationship. Inhibition of microsomal lipid peroxidation by 7,8-dihydroxy-4-methylcoumarin (DHMC, 2) and 7,8-diacetoxy-4-methylcoumarin (DAMC, 3) was intriguing. We also found that dihydroxy and diacetoxy derivatives of 4-methylthionocoumarin were more potent in comparison to the corresponding coumarin derivatives in inhibiting TNF-α induced expression of ICAM-1. The effect of nine different xanthones has been examined on the modulation of cytokine-induced expression of ICAM-1 in human endothelial cells. 1,4-Dihydroxyxanthone (10) showed enhanced antioxidant activity as well as the inhibition of the expression of cell adhesion molecules, such as ICAM-1, VCAM-1 and E-selectin on endothelial cells in a concentration and time dependent manner. Antioxidant activity of different pyrazoles and pyrazolylacrylonitriles and antiinvasive activity of flavones and isoflavones against solid tumors have also been studied

Design, synthesis and evaluation of benzofuran-acetamide scaffold as potential anticonvulsant agent

A series of N-(2-(benzoyl/4-chlorobenzoyl)-benzofuran-3-yl)-2-(substituted) acetamide derivatives (4a-l, 5a-l) was synthesized in good yield. All the synthesized compounds were in agreement with elemental and spectral data. The anticonvulsant activity of all synthesized compounds was assessed against the maximal electroshock induced seizures (MES) model in mice. Neurotoxicity was evaluated using the rotarod method. The majority of compounds exhibited anticonvulsant activity at a dose of 30 mg kg–1 body mass during 0.5–4 h, indicating their ability to prevent seizure spread at low doses. Relative to phenytoin, compounds 5i [N-(2-(4-chlorobenzoyl)-benzofuran-3-yl)-2-(cyclohexyl(methyl)amino)-acetamide] and 5c [N-(2-(4-chlorobenzoyl)-benzofuran-3-yl)-2-(4-methylpiperidin-1-yl)acetamide] demonstrated comparable relative anticonvulsant potency of 0.74 and 0.72, respectively, whereas compound 5f [(N-(2-(4-chlorobenzoyl)-benzofuran-3-yl)-2-(4-(furan-2-carbonyl)-piperazin-1-yl) acetamide] exhibited the lowest relative potency of 0.16. The ALD50 of tested compounds ranged from 1.604 to 1.675 mmol kg–1 body mass. The ED50 of synthesized compounds ranged from 0.055 to 0.259 mmol kg–1 (~23.4 to 127.6 mg kg–1) body mass. The pharmacophore mapping of the examined compounds on standard drugs (phenobarbital, phenytoin, ralitolin and carbamazepine) strongly suggests that these compounds may exert their anticonvulsant activity via the same established mechanism as that of known drugs

Therapeutic Strategies in the Management of COVID-19

Since December 2019, SARS-CoV-2 (COVID-19), novel corona virus has caused pandemic globally, with rise in the number of cases and death of the patients. Vast majority of the countries that are dealing with rise in the active cases and death of patients suffering from novel corona viruses COVID-19 are trying to content the virus by isolating the patients and treating them with the approved antiviral that have been previously used in treating SARS, MERS, and drugs that are used to treat other viral infections. Some of these are under clinical trials. At present there are no therapeutically effective antiviral present and there are no vaccines or drugs available that are clinically approved for treating the corona virus. The current strategy is to re-purpose the available drugs or antiviral that can minimise or reduce the burden of the health care emergencies. In this article the reuse of antiviral, US-FDA approved drugs, plant based therapeutic, anti-malarial, anti-parasitic, anti–HIV drugs and the traditional medicines that are being currently used in treating the symptoms of COVID–19 patients is discussed emphasis is also given on the treatment using monoclonal antibodies. The present article provides the therapeutic strategies that will qualify as one of the best available treatment for the better management of the COVID–19 patients in order to achieve medical benefits

Fatty Acids Analysis and Antioxidant Activity of a Lipid Extract obtained from Mercurialis annua L. grown wildly in Jordan

Aerial parts of Mercurialis annua L. were used in the present study, and fatty acid content in lipid extract was determined using GC-FID. The major fatty acids identified were α–linolenic acid (20.3%), heptadecanoic acid (12.8%), palmitic acid (11.9%), pentadecanoic acid (11.7%), cis-10-pentadecenoic acid (11.2%), linoleic acid (7.7%), tridecanoic Acid (4.6%), stearic (4.4%), cis-11,14-eicosadienoic acid (3.8%), beside of minor fatty acids (palmitoleic acid, cis-13,16-docosadienoic acid, arachidic acid, behenic acid, cis-10-heptadecenoic acid and myristic acid). Antioxidant properties of the extract were determined via DPPH radical scavenging, β-carotene bleaching assay and NO radical scavenging assay. The extract produced significant antioxidant activity in-vitro. The data shown here may broaden our knowledge on composition and antioxidant activity of lipid constituents from Mercurialis annua L

Metal–Polymer Nanocomposites: A Promising Approach to Antibacterial Materials

There has been a new approach in the development of antibacterials in order to enhance the antibacterial potential. The nanoparticles are tagged on to the surface of other metals or metal oxides and polymers to achieve nanocomposites. These have shown significant antibacterial properties when compared to nanoparticles. In this article we explore the antibacterial potentials of metal-based and metal–polymer-based nanocomposites, various techniques which are involved in the synthesis of the metal–polymer, nanocomposites, mechanisms of action, and their advantages, disadvantages, and applications

Stability-Indicating HPLC Determination of Gemcitabine in Pharmaceutical Formulations

A simple, sensitive, inexpensive, and rapid stability indicating high performance liquid chromatographic method has been developed for determination of gemcitabine in injectable dosage forms using theophylline as internal standard. Chromatographic separation was achieved on a Phenomenex Luna C-18 column (250 mm × 4.6 mm; 5μ) with a mobile phase consisting of 90% water and 10% acetonitrile (pH 7.00±0.05). The signals of gemcitabine and theophylline were recorded at 275 nm. Calibration curves were linear in the concentration range of 0.5–50 μg/mL. The correlation coefficient was 0.999 or higher. The limit of detection and limit of quantitation were 0.1498 and 0.4541 μg/mL, respectively. The inter- and intraday precision were less than 2%. Accuracy of the method ranged from 100.2% to 100.4%. Stability studies indicate that the drug was stable to sunlight and UV light. The drug gives 6 different hydrolytic products under alkaline stress and 3 in acidic condition. Aqueous and oxidative stress conditions also degrade the drug. Degradation was higher in the alkaline condition compared to other stress conditions. The robustness of the methods was evaluated using design of experiments. Validation reveals that the proposed method is specific, accurate, precise, reliable, robust, reproducible, and suitable for the quantitative analysis

HPLC profiling of selected phenolic acids and flavonoids in Salvia eigii, Salvia hierosolymitana and Salvia viridis growing wild in Jordan and their in vitro antioxidant activity

Background Salvia eigii., Salvia hierosolymitana and Salvia viridis are native to the Mediterranean region, and are used in traditional medicine for the treatment of many ailments. In the current investigation, the methanolic extracts obtained from the air dried aerial parts of S. eigii, S. hierosolymitana and S. viridis from Jordan were screened for their total phenolics content (TPC), total flavonoids content (TFC) and their in vitro antioxidant activity. Additionally, the presence of four bioactive phenolic acids including gallic acid, caffeic acid, rosmarinic acid and salvianolic acid B and other seven flavonoids including luteolin-7-O-glucoside, apigenin, apigenin-7-O-glucoside, rutin, nariginin, hesperidin and quercetin was determined using Liquid chromatography-Electron Spray Ionization-Tandom Mass Spectrometry (LC-ESI-MS/MS). Methods Antioxidant activity of the obtained three extracts were examined via the DPPH•, ABTS• + radical scavenging methods in addition to Ferrous Ion Chelating (FIC) effect. TFC and TPC of the extracts were measured using the aluminum chloride colorimetric method and the Folin-Ciocalteau method, respectively. The presence and concentration of the selected 11 compounds was further determined through LC-ESI-MS/MS. Results The results indicated that three Salvia species had high total flavonoids content expressed in mg quercetin/g dry extract (S. heirosolymitana: 770.85 ±  5.26; S. eigii: 520.60 ±  6.24, S. viridis: 311.36 ±  4.41). S. heirosolymitana had the highest DPPH• activity (0.184 ±  1.22 × 10−2 mg/ml) and FIC effect (0.354 ±  0.018 mg/ml). S. heirosolymitana had slightly higher ABTS• + scavenging activity than S. eigii (0.176 ±  1.16 × 10−2 mg/ml; 0.183 ±  0.031 mg/ml, respectively). All 11 compounds were detected in the extracts of the three Salvia species. Luteolin-7-O-glucoside was detected in high concentration levels in the three species (1756.73, 21651.36, and 26125.14 mg/kg dry plant; S. eigii, S. hierosolyimitana and S. viridis, respectively), yet rosmarinic acid had the highest contribution to both S. hierosolymitana (27124.93 mg/kg) and S. eigii (15783.33 mg/kg). Notably, S. hierosolymitana and S. viridis contained salvianolic acid B (896.11; 890.9 mg/kg). Conclusions The three Salvia species exhibited good antioxidant activity, especially S. heirosolymitana due to its high TPC, TFC, and the presence of high concentration levels of romarinic acid and other phenolic acids and flavonoids. This is the first phytochemical and antioxidant evaluation of S. eigii, S. hierosolymitana and S. viridis from Jordan. Prior to this investigation, no phytochemical investigation on S. eigii was reported