Posted by admin on May 31, 2023 in |
The oral bioavailability of lumefantrine (LUMF) is low and erratic owing to its low aqueous solubility and P-glycoprotein (P-gp) mediated efflux. The present investigation aims to develop amorphous solid dispersions (SD) of LUMF co-loaded with piperine (PIP), a P-gp and CYP3A4 inhibitor, to improve its dissolution and thereby oral bioavailability. LUMF-SDs were prepared by using Polyvinyl-pyrrolidone, grade Povidone K30 (PVP) as a polymeric carrier, at three different ratios with increasing concentrations of polymer, employing melt method. DSC, XRD and FTIR characterized the PIP-LUMF-PVPSD at ratio of 1:6:18demonstrating higher aqueous solubility of LUMF. The DSC thermogram and XRD diffractogram confirmed the loss of crystallinity of both LUMF and PIP in PIP-LUMF SD, resulting in improved dissolution. Moreover, the possible molecular interactions between LUMF and PIP and /or PVP were investigated by FTIR studies. Crystallinity being a function of time, the stability of LUMF-PIP-PVP SD exposed to stressed humidity and temperature conditions (40 °C/75% RH) for 90 days was validated by DSC and release studies. These findings suggest that the SD...
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Posted by admin on May 31, 2023 in |
This study focuses on preparing and evaluating polymeric nanoparticles made of pegylated PLGA. In this study, both double-emulsion solvent evaporation and single-emulsion solvent evaporation were employed to formulate the pegylated PLGA nanoparticles with PVA as the surfactant. For the encapsulation of the hydrophobic drug Resveratrol, formulations were successfully prepared and tested for their particle size, polydispersity index, zeta potential, drug loading and entrapment efficiency. Scanning electron microscopy was used to observe the morphology and surface characteristics of the nanoparticles. The results demonstrated successful fabrication of the Resveratrol loaded pegylated PLGA nanoparticles. PVA was demonstrated in the present study to be a promising surfactant for the encapsulation and delivery of poorly water-soluble compounds as pegylated PLGA nanoparticles with the desired particle size, morphology and drug loading. PLGA nanoparticles encapsulated with Resveratrol had been successfully used to deliver the drug to the target site by pegylated PLGA...
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Posted by admin on May 31, 2023 in |
Oxidative stress and cholinergic deficit are major culprits of cognitive impairment. Intake of green leafy vegetables – rich in antioxidant phytoconstituents- strongly correlates with memory-preserving capacity. Our earlier work showed that hydromethanol (HM) extract of Chenopodium album (a common leafy vegetable) had strong acetylcholinesterase inhibitory and antioxidant activity in-vitro. The objective of the present study was to isolate the bioactive fraction/constituent from HM extract of C. album and substantiate its memory-enhancing capacity with in-vitro and in-vivo evidence. The HM extract was fractionated by solvent portioning and column chromatography and the antioxidant and acetylcholinesterase inhibition by fractions and sub-fractions thus obtained were assessed by DPPH and Ellman assays, respectively. The fraction F6 showed best potential in-vitro. Subsequently, the anti-amnesic capacity of HM extract and F6 was assessed using a scopolamine-induced memory impairment mouse model. Morris Water Maze test was used to determine memory. Biochemical parameters and histopathological studies of brain were also evaluated to elucidate anti-amnesic mechanism. In-vivo studies confirmed that F6 protected against scopolamine-induced memory impairment and significantly reduced...
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Posted by admin on May 31, 2023 in |
Two simple and sensitive evulsions spectrophotometric methods have been described for the assay of Cycloserine either in pure form or in pharmaceutical formulations. The developed methods involve formation of coloured chloroform extractable ion – pair complexes of the drug with bromophenol blue (BPB) and bromo cresol green (BCG) in acidic medium. For two methods, the extracted complexes showed absorbance maxima at 408 and 419.5nm. Beer’s law is obeyed in the concentration ranges 2.0-20 and 2.5-25μg/mL with BPB and BCG respectively. The effects of concentration of dye, pH and interference of recipients have been studied and optimized. The limit of detection and quantification has been determined for two methods. These two are very accurate methods of physical and instrumental mode of experiments. Two methods have been validated as per the guidelines of ICH. The methods have been applied to the determination of drug in commercial tablets and results of analysis were validated statistically through recovery...
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Posted by admin on May 31, 2023 in |
Central and eastern Brazil is home to the cactus species Cereus jamacaru, also called mandacaru or cardeiro. It frequently reaches a height of 6 metres. For animal feed, a kind without thorns is utilized. The most typical type is quite thorny; however, if the thorns are The native Brazilian cactus Cereus jamacaru D.C., also known as “mandacaru,” grows naturally in the Caatinga biome and is characterized as a source of food and medicines used to cure kidney inflammation, urinary infection, and rheumatism. However, the antioxidant activity and phenolic chemicals have not yet been assessed. The current study’s phytochemical examination of the ethanolic extract to assess the phytochemical, antioxidant, and anti-diabetic effects of C. jamacaru root extracts showed the Presence of terpenoids and flavonoids, saponins, alkaloids, steroids, coumarin and carbohydrates. This study has demonstrated that C. jamacaru root extract contains primary and secondary metabolites that can be pharmacologically useful and possess some antidiabetic and antioxidant properties. It was also discovered that C. jamacaru root ethanol extract possessed antioxidant and antidiabetic...
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