• Mathiesen Fanning posted an update 6 months ago

    Low aqueous solubility and bioavailability is the limiting factor to achieve desired therapeutic efficacy for variety of new and existing drug moieties. The goal of the present study was to explore the effects of β-cyclodextrin (βCD) and hydroxypropyl-β-cyclodextrin (HPβCD) on the solubility and dissolution profile of diflunisal (DIF) prepared by using two different methods (physical mixing and solvent evaporation) at DIF-cyclodextrins weight ratios of 11, 12 and 14. The phase solubility studies demonstrated that DIF solubility increased proportionally with an increase in βCD and HPβCD concentration. The inclusion complexes were subjected to characterization of scanning electron microscopy (SEM), fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and X-ray diffractometry (XRD). Solvent evaporation yielded higher DIF solubility than physical mixing method. HPβCD-DIF inclusion complexes yielded higher dissolution profile than βCD complexes when prepared under same experimental design. FTIR, DSC and XRD confirmed the successful inclusion of DIF into cyclodextrin (βCD/HPβCD) by both preparation methods with enhanced water solubility and drug release in comparison with pure drug.Although ebastine (EBT) can impede histamine-induced skin allergic reaction and persuade long acting selective H1 receptor antagonistic effects but its poor water solubility circumscribed its clinical application. The main objective of this research work was to improve the aqueous solubility and oral bioavailability of EBT by preparing EBT-loaded bilosomes (EBT-PC-SDC-BS). A thin film hydration method was used to prepare ebastine loaded bilosomes. The prepared-formulations were optimized considering size, morphology and entrapment efficiency. The SEM images revealed regular and spherical shape of bilosomes. Average size of the prepared EBT-PC-SDC-BS was 665.8 nm and zeta potential was around-32.9 mV with 89.05 % average entrapment efficiency (EE).Importantly, the solubility of EBT in water was amplified up to 17.9 μg/ml compared to pure drug (2 μg/mL) reflecting a highest solubility increase of 751 %. In vitro drug release results of prepared EBT-PC-SDC-BS exhibited improved release behavior. Finally, it is established from the results that the EBT-PC-SDC-BS could function as a favorable nano-carrier system to improve the solubility as well as dissolution of EBT.The current study was designed to determine the outcome of banana fruit pulp (BFP) on repeated noise stress exposure (NSE)-induced behavioral deficits and oxidative stress in male mice. BFP (600mg/kg b.w) was administered orally once daily for 2 weeks prior exposure to noise stress. Mice were exposed to NS for 4 h after administration of BFP for 2 weeks. Control mice were administered drinking water and similar treatment as given to test animals. At the end of the treatment behavioral changes were monitored. Animals were sacrificed following behavioral assessment and the brain and plasma samples were collected for biochemical analysis. Repeated NS-induced behavioral deficits (anxiety and depression), impaired learning and memory and produced oxidative stress. Administration of BFP inhibited NS-induced behavioral deficits (anxiolytic and antidepressant effects) and improved cognitive abilities. Brain lipid per oxidation was also decreased with concomitant increase of antioxidant enzyme activities. Repeated noise stress increased plasma corticosterone levels. A significant decrease of plasma corticosterone was observed on unstressed BFP treated animals while this decrease was comparable in stressed + BFP animals. Decreased levels of acetylcholinesterase in BPF+NS treated animals indicated increased cholinergic function which improves learning and memory. Repeated oral administration of BFP induced cognitive improving ability, anti-stress effect and potentiated antioxidant defence mechanism in both control and NS mice. Thus, it is suggested that dietary supplementation of BFP has a curative effect against NS-induced psychiatric and cognitive related disorders which merits deliberation and additional appraisal.Silver nanoparticles were synthesized using extra virgin olive oil (Olea europaea L.) and sunflower oil (Helianthus annuus L.) and characterized by UV-vis spectroscopy, X-ray powder diffraction (XRD) and scanning electron microscopy (SEM). The brown color solution of olive oil nanoparticles (EVOO-NPs) and sunflower oil nanoparticles (SFO-NPs) showed typical absorption at 418 nm and 434 nm respectively. The morphology of extra virgin olive oil was found to be in semi cubic shapes with particle size of 23.45 nm (XRD) and 42.30 nm (SEM) while particle size of (SFO-NPs) had 42.30 nm (XRD) and 46.80 nm (SEM). Antimicrobial activities of crude extra virgin olive oil (EVOO), crude sunflower oil (SFO), synthesized nanoparticle from (EVOO-NPs) and (SFO-NPs) against human pathogenic strains were investigated. Synthesized nanoparticle from each oil showed a potent antimicrobial activity against all tested micro-organisms than crude oil which increased by (81.14% to 174.65 %) and by (111.65% to 192.31 %) than (EVOO) and (SFO) respectively. Both (EVOO-NPs) and (EVOO) had more antimicrobial activities than (SFO-NPs) and (SFO). EVOO (NPs) and SFO (NPs) showed maximum antibacterial activities against K. pneumoniae. Therefore (EVOO-NPs) and (SFO-NPs) could be used as safe natural product against multidrug resistant microbes.Anxiety disorder is a psychiatric disorder characterized by extreme fear or worry. read more It is highly prevalent worldwide which affects daily life and is also an enormous health burden. Neurokinin 1 receptor (NK1R) is a G protein coupled receptor, expressed in both central and peripheral nervous system, involved in affective behaviors. NK1R has established role in anxiety and it is also an important target for pathogenesis of anxiety disorder. Therefore, it has been hypothesized in previous studies that the blockades of NK1R may have antidepressant and anxiolytic effects. The present study deals with the molecular mechanism of protective activity of eugenol against anxiolytic disorder. A pre-clinical animal study was performed on 42 BALB/c mice. Animals were given stress through conventional restrain model. The mRNA expression of NK1R was analyzed by real time RT-PCR. Moreover, the NK1R protein expression was also examined by immunohistochemistry in whole brain and mean density was calculated. The mRNA and protein expressions were found to be increased in animals given anxiety as compared to the normal control.

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