Quercetin, one of the flavonoids family member, can be found in many vegetables, fruits, and beverages with a noticeable nutritional pharmacological properties. This study was aimed to evaluate the ability of quercetin to inhibit lipopolysaccharide (LPS) that induced lethal toxicity in vivo, and to elucidate the importance of the quercetin as an antitumor agent in breast cancer cell line MCF-7.In vivo experiments included the effect of hesperidin and LPS on the liver and spleen of male mice. In the liver, the antioxidant activity was measured by estimating the concentration of glutathione (GSH), and catalase (CAT), while in the spleen, the concentration of cytokines was measured including IL-33 and TNF-α. In vitro experiments included MTT assay, colonogenicity test and Sulforhadamine 101 to assess breast cancer cells morphological apoptosis. The studies revealed the following results: highly significant increase in IL-33 and TNF-αcytokine levels in LPS challenge mice along with significant glutathione (GSH), and catalase (CAT) level increased compared to control group. The cytotoxicity on MCF-7 cell line showed significant differences between groups treated with different concentrations in comparison with control groups in a concentration-dependent manner. The colony measurement test showed that quercetin significantly inhibited colony formation of MCF7 cells compared to control. Apoptotic morphological results showed clear changes in the shape associated with a later stage of apoptosis, including cell shrinking and chromatin condensation. The obtained results indicate that hesperidin might be a potential beneficial compound as a preventive agent
Itraconazole (ITZ) is an antifungal drug (BCSII) used for the treatment of local and systemic fungal infections. Furthermore, ITZ used as an antifungal prophylaxis for immunocompromised patients.
The objective of the study is to overcome the two problems of low and pH dependent solubility of ITZ by its preparation as floating microparticles.
Firstly, pH-dependent floating microparticles were prepared using oil in water solvent evaporation method, from which the best one (F7) selected as a best pH-dependent formula with composition of ITZ (200mg),EC (800mg), HPMC 15cps (200mg) and safflower oil (2ml) .Then, F7 was compared with the selected Relatively pH-independent ITZ floating microparticles formula wit
... Show MoreSelexipag is an orally selective long-acting prostacyclin receptor agonist, which indicated for the treatment of pulmonary arterial hypertension. It is practically insoluble in water ( class II, according to BCS). This work aims to prepare and optimized Selexipag nanosuspensions to achieve an enhancement in the in vitro dissolution rate. The solvent antisolvent precipitation method was used for the production of nanosuspension, and the effect of formulation parameters (stabilizer type, drug: stabilizer ratio, and use of co-stabilizer) and process parameter (stirring speed) on the particle size and polydispersity index were studied. SLPNS prepared with Soluplus® as amain stabilizer (F15) showed the smallest particle size 47nm wi
... Show MoreStaphylococcal enterotoxin‐B (SEB) is one of the most potent bacterial superantigens that exerts profound toxic effects by inducing a cytokine storm. Inhaled SEB can cause acute respiratory distress syndrome (ARDS), which is often fatal and with no effective treatments.
Efficacy of Δ9‐tetrahydrocannabinol (THC) was tested in a mouse model of SEB‐mediated ARDS, in which lung inflammation, alterations in gut/lung microbiota and production of short‐chain fatty acids (SCFAs) was measured. Gene dysregulation of lung epithelial cells was studied by transcriptome arrays. F
Olmesartan medoxomil (OM) has low bioavailability and limited solubility. To enhance bioavailability, fast dissolving films (FDF) with mixed micelles of soluplus (SPL) and solutol HS15 (STL H15) were developed using solvent casting. The optimised formula, FM2, used polyvinyl alcohol (PVA) and showed high entrapment efficiency, rapid disintegration, and significant improvement in OM bioavailability compared to the market tablet (Olmetec®). FM2 also demonstrated stability and potential for enhanced drug delivery.
Irinotecan induced-mucositis is an inflammatory event of intestine caused by an increase in concentration of active metabolite 7ethyl10-hydroxycamptothecin (SN38) in the intestine. Irinotecan must first be converted by a carboxylesterase (CES) to the active metabolite (SN38), which is subsequently glucuronidated by the hepatic enzyme to SN38G. The SN-38G is deconjugated in the intestine to SN-38 via ?-glucuronidase produced by the intestinal bacterial flora, which accounts for SN-38 delayed intestinal mucositis of irinotecan. To study the protective effect of mentha in irinotecan-induced mucositis, intestinal mucositis induced by I.P injection of irinotecan (75mg/Kg/day) for 4 days. Mentha ethanolic extract orally administered to
... Show MoreThe antidiabetic thiozolidinediones (TZDs) a class of peroxisome proliferators-activated receptor (PPAR) ligands has recently been the focus of much interest for their possible role in regulation of inflammatory response. The present study was designed to evaluate the anti-inflammatory activity of pioglitazone in experimental models of inflammation in rats. The present study was conducted to evaluate the anti inflammatory effect of TZDs (pioglitazone 3mg/Kg) on acute, sub acute and chronic model of inflammation by using egg-albumin and formalin–induced paw edema in 72 rats, relative to reference drugs Dexamethasone 5mg/Kg and Piroxicam 5mg/Kg. In each inflammation model, 24 rats wer
... Show MoreExposure to lead results in significant accumulation in most of vital organs, and free radical damage has been proposed as a cause of lead-induced tissue damage, where oxidative stress is a likely molecular mechanism. This study was designed to evaluate therapeutic effects of melatonin in lead-induced organ toxicity in rats. The therapeutic effects of melatonin on lead induced toxicity in rats were evaluated using 36 rats, which were allocated into 3 groups and treated as follows: Group I, includes 12 rats injected subcutaneously with 0.2 ml physiological saline for 30 days, followed by treatment with a daily dose of 20mg/kg melatonin, administrated I.P for the successive 30 da
... Show MorePatch in transdermal drug delivery(TDDS) used to overcome the hypodermic drawback, but these patch also have absorption limitation for hydrophilic and macromolecule like peptide and DNA. So that micronized projection have the ability for skin penetration developed named as microneedle. Microneedle drug delivery system is a novel drug delivery to overcome the limitation of TDDS like skin barrier restriction for large molecule. Microneedle patch can penetrate through skin subcutaneous into epidermis, avoiding nerve fiber and blood vessel contact. There are many type of microneedle patch like solid, polymer, hallow, hydrogel forming microneedle and dissolving microneedle with different method of microfabrication