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1 cells. Conclusion These findings suggest that M. peregrina seed extract can be used to treat and prevent inflammatory diseases through the inhibition of inflammatory mediators.Objectives Enterococcus faecalis is the major reason for biofilm-related infections and it also interacts with Staphylococcus aureus in biofilms. Gelatinase (gelE) enzyme is an important virulence factor of E. faecalis for biofilm formation. This study aimed to compare the biofilm producing E. faecalis isolates from urine and urinary catheters. The influence of S. aureus on the growth of E. faecalis biofilm cells was also investigated in a dual biofilm model in vitro. Another aim was to evaluate E. faecalis gelE gene expression during biofilm formation. Materials and methods Firstly, crystal violet staining was used to measure the total biofilm biomass of the isolates. Secondly, plate counting was performed to determine the biofilm formation ability of E. faecalis isolates and the effect of S. aureus on E. faecalis biofilm formation. Finally, the gelE expression profile of the isolates was assessed by quantitative real time-polymerase chain reaction. Results According to crystal violet staining and plate counting, all E. faecalis isolates were biofilm producers and the number of E. faecalis sessile cells increased in the presence of S. aureus. Among the 21 E. faecalis isolates, ten expressed high levels of the gelE gene, while eight of them had low expression profiles (p less then 0.05). Conclusion When they grow together, S. aureus may give some advantages to E. faecalis such as increasing sessile cell growth. The expression of the gelE gene was not affected by E. faecalis biofilm formation of the isolates collected from the patients with urinary tract infections.Objectives Research and development in oral drug delivery has evolved to the changeover of solid dosage forms from tablets to oral films. These films offer an elegant route for systemic drug delivery, with an advantage for patients who are suffering from difficulty in swallowing larger oral dosage forms. Aphthous ulcers are the most common oral lesions and are round or oval, with a grayish yellow, crateriform base. For the treatment of aphthous ulcers various marketed product are available, such as vitamin B12 tablets, benzydamine hydrochloride mouthwash or spray, steroid lozenges, and local anesthetics. Hence hydrocortisone is selected as the drug of choice for the treatment of aphthous ulcers, exhibiting anti-inflammatory and immunosuppressant properties that inhibit the clinical manifestations. The main aim of the present study was to develop a hydrocortisone film in order to improve the therapeutic efficacy and bioavailability of hydrocortisone for the treatment of aphthous ulcers. Materials and methods Tand increased patient compliance.Objectives The aim of this investigation was to develop an extended release formulation of diltiazem hydrochloride (DL) for once- and twice-daily administration, based on Eudragit (Eud) RL and RS microspheres using emulsion solvent evaporation. Materials and methods Formulations with different drug-polymer concentrations were produced and characterized in terms of yield, encapsulation efficiency (EE), particle size, and surface morphology. The drug release and thermal behavior of the microspheres were also investigated. Selected microspheres were then coated with Eud RS by continuous solvent evaporation, in order to modify the microspheres' properties and burst release. Results According to the results, the EE was in the range of 56%-93% for uncoated microspheres. The mean particle size of microspheres was different from 470 to above 1000 μm, based on various formulation variables. No difference was observed between the mean size of particles prepared with Eud RL and Eud RS. Microspheres showed sustained release behavior, which was affected by the drugpolymer ratio as well as particle size. Coating the microspheres not only improved the EE values (82%-92%) but also reduced the mean dissolution rate as well as the burst release. Conclusion Microspheres prepared with DLEud RL ratios of 13 and 14 showed release profiles in accordance with the USP criteria for a DL extended release product for dosing every 12 and 24 h, respectively.Objectives The present study aimed to enhance the aqueous solubility of methanol extract of leaves of Vinca rosea (family Apocynaceae) by particle-size reduction using milling and to evaluate its antidiabetic activity. Materials and methods The methanol extract (ME) was micronized using a vibratory ball mill, operated at a vibratory speed of 15 Hz for 60 min at room temperature, and the resulting extract micronized ME (MME) was investigated to determine particle size, solubility, UV/visible profile, and in vitro antidiabetic activity. Results The average particle size of MME was 0.753±0.227 μm, which was less than half of that of the ME (2.007±0.965 μm). The solubility of MME was greater than that of the ME. MME exhibited 65.63%, 18.0%, and 96.87% higher antidiabetic activity in the glucose uptake by the yeast cells method, hemoglobin glycosylation assay, and the alpha amylase inhibition assay, respectively (p less then 0.05). Conclusion The results of the present study indicate that micronization effectively enhanced the aqueous solubility and antidiabetic activity of methanol extract of leaves of Vinca rosea.Objectives Norfloxacin is a synthetic broad-spectrum antibacterial drug having poor bioavailability and pH-dependent solubility. The purpose of the present study was to develop a gastroretentive floating multiparticulate drug delivery system for norfloxacin. Materials and methods Norfloxacin core pellets were prepared using microcrystalline cellulose (MCC) and polyvinylpyrrolidone K30 (PVP K30) by extrusion and spheronization. A 3-level, 3-factor, 17-run experimental Box-Behnken design was adopted to optimize levels of variables in the pellets' formulations. The selected independent variables were amounts of MCC and PVP K30 and spheronizing speed and the dependent variables were aspect ratio and hardness of pellets. Sodium bicarbonate and hydroxypropyl methylcellulose K15M in the ratios of 11, 12, and 21 (w/w) on a dry solid basis were incorporated into the norfloxacin pellets and they were further coated with Eudragit RL 100 using a fluidized bed processor to obtain weight gain of 5%, 10%, and 15% w/w. The f The significant outcome obtained in the study is that such an approach can be effectively employed for improvement of the bioavailability of drugs having poor absorption in the lower part of the gastrointestinal tract with enhanced therapeutic efficacy.Objectives The extracts of Ferulago species are used as aphrodisiacs in Turkey and so we aimed to demonstrate in vivo and in vitro the relaxant effect of four Ferulago species' extracts on the corpus cavernosum (CC). Materials and methods A total of 30 adult male Sprague Dawley rats were divided into control and diabetic groups. Diabetes was induced by a single intraperitoneal injection of 40 mg/kg streptozotocin. In vivo erectile responses were obtained by stimulation of the cavernosal nerves and repeated after intracavernosal injection of extracts in rats, and the data were expressed as intracavernosal pressure (ICP)/mean arterial pressure and total ICP. The relaxant and contractile responses of CC strips were analyzed in the presence or absence of extracts. Results The extracts were active in both control and diabetic rats. The extract-induced maximum relaxation responses (especially of methanol extract of the root of Ferulago bracteata) (98.30±2.6%) were decreased after incubation with L-NAME (44.8±1.8). ODQ, a soluble guanylate cyclase inhibitor, inhibited 77% of extract-induced maximum relaxation in the CC from the control rats. Conclusion These species can be utilized in erectile dysfunction and may be an herbal alternative to synthetic drugs.Objectives Pharmaceutical cocrystals are a promising tool to enhance the solubility and dissolution of poorly soluble drugs. Zaltoprofen (ZFN) is nonsteroidal anti-inflammatory drug with a prevalent solubility problem. The present study was undertaken to enhance the solubility and dissolution of ZFN through pharmaceutical cocrystals by screening various coformers. Materials and methods Cocrystals of ZFN were prepared in 11 and 12 ratio of drugcoformer by the dry grinding method. The melting point and solubility of the crystalline phase were determined. The potential cocrystals were characterized by differential scanning calorimetry (DSC), infrared spectroscopy, and powder X-ray diffraction (PXRD). Selleckchem LY3473329 Cocrystals were subjected to dissolution rate and stability study. Results ZFN-nicotinamide (NIC) cocrystals demonstrated deviation in melting point and solubility. The cocrystals were obtained in both 11 and 12 ratios with NIC. The infrared analysis noticeably indicated the shifting of characteristic bands of ZFN. The crystallinity of the cocrystals was evident from the XRPD pattern and notable difference in the 2θ values of intense peaks. The DSC spectra of the cocrystals exhibited altered endotherms analogous to melting point. The cocrystals showed a faster dissolution rate and a 55% increase in the extent of dissolution compared to pure drug. The cocrystals were stable at room temperature and accelerated conditions. Conclusion The prepared cocrystals exhibited greater solubility and dissolution compared to the pure drug and were stable at room temperature and accelerated conditions.Objectives The involvement of T-type calcium channels in cell proliferation and the role of sodium channels in cell migration have been extensively studied in angiogenesis. In the present study, flunarizine, a dual sodium/calcium channel blocker; was selected to evaluate its anti-angiogenic potential. This can be therapeutically beneficial in diseases caused by pathologically excessive angiogenesis. Materials and methods The anti-angiogenic activity of ion channel blocker was screened by chick chorioallantoic membrane assay (in ovo), rat aortic ring assay, endothelial cell proliferation assay, transwell migration assay, Matrigel cord-like morphogenesis assay (in vitro), and sponge implantation method (in vivo). The anti-angiogenic activity of the test drug was compared with the standard anti-angiogenic drug bevacizumab and, in addition, the test responses were compared with the angiogenic factor vascular endothelial growth factor at a maximal concentration of 500 pM. Results All the groups were compared with and sodium channels. Further studies on the structural modifications of flunarizine for repurposing this ion channel modulator will lead to treatment of the diseases due to excessive angiogenesis from the root cause.Objectives The aim of this study was to evaluate the influence of metal ions present in soil as well as in leaf samples of Calendula officinalis and Phlebodium decumanum for the treatment of psoriasis. Materials and methods To meet the objective, soil and leaf samples were estimated for metal ions by atomic absorption spectrophotometer to determine the influence in antipsoriatic activity. Thereafter imiquimod-induced dermatitis lesions were created in grouped mice. Two plant extracts (aqueous) separately as well as in combinations and standard Retino-A (0.05%) were used. Psoriasis severity index (PSI) was evaluated according to the phenotypic (redness, erythema, and scales) and histological features (epidermal thickness). Further content of phytochemicals in terms of extract was correlated with the effect of psoriasis activity. Results We observed redness, erythema, and scales and the histological features and found a progressive reduction (P less then 0.05) in the severity of psoriatic lesions (redness, erythema, and scales) from days 7 to 21 and decreased epidermal thickness in animals treated with combined extracts at a dose of 200 mg/kg b.
Website: https://www.selleckchem.com/products/muvalaplin.html
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