Turkish Journal of Pharmaceutical Sciences

Turkish Journal of Pharmaceutical Sciences

Basic info

  • Publisher: Galenos Publishing House
  • Country of publisher: turkey
  • Date added to EuroPub: 2019/Aug/08

Subject and more

  • LCC Subject Category: Medicine, Pharmacology
  • Publisher's keywords: Medicine, Pharmaceutical Sciences
  • Language of fulltext: english

Publication charges

  • Article Processing Charges (APCs): No
  • Submission charges: No
  • Waiver policy for charges? No

Editorial information

Open access & licensing

  • Type of License: CC BY-NC-ND
  • License terms
  • Open Access Statement: Yes
  • Year open access content began: 2004
  • Does the author retain unrestricted copyright? False
  • Does the author retain publishing rights? False

Best practice polices

  • Permanent article identifier: DOI
  • Content digitally archived in: Nopolicy
  • Deposit policy registered in: None

This journal has '17' articles

Synthesis and Swelling Behavior of Sodium Alginate/Poly(vinyl alcohol) Hydrogels

Synthesis and Swelling Behavior of Sodium Alginate/Poly(vinyl alcohol) Hydrogels

Authors: Lachakkal Rudrappa SHIVAKUMARA, Thippaiah DEMAPPA
( 0 downloads)
Abstract

Objectives: Hydrogels are macromolecular networks able to absorb and release water/biological fluids in a reverse-phase manner, in response to specific environmental stimuli. Such stimuli-sensitive behavior makes hydrogels interesting for the design of smart devices applicable to a variety of technological fields. They are able to absorb and retain 10-20% and up to 1000 times the water or biological fluids than their dry weight can. The aim of this study was to extend the work on drug delivery in the stomach at pH 2-2.2. Materials and Methods: The authors synthesized sodium alginate (SA)/poly(vinyl alcohol) (PVA) hydrogels. These hydrogels were characterized by fourier transform infrared spectroscopy and scanning electron microscopy, and the swelling properties of the hydrogels were examined at different pH values, in different salts, at different temperatures, and in different acids and bases. Results: The authors studied and reported the swelling effects or variations such as the effects of salts, acids, bases, temperature, and pH. The results for the crosslinking agent glutaraldehyde showed that 8 mL of glutaraldehyde had a higher swelling rate compared to that of 10 mL and 12 mL. Conclusion: In this work the authors studied the swelling degree in different acids and bases. It is concluded that the degree of swelling decreases with increases in the concentration of glutaraldehyde and also depending on the concentrations of the acids. The swelling degrees of PVA/SA hydrogels gradually increase with increases in the concentrations of acids (low pH). The swelling of hydrogels decreases with increases in pH (>7) or at high alkaline. Based on the results for salt solutions the swelling behavior was found to be in the order: K+>Na+>Ca2+>Mg2+.

Keywords: Swelling, pH, crosslinking agent, buffer solution, sodium alginate, PVA
Evaluation of the Antidiabetic Activity of Alchemilla persica Rothm. in Mice with Diabetes Induced by Alloxan

Evaluation of the Antidiabetic Activity of Alchemilla persica Rothm. in Mice with Diabetes Induced by Alloxan

Authors: Serkan ÖZBİLGİN, Hanefi ÖZBEK, Neriman İpek KIRMIZI, Burçin ERGENE ÖZ*, Ekin KURTUL, Bade Cevriye ÖZRENK, Gülçin SALTAN İŞCAN, Özlem BAHADIR ACIKARA
( 0 downloads)
Abstract

Objectives: Alchemilla species are used in Turkish folk medicine for the treatment of many diseases together with diabetes. Alchemilla persica, belonging to this genus, is widely distributed in Eastern Anatolia as well as in Caucasia, northern and northeastern Iran, and northern Iraq. Materials and Methods: Methanolic-water extracts of the aerial parts and roots of A. persica were evaluated for their hypoglycemic activities in mice with alloxan-induced diabetes in order to verify its usage in folk medicine. Results: None of the tested extracts exhibited a significant lowering effect on blood glucose levels. However, the aerial parts notably increased blood glucose levels at doses of 100 mg/kg and 200 mg/kg. Conclusion: A. persica usage as an antidiabetic is not confirmed in the present study.

Keywords: Alchemilla persica, alloxan, antidiabetic activity, diabetes, hypoglycemic activity
Palmitic Acid–Pluronic F127–Palmitic Acid Pentablock Copolymer as a Novel Nanocarrier for Oral Delivery of Glipizide

Palmitic Acid–Pluronic F127–Palmitic Acid Pentablock Copolymer as a Novel Nanocarrier for Oral Delivery of Glipizide

Authors: Vipan Kumar KAMBOJ, Prabhakar Kumar VERMA
( 0 downloads)
Abstract

Objectives: The aim of the present study was to develop nanotechnology-based oral formulations of glipizide to enhance the bioavailability and eliminate the frequent oral administration of the conventional dosage form. Glipizide is an antidiabetic drug with a short biological half-life and limited oral bioavailability. Novel palmitic acid–pluronic F127–palmitic acid (PA-F127) pentablock copolymer-based prolonged release glipizide nanoparticles (GNs) were prepared and screened for in vitro and in vivo studies. Materials and Methods: GNs were prepared using a novel PA-F127 pentablock copolymer by solvent evaporation technique. The prepared nanoparticles were evaluated for particle size, polydispersity index (PDI), zeta potential, entrapment efficiency, percentage yield, and drug excipient compatibility using fourier transform infrared spectroscopy (FTIR) and differential scanning calorimeter (DSC) analysis, X-ray diffraction, scanning electron microscopy, in vitro drug release studies, stability studies, and in vivo pharmacokinetic studies. Results: The results of FTIR and DSC analysis revealed the absence of drug–excipient interactions. The optimized GN1 had particle size 242.60±4.20 nm, PDI 0.171±0.014, and zeta potential -21.41±0.462 mV. The prepared nanoparticles were spherical and showed semi-amorphous characteristics. The in vitro release studies showed 34.43±4.8% drug was released in the first 8 h and 56.11±4.12% glipizide was released further over 24 h. The GN1 was found to be stable at 5±3°C for up to 3 months. Pharmacokinetic studies showed that the orally administered GN1 was superior with Cmax 2.35-fold, tmax 1.6-fold, area under the curve (AUC0→∞) 3.3-fold, and mean residence time 1.2-fold as compared to pure glipizide (p<0.05). Conclusion: The bioavailability of the newly developed GN1 was successfully increased and the problem of frequent oral administration with the conventional dosage form can be overcome for diabetes treatment.

Keywords: Glipizide, nanoparticles, palmitic acid, pluronics, bioavailability
The Anticancer and Anti-inflammatory Effects of Centaurea solstitialis Extract on Human Cancer Cell Lines

The Anticancer and Anti-inflammatory Effects of Centaurea solstitialis Extract on Human Cancer Cell Lines

Authors: Mehlika ALPER, Hatice GÜNEŞ
( 0 downloads)
Abstract

Objectives: Natural products originating from plants have been used for many years in the treatment of various diseases, including cancer. Centaurea solstitialis subsp. solstitialis is used in Turkish folk medicine. This study was the first to determine the in vitro biological effects of ethanolic extract from the flowering parts of C. solstitialis L. subsp. solstitialis collected from Muğla Province. Materials and Methods: The cytotoxic effect was evaluated against Daudi, A549, and HeLa cancer cells and one normal BEAS-2B cell line using the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5- dipenyltetrazolium bromide) assay. Flow cytometric analysis and the caspase-3 activity assay were performed to detect apoptotic cell death. Angiogenic factor [vascular endothelial growth factor (VEGF)] secretion and the release of interleukin (IL)-1α, IL-6, and tumor necrosis factor (TNF)-α by cells treated with the extract were measured using enzyme-linked immunosorbent assay. Results: The extract exhibited cytotoxic effects against all the cancer cell lines used but HeLa and Daudi were the most sensitive cells, with IC50 values of 63.18 μg/mL and 69.27 μg/mL, respectively. Selective cytotoxicity was observed between the HeLa and normal BEAS-2B cell lines. The extract arrested the cell cycle at the S and G2 phases. In addition, apoptotic cell death was detected in HeLa and A549 cells. Moreover, the plant extract caused a significant decrease in VEGF secretion in A549 cells and a fluctuation in IL-1α, IL-6, and TNF-α secretion in A549 and Daudi cells. Conclusion: These observations suggest that the flowering parts of C. solstitialis may be a potential source in the development of natural drugs for the treatment of cancer and modulation of cytokine secretion.

Keywords: Centaurea solstitialis, cancer cell lines, anti-cancer, anti-inflammatory
An In Vitro Study on the Cytotoxicity and Genotoxicity of Silver Sulfide Quantum Dots Coated with Meso-2,3-dimercaptosuccinic Acid

An In Vitro Study on the Cytotoxicity and Genotoxicity of Silver Sulfide Quantum Dots Coated with Meso-2,3-dimercaptosuccinic Acid

Authors: Deniz ÖZKAN VARDAR, Sevtap AYDIN, İbrahim HOCAOĞLU, Havva YAĞCI ACAR, Nursen BAŞARAN
( 0 downloads)
Abstract

Objectives: Silver sulfide (Ag2S) quantum dots (QDs) are highly promising nanomaterials in bioimaging systems due to their high activities for both imaging and drug/gene delivery. There is insufficient research on the toxicity of Ag2S QDs coated with meso-2,3-dimercaptosuccinic acid (DMSA). In this study, we aimed to determine the cytotoxicity of Ag2S QDs coated with DMSA in Chinese hamster lung fibroblast (V79) cells over a wide range of concentrations (5-2000 μg/mL). Materials and Methods: Cell viability was determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and neutral red uptake (NRU) assays. The genotoxic and apoptotic effects of DMSA/Ag2S QDs were also assessed by comet assay and real-time polymerase chain reaction technique, respectively. Results: Cell viability was 54.0±4.8% and 65.7±4.1% at the highest dose (2000 μg/mL) of Ag2S QDs using the MTT and NRU assays, respectively. Although cell viability decreased above 400 μg/mL (MTT assay) and 800 μg/mL (NRU assay), DNA damage was not induced by DMSA/Ag2S QDs at the studied concentrations. The mRNA expression levels of p53, caspase-3, caspase-9, Bax, Bcl-2, and survivin genes were altered in the cells exposed to 500 and 1000 μg/mL DMSA/Ag2S QDs. Conclusion: The cytotoxic effects of DMSA/Ag2S QDs may occur at high doses through the apoptotic pathways. However, DMSA/Ag2S QDs appear to be biocompatible at low doses, making them well suited for cell labeling applications.

Keywords: Meso-2,3-dimercaptosuccinic acid coated silver sulfide quantum dots, genotoxicity, apoptosis
Phytochemical Screening and Metallic Ion Content and Its Impact on the Antipsoriasis Activity of Aqueous Leaf Extracts of Calendula officinalis and Phlebodium decumanum in an Animal Experiment Model

Phytochemical Screening and Metallic Ion Content and Its Impact on the Antipsoriasis Activity of Aqueous Leaf Extracts of Calendula officinalis and Phlebodium decumanum in an Animal Experiment Model

Authors: Kuntal DAS, Someswar DEB, Tejaswini KARANTH
( 0 downloads)
Abstract

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<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.w. Furthermore, plant samples procured from the Nandi Hills, Bangalore, showed better uptake of metals with respect to Fe (2.05 mg/kg), Cu (0.78 mg/kg), and Zn (1.12 mg/kg), which showed a positive impact on procurement of maximum amount of extracts that further correlated with the activity, indicating a significant reduction in psoriatic lesions. Conclusion: The results revealed that the significant dose-dependent antipsoriasis activity of combined aqueous extracts of C. officinalis and P. decumanum as well as metal ions had an impact on the procurement of extracts and said activity.

Keywords: Epidermal thickness, correlation, Calendula officinalis, Phlebodium decumanum, PSI, psoriasis
Anti-Angiogenic Activity of Flunarizine by In Ovo, In Vitro, and In Vivo Assays

Anti-Angiogenic Activity of Flunarizine by In Ovo, In Vitro, and In Vivo Assays

Authors: Chandana KAMILI*, Ravi Shankar KAKARAPARTHY, Uma Maheshwararao VATTIKUTI
( 0 downloads)
Abstract

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 the control group using one-way ANOVA, followed by a post hoc test, Dunnett’s test, to compare the mean of all the groups with the control mean. In the chick chorioallantoic membrane assay, the number of branching points and angiogenic score were evaluated and significant results were observed at 10-5 M and 10-4 M. In the aortic ring assay a reduction in the area of sprouts was observed with 5-10 μM and significant reductions in the weight of sponges, number of blood vessels formed, and hemoglobin content were observed at all three tested concentrations of flunarizine in the sponge implantation method. In the studies on human umbilical vein endothelial cells the test drug (1-100 nM) showed significant inhibition of proliferation and migration and a decrease in the network length of cord-like tubes in a dose-dependent manner. Conclusion: Flunarizine has significant anti-angiogenic action by inhibiting cell proliferation, migration, and cord-like tube formation, which resulted from blocking of the T-type calcium 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.

Keywords: Anti-angiogenesis, chick chorioallantoic membrane assay, rat aortic ring assay, sponge implantation method, human umbilical vein endothelial cells, flunarizine
Superior Solubility and Dissolution of Zaltoprofen via Pharmaceutical Cocrystals

Superior Solubility and Dissolution of Zaltoprofen via Pharmaceutical Cocrystals

Authors: Prabhakar PANZADE*, Giridhar SHENDARKAR
( 0 downloads)
Abstract

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 1:1 and 1:2 ratio of drug:coformer 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). 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 1:1 and 1:2 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.

Keywords: Pharmaceutical cocrystal, zaltoprofen, solubility, dissolution
Effect of Extracts of the Aerial Parts and Roots from Four Ferulago Species on Erectile Dysfunction in Rats with Streptozotocin-Induced Diabetes

Effect of Extracts of the Aerial Parts and Roots from Four Ferulago Species on Erectile Dysfunction in Rats with Streptozotocin-Induced Diabetes

Authors: Songül KARAKAYA*, Didem YILMAZ ORAL, Serap GÜR, Hayri DUMAN, Ceyda Sibel KILIÇ
( 0 downloads)
Abstract

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.

Keywords: Aphrodisiacs, Apiaceae, Ferulago, erectile function
Development and Optimization of a Floating Multiparticulate Drug Delivery System for Norfloxacin

Development and Optimization of a Floating Multiparticulate Drug Delivery System for Norfloxacin

Authors: Vaibhav SALVE, Rakesh MISHRA, Tanaji NANDGUDE
( 0 downloads)
Abstract

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 1:1, 1:2, and 2:1 (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 fourier transform infrared spectrum, scanning electron microscopy, physical characterization, particle size distribution analysis, floating studies, and in vitro drug release studies of the pellets were evaluated. Results: Among the floating multiparticulate pellets batches, batch B-22 was found to be optimized based on the criteria of attaining the minimum floating lag time (<10 min) and the maximum value of drug released 82.11% in 8 h. The percentage drug release for batches B-21 and B-23 was 91.12% in 5 h and 60.67% in 8 h, respectively. The drug release studies indicated that as the Eudragit RL 100 polymer coat increases the drug release decreases, producing sustained release of norfloxacin. The floating studies revealed that 70%-90% of pellets remained floating for up to 8 h. All the batches have excellent flow properties with angle of repose in the range of 25.5±0.49° to 28.02±0.30°, and Carr’s index and Hausner’s ratio in the range of 5% to 15% and 1.05±0.3 to 1.14±0.3, respectively. Conclusion: 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.

Keywords: Gastroretentive, floating multiparticulate, norfloxacin, spheronization, Box–Behnken design
Impact of Particle-Size Reduction on the Solubility and Antidiabetic Activity of Extracts of Leaves of Vinca rosea

Impact of Particle-Size Reduction on the Solubility and Antidiabetic Activity of Extracts of Leaves of Vinca rosea

Authors: Khalid HUSSAIN, Abida QAMAR, Nadeem Irfan BUKHARI, Amjad HUSSAIN, Naureen SHEHZADI, Shaista QAMAR, Sajida PARVEEN
( 0 downloads)
Abstract

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<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.

Keywords: Vinca rosea, methanol extract, micronization, solubility, antidiabetic activity
Design and In Vitro Evaluation of Eudragit-Based Extended Release Diltiazem Microspheres for Once- and Twice-Daily Administration: The Effect of Coating on Drug Release Behavior

Design and In Vitro Evaluation of Eudragit-Based Extended Release Diltiazem Microspheres for Once- and Twice-Daily Administration: The Effect of Coating on Drug Release Behavior

Authors: Noushin BOLOURCHIAN, Maryam BAHJAT
( 0 downloads)
Abstract

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 drug:polymer 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 DL:Eud RL ratios of 1:3 and 1:4 showed release profiles in accordance with the USP criteria for a DL extended release product for dosing every 12 and 24 h, respectively.

Keywords: Coating, diltiazem hydrochloride, Eudragit RL and RS, extended release, microspheres
Formulation Design of Hydrocortisone Films for the Treatment of Aphthous Ulcers

Formulation Design of Hydrocortisone Films for the Treatment of Aphthous Ulcers

Authors: Mohammed Gulzar AHMED*, Sanjana ADINARAYANA
( 0 downloads)
Abstract

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 antiinflammatory 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: The hydrocortisone film was developed containing various concentrations of methylcellulose and propylene glycol (1.0- 2.0% w/v) by solvent casting. The prepared films were evaluated for various characterization studies like film forming capacity, visual appearance, thickness, weight variation, folding endurance, surface pH, drug content, disintegration time, tensile strength, in vitro release study, ex vivo study, and stability studies. Results: A total of five formulations were developed, out of which formulation F2 (1.25% w/v) is considered the optimized formulation as it showed the best results with respect to all characterization studies. A disintegration time of 44 s and maximum in vitro drug release, i.e. 97.55%, were observed. Further, no significant changes were observed during stability studies for the optimized formulation. Conclusion: Hydrocortisone oral films can be formulated as a potentially useful tool for effective treatment of aphthous ulcers with improved bioavailability, rapid onset of action, and increased patient compliance.

Keywords: Aphthous ulcers, hydrocortisone, oral films, solvent casting method, tensile strength, ex vivo study
Investigation of Gelatinase Gene Expression and Growth of Enterococcus faecalis Clinical Isolates in Biofilm Models

Investigation of Gelatinase Gene Expression and Growth of Enterococcus faecalis Clinical Isolates in Biofilm Models

Authors: Didem KART, Ayşe Semra KUŞTİMUR
( 0 downloads)
Abstract

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<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.

Keywords: Dual biofilm, E. faecalis, S. aureus, gelatinase, quantitative reverse transcription polymerase chain reaction
In Vitro Macrophage Nitric Oxide and Interleukin-1 Beta Suppression by Moringa peregrina Seed

In Vitro Macrophage Nitric Oxide and Interleukin-1 Beta Suppression by Moringa peregrina Seed

Authors: Shaymaa Fadhel Abbas ALBAAYIT, Ahmed Salim Kadhim AL-KHAFAJI, Hiba Sarmed ALNAIMY
( 0 downloads)
Abstract

Objectives: Moringa peregrina has long been used in folk medicine to treat diseases including fever, headache, burns, constipation, gut pains, and inflammation. Nitric oxide (NO) and interleukin-1β (IL-1β) play an important role in the pathophysiology of inflammation. The objectives of this study were to determine the effect of M. peregrina seed ethanolic extract (MPSE) on the viability of and NO and IL-1β production by lipopolysaccharide (LPS)-activated macrophage (J774A.1) cell line. Materials and Methods: The 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide assay was used to determine the cytotoxic effect of MPSE treatment at concentrations ranging from 31.15 to 1000 μg/mL. The NO concentration was determined by Griess assay and IL-1β proinflammatory cytokine concentration by enzyme-linked immunosorbent assay in the supernatant of MPSE-treated LPS-activated J774A.1 cell culture. Results: The results show that the MPSE was not cytotoxic at 1000 μg/mL but significantly (p<0.001) inhibited NO and IL-1β production by the LPS-activated macrophage J774A.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.

Keywords: Moringa peregrina, nitric oxide, interleukin-1β, inflammation

About Europub

EuroPub is a comprehensive, multipurpose database covering scholarly literature, with indexed records from active, authoritative journals, and indexes articles from journals all over the world. The result is an exhaustive database that assists research in every field. Easy access to a vast database at one place, reduces searching and data reviewing time considerably and helps authors in preparing new articles to a great extent. EuroPub aims at increasing the visibility of open access scholarly journals, thereby promoting their increased usage and impact.