فهرست مطالب
Journal of Reports in Pharmaceutical Sciences
Volume:10 Issue: 1, Jan-Jun 2021
- تاریخ انتشار: 1400/04/12
- تعداد عناوین: 23
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Pages 1-4Background and Purpose
Muscari Miller. (Asparagaceae family) contains about 50 species worldwide, which are distributed in the Central and Southeastern Europe, Southern Russia, Africa, and some area of Asia such as Iran, Iraq, Afghanistan, Anatolia, and Syria. This study was designed to assess the antioxidant and antimalarial activities of Muscari inconstrictum Rech. f. seeds as one of the Iranian species of Muscari genus. In addition, preliminary phytochemical analysis of the extracts with different polarities was performed.
Materials and MethodsThe essential oil of M. inconstrictum seeds was prepared using Clevenger and extracted with n-hexane, chloroform, and methanol (MeOH) by Soxhlet apparatus. Gas chromatography-mass spectrometry (GC-MS) was used for the characterization of essential oil. Total phenol and flavonoid contents were measured using Folin–Ciocalteu and aluminum chloride reagents. Free radical scavenging and antimalarial activities were investigated via 2, 2-diphenyl-1-picrylhydrazyl (DPPH) and cell-free ß-hematin formation methods.
ResultsGC-MS analysis of the volatile oil of seeds demonstrated the presence of sesquiterpenoid, alkanes, fatty acid, and linear alcohol structures as the main constituents. Among different extracts of M. inconstrictum seeds, the methanolic extract showed significant antioxidant activity, which can be related to the presence of flavonoid and other phenolic structures. Furthermore, chloroform extract is introduced as the most potent antimalarial part.
ConclusionIt seems that further studies on the M. inconstrictum seeds are necessary to focus on pure compounds and their biological activities.
Keywords: Antimalarial, antioxidant, gas chromatography-mass spectrometry, Muscari -
Pages 5-14Background
Plant gums are extensively being exploited as pharmaceutical excipients due to the ease of availability, biodegradability, and reduced costs.
AimThis study investigated the application of the fruit gum of Crysophyllum albidum (CFG) as a matrix former in the formulation of chlorpheniramine maleate and theophylline hydrochloride tablets.
Materials and MethodsThe gum was extracted using acetone and evaluated for flow, swelling, and hydration capacity. Effects of temperature on CFG and drug compatibility were evaluated using differential scanning calorimetry (DSC). Granules containing CFG at 10, 20, and 30% w/w were prepared using the wet granulation method and evaluated for flow properties. Compressed tablets were evaluated for uniformity of weight, hardness, friability, and drug content. In vitro drug release studies were carried out in simulated gastric (pH 1.2) and simulated intestinal (pH 6.8) fluids. Pearson’s similarity correlations were used to analyze results.
ResultsCFG had a swelling capacity of 22% and hydration capacity of 1.44 with an angle of repose of 30o and Carr’s index of 7.6 signifying good flow. DSC thermogram returned an endothermic glass transition peak at 72.1o C with no appreciable shifts in the peak when CFG was incorporated into the drug. Tablet hardness and friability were concentration dependent with values of 6.5–8.5kg F and 0.04–0.4%, respectively; drug content was within official specifications. Formulations containing 30%w/w CFG sustained drug release for over 12h and showed better ability to control drug release than HPMC at same concentration.
ConclusionThis study shows the propensity of CFG to be used in the formulation of sustained-release tablet formulations.
Keywords: Crysophyllum albidum, fruit gum, matrix-former, sustained release, tablet properties -
Pages 15-21
For the first time, a new, simple, precise reversed-phase high-performance liquid chromatography method was developed for the simultaneous estimation of metronidazole, furazolidone, and dicyclomine hydrochloride in capsule dosage form. The method was performed with Thermo, C8 (150 mm×4.6) column. The best separation was achieved by gradient elution with mobile phase of acetonitrile, water (40:60), and 20 mm phosphate buffer with 10% w/v sodium hydroxide (pH 7.5) with a detection wavelength of 215 nm. The separation was completed within 15 min of runtime. The retention time of metronidazole, furazolidone, and dicyclomine hydrochloride was found to be 1.79, 2.45, and 11.50 min, respectively. The proposed method was found to be linear. The method was statistically validated as per the ICH guidelines and shown to be simple, accurate, precise, linear, and reproducible in the range of 40.2–60, 40.2–60.4, and 3–5 µg/mL for metronidazole, furazolidone, and dicyclomine, respectively. For the first time, the developed method foretells the suitability of the method for the simultaneous estimation of three drugs in the commercially available dosage forms.
Keywords: Dicyclomine hydrochloride, furazolidone, metronidazole, RP-HPLC, simultaneous estimation -
Pages 22-28Background
Preeclampsia (PE) is pregnancy disorder that is characterized by hypertension, proteinuria, and an enhanced maternal systemic inflammatory response. PE affects 5% to 10% of all pregnancies and remains a leading factor of fetal and maternal morbidity and mortality. The existence of oxygen deprivation is involved in PE. Inflammation is a requisite to the pathogenesis of PE. Quercitrin belongs to the flavonoid group that is known to have antioxidant and anti-inflammatory activity.
AimsThis study aims at determining the potential of quercitrin to reduce the percentage of apoptosis, levels of lipid peroxidase (MDA), and FGF2 in the human endothelial cell (EA.hy926) line that is induced by hypoxia (2% O2 ) as a PE model.
Materials and MethodsFive treatments were used in this study (negative control, vehicle control, hypoxia control, quercitrin 25 µg/mL, and quercitrin 6.25 µg/mL) to determine the live, necrotic, and apoptotic cells percentage; MDA and FGF2 levels toward hypoxia-induced endothelial cells as a PE model. ELISA method was used to measure the MDA and FGF2 levels. Live, necrotic, and apoptotic cells were measured by using the flow cytometry method.
ResultQuercitrin was capable of decreasing the MDA and FGF2 levels compared with hypoxia control; of increasing live cells percentage; and of decreasing apoptotic and necrotic cells percentage compared with hypoxia control cells.
ConclusionThis study showed that quercitrin possesses antioxidant and anti-inflammatory properties that can decrease the percentage of the apoptotic cells, suppress MDA levels and FGF2 levels, and increase live cells percentage in hypoxia-induced endothelial cells as a PE model.
Keywords: Apoptotic, hypoxia, preeclampsia, quercitrin -
Pages 29-34Context
Ulcerative colitis (UC) is a chronic, idiopathic, and recurrent disease with unknown etiology. Achillea wilhelmsii has been introduced as a herbal remedy for gastrointestinal ulcers and UC in traditional Persian medicine.
AimsWe examined the effectiveness of A. wilhelmsii aqueous extract against acetic-acid-induced UC in rats. Settings and Design: Fifty-six male Wister albino rats weighing 180–200 g were randomly divided into eight groups and after induction of UC were treated with five doses of aqueous extract of A. wilhelmsii.
Materials and MethodsAfter induction of UC by acetic acid, the aerial parts of A. wilhelmsii (6.25, 12.5, 25, 50, and 100mg/kg) were administered orally. On 11th day, the animals were euthanized by overdose of ether inhalation and the intestinal tissue was rapidly dissected for macroscopic, histological, and microscopic scores. Statistical Analysis Used: Data were analyzed by stats Directver.2.7.9 (SAS, Cary, North Carolina). One-way analysis of variance (ANOVA) followed by Newman–Keul’s post hoc test for multiple comparisons. A value of P < 0.05 was considered as significant level. Results were expressed as mean ± standard error of the mean (SEM).
ResultsAll doses of A. wilhelmsii extract significantly reduced macroscopic and microscopic scores of colitis without significant changes in bodyweight of animals.
ConclusionsTreatment of the rats with A. wilhelmsii extract improved UC via its anti-inflammatory, antioxidant, and antimicrobial activities. According to the results of this study, A. wilhelmsii has a therapeutic effect against acetic-acid-induced UC in the animal model.
Keywords: Achillea wilhelmsii C. Koch, antioxidant, herbal remedy, inflammation, ulcerative colitis -
Pages 35-41
Solubility is an important physicochemical factor for any drug molecule that affects its absorption along with its therapeutic effectiveness. Drug absorption is predominantly dependent upon its prompt dissolution. In the case of poorly water-soluble drugs, dissolution is the rate-limiting step in the process of drug absorption. Microspheres were prepared by solvent evaporation method using polymers namely Eudragit L100 and Eudragit RL100. Direct compression technique was used for the preparation of tablets. Tablets were prepared with MCC and PVP K-30 as polymers using an 8mm punch on a rotary press machine with a constant force. Microspheres and the prepared tablets were evaluated using various evaluation tests. The prepared microspheres showed >80% entrapment efficiency and percent yield. Batch F3 exhibited the highest drug release up to 98.30%. Fourier transform infrared (FT-IR) studies revealed no drug–polymer interaction. The results of SEM exhibited that the microspheres are spherical in shape with an average size 5µm. The result of all batches was within an acceptable limit. F2 batch tablet showed a higher drug release of 98.30% as compared with other batches. It was concluded that microcrystalline cellulose or PVP K-30, when used separately, caused retardation in drug release, whereas when used in combination (1:1) it achieved drug release in a controlled manner.
Keywords: Direct compression, microspheres, solvent evaporation, tablet -
Development and Evaluation of Injectable Hydrogel as a Controlled Drug Delivery System for MetforminPages 42-52Aim
Chitosan-dialdehyde cellulose/DAC-based injectable hydrogel for controlled release of Metformin.
Materials and MethodsBiomaterial-based injectable hydrogel was prepared by incorporating chitosan and dialdehyde cellulose. Dialdehyde cellulose (A cross-linker) was prepared by periodate oxidation method. The antidiabetic agent metformin was easily mixed with the chitosan and dialdehyde cellulose cross-linked solution, for the controlled drug delivery applications. The prepared injectable hydrogel showed the shear thinning property.
ResultsIR spectra confirmed the presence of cross-linked network between chitosan and dialdehyde cellulose. The physical appearance, injectability, pH, sol–gel phase transition, drug content, DSC, FTIR, and SEM studies were investigated. DSC and SEM studies revealed the degradation pattern and the topographical nature of prepared injectable hydrogel, respectively. The %drug release of metformin was found to be 87.25% prolonged for 84h. The drug release pattern revealed the effective controlled drug delivery of metformin as compared to marketed tablet formulation.
ConclusionThe study suggested that the controlled drug delivery system can be incorporated into the injectable hydrogel system; it would be more potential as compared to conventional controlled drug delivery system and preformed hydrogel system.
Keywords: Controlled drug delivery, FTIR, injectable hydrogel, metformin, shear-thinning property -
Pages 53-59
A simple free labeled electrochemical immunosensor based on chitosan (CHI) and quantum dots (QDs) was developed for the determination of procalcitonin (ProCT) antigen (Ag) which can act as a target biomarker of infectious diseases. The antibodies of the ProCT biomarker were successfully incubated on the CHI-QDs platform. Electrochemical impedance spectroscopy and cyclic voltammetry were used for the evaluation and characterization of various layers coated onto the electrode. Under the optimum conditions, the electron transfer resistance (Rct) of the immunosensor was altered linearly by the ProCT concentration. The proposed immunosensor was proportional to the ProCT biomarker concentration from 0.005 to 0.35ng/mL with a calculated detection limit of 0.015 pg/mL. The proposed biosensing device also exhibited high stability and reproducibility, which can be used for the quantitative assay of the ProCT biomarker in clinic analyses.
Keywords: Carbon paste electrode, Chitosan, electrochemical impedance spectroscopy, immunosensor, quantum dots -
Pages 60-65Background
The anti-inflammatory effect of memantine (MEM) was investigated using carrageenaninduced hind paw edema model in rats.
Materials and MethodsThirty male Wistar rats were randomly assigned to five groups (n = 6). Group 1 received 0.1mL of 1% carrageenan at the right hind paw. Group 2 received dexamethasone (10mg/kg) and Groups 3, 4, and 5 received 5, 10, and 20mg/kg MEM intraperitoneally (ip), 20min after injection of carrageenan into the right hind paw, respectively. Animals’ paw thickness was measured at 0, 1, 2, 3, 4, and 5 h after carrageenan injection. Then, animals were euthanized and myeloperoxidase (MPO) and malondialdehyde (MDA) levels were measured in the paw tissues. The tissue samples were further examined histopathologically using light microscopy. One-way ANOVA and Tukey post hoc test was used to compare the mean values between the groups.
ResultsTreating with MEM at all doses significantly decreased hind paw thickness at 2 (P < 0.05 and P < 0.01 at MEM 10mg/kg and MEM 5 and 20mg/kg, respectively), 3 (P < 0.001), and 4 (P < 0.001 at 5mg/kg and P < 0.01 at MEM 10 and 20mg/kg) hours after carrageenan injection in comparison to the carrageenan group. There was a significant (P < 0.05 and P < 0.001, respectively) reduction in MPO activity and MDA levels in MEM-treated groups when compared with the carrageenan group.
ConclusionThis study showed that MEM decreased paw edema, leukocyte infiltration, MPO activity, and MDA levels, and MEM can be considered as an effective anti-inflammatory agent.
Keywords: Carrageenan, inflammation, lipid peroxidation, memantine, myeloperoxidase -
Pages 66-70Background
Helicobacter pylori is a major cause of peptic ulcer. On the other hand, cumin (Cuminum cyminum L.) is an effective medicinal plant for the treatment of gastrointestinal disease in traditional Persian medicine. This study aimed at investigating the synergistic effect of the decoction of cumin with the three- and four-drug protocols against H. pylori in patients with peptic ulcer. Patients with peptic ulcer infected with H. pylori were treated with cumin decoction, three- and four-drug protocols, and their co-administration to eradicate H. pylori.
Materials and MethodsPatients were randomly divided into five groups, including group (1) omeprazole with cumin decoction, (2) cumin decoction with the threeprotocol treatment, (3) cumin decoction with the four-drug protocol treatment, and (4 and 5) three- and four-drug protocols alone. The cumin fruit powder was given to patients in 3-g packages and decoction was prepared according to the traditional Iranian medicine guidelines. H. pylori eradication was measured by the 14C–urea breath test (14C-UBT) after 4 weeks of intervention. The Kolmogorov–Smirnov test, χ2 test, logistic regression, and ANOVA (SPSS, 11.5) were used for data analyses.
ResultsIn total, 75 patients (48 male and 27 female patients) participated in this study. The results showed that eradication of H. pylori was observed in all five study groups. Eradication of H. pylori in cumin decoction with the three-drug protocol group was more than the other groups (85.72%), although this difference was not statistically significant. In addition, this eradication was 61.5% in the cumin + omeprazole group, while the H. pylori eradication rates for the three-drug and four-drug protocols were 77.8% and 58.33%, respectively.
ConclusionsThe results showed that decoction of cumin could be used as a complementary treatment alongside conventional medicine therapy to increase the H. pylori eradication.
Keywords: Cuminum cyminum L, four-drug treatment protocol, Helicobacter pylori eradication, pepticulcer, three-drug treatment protocol -
Pages 71-76Background
Epithelialization is an indicator of wound healing. Platelet-rich plasma (PRP) may accelerate the epithelialization of the wound due to high amount of growth factors. Generally, allogeneic PRP provides a smaller immunological effect than autologous PRP. By a freeze-drying method, it is assumed that allogeneic PRP has lower allergenic activity. Aims and
ObjectivesThe aim of this study was to investigate the effect of allogeneic freeze-dried PRP on wound healing of a full-thickness wound in New Zealand rabbits. About 2 × 2 cm2 full-thickness wounds were created on rabbits using a template on both sides of the dorsum and divided into treatment group and control group. The treatment group was treated with allogeneic freeze-dried PRP and the control group was treated with moist dressing. Acceleration of wound healing was shown by the epithelialization and measured on day 7 using digital Visitrak. Nine New Zealand rabbits were used in this study.
ResultsIn the treatment group, the epithelialization was significantly higher 3.00 ± 0.96 cm2 than the control group 1.35 ± 0.85 cm2 (P < 0.000) by independent t test. Another finding of our study was the allergic reaction was not observed after the administration of allogeneic freeze-dried PRP in rabbits.
ConclusionOur results indicate that allogeneic freeze-dried PRP accelerates epithelialization compared to the control group and does not cause an allergic reaction in full-thickness wounds in rabbits. The effect of allogeneic PRP, prepared with a freeze-drying method, on the process of wound healing is reported for the first time in this article.
Keywords: Allogeneic, epithelialization, freeze-dried PRP, full-thickness wound -
Pages 77-86Introduction
Biopharmaceutics classification system class II drugs show unpredictable bioavailability based on their solubility. Unfortunately, very few products were manufactured by this technique owing to their poor flowability and stability. The objective of the current investigation was used to improve the flowability by surface solid dispersion (SSD; SD with surface adsorption technology) and improve the absorption of racecadotril (RT) under low pH conditions (i.e., in stomach) to show anti-diarrheal effect by reducing water and electrolyte secretion into the intestine.
Materials and MethodsSSDs and physical mixtures (PMs) were prepared using various ratios of hydrophilic carriers (polyethylene glycol 4000, polyethylene glycol 6000, and Gelucire 50/13) and an adsorbent (lactose monohydrate). Fourier-transform infrared spectroscopy, differential scanning calorimetry, X-ray diffractometry , and dissolution studies (in vitro) were conducted to characterize SSDs and PMs.
ResultsPhase solubility curves represent AL type, indicating that the solubility of drug linearly increased with an increase in the concentration of carrier. Characterization studies indicated that no interactions between carrier and drug. Solid-state characterization showed a reduction in crystallinity that further supports increment in solubility and dissolution. The optimized formulation (SDG4) showed 99.84 ± 1.5% drug release in 15min compared to RT plain drug (11.95 ± 1.72%). In vivo bioavailability studies of SDG4 revealed a significant (P < 0.05) increase in Cmax 65.38 ± 1.34 µg/mL (1.75-fold) with increased relative bioavailability (180.22-fold) against the RT plain drug.
ConclusionFormulation of SD with surface adsorption method could enhance solubility, dissolution, and bioavailability of RT.
Keywords: Bioavailability, flowability, gelucire, solubility, surface solid dispersion -
Pages 87-92
The antioxidant capacity of Artocarpus altilis leaf extract may offer protection against stress oxidativeinduced damage to pancreatic cells. This study aimed to examine the effect of Artocarpus leaf extract on pancreatic islets structure, blood glucose (BG), and insulin serum levels in alloxan-induced diabetic rats. Diabetes mellitus was induced in rats with an intraperitoneal injection of alloxan (155mg/kg). Rats’ BG levels were measured daily. Only rats with BG >250mg/dL (n = 25) proceeded to receive different treatments: placebo, Artocarpus leaf extract at the dose of 100, 200, or 400mg/kg, or insulin 6 IU/200g. All treatments were administered daily for 14 days before blood and pancreatic tissue samples were collected. Five healthy rats (n = 5) were included to serve as normal controls. The result shows that alloxan-induced atrophy of pancreatic islets and Artocarpus leaf extract administration at all given doses reduced the severity of pancreatic islet’s atrophy. However, only at 400mg/kg dose, Artocarpus leaf extract significantly reduced rats’ BG level (P < 0.05), similar to that of insulin-treated rats. Artocarpus leaf extract, especially at 100 and 400mg/kg doses, also improved insulin serum levels compared with placebo treatment (P < 0.05). In conclusion, Artocarpus leaf extract protected rats’ pancreatic islets against alloxan-induced damage. This protection could improve the BG and insulin serum levels in Artocarpus-treated rats.
Keywords: Alloxan, Artocarpus altilis, blood glucose, insulin, pancreatic islets -
Pages 93-100
Due to the rapid development of antibiotic resistance, the strong need for alternative strategies to tackle this problem is inevitable. The objective of this study was to prepare and evaluate the antibacterial effects of a pharmaceutical gel containing herbal extracts including Lawsonia inermis (henna) and Matricaria chamomilla. Using hydroxypropyl methylcellulose (HPMC), carboxymethylcellulose (CMC), and propylene glycol (PEG), the pharmaceutical gel was formulated and the physical properties of the formulation were specified at 37 ± 2°C. The total phenolic content (TPC) of extracts was determined using the Folin–Ciocalteu method and expressed as mg gallaic acid (GA) per gram extract (Ex). The release of the polyphenol compounds from the optimum formulation was investigated using the Franz cell device. Eventually, the disc diffusion method was used to evaluate the antibacterial activity of optimum formulation against the two pathogenic bacteria strains Staphylococcus aureus and Pseudomonas aeruginosa. The results showed that the optimum formulation was stable at least for 3 months. The TPC of the aqueous extract of henna leaves, the hydroalcoholic extract of chamomile flowers, and the optimum formulation was 57.8, 181.08, and 202.75 mg GA/g Ex, respectively. Nearly 80% of the phenolic compounds in the optimum formulation were released over 4 h. The phenolic compounds have inhibitory effects on the growth of S. aureus and P. aeruginosa. On the basis of this finding, the formulation had excellent stability, viscosity, homogeneity, extrudability, and antibacterial activity which can be employed as a topical pharmaceutical gel in cutaneous burn infection treatment.
Keywords: Antibacterial gel, burn infections, Lawsonia inermis, Matricaria chamomilla -
Pages 101-109Introduction
Herbal medicines play a significant role in global health-care systems. In this investigation, a polyherbal syrup has been reformulated pursuant to Iranian traditional medicine and its antidepressant effect has been evaluated.
Materials and MethodsThe syrup was prepared by decocting a mixture containing: Lavandula angustifolia, Melissa officinalis, Echium amoenum, Cordia myxa, Glycyrrhiza glabra, Ziziphus jujuba, Foeniculum vulgare, Fumaria parviflora, Adiantum capillus-veneris, and Alhagi spp. along with glycerin and potassium sorbate. Physicochemical characteristics of the syrup were examined. An accelerated stability test was carried out for syrup as well. Moreover, antidepressant evaluations were performed by the forced swimming test using the drug as gavage (3.3mL/kg/day) for three consecutive weeks. The serum levels of serotonin (5-HT), noradrenaline (NA), and brain-derived neurotropic factor (BDNF) were determined in rats as well. Finally histopathological examinations were done on liver, kidney and spleen.
ResultsThe herbal syrup was brown in color with a special taste and flavor. Density, pH, viscosity, dry residue, and total phenolics content were 1.085g/ml, 5.56, 5.35 cP, 15.22%, and 194mg/100mL, respectively. The syrup was stable during accelerated stability tests, and no significant changes were observed. The polyherbal syrup exhibited significant antidepressant effects by decreasing immobility time through increasing in NA and 5-HT levels without affecting BDNF levels. Formulated syrup also did not have any toxic effects on the liver, kidney, and spleen.
ConclusionThe syrup could be an appropriate candidate for pharmaceutical companies after complementary tests such as toxicity and clinical trials.
Keywords: Depression, forced swimming test, Iranian traditional medicine, syrup -
Pages 110-117Introduction
Chemotherapy-induced adverse drug reactions (ADRs) are one of the major consequences of cancer therapy that affects patients’ quality of life, outcomes of the treatment, morbidity, and mortality and increases the economic burden. The study’s objective was to evaluate the incidence, causality, severity, and preventability and to calculate the direct medical cost of chemotherapy-induced ADRs among cancer patients.
Materials and MethodsA prospective observational study was conducted for 8 months in patients above 18 years and receiving chemotherapy. ADRs were evaluated for their causality, severity, and preventability using different ADR assessment scales, and the economic burden for different ADRs was based on their direct medical costs.
ResultsA total number of 230 patients were enrolled in the study, out of which 84 patients developed 148 ADRs. Patients who received chemotherapy showed a higher incidence of ADRs in 45–55 years of age group (30.95%), females (69.04%), solid tumors (92.85%), stage III (55.95%), and double regimen (61.90%). Paclitaxel and carboplatin were reported to cause most ADRs, such as anemia (14.18%) and leucopenia (6.75%). ADRs were assessed using scales. As per the WHO-UMC scale, 59.4% ADRs were possible, followed by probable (39.2%). The majority of the ADRs were mild (52%) in severity. About 41.9% reactions were probably preventable, and 3.4% were definitely preventable.
ConclusionThe overall incidence of ADRs was 36.52%. The direct medical cost incurred for the management of ADRs was 457.23 USD.
Keywords: Causality, costs, incidence, preventability, severity -
Pages 118-123Background
Paroxetine has been a commonly prescribed antidepressant for treatment of major depression and various anxiety disorders for almost 30 years due to its fewer side effects and toxicity compared with its counterparts. Despite several investigations performed, the paroxetine immunoregulatory effect in healthy subjects is still controversial. In this study, the paroxetine effect on the cell proliferation along with IL-4 and interferon-gamma (IFN-γ) secretion in peripheral blood mononuclear cells (PBMCs) of physically and mentally healthy subjects is investigated.
Materials and MethodsBlood was drawn from 20 healthy subjects and PBMCs were isolated. Cells were treated with paroxetine and/or phytohemagglutinin (PHA) for 72 h. IL-4 and IFN-γ concentrations were assessed in the supernatant using an enzyme-linked immunosorbent assay. The BrdU cell proliferation assay was also performed to evaluate the paroxetine effect on PBMCs in the absence or presence of PHA.
ResultsParoxetine (25 μM) significantly inhibited the production of IL-4 and IFN-γ in PHA-stimulated human PBMC cultures. Surprisingly, paroxetine suppressed cell proliferation in the unstimulated culture in a dose-independent manner. Paroxetine also attenuated cell proliferation in the PHA-stimulated culture, especially at 25 μM concentration.
ConclusionThe obtained results suggest that paroxetine can be a potent therapeutic option in inflammatory diseases by balancing immune responses.
Keywords: Cell proliferation, IFN-γ, IL-4, paroxetine, PBMC -
Pages 124-129Objective
Interferon-alpha (IFNa) is a cytokine with various biological roles but it may induce psychological adverse effects. Introducing alternative medicine is essential to prevent this side effect. This study was performed to determine the antidepressant effects of creatine (Crt) and α-lipoic acid (ALA).
Materials and MethodsFemale albino mice (6–8 weeks old) were used. IFNa (16×105 IU/kg/day, SC), Crt (5 and 10 mg/kg, gavage feeding tube), and ALA (20 and 40 mg/kg, IP) were administered for 6 days. After the locomotor test, behavioral parameters of depression, including immobility during the forced swimming test (FST), and finally serum malondialdehyde (MDA) were measured as factors for oxidative stress.
ResultsThere was not important difference regarding the locomotor test. Crt 5 mg/kg and ALA 40 mg/kg when administered alone reduced the immobility time during FST when compared with the control groups (75±15 and 82±16 s, respectively, P < 0.05). Crt 5 mg/kg and IFN co-administration reduced the immobility time to 108±23 s, which was lower than that of the IFNa alone group (156±8 s, P < 0.05). Administrating ALA 40 mg/kg and IFNa together showed same results (95±11 s vs. IFNa alone group, P < 0.01). The results of measuring MDA did not show noticeable difference.
ConclusionIn general, improvement of behavioral parameters in mice treated with Crt and ALA indicates a clear effect of these two compounds in modulating mood and depressive behaviors. Although MDA level differences were not observed, Crt and ALA modulation in the neurotransmitter system may be involved in their antidepressant effects.
Keywords: Alpha lipoic acid, creatine, depression, interferon alpha, malondialdehyde -
Pages 130-136Context
People all over the world are suffering from cancer. Liver cancer is considered the second most common malignancy among Egyptian men and the sixth most common malignancy among Egyptian women. Plant-derived antioxidants are believed to prevent or delay the occurrence of many chronic diseases such as cancer. Ailanthus altissima has been used in many traditional prescriptions.
AimsThe current study aimed at investigating the phytochemical profile of A. altissima leaves’ extract and its derived fractions, determining their content of phenolics and flavonoids as well as assessing their antioxidant and cytotoxic potential.
Materials and MethodsThe phytochemical screening was carried out using standard methods. The total phenolic, flavonoid, and flavonol contents were determined using Folin-Ciocalteu, aluminum chloride, and aluminum chloride/ sodium acetate assays, respectively. The antioxidant activity was evaluated using different in vitro
methodsDPPH• , total antioxidant capacity, hydroxyl (• OH), nitric oxide (NO• ) radical scavenging activities, and permanganate-reducing antioxidant capacity (PRAC). The antiproliferative potential against HepG2 cells was evaluated using sulforhodamine-B assay (SRB).
ResultsThe results showed that the ethyl acetate fraction had the highest content of phenolics, flavonoids, and flavonols (551.72 ± 1.81mg GAE/g ext., 371.24 ± 4.36mg RE/g ext., and 100.47 ± 1.30mg QE/g ext., respectively). It also had the most potent reducing power (DPPH• SC50 = 7.19 ± 0.05 µg/mL, TAC= 369.88 ± 1.51mg AAE/g ext., • OH SA = 95.46 ± 0.14%, NO• SA = 40.65 ± 0.91%, and PRAC = 77.19 ± 0.27%). The n-butanol fraction exhibited the most potent cytotoxic potential against HepG2 cells (IC50 = 16.70 µg/mL).
ConclusionA. altissima leaves could be considered potent antioxidant and cytotoxic alternatives.
Keywords: Ailanthus altissima, antioxidant activity, cytotoxic activity, phytochemical screening, totalflavonols, total phenolics -
Pages 137-147
One of the most important parameters in pharmacy is drug solubility. Solubility affects the efficacy of a drug. Drug solubility has an important role in determining the concentration of a drug to achieve the necessary pharmacological response, as all drugs absorbed by the body must be in the form of a solution. Drug solubility is quite a common issue and affects the bioavailability of a drug in the body. Drugs with low solubility are poorly absorbed, resulting in poor bioavailability. Many methods have been developed for increasing the solubility of a drug. In this review, we will describe possible efforts for improving the solubility of a drug, e.g., reducing particle size, surfactants, the use of nanosuspension technology, solid dispersion, salt formation, pH adjustment, hydrotropy, cocrystal, amorphous compound formation, and inclusion complexes. The main objective of this review was to focus on efforts that can increase the solubility of a drug to obtain good drug efficacy.
Keywords: Poor soluble drug, solubility, solubility enhancement method -
Pages 148-152Background
A literature survey showed that significant work has been done to evaluate antimicrobial activity of medicinal plants and their constituents. Thousands of phytoconstituents are tested against a wide range of microbial strains in vitro, in vivo, and clinically. Black cumin oil obtained from the seeds of Nigella sativa L. is used as carminative, stimulant, diuretic, emmenagogue, lactagogue, and anthelmintic. Seed oil is applied externally on skin as antiseptic, emollient, and to prevent cold symptoms. Many studies have displayed the antimicrobial activity of black seed oil against a variety of microorganisms including Gram-positive and Gram-negative bacteria. In the present study, a comparative antibacterial activity of black cumin oil of Saudi Arabian, Syrian seeds, and marketed/branded oil was undertaken.
Materials and MethodsBlack cumin oil (12%) is obtained from Saudi and Syrian originated seeds by the soxhlet extraction method. Agar disc diffusion method was applied for antibacterial activity of each oil and two marketed oils. Antibacterial activity of different black cumin oil samples has been evaluated against standard Escherichia coli, standard Klebsiella pneumonia, and standard Staphylococcus aureus. Phytochemical screening is also done to check the presence of phytoconstituents, which might be responsible for the activity.
ResultsAll black cumin oil samples are found to be sensitive to S. aureus only. Black cumin of Saudi originated seeds showed higher activity than Syrian. Seeds oil of Syria had almost similar activity to one of the marketed oils (M1). Another marketed black cumin oil (M2) showed highest antibacterial activity among all types of oils. Phytochemical screening of these oils showed the presence of steroids and alkaloids, which might be responsible for the activity. Several factors that affect the phytochemical variations are environmental, geographical, agricultural, and extraction conditions, which result in differences in their antibacterial activity.
ConclusionThe results of this study showed that all samples of black cumin oils have antibacterial activity against S. aureus (Gram-positive bacteria). Therefore, they might be considered as possible alternatives to antibiotics for the treatment of S. aureus infections.
Keywords: Agar disc diffusion method, antibacterial activity, black cumin (Nigella sativa) seed oil, photochemical screening