Advanced Pharmaceutical Bulletin
Volume:2 Issue: 1, Jun 2012

Toxoplasma gondii is a widespread protozoan parasite that infects a broad range of warm blooded animals as well as humans. The present study was investigated to evaluate the effects of allium cepa on renal failur in male rats which experimentally infected by Toxoplasma gondii, RH strain. Wistar male rat (n=40) were allocated into four groups, group one that received tachyzoites of T. gondii (ip) (n=10), group two that received tachyzoites of T. gondii (ip), plus fresh onion juice by gavages method (n=10), group three received just fresh onion juice by gavages method (n=10) and control group (n=10) that received nothing. Animals were kept in standard condition. In 30 day after inducing Toxoplasma infection, 5cc blood was collected for serum protein and TAC levels. Kidney tissues of Rat in whole groups were removed and prepared for apopetosis analysis. Serum protein and kidneys weights were significantly decreased in groups that were infected with T. gondii, in comparison to control and onions groups. Kidneys Apopetosis in toxoplasma group significantly increased in comparison to control group (P<0.05).level of TAC was significantly increased in groups that received onio juice (P<0.05). This study showed that T. gondii have significantly effect on serum protein and TAC, apopetosis and fresh onion juice returned and treated this harmful effect, so it is suggested that eating of onion is useful in toxoplasma infection.

Non-viral vectors have been widely proposed as safer alternatives to viral vectors, and cationic polymers have gained increasing attention because they can form self-assembly with DNA. Chitosan is also considered to be a good candidate for gene delivery systems, since it is already known as a biocompatible, biodegradable, and low toxic material with high cationic potential. However, low solubility and transfection efficiency need to be overcome prior to clinical trial. In this work, we focus on alkyl modified chitosan which might be useful in DNA condensing and efficient gene delivery. N, N- Diethyl N- Methyl (DEMC) and N- Triethyl Chitosan (TEC) were synthesized from chitosan polymer. In order to optimize the polymers for gene delivery, we used FITC-dextran (FD). Then the optimized polymer concentrations were used for gene delivery. Fluorescent microscope was used, in order to evaluate the polymers’ efficiency for gene delivery to human embryonic kidney epithelial cells (HEK 293T). This modification increased chitosan’s positive charge, thus these chitosan derivatives spontaneously formed complexes with FD, green fluorescence protein plasmid DNA (pEGFP), red fluorescence protein plasmid DNA (pJred) and fluorescent labeled miRNA. Results gained from fluorescent microscope showed that TEC and DEMC were able to transfer FD, DNA and miRNA (micro RNA) to HEK cell line. We conclude that these chitosan derivatives present suitable characteristics to be used as non-viral gene delivery vectors to epithelial cells.

Azithromycin (AZI) is a new macrolide antibiotic with a better activity against intracellular gram negative bacteria in comparison with Erythromycin. The purpose of this research was to prepare AZI nanoparticles (NPs) using PLGA polymer and to compare the effectiveness of prepared nanoparticles with untreated AZI solution. AZI NPs were prepared by Modified Quasi-Emulsion Solvent Diffusion method. The antibacterial activities of prepared NPs in comparison with AZI solution were assayed against indicator bacteria of Escherichia coli (PTCC 1330), Haemophilus influenzae (PTCC 1623) and Streptococcus pneumoniae (PTCC 1240) using agar well diffusion. Inhibition zone diameters (IZD) of nano-formulation were compared to the corresponding untreated AZI. Mean Inhibitory Concentration (MIC) values of AZI were also determined using serial dilution method in nutrient broth medium. Mean IZD of nano-formulations for all indicator bacteria were significantly higher than that of untreated AZI (P<0.01). The enhanced antibacterial efficacy was more dominant in the gram positive species. The MIC values of NPs against the tested bacteria were reduced 8 times in comparison to those of untreated AZI. These results indicated an improved potency of AZI NPs which could be attributed to the modified surface characteristics as well as increased drug adsorption and uptake.

Agglomeration in suspension is a size enlargement method that facilitates operation of solid processing and preserves the solubilization properties of fine particles. A small quantity of binder liquid is added into a suspension of microparticles, directly in the stirred vessel where the precipitation or crystallization took place. This study deals with the evaluation of the effect of agitation time before and after addition of binder liquid on agglomerates properties in order to give some insights into the mechanism of the formation of the agglomerates. Carbamazepine is used as a model drug and isopropyl acetate is used as binder liquid. The agglomerates characterization includes the particle size, morphology and density. The results showed that, by increasing the agitation time before addition of binder liquid, smaller agglomerates with less density and irregular forms composed of larger crystals were obtained. However, with increasing agitation time after addition of binder liquid the agglomerates size and density increases and morphology improves. Indeed, by continuing agitation along the course of agglomeration the properties of the particles change gradually but substantially. With optimized agitation time before and after addition of binder liquid, spherical and dense agglomerates can be obtained

We report here the antimycobacterial activity of some already synthesized tetrazole derivatives containing tetrazole against Mycobacterium tuberculosis strain H37Rv. In vitro evaluation of the antitubercular activity was carried out within the Tuberculosis Antimicrobial Acquisition & Coordinating Facility (TAACF) screening program for the discovery of novel drugs for the treatment of tuberculosis. Under the direction of the US National Institute of Allergy and Infectious Diseases (NIAID), Southern Research Institute that coordinates the overall program. The method of TAACF was followed for evaluation of activity. This new structural class of compounds showed high activity against the bacilli. The activity depends on the substituent’s present in azatidinone core. Compounds having a 4-MeOC6H4 4-N(CH3)2C6H4 group as the substituent on β-lactam ring were active. The highest activity was registered for compounds having 4-MeOC6H4 as substituent. The new compounds showed high potency and promising antitubercular activity and should be regarded as new hits for further development as a novel class of Antimycobacterium tuberculosis agents.

The purpose of this paper is to enhance the solubility of clarithromycin (CLR) using nonionic surfactants and some type of acids for preparation of the new formulations. Myrj 52 and chremophor (2.5 and 5% w/v) were used in two concentrations. To investigate solubility, the formulations were shaken for 48 hours at room temperature. For stability test, lyophilized samples were maintained in refrigerator at 4° C, and in oven at 40° C. Drug analysis was performed by reverse phase high performance liquid chromatography (HPLC) with ultraviolet detection. Solubility tests indicated that lactobionic acid was the most effective to increase clarithromycin solubility and chremophor showed higher enhancing effect than myrj 52 on CLR solubility. The stability tests results also confirmed that shelf-lives of all formulations have been the equivalent to 24 months. On the whole, formulations described in this article may be very suitable for industrial-scale manufacturing and clinical application.

The purpose of this work was to preparation of vancomycin (VCM) biodegradable nanoparticles to improve the intestinal permeability, using water-in-oil-in-water (W/O/W) multiple emulsion method. The vancomycin-loaded nanoparticles were created using double-emulsion solvent evaporation method. Using Eudragit RS100 as a coating material. The prepared nanoparticles were identifyed for their micromeritic and crystallographic properties, drug loading, particle size, drug release, Zeta potential, effective permeability (Peff) and oral fractional absorption. Intestinal permeability of VCM nanoparticles was figured out, in different concentrations using SPIP technique in rats. Particle sizes were between 362 and 499 nm for different compositions of VCM-RS-100 nanoparticles. Entrapment efficiency expansed between 63%-94.76%. The highest entrapment efficiency 94.76% was obtained when the ratio of drug to polymer was 1:3. The in vitro release studies were accomplished in pH 7.4. The results showed that physicochemical properties were impressed by drug to polymer ratio. The FT-IR, XRPD and DSC results ruled out any chemical interaction betweenthe drug and RS-100. Effective intestinal permeability values of VCM nanoparticles in concentrations of 200, 300 and 400 µg/ml were higher than that of solutions at the same concentrations. Oral fractional absorption was achieved between 0.419-0.767. Our findings suggest that RS-100 nanoparticles could provide a delivery system for VCM, with enhanced intestinal permeability.

The aim of present study was to investigate the effect of chemical agents on the clinical isolates in Madani Heart Hospital, Tabriz, Iran. The minimum bactericide concentration (MBC) of disinfectants including chlorhexidine (Fort), peracetic acid (Micro) and an alcohol based compound (Deconex) on selected bacteria at various dilutions were determined by the standard suspension technique. MBC of Micro, Fort and Deconex were 2-128 mg/L, 2-64 mg/L and 4 - 32 mg/L, respectively. The Gram negative bacteria were more resistance to disinfectant relation to Gram positive bacteria. The results showed that these agents are able to eradicate the bacteria and they can be used lonely.

The aim of this investigation was to study the factors responsible for drug addiction amongst the inmates of Tabriz and Qom prisons, to further understand the reasons for drug abuse particularly in the young and find improved methods for combating these widespread problems. A multi-choice questionnaire was provided to inmates to potentially assess the reasons for their drug addiction psychiatric, personal, social, economical, and political factors were thought to be implicated. Two hundred drug addicted prisoners were individually interviewed randomly in both Tabriz and Qom prisons. A questionnaire including questions about the inmates’ demographic characteristics and 49 multiple answers questions, was provided to identify the effects of different reasons for drug addiction for instance: psychiatric, personal, social, economical, and political factors. The collected data were analyzed by Student t-test and chi-squared test using SPSS software. The results showed that the following factors could lead to drug addiction e.g. company with addicted friends and offenders, curiosity, imitation, illiteracy, family problems, crowded family, poverty, unemployment, and lack of self confidence. There were significant differences between Tabriz and Qom prisoners in relation to age, starting age of addiction, job, income, education, class of addiction, marital status, and hobbies. Mean age, mean starting age of addiction, poverty, alcohol drinking before addiction, marital status, heroin addiction, codeine and benzodiazepines abuse were significantly greater for Tabriz prisoners than those of Qom. It is clear that the governmental programs for reducing unemployment, creation of safe hobbies, proper control on drug dispensing in the pharmacies, proper birth control programs, and encouragement to higher education could alleviate addiction problem in Iran.

This article describes preparation and characterization of beads of alginate containing probiotic bacteria of Lactobacillus acidophilus DMSZ20079. Fourteen formulations using different alginate (ALG) and CaCl2 concentrations as well as hardening times were prepared using extrusion technique. The prepared beads were characterized in terms of size, morphology, encapsulation efficiency and bacterial viabilities in acid (pH 1.8, 2 hours) condition. The results showed that spherical beads with narrow size distribution ranging from 1.32±0.04 to 1.70±0.07 mm were achieved with encapsulation efficiency higher than 98%. Surface response analysis revealed that alginate concentration was the important factor for the size, shape and encapsulation efficiency of prepared beads. Furthermore, survived bacteria after acid exposure in all prepared beads (63-83%) were significantly higher than those of untreated cells (39%) and enhanced by increasing alginate concentration. Surface response analysis revealed that the effect of all three factors of alginate and CaCl2 concentrations as well as hardening times were significant in acid viability, however alginate concentration played the most important role according to its regression coefficient. Among alginate and CaCl2 concentrations as well as hardening times, alginate concentration was the most variable in the characteristics of Alginate beads.

Induction of oxidative stress by Organophosphate compounds (OPs) has been previously reported. In the present work, the mechanism of protective effects of N-acetylcysteine as a glutathion (GSH) prodrug against malathion–induced cell toxicity was investigated. In this work, freshly isolated rat hepatocytes were used to determine the effect of NAC on malathion-induced cytotoxicity, formation of reactive oxygen species (ROS) and mitochondrial dysfunction. Rat hepatocytes were isolated using collagenase perfusion and then cell viability, mitchondrial membrane potential (MMP) and ROS formation were determined using trypan blue exclusion, Rhodamine 123 fluorescence and fluorogenic probe, 2', 7' -dichlorofluorescin diacetate (DCFH-DA), respectively. Despite the protective effect of NAC on malathion-induced cell toxicity and MMP dysfunction, its efficacy against ROS formation was not adequate to completely protect the cells. Cytotoxic effects of malathion regardless of its cholinergic feature, is started with gradual free radical production but, the main factor that causes cell death, is mitochondrial dysfunction, so that reduction of ROS formation alone is not sufficient for cell survival, and the maintenance of mitochondrial integrity through different mechanisms is the most ameliorative factor specially at high levels of cell damage, as NAC seemed to protect cells with various fashions apart from ROS scavenging in concentrations higher than malathion’s LC50.

This research paper presents antioxidant and antimicrobial activities of Pedicularis sibthorpii and Pedicularis wilhelmsiana which grow in Azerbaijan/Iran with claimed a lot of therapeutic effects. DPPH assay and agar well diffusion method were carried out to determine antioxidant and antimicrobial activities respectively. Methanolic extract showed better antioxidant activity compared to other crude extracts (n-hexane and dichloromethane). Methanolic extracts of both Pedicularis sibthorpii and Pedicularis wilhelmsiana were found to have antibacterial activity especially against gram positive strains of S. ureus, S.epidermidis. No antifungal activity was observed in the tested extracts. Existence of some phenolic compounds in methanolic extracts, such as phenylethanoids and flavonoids (found in other species of Pedicularis), which cause both antioxidant and antibacterial activities, is probable. Antimicrobial and antioxidant activity of the methanolic extracts supports further studies related to phytochemical investigation and bioassay of different fractions to isolate pure compounds of plants.

Celecoxib is nonsteroiddal anti-inflammatory drug that has been used extensively to treat patients with arthritis. The aim of the present study was to formulate and characterize liposomal vesicles loaded with celecoxib. Liposomes were prepared by thin film method using soya lecithin and cholesterol. The release of drug was determined using a dialysis membrane method. Liposomes were characterized by Differential Scanning Calorimetery (DSC), Transmission Electron Microscopy (TEM) and their particle size was also determined. The results showed that the drug encapsulation efficiency was 67.34% and there was 67.16% release after 0.5, 1, 2, 3, 4, 5, 6, 7, 8 and 24 h. Results of particle size determination showed a mean size of 677nm and nanoparticles were spherical as shown by TEM. The DSC curve of lecithin, cholesterol and celecoxib were different from celecoxib containing liposome. The results of characterization of the vesicles indicated the potential application of celecoxib loaded liposome as carrier system.

The leaves of Gynura procumbens (Lour.) Merr. has been traditionally used as anticancer. Ethanolic extract of G. procumbens leaves (EGP) showed cytotoxic activity and anticancer activity in animal cancer model. This study was conducted to observe antiproliferative effect using male rat's liver cells induced by 7,12-dimethylbenz(a)antracene (DMBA). Forty days old Sprague Dawley male rats were divided into 4 groups, (1) 0.5 % CMC Na, (2) 20 mg/kg BW DMBA p.o ten times in three weeks, (3) DMBA+300 mg/kg BW of EGP, and (4) DMBA+750 mg/kg BW of EGP. The extract was dissolved into 0.5 % CMC-and administered daily per oral one week before, during and terminated 1 week after the DMBA induction. After sixthteen week experiment, rat livers were sectioned and stained with Haematoxyllene and Eosin (H&E) and AgNOR. Histopatology profile showed no primary liver tumor on DMBA group. mAgNOR value of DMBA+300 mg/kg BW EGP showed significant antiproliferative effect compared to DMBA group. Ethanolic extract of G. procumbens leaves showed antiproliferative activity on male rats liver induced by DMBA.

The paper tried to systematically investigate the in vitro antioxidant activity of Rhizoma Cibotii (RC) for the first time. The methanol extract from RC (MERC) was prepared then systematically investigated by various antioxidant assays, including: DPPH• (1, 1-diphenyl-2-picrylhydrazyl radical), ABTS•+ (3-ethylbenzthiazoline-6- sulfonic acid diammonium salt radical), •O2- (superoxide anion radical), •OH (hydroxyl radical) scavenging assays, Fe3+ reducing power, Cu2+ reducing power assays, compared with positive controls Trolox (± -6 -hydroxyl -2,5, 7, 8-tetramethlychromane-2-carboxylic acid) and BHA (butylated hydroxyanisole). Its total phenolics and caffeic acid content were also measured by Folin-Ciocalteu method and HPLC, respectively. MERC exhibited effective antioxidant activity in dose-dependent manners and its IC50 values were calculated as 44.2 ± 0.62, 19.84 ± 0.31, 137.66 ± 2.90, 22.94 ± 0.90, 289.73 ± 46.17, 53.52 ± 1.51 µg /mL，for DPPH•, ABTS•+, •O2-, •OH scavenging assays, Fe3+ reducing power, Cu2+ reducing power assays, respectively. Its total phenolics content was 50.88 ± 1.24 mg CAE /g and the caffeic acid content was 1.82 ± 0.19 mg/g. Rhizoma Cibotii has effective in vitro antioxidant activity which may attribute to its total phenolics, among which caffeic acid can be considered as one of the active components. The pharmacological effects or healthcare functions of whole RC may result from the synergistic effects caused by the combination of its components and its antioxidant effect plays an important role in the synergistic effects.

Lamivudine is cytosine and zidovudine is cytidine and is used as an antiretroviral agents. Both drugs are available in tablet dosage forms with a dose of 150 mg for LAM and 300 mg ZID respectively. The method employed is based on first order derivative spectroscopy. Wavelengths 279 nm and 300 nm were selected for the estimation of the Lamovudine and Zidovudine respectively by taking the first order derivative spectra. The conc. of both drugs was determined by proposed method. The results of analysis have been validated statistically and by recovery studies as per ICH guidelines. Both the drugs obey Beer’s law in the concentration range 10-50 μg mL-1,for LAM and ZID; with regression 0.9998 and 0.9999, intercept – 0.0677 and – 0.0043 and slope 0.0457 and 0.0391 for LAM and ZID, respectively.The accuracy and reproducibility results are close to 100% with 2% RSD. A simple, accurate, precise, sensitive and economical procedures for simultaneous estimation of Lamovudine and Zidovudine in tablet dosage form have been developed.

An improved and economical method has been described for the synthesis of erlotinib hydrochloride, as a useful drug in treatment of non-small-cell lung cancer. Erlotinib hydrochloride was synthesized in seven steps starting from 3, 4-dihydroxy benzoic acid. In this study, we were able to modify one of the key steps which involved the reduction of the 6-nitrobenzoic acid derivative to 6-aminobenzoic acid derivative. An inexpensive reagent such as ammonium formate was used as an in situ hydrogen donor in the presence of palladium/charcoal (Pd/C) instead of hydrogen gas at high pressure. This proposed method proceeded with 92% yield at room temperature. Synthesis of erlotinib was completed in 7 steps with overall yield of 44%. From the results obtained it can be concluded that the modified method eliminated the potential danger associated with the use of hydrogen gas in the presence of flammable catalysts. It should be mentioned that the catalyst was recovered after the reaction and could be used again.

Aflatoxins (AFs) are a group of mycotoxins and secondary metabolites of various species of Aspergillus. There are various forms of aflatoxins including B1, B2, G1, G2, M1 and M2 types. Aflatoxins cause important health problems and have high potential effect on liver cancer. Therefore, numerous investigations have been conducted during last three decades. The aim of this work is to determine the contamination levels of nuts used by the confectionaries in Tabriz. A total of 142 samples including 35 almond, 26 walnut, 4 seeds of apricot, 6 sunflower seeds kernel, 6 sesame seed, 6 peanuts, 32 pistachio,13 hazelnuts and 14 cashews samples were collected from Tabriz confectionaries. The ELISA method was employed for the screening of total aflatoxins. In 13 cases (28.1% of pistachios, 5.1% of walnuts and 7.1% of cashews) contamination rate of higher than 15 ppb were observed. The HPLC method was applied for the confirmation of ELISA results. Aflatoxin B1 was the highest detected AFs. The overall results of the tested samples indicated that the rate of contamination of pistachios is higher than the other tested samples.

Several evidences show that serotonergic neurons play a role in the regulation of movements executed by the basal ganglia. Recently we have reported that single dose of buspirone improved 6-hydroxydopamine (6-OHDA) and haloperidol-induced catalepsy. This study is aimed to investigate effect of chronic intraperitoneal (i.p.) administration of buspirone on 6-OHDA-induced catalepsy in male Wistar rats. Catalepsy was induced by unilateral infusion of 6-OHDA (8 μg/2 μl/rat) into the central region of the SNc and was assayed by the bar-test method 5, 60, 120 and 180 min after drugs administration in 10th day. The effect of buspirone (0.5, 1 and 2 mg/kg, i.p. for 10 days) was assessed in 6-OHDA-lesioned rats. The results showed that chronic injection of buspirone (0.5, 1 and 2 mg/kg, i.p. for 10 days) decreased catalepsy when compared with the control group. The best anticataleptic effect was observed at the dose of 1 mg/kg. The catalepsy-improving effect of buspirone was reversed by 1-(2-methoxyphenyl)- 4-[4-(2-phthalimido) butyl]piperazine hydrobromide (NAN-190), 0.5 mg/kg, i.p.,as a 5-HT1A receptor antagonist. Our study indicates that chronic administration of buspirone improves catalepsy in a 6-OHDA-induced animal model of parkinson's disease (PD). We also suggest that buspirone may be used as an adjuvant therapy to increase effectiveness of antiparkinsonian drugs. In order to prove this hypothesis, further clinical studies should be done.

Cytotoxic agents are a main part of therapeutic process against the observed tumors, which lead to some unwished damages, due to drug uptake by normal body cells causing various tissue/organ failures associated with formal administration manners. But nowadays the risk is reduced by new target therapy techniques, of which the observed physical nature of micelles and nanosilver particles, governing their special behavior, could help using micelle-coated silver nanoparticles as a novel adjuvant for cancer target therapy.