Iranian Journal of Pharmaceutical Research

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In Collaboration with School of Pharmacy, SBMU

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The IJ Pharmaceutical Research (IJPR) is a peer-reviewed multi-disciplinary pharmaceutical publication, scheduled to appear annually and serve as a means for scientific information exchange in the international pharmaceutical forum. Specific scientific topics of interest to the journal include but are not limited to: pharmaceutics, industrial pharmacy, pharmacognosy, toxicology, medicinal chemistry, novel analytical methods for drug characterization, computational and modeling approaches to drug design, bio-medical experience, clinical investigation, rational drug prescribing, pharmacoeconomics, biotechnology, nanotechnology, biopharmaceuticals, and physical pharmacy.

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Cost-Utility Analysis of Trastuzumab-Emtansine Versus Trastuzumab for the Treatment of Residual Invasive HER-2-Positive Breast Cancer in Iran
(Brieflands, 2024-12-31) Homa Hemati; Marzieh Nosrati; Meysam Seyedifar
Background: Breast cancer is one of the most common types of cancer in women, and its incidence is increasing in Iran. HER-2-positive breast cancer is invasive and often associated with poorer outcomes. Patients with this type of breast cancer can develop resistance to medications like trastuzumab. Trastuzumab-emtansine (TDM1) is a medication developed to reduce cancer cell resistance to trastuzumab. The TDM1 has been shown to decrease the incidence of death and recurrence in breast cancer. Objectives: This study aimed to evaluate the cost-utility and calculate the budget impact of TDM1 versus trastuzumab for the treatment of residual invasive HER-2-positive breast cancer. Methods: A Markov model with a lifetime horizon was developed, incorporating four health states. Women aged 45 with residual invasive HER-2-positive breast cancer entered the model. The study adopted a healthcare system perspective, with costs reported in 2021 US dollars. Discount rates of 7% for costs and 3% for utility values were applied. Utility values and transition probabilities were derived from published literature. Costs were estimated based on guidelines, expert opinions, and Iranian tariffs. Iran’s pharmacoeconomic threshold of 1085$ was used for comparison. The incremental cost-effectiveness ratio (ICER) and budget impact of TDM1 were calculated, and sensitivity analyses were conducted to assess the robustness of the model. Results: The model indicated that treatment with TDM1 resulted in a 1.59 quality-adjusted life year (QALY) increase, with an additional cost of 1408$. This was deemed cost-effective, considering Iran’s pharmacoeconomic threshold of 1085$ (calculated ICER: 886$ per QALY gained). One-way sensitivity analysis revealed that the model was sensitive to the costs of TDM1 and trastuzumab, the discount rates for utility values and costs, and the probability of achieving invasive disease-free survival (IDFS). Probabilistic sensitivity analysis showed that 59.61% of simulations fell below Iran’s pharmacoeconomic threshold, supporting the model's robustness. The budget impact analysis revealed that the additional budget required for TDM1 treatment over a three-year period was 1,120,546$ compared to trastuzumab. Conclusions: Although TDM1 imposes higher costs, it is more cost-effective than trastuzumab for the treatment of residual invasive HER-2-positive breast cancer in Iran.
Evaluation of Oral Nano-Silymarin Formulation Efficacy in the Prevention of Hand-Foot Syndrome and Neuropathy Induced by XELOX or m-FOLFOX6 Regimens in Metastatic Colorectal Cancer: A Triple-Blinded, Randomized Clinical Trial
(Brieflands, 2024-12-31) Hedyieh Karbasforooshan; Hossein Rahimi; Omid Arasteh; Abolghasem Allahyari; Mehdi Varmaghani; Mahdi Jannati; Vahid Ghavami; Mahmoodreza Jaafari; Sepideh Elyasi
Background: Folinic acid, fluorouracil, and oxaliplatin (FOLFOX) and oxaliplatin and capecitabine (XELOX) are the most widely used chemotherapy regimens for treating metastatic colorectal carcinoma (CRC). These regimens are associated with various adverse reactions, including neuropathy and hand-foot syndrome (HFS). Silymarin, a flavonoid derived from Silybum marianum, has a wide range of biological activities. It has been used to counteract chemotherapy side effects due to its antioxidant, anti-apoptotic, and anti-inflammatory properties. Objectives: The purpose of this study was to assess the preventive effect of nano-silymarin on neuropathy and HFS induced by the FOLFOX6 and XELOX regimens. Methods: A randomized, triple-blinded, placebo-controlled clinical trial was conducted on 60 patients who were randomly assigned to receive 70 mg capsules containing 15% silymarin nano micelles twice a day after meals, starting from the first day of the first chemotherapy course and continuing for six courses of the XELOX or m-FOLFOX6 regimen. The severity of adverse effects was assessed after the third and sixth courses based on the National Cancer Institute Common Terminology Criteria for Adverse Events (NCI-CTCAE) version 5. Results: The median CTCAE scores for HFS and neuropathy were significantly lower in the nano-silymarin group at the end of the third course (P < 0.001). However, the difference remained significant only for HFS at the end of the sixth course (P = 0.022). Additionally, the scores increased significantly in both the placebo and nano-silymarin groups during the therapy (P < 0.05). Conclusions: Nano-silymarin may be considered an adjuvant medication for the prevention of certain chemotherapy-induced adverse reactions. Further research with larger sample sizes and various doses of nano-silymarin is recommended for a more comprehensive evaluation.
The Effect of Intrauterine Administration of Growth Hormone on IVF Success Rate in Recurrent Implantation Failure Women: A Randomized Clinical Trial
(Brieflands, 2024-12-31) Fatemeh Amirkhanloo; Mohammad Javanbakht; Sarah Lotfi; Ghazal Sahraiyan; Razieh Akbari; Elham Feizabad; Shima Rahimi; Mahbod Ebrahimi; Firouzeh Akbari Asbagh; Fateme Davari Tanha
Background: The positive effects of growth hormone (GH) on the endometrium, including increased endometrial blood supply and enhanced expression of cytokines associated with endometrial receptivity, have been noted. However, data on the effect of GH on the endometrium remain limited. Objectives: This study aimed to investigate the effect of intrauterine administration of GH on the IVF success rate in women with recurrent implantation failure (RIF). Methods: This randomized double-blind clinical trial was conducted on 60 infertile women under 40 years old with a Body Mass Index (BMI) below 30 kg/m², all diagnosed with RIF—defined as at least three failed pregnancies after transferring a minimum of four good-quality embryos due to unknown causes. Women with uterine malformations, Asherman syndrome, cavity-distorting lesions, severe endometriosis, or other underlying diseases were excluded. After six days of estrogen therapy, transvaginal ultrasound (TVS) was performed to measure and compare the thickness and quality of the endometrium. Participants were divided into two groups. In the intervention group, 10 units of GH were administered using an IUI catheter positioned one centimeter above the cervical os. Study outcomes included changes in endometrial thickness (ET) and quality, as well as pregnancy rates. Primary endpoints were changes in ET and quality, while secondary endpoints were pregnancy rates. Adverse drug responses were also evaluated. Results: The mean age was 34.96 ± 4.04 years, and the mean BMI was 24.89 ± 2.91 kg/m², with no significant differences in baseline variables between the study groups. The average ET on the 8th day of the cycle was 5.38 ± 0.96 mm in the intervention group and 5.20 ± 0.80 mm in the control group, showing no significant difference (P = 0.467). The ET on the day of initiating progesterone was 7.60 ± 1.03 mm in the intervention group and 7.40 ± 0.60 mm in the control group, with no significant difference (P = 0.264). The odds ratio for achieving a high-quality endometrium was 2.37 (95% CI 0.80 - 6.98, P = 0.116) for the GH group compared to the non-GH group. The odds ratio for achieving a clinical pregnancy was 3.06 (95% CI 0.54 - 17.37, P = 0.205) for the GH group compared to the non-GH group. Two cases of cervicitis were reported in the GH group. Conclusions: Intrauterine administration of GH appears to enhance endometrial receptivity in women with RIF.
Predictive Insights Into Bioactive Compounds from Streptomyces as Inhibitors of SARS-CoV-2 Mutant Strains by Receptor Binding Domain: Molecular Docking and Dynamics Simulation Approaches
(Brieflands, 2024-12-31) Hourieh Kalhor; Mohammad Hossein Mokhtarian; Hamzeh Rahimi; Behzad Shahbazi; Reyhaneh Kalhor; Tahereh Komeili Movahed; Hoda Abolhasani
Background: The receptor-binding domain (RBD) of the spike protein of SARS-CoV-2 interacts with the angiotensin-converting enzyme 2 (ACE2) receptor in humans. To date, numerous SARS-CoV-2 variants, particularly those involving mutations in the RBD, have been identified. These variants exhibit differences in transmission, pathogenicity, diagnostics, and vaccine efficacy. Objectives: Although therapeutic agents are currently available to inhibit SARS-CoV-2, most provide supportive and symptomatic relief. Moreover, different variants may exhibit resistance to these treatments. This study aimed to identify a potential compound with favorable antiviral effects against SARS-CoV-2 variants. Methods: The study explored drug discovery through structure-based virtual screening of natural products (NPs) from the StreptomeDB database, targeting the ACE2-binding pocket of the SARS-CoV-2 RBD protein. The analysis included the wild-type protein (PDB ID: 6VW1) as well as the Alpha, Beta, Delta, Lambda, Omicron/BA.1, and Omicron/BA.2 variants. Results: In silico screening identified ‘Stambomycin B’ as a potential compound with the highest binding affinity. Molecular dynamics simulations of the complexes, conducted over 100 ns, confirmed the prediction that ‘Stambomycin B’ could inhibit different SARS-CoV-2 variants effectively. Conclusions: This study concludes that ‘Stambomycin B’, a macrolide compound produced by Streptomycesambofaciens, may be a candidate NP for effectively combating all mutants that occur in the binding of SARS-CoV-2 RBD to ACE2, even those that may arise in the future.
Dual Modulation of Canonical and Non-canonical TGF-β/ROS/Erk1/2 Pathways: Synergistic Activation of Nrf-2 and Antioxidant Enzymes (SOD1, GPx, HO-1) by Quercetin Loaded in Solid Lipid Nanoparticles and Curcumin in Atherosclerosis Therapy
(Brieflands, 2024-12-31) Masoumeh Shamsi; Ghorban Mohammadzadeh; Mahdi Hatami; Mohammadreza Roshanazadeh; Mojgan Noor-Behbahani; Mojtaba Rashidi
Background: Atherosclerosis remains the leading cause of mortality worldwide, highlighting the urgent need for innovative treatments targeting chronic inflammation. Recent research indicates that quercetin (quercetin) and curcumin, two naturally occurring compounds, have potential therapeutic benefits in cardiovascular diseases. Objectives: This study focuses on the novel synthesis of nano-quercetin (N-QCT) encapsulated in solid lipid nanoparticles (SLNs) and investigates the synergistic cardioprotective effects of N-QCT and curcumin on human vascular smooth muscle cells (VSMCs). The underlying molecular mechanisms, particularly the involvement of the TGF-β signaling pathway in VSMCs, are explored. Methods: The VSMCs, including TGF-β-stimulated VSMCs, were treated with N-QCT, curcumin, or a combination of both. The MTT assay was performed to evaluate the cytotoxic effects of these treatments. The cytotoxicity of various concentrations of curcumin and QCT was used to calculate the Combination Index (CI), with CI analysis quantifying synergy or antagonism. Furthermore, following TGF-β stimulation, antioxidant enzyme activity, nuclear transcription factor erythroid 2-related factor (Nrf2) mRNA expression, reactive oxygen species (ROS) production, NADPH oxidases (NOX) expression, and extracellular signal-regulated kinase (Erk)1/2 phosphorylation were measured in the treated VSMCs. Results: The N-QCT and curcumin significantly influenced Nrf2 mRNA expression and upregulated downstream antioxidant enzymes, including HO-1, GPx, and SOD1. The combination treatment further enhanced Nrf2 protein expression and modulated Erk1/2 phosphorylation. Notably, the synergistic effect of the combination produced pronounced cardioprotective outcomes, characterized by reduced ROS production and decreased phosphorylation of Erk1/2 via the TGF-β/NOX/Erk1/2 and ROS/Nrf2 signaling pathways. Conclusions: The findings demonstrate that the combination of QCT encapsulated in SLNs and curcumin synergistically reduces oxidative stress and inflammation in TGF-β-stimulated VSMCs. This effect is achieved through the inhibition of ROS/Erk1/2 signaling and the activation of Nrf2 and antioxidant enzymes. These natural compounds, when used together, represent a promising therapeutic approach for mitigating the inflammatory processes associated with atherosclerosis.
Pethidine, Maybe a Rearrangement in the Pharmaceutical Group is Needed!
(Brieflands, 2024-12-31) Reza Aminnejad; Ali Solhpour; Sahar Kavousi Sisi
This article does not have an abstract.
Erratum for Ruthenium (II) Complexes Based on Phenanthroline-Tetrazole as Possible Anticancer Agents [Iran J Pharm Res. 2023;22(1): e136738]
(Brieflands, 2024-12-31) Saeid Abaspour; Behzad Soltani; Hamed Hamishehkar; Moayad Hossaini Sadr
This article does not have an abstract.
The Glucagon-Like Peptide-1 (GLP-1) Receptor Agonist Liraglutide Regulates Sirtuin-1-Mediated Neutrophil Extracellular Traps to Improve Diabetes-Induced Bone Metabolism Imbalance
(Brieflands, 2024-12-31) Shuai Zhong; Liangzhi Huang; Tingting Lin; Yanyan Li; Bin Deng; Dezhi Kong; Zhanlin Liao; Zugui Huang
Background: Diabetes mellitus (DM) is a chronic metabolic disorder that disrupts normal bone remodeling. Objectives: This study aimed to investigate how the glucagon-like peptide-1 (GLP-1) receptor agonist liraglutide (LIR) addresses bone metabolism imbalances induced by type-II diabetes. Methods: Type-II diabetic rat models were established through a single intraperitoneal injection of streptozotocin (STZ). Blood glucose levels were measured using a blood glucose meter, and insulin levels were assessed using an assay kit. Bone formation markers [alkaline phosphatase (ALP), osteocalcin (OCN), and procollagen I N-terminal propeptide (PINP)] and bone resorption markers [tartrate-resistant acid phosphatase (TRACP) and CTX-1] were monitored using assay kits. Bone marrow mesenchymal stem cells (BMSCs) were cultured in vitro under high-fat and high-glucose (HFHS) conditions to mimic diabetic bone metabolism dysregulation. Neutrophil extracellular traps (NETs) formation was examined through immunofluorescent staining and Western blot analysis. Results: Liraglutide was found to reduce STZ-induced NETs formation, as indicated by decreased expression of cit-H3 by 36.90% - 53.57%, myeloperoxidase (MPO) by 55.81% - 65.12%, NE by 53.95% - 65.17%, and PAD4 by 46.81% - 63.83%, alongside increased Sirtuin-1 (SIRT1) expression in femur tissue (70.71% - 91.19%). In vitro, LIR enhanced osteogenesis and inhibited apoptosis, effects that were partially reversed by SIRT1 knockdown. Additionally, SIRT1 knockdown partially restored LIR-induced reductions in oxidative stress, inflammation, and NETs formation. Conclusions: LIR mitigates diabetes-induced bone metabolism imbalance by inhibiting NETs formation through SIRT1 mediation.
Expression of Concern for Correlation between Sun Protection Factor and Antioxidant Activity, Phenol and Flavonoid Contents of Some Medicinal Plants [Iran J Pharm Res. 2014;13(3): e125511]
(Brieflands, 2024-12-31) Editor-in-Chief IJPR
This article does not have an abstract.
Excretion of Acebutolol and its Major Metabolite Diacetolol into Infant Blood Circulation and the Breast Milk
(Brieflands, 2003-07-31) S. Abolfazl Mostafavi; Dora A. Stinson; Kent Dooly; Fakhreddin Jamali
Acebutolol (AC) is a chiral β-adrenergic blocking drug, which is useful clinically as the racemate in treating hypertension and is metabolized to an equipotent chiral metabolite, diacetolol (DC). In this paper we report a case of a 32 year old woman who was receiving AC during her pregnancy and lactating time for management of hypertension. The maternal plasma level and breast milk as well as cord blood collected to see whether the drug is transferred to the fetus through the mother stereoselectively. A stereospecific high-performance liquid chromatographic (HPLC) assay was used to measure the enantiomeric concentrations of AC and DC. AC and DC enantiomers are stereoselectively excreted into the milk, although the concentrations of DC enantiomers were higher than those of AC. AC concentrations were very low in both cord artery and vein samples four hours after taking the drug however, the stereoselective concentrations of metabolite, DC, was found in these samples. In conclusion, AC and DC enantiomers are excreted in human breast milk in concentrations much higher than that in maternal plasma. Furthermore, DC was found in the infant's plasma indicating that accumulation of metabolite did occur in this infant.
Quercetine, a Major Flavonol Aglycon from Tanacetum balsamita L.
(Brieflands, 2003-10-31) Bahman Nickavar; Gholamreza Amin; Nacim Mehregan
From the aerial parts of Tanacetum balsamita L. (Compositae) a flavonol aglycon was iso-lated using chromatographic techniques. The structure of this compound was determined usingspectroscopic methods (UV, H-NMR and MS) as 3',4',5,7-Tetrahydroxy flavonol (Quercetin).
Preparation and Characterization of Poly-(methyl ethyl cyanoacrylate) Particles Containing 5-Aminosalicylic acid
(Brieflands, 2005-01-31) Hashem Montaseri; MS Sayyafan; Hosnieh Tajerzadeh
Poly-(alkylcyanoacrylate) ester particles have been used for the preparation of different formulations ranging from ophthalmic delivery systems to cancer chemotherapy carriers in clinic. The aim of this study was to prepare and characterize poly-(methyl ethyl cyanoacrylate) (PMECA) particles containing 5-aminosalicylic acid (5-ASA). PMECA particles were prepared using the inverse emulsification polymerization technique. The effects of various formulation parameters such as dispersed phase volume, polymer to drug weight ratio, and surfactant concentration on loading efficiency and size of the prepared particles were investigated. The amount of drug was determined by UV spectrophotometery at 331 nm. Morphological characteristics of particles and particle size analysis were studied by Scanning Electron Microscopy (SEM) and Laser Light Scattering techniques, respectively. The results showed that there was no linear relationship between the dispersed phase volume (DPV) and loading efficiency of 5-ASA in the range of 20-50%. Increasing polymer/drug weight ratio in the range of 1-15, enhanced the loading efficiency from 11.4 to 78.2% in a linear mode (r=0.987). Increasing the surfactant concentration in the range of 1-3% did not increase the loading efficiency of the prepared particles, and increasing the concentration to 5% even decreased the loading efficiency of particles. Laser light scattering and SEM evaluations showed that in all prepared formulations, particles were in a mixture of micro and nanospheres and micro and nanocapsules and 50 percent of particles had mean sizes in the range of 6.4-10.1 micrometer. Although our results showed significant differences in the mean particle size between some of the prepared formulations, this variation was not practically important. It was concluded that by using proper conditions, it is possible to use PMECA as a polymeric matrix for loading of 5-ASA and the other hydrophilic drugs.
The Pharmacological Effects of Odonthobuthus doriae Scorpion Venom and Its Extracted Fractions on Neuro-Muscular Transmission
(Brieflands, 2006-04-30) Amir Jalali; Zahra Hossininasab; Zynab Ehsani; Amir-Abbas Zare; Afshin Zarghi; Hossein Vatanpour
The effect of Odonthobuthos doriae (O.d) scorpion venom at 0/3, 1 and 3, 10 µg/ml concentrations were investigated on nerve-muscle transmission, using the Twitch tension technique. A concentration of 0.3 µg/ml caused a small change in the twitch height in response to indirect muscle stimulation, but higher concentrations (1, 3, 10 µg/ml) caused a transient augmentation in twitch response followed by a large contracture in the chick biventer cervices (CBC) preparation. This effect could be defined as a complex action of the venom, predominately presynaptic, in which its’ effects on postjunctional synapses is also maintained.
Development and Characterization of Bioadhesive Gel of Microencapsulated Metronidazole for Vaginal Use
(Brieflands, 2010-07-31) Nayak Bhabani Shankar; Rout Prasant Kumar; Nayak Udaya Kumar; Bhowmik Benoy Brata
The present study concerned with the development and characterization of metronidazole microcapsules prepared by thermal change method using different ratios (1:1, 1:2 and 1:4) of ethyl cellulose in order to select the best microcapsule formulation with a good encapsulation efficiency and drug release profile. The obtained microcapsules were discrete, spherical with free flowing properties and evaluated for particle size, shape, flow properties, wall thickness, drug encapsulation efficiency and in vitro release performance. The drug carrier interactions were investigated in solid state by FT-IR spectroscopy and scanning electron microscopy. The microcapsules with a narrow size range of 23-68 μm showed higher encapsulation efficiency. The selected microcapsule formulation, MC3 (Drug polymer ratio 1:4) was employed for gel formulation with a variety of carbopol polymers (carbopol-934, 940, 974 and 980) by mechanical stirring method in order to develop a sustained release microencapsulated metronidazole microcapsules-containing bioadhesive gel. The prepared bioadhesive gels were evaluated for pH, spreadability, extrudability, viscosity, vaginal irritation, in vitro drug release, bioadhesion, accelerated stability and in vitro drug release kinetic. In vitro experiments indicated a sustained release over 24 h and an acceptable bioadhesion quality for formulation F3. Hence, it can be concluded that the formulation F3 has potential to deliver metronidazole in a controlled and constant manner for prolong period over other formulations and can be adopted for a successful delivery of metronidazole for vaginal use.
Gastroprotective Effect of Hydroalcoholic Extract of Aloe buettneri
(Brieflands, 2011-01-31) Kossi Metowogo; Kwashie Eklu-Gadegbeku; Amégnona Agbonon; Kodjo A. Aklikokou; Messanvi Gbeassor
Aloe buettneri A. Berger is commonly used in traditional Togolese medicine to treat inflammatory and gastric ulcers. The present study examined the gastro-protection effect of the hydro-alcoholic extract of A. buettneri on mucus production and gastric pH. A gastric ulcer is induced by ethanol 95° alone (1 mL/kg body weight), after pre-treatment with indomethacin (300 mg/kg) or by utilising L-NAME (40 mg/kg IV). In addition gastric mucus was removed by scraping and subsequently weighed. The experiment focused entirely on rats that had been subjected to fasting. The hydro-alcoholic extract of A. buettneri (500 mg/kg) significantly inhibited ulcers that were induced by ethanol, indomethacin or L-NAME pre-treatment. A. buettneri was shown to increase the production of gastric mucus. Furthermore L-arginine significantly decreased the size of the induced ulcers. The results achieved in the study carried out suggest that A. buettneri posses gastro-protective properties.
Cytotoxic Effect of Some 1, 4-Dihydropyridine Derivatives Containing Nitroimidazole Moiety
(Brieflands, 2011-07-31) Ramin Miri; Katayoun Javidnia; Zahra Amirghofran; Seyyed Hossein Salimi; Zahra Sabetghadam; Savis Meili; Ahmad Reza Mehdipour
The 1,4-dihydropyridine (DHP) derivatives are a known class of calcium channel blockers. Some derivatives of DHP showed significant cytotoxicity. It was shown that this effect may not be the result of interaction with Ca2+ channels. In this study, we performed an investigation about the intrinsic cytotoxicity of some derivatives of DHP containing nitroimidazole moiety on their C4 position on four different cancer cell lines (Raji, K562, Fen and HeLa). The result showed that these compounds had moderate-good cytotoxic activity. In addition, QSAR model shows the importance of N atom in cytotoxicity; Ca2+ channels.
The Effects of Berberis vulgaris Fruit Extract on Serum Lipoproteins, apoB, apoA-I, Homocysteine, Glycemic Control and Total Antioxidant Capacity in Type 2 Diabetic Patients
(Brieflands, 2012-04-30) Farzad Shidfar; Shima Seyyed Ebrahimi; Sharieh Hosseini; Iraj Heydari; Shahrzad Shidfar; Giti Hajhassani
Type 2 diabetes is a well-known endocrine and metabolic disorder which has reached epidemic proportions worldwide and represents a serious public health concern. Hyperglycemia and dyslipidemia are two major abnormalities which are major cardiovascular risk factors. Berberine is a major alkaloid in Berberis vulgaris fruit extract (BVFE) which have important role in regulation of serum glucose and fat metabolism in-vivo and in-vitro but its role in type 2 diabetes have not been extensively examined.
^99mtc-Ubiquicidin [29–41], a Promising Radiopharmaceutical to Differentiate Orthopedic Implant Infections from Sterile Inflammation
(Brieflands, 2013-04-30) Davood Beiki; Gholamali Yousefi; Babak Fallahi; Mohammad Naghi Tahmasebi; Ali Gholamrezanezhad; Armaghan Fard-Esfahani; Mostafa Erfani; Mohammad Eftekhari
Ubiquicidin (UBI) [29-41] is a synthetic cationic antimicrobial peptide that preferentially binds to bacterial cell membrane at the site of infection. We aimed to assess diagnostic value of 99mTc-UBI [29-41] as a radiopharmaceutical in differentiation of bacterial infection from sterile inflammation in suspected orthopedic implants. Nine patients suspected for orthopedic implant infection, all males with the mean age of 41.6 ± 20.9 years, were studied. A dose of 10 MBq/Kg (range : 555-740 MBq) 99mTc-UBI [29-41] was injected intravenously. A dynamic study followed by static whole body imaging at 30, 60 and 120 min post-radiotracer injection was acquired. Periprosthetic tissue culture was considered the closest test to a gold standard for diagnosing infections and scintigraphic scans were categorized as true- or false-positive and true- or false-negative, considering the bacterial culture as the gold standard. No adverse reaction was observed during or after the radiotracer injection days. There were five true positive, four true negative and no false positive and false negative scans. Sensitivity, specificity, positive predictive value (PPV) and negative predictive value (NPV) were all calculated as 100%. We found a high diagnostic accuracy for 99mTc-UBI [29-41] scintigraphy in differentiation of bacterial infection from sterile inflammation in suspected orthopedic implants. Therefore, 99mTc-UBI [29-41] scintigraphy might be potentially recommended as a safe and promising imaging modality in these settings. However, further studies on a larger number of patients and different pathologies are still needed.
Synergistic Effect and Mechanism of Cineole and Terpineol on In-vitro Transdermal Delivery of Huperzine A from Microemulsions
(Brieflands, 2013-04-30) Jun Shi; Wen-Juan Cong; Yi-Ming Wang; Qing-Fei Liu; Guo-An Luo
The aim of the present study was to investigate the influence and the mechanisms of cineole and terpineol on the in-vitro transdermal delivery of huperzine A from microemulsions, and their potential synergistic effect on the permeation enhancement. The transdermal delivery of huperzine A from microemulsions with different concentrations of cineole and terpineol through the rat abdominal skin was determined by Franz-type diffusion cells. The partition coefficient of huperzine A between the full thickness skin and microemulsion was determined. Attenuated total reflection-Fourier transform infrared spectroscopy (ATR-FTIR) was carried out to analyze the effects of cineole and terpineol on the biophysical properties of the stratum corneum (SC) and the mechanisms of permeation enhancement. These results indicated that cineole and terpineol could synergistically increase the transdermal delivery of huperzine A from microemulsions through increasing the partition and diffusion coefficients of huperzine A. ATR-FTIR studies further validated the synergistic effect and revealed that the enhancing mechanisms were due to increasing the disorderliness and fluidity of SC lipid alkyl chains, disrupting the structure of keratin in SC, and extracting SC lipids. In conclusion, cineole and terpineol, acting synergistically to enhance the transdermal delivery of huperzine A from microemulsions, might provide an alternative permeation enhancer combination for the transdermal delivery of huperzine A.
Isolation, Purification, Characterization and Effect upon HepG2 Cells of Anemaran from Rhizome Anemarrhena
(Brieflands, 2013-10-31) Qian-Qian Jiang; Yun-Ping Zhao; Wen-Yuan Gao; Xia Li; Lu-Qi Huang; Pei-Gen Xiao
The rhizome of Anemarrhena asphodeloides is used as food and traditional Chinese medicine for its hypoglycemic effect. The aim of this study was to investigate the isolation, purification and hypoglycemic activity of Anemaran as the active component. The influence factors (isolation duration, ratio of residuals to water and extracting times) during the isolation process were evaluated. The optimal conditions for NA and AA were extraction temperature 90ºC and 100ºC, duration 1h and 1.5 h, extraction time 3 and 3, and the solid–liquor ratio 1:20 and 1:15, respectively. Neutral and acid Anemaran (NA and AA) were isolated from the rhizome of Anemarrhena asphodeloides. Five fractions of NA-1, NA-2, NA-3, AA-1 and AA-2 were obtained after crude neutral and acid Anemaran purified through DEAE- 52 cellulose anion-exchange column. The characterizations of Anemaran and its different fractions were both analyzed by Fourier transform infrared spectroscopy (FT-IR) and scanning electron micrographs (SEM). Structural properties of different fractions were examined by FT-IR. Strong characteristic absorption peaks were observed at around 1744 cm−1and 1650 cm−1 caused by the C=O group of uronic acids, and the band between 1440 cm−1 and 1395 cm−1 associated with the stretching vibration of C–O of galacturonic acid. Neither the crude neutral, nor the acid anemaran significantly inhibited the growth of HepG2 cells in-vitro, which indicated the low cytotoxicity of the anemaran. Furthermore, both neutral and acid anemaran showed hypoglycemic effect. The hypoglycemic effect of neutral anemaran was much higher than that of acid anemaran.

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