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Journal of Pharmacy and Pharmacology

Fei Li, Karyn D Howard, Michael J Myers
OBJECTIVES: P-glycoprotein (P-gp) is responsible for the efflux of a broad variety of human and veterinary drugs. Canine P-gp polymorphisms alter drug disposition and toxicity, but their impact on the disposition of enantiomeric drugs is unknown. Using fexofenadine as a model compound, we developed and validated HPLC-fluorescence methods to determine the effect of P-gp on the disposition of fexofenadine and its enantiomers. METHODS: A chiral CD-Ph column was used for the separation of (R) and (S)-fexofenadine...
January 16, 2017: Journal of Pharmacy and Pharmacology
Zahra Hami, Seyed Mahdi Rezayat, Kambiz Gilani, Mohsen Amini, Mahmoud Ghazi-Khansari
OBJECTIVES: The pH-sensitive doxorubicin (DOX)-conjugated and docetaxel (DTX)-conjugated poly(lactic acid)-poly(ethylene glycol)-folate (PLA-PEG-FOL)-based polymeric micelles were developed and characterized in this study. KEY FINDINGS: The drugs were released from the micelles (particle size, ~185 nm) in a pH-dependent manner. The drug-conjugated PLA-PEG-FOL micelles showed higher cellular uptake than nontargeting ones. Single agent and combination in-vitro cytotoxicity studies were also performed using the two drugs in both free and their micellar forms in SKOV3 human ovarian cancer cells using three different cytotoxicity assays...
January 3, 2017: Journal of Pharmacy and Pharmacology
Luiz Eduardo Nunes Ferreira, Bruno Vilela Muniz, Jonny Burga-Sánchez, Maria Cristina Volpato, Eneida de Paula, Edvaldo Antonio Ribeiro Rosa, Francisco Carlos Groppo
OBJECTIVES: Modified drug delivery systems have been developed to improve pharmacological properties of local anaesthetics. However, the inflammatory potential of these formulations was not investigated. This study compared the in-vitro effects of ropivacaine (ropi) in plain, liposomal (MLV) or 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) formulations on cell viability, apoptosis and cytokine (IL-1α, TNF-α, IL-6 and IL-10) release. METHODS: Human immortalized keratinocytes (HaCaT) and human immortalized gingival fibroblasts (HGF) were exposed to 1-100 μm ropi concentrations...
December 29, 2016: Journal of Pharmacy and Pharmacology
Teagan L Brown, Tereen Thomas, Jessica Odgers, Steve Petrovski, Marion Joy Spark, Joseph Tucci
BACKGROUND: Resistance of bacteria to antimicrobial agents is of grave concern. Further research into the development of bacteriophage as therapeutic agents against bacterial infections may help alleviate this problem. OBJECTIVES: To formulate bacteriophage into a range of semisolid and solid dosage forms and investigate the capacity of these preparations to kill bacteria under laboratory conditions. METHODS: Bacteriophage suspensions were incorporated into dosage forms such as creams, ointments, pastes, pessaries and troches...
December 29, 2016: Journal of Pharmacy and Pharmacology
Sara M Hanning, Mine Orlu Gul, Irmgard Toni, Antje Neubert, Catherine Tuleu
OBJECTIVE: To provide an overview of non-parenteral clonidine formulations and assess the feasibility of their use for paediatric sedation. METHODS: A literature search was conducted using electronic databases and a combination of search terms. Forty articles met the inclusion criteria. Publications were grouped into different dosage forms and assessed for their potential application for sedation of children in intensive care. KEY FINDINGS: Several routes of clonidine administration have been investigated for numerous indications in children, including perioperative sedation and analgesia...
December 29, 2016: Journal of Pharmacy and Pharmacology
Sandeep Kumar, Gaurav Bhanjana, Ritesh Kumar Verma, Dinesh Dhingra, Neeraj Dilbaghi, Ki-Hyun Kim
OBJECTIVES: Present modalities for the diagnosis and treatment of diabetes still suffer from certain limitations such as erratic absorption, need of high dose, poor sensitivity or specificity, resistance, substantial morbidity and mortality, long-term complications, and patient-to-patient variability with lifetime treatment. METHODS: This study focused on the development of a water-in-oil-in-water metformin nanoemulsion as an effective method in diabetes treatment...
December 29, 2016: Journal of Pharmacy and Pharmacology
Jianyun Wang, Qianqian Yang, Yaxing Nie, Hao Guo, Fan Zhang, Xueyan Zhou, Xiaoxing Yin
OBJECTIVES: Nitric oxide (NO) plays an important role in the progression of early-stage diabetic nephropathy (DN), which is found to contribute to extracellular matrix (ECM) accumulation in mesangial cells (MCs). As a cofactor for NO production, tetrahydrobiopterin (BH4 ), a folacin analogue, may be responsible for the ECM accumulation and proliferation of MCs. This study was to investigate the effects of BH4 on glomerulosclerosis in early-stage DN. METHODS: In in vitro studies with cultured mesangial cells and in vivo studies with streptozotocin-induced diabetic rats, BH4 levels were assayed by HPLC; NO was determined by Griess agents; laminin and collagen IV were determined by enzyme-linked immunosorbent assay; the inducible NO synthase protein was determined by immunofluorescence staining and Western blot; and mesangial matrix expansion and MC proliferation in the renal cortex were observed by periodic acid-schiff staining and transmission electron microscopy, respectively...
December 29, 2016: Journal of Pharmacy and Pharmacology
Dana Abu-Geras, Dunja Hadziomerovic, Andrew Leau, Ramzan Nazim Khan, Sajni Gudka, Cornelia Locher, Maryam Razaghikashani, Lee Yong Lim
OBJECTIVE: To examine factors that might affect the ability of patients to accurately halve tablets or measure a 5-ml liquid dose. METHODS: Eighty-eight participants split four different placebo tablets by hand and using a tablet splitter, while 85 participants measured 5 ml of water, 0.5% methylcellulose (MC) and 1% MC using a syringe and dosing cup. Accuracy of manipulation was determined by mass measurements. KEY FINDINGS: The general population was less able than pharmacy students to break tablets into equal parts, although age, gender and prior experience were insignificant factors...
December 28, 2016: Journal of Pharmacy and Pharmacology
Sai-Qi Wang, Cong Wang, Jun-Wei Wang, Dong-Xiao Yang, Ran Wang, Chuan-Jin Wang, Hui-Ju Li, Hong-Ge Shi, Yu Ke, Hong-Min Liu
OBJECTIVES: To study the antitumour activity of a novel derivative of oridonin named geridonin in vitro and in vivo. METHODS: MTT and colony formation assay were used to test the cytotoxicity of geridonin; apoptosis, cell cycle arrest and the levels of reactive oxygen species were measured by flow cytometry; JC-1 staining assay was used to examine the mitochondrial membrane potential; the MGC 803 xenograft model was established to evaluate the antitumour effect of geridonin in vivo; H&E staining was performed for the histological analysis...
December 28, 2016: Journal of Pharmacy and Pharmacology
Mohammad Hossein Asghari, Mohammad Abdollahi, Marcos Roberto de Oliveira, Seyed Mohammad Nabavi
OBJECTIVES: Acute poisoning with aluminium phosphide (AlP) is a major cause of mortality in developing countries. AlP mortality is due to cardiac dysfunction leading to cardiomyocyte death. The main mechanism is an inhibition of cytochrome c oxidase in the cardiomyocyte mitochondria, resulting in a decreased ATP production and oxidative stress. Unfortunately, the administration of exogenous drugs does not meet the desired requirements of an effective therapy. Melatonin is an amphiphilic molecule and can easily pass through all cellular compartments with the highest concentration recorded in mitochondria...
December 20, 2016: Journal of Pharmacy and Pharmacology
Magdalena Dzajkowska, Kotlowska Hanna, Madanecka Anna, Szczepanska Maja, Doniza Dagmara, Sosnowicz Anna, Sznitowska Malgorzata
OBJECTIVE: The aim was to develop prolonged-release minitablets (MT) with carbamazepine (CBZ). METHODS: Matrix-type 3-mm MT (5 mg CBZ) were prepared by direct compression using hydrophilic (hypromellose) or hydrophobic polymers (ethylcellulose, Kollidon SR, glyceryl behenate). Coated prolonged-release MT (2.5 mm/3 mg of CBZ) were produced using ethylcellulose or Eudragit RL/RS. The release tests were performed in a basket apparatus with water or 1% sodium lauryl sulphate solution as dissolution media...
December 20, 2016: Journal of Pharmacy and Pharmacology
Tapan Behl, Anita Kotwani
OBJECTIVES: Terminalia catappa has shown potent antidiabetic activity in the past; however, the exact molecular mechanisms by which it acts have not been elucidated. This review aims at exploring several hypotheses which have been proposed to explain its mechanism of action, including reduction in oxidative stress, inflammation, angiogenesis, lipid profile correction and direct hypoglycaemic actions. METHODS: A thorough review of all the articles, research as well as reviews, available regarding the concerned topic was performed...
December 20, 2016: Journal of Pharmacy and Pharmacology
Haixia Zhao, Jing Liu, Laixin Song, Zhencai Liu, Guifang Han, Ding Yuan, Ting Wang, Yaoyan Dun, Zhiyong Zhou, Zhaoqi Liu, Yongjun Wang, Changcheng Zhang
OBJECTIVES: Inflammation can cause degenerative changes of reproductive function. Oleanolic acid (OA), the effective component from Ligustrum lucidum Ait., exhibits significantly anti-inflammation and antiageing activity. However, whether OA restores testicular dysfunction via inhibition of inflammation with ageing is unclear. Here, in a natural ageing rat model, we investigated the protection effects of OA and its mechanism of action. METHODS: Eighteen-month-old Sprague Dawley (SD) rats were randomly divided into ageing control group and two OA-treated groups (5 and 25 mg/kg)...
December 9, 2016: Journal of Pharmacy and Pharmacology
Yuan-Ri Guo, Se-Young Choung
OBJECTIVES: In a previous study, we reported that Aster spathulifolius Maxim extract (ASE) inhibited lipid accumulation and adipocyte differentiation in 3T3-L1 cells. Of the components in ASE, germacrone (GM) was identified as a potent bioactive constituent. GM is known for its anticancer and antiviral activity. However, the effects of GM and the molecular mechanism by which GM regulates adipogenesis and lipolysis were not reported. Therefore, we investigated the effect of GM on adipogenesis and lipolysis and to elucidate its underlying molecular mechanism...
December 5, 2016: Journal of Pharmacy and Pharmacology
Rahila Amber, Muhammad Adnan, Akash Tariq, Sakina Mussarat
OBJECTIVES: Bronchitis is a common respiratory tract infection of humans mainly caused by influenza virus, rhinovirus, adenovirus, coronavirus and respiratory syncytial virus. The aim of this review was to gather fragmented literature on ethnomedicinal plants used against bronchitis in the Himalayan region and their in-vitro validation against bronchitis causing viral pathogens. KEY FINDINGS: Present review contains ethnomedicines of total 55 plants from different countries of the Himalayas...
December 1, 2016: Journal of Pharmacy and Pharmacology
Jiejun Zhu, Shiping Liao, Liming Zhou, Lihong Wan
OBJECTIVES: Tanshinone IIA (Tan IIA) may exert significant protective effects against the neurotoxicity induced by β-amyloid protein (Aβ). This study was designed to investigate the possible neuroprotective mechanism of Tan IIA on Aβ25-35 -induced spatial memory impairment in mice. METHODS: After 3 weeks of preventive treatment (Tan IIA or oil), all male Kunming mice were subjected to Aβ25-35 (10 μl, intracerebroventricularly (i.c.v.)) to establish the spatial memory impairment model...
November 23, 2016: Journal of Pharmacy and Pharmacology
Elsa Lilienberg, Ilse R Dubbelboer, Erik Sjögren, Hans Lennernäs
OBJECTIVES: In liver cancer treatment, lipiodol is used as a pharmaceutical excipient to improve delivery of the cytostatic drug doxorubicin (DOX). As DOX and its metabolite doxorubicinol (DOXol) cause serious off-target adverse effects, we investigated the effects of drug-free lipiodol or ciclosporin (CsA) on the tissue distribution (Kp ) of DOX and DOXol in relevant pig tissues. METHODS: Four treatment groups (TI-TIV) all received an intravenous DOX solution at 0 and 200 min...
November 23, 2016: Journal of Pharmacy and Pharmacology
Aoi Matsushima, Keisuke Oda, Nobuhiro Mori, Teruo Murakami
OBJECTIVES: Evaluation of the function of multidrug resistance-associated proteins (MRPs) expressed in erythrocytes and screening of endogenous MRPs modulator(s) in glycerol-induced acute renal failure (ARF) rats. METHODS: Concentrations of 2,4-dinitrophenyl-S-glutathione (DNP-SG), a substrate for MRPs, in erythrocytes after administration of 1-chloro-2,4-dintrobenzene (CDNB), a precursor of DNP-SG, were determined in control and ARF rats. The screening of endogenous MRPs modulator(s) was performed using washed erythrocytes and inside-out erythrocyte membrane vesicles (IOVs) in vitro...
November 18, 2016: Journal of Pharmacy and Pharmacology
Anjali Joshi, Daniel Gbadero, Fredrick Esseku, Olufikayo J Adesanya, Moji C Adeyeye
OBJECTIVE: The bioequivalence study was conducted to compare the developed paediatric fixed-dose combination (FDC) zidovudine/lamivudine/nevirapine (60/30/50 mg) tablet - the test formulation - with the combined mixture of single-entity innovator products (reference product). METHODS: A single-dose open-label randomized two-way crossover study was conducted in healthy adult African volunteers after an informed consent was obtained. The 24 volunteers, divided into two groups, were administered the products after an overnight fast on two treatment days with 14 days of washout period...
November 18, 2016: Journal of Pharmacy and Pharmacology
Brittney J Mills, Jennifer S Laurence Chadwick
OBJECTIVES: Protein-based therapeutics garner significant attention because of exquisite specificity and limited side effects and are now being used to accomplish targeted delivery of small-molecule drugs. This review identifies and highlights individual chemical attributes and categorizes how site-specific changes affect protein stability based on published high-resolution molecular analyses. KEY FINDINGS: Because it is challenging to determine the mechanisms by which the stability of large, complex molecules is altered and data are sparse, smaller, therapeutic proteins (insulin, erythropoietin, interferons) are examined alongside antibody data...
November 10, 2016: Journal of Pharmacy and Pharmacology
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