ISRN Pharmaceutics

Since binding of a drug molecule to human serum albumin (HSA) significantly affects the pharmacokinetics of the drug, it is highly desirable to predict the binding affinity of the drug. Profen drugs are a widely used class of nonsteroidal anti-inflammatory drugs and it has been reported that several members of the profen class specifically bind to one of the main binding sites named site II. The actual binding mode of only ibuprofen has been directly confirmed by X-ray crystallography. Therefore, it is of interest whether other profen drugs are site II binders...

Despite the great efforts in the areas of early diagnosis and treatment of cancer, this disease continues to grow and is still a global killer. Cancer treatment efficiency is relatively high in the early stages of the disease. Therefore, early diagnosis is a key factor in cancer treatment. Among the various diagnostic methods, molecular imaging is one of the fastest and safest ones. Because of its unique characteristics, magnetic resonance imaging has a special position in most researches. To increase the contrast of MR images, many pharmaceuticals have been known and used so far...

The aim of the proposed research work was to develop a novel dual-compartment capsule (NDCC) with polymeric disc for gastroretentive dosage form, which will ultimately result in better solubility and bioavailability of Ofloxacin. Floating ring caps were formulated by using different natural polymers, separating ring band and swellable polymer located at the bottom of capsule. Formulated ring caps were assessed for coating thickness, In vitro buoyancy, In vitro drug release, release kinetics and stability studies...

The aim of this investigation was to develop and optimize bisoprolol fumarate matrix tablets for sustained release application by response surface methodology based on 2(3) factorial design. The effects of the amounts of calcium alginate, HPMC K4M, and Carbopol 943 in bisoprolol fumarate matrix tablets on the properties of bisoprolol fumarate sustained release matrix tablets like drug release and hardness were analyzed and optimized. The observed responses were coincided well with the predicted values by the experimental design...

Niosomes have potential applications in topical drug delivery system. The objective of the study was to formulate and evaluate the niosome of Itraconazole. Surfactant : cholesterol ratio and quantity of ethanol used were studied by applying factorial design. Formulated niosomes were evaluated for vesicle size, entrapment efficiency, drug release, skin permeation, and antimycotic activity. Vesicle size, entrapment efficiency, and drug release were markedly dependent on surfactant : cholesterol ratio and quantity of ethanol used...

Over the last three decades industrial adaptability has allowed hot-melt extrusion (HME) to gain wide acceptance and has already established its place in the broad spectrum of manufacturing operations and pharmaceutical research developments. HME has already been demonstrated as a robust, novel technique to make solid dispersions in order to provide time controlled, modified, extended, and targeted drug delivery resulting in improved bioavailability as well as taste masking of bitter active pharmaceutical ingredients (APIs)...

Traditional antacids and alginate-based reflux suppressants are OTC products commonly used to treat reflux symptoms. There has been a lack of innovation of new formulations in this therapy area despite consumers finding established products unpalatable. Here we evaluate a novel product formulation which takes the form of quick-dissolving alginate granules in single-dose sachets (Gaviscon Direct Powder (GDP)). Market research and taste evaluation confirmed that reflux sufferers considered GDP to have good flavour and taste, no chalky aftertaste and dissolved rapidly in the mouth with 68% noting so within 10 seconds...

The Punica granatum L. var. granatum (pomegranate) has been demonstrated to exert antitumor effects on various types of cancer cells. The present study aimed to evaluate the medicinal herbs Punica granatum L. var. spinosa (apple punice) that are native to Iran. This study was determined to test the possible cytotoxic activity and induction of apoptosis on human prostate cell lines. The effect of ethanol extracts of the herbs on the inhibition of cell proliferation was assessed by MTT colorimetric assay. PC3 cell lines treated with the extracts were analyzed for the induction of apoptosis by cell death detection (ELISA) and TUNEL assay...

The objective of the present study is to explore the efficient chemical penetration enhancer among the various enhancers available in overcoming the stratum corneum barrier in transdermal delivery of Alfuzosin hydrochloride (AH). The different enhancers were incorporated in 2% Carbopol gel which was selected as a control and evaluated by in vitro diffusion studies through dialysis membrane and permeation through the rat abdominal skin using Keshary-Chien diffusion cells. All the enhancers increased the release rate through the dialysis membrane when compared with control except oleic acid which decreased the release rate but showed maximum solubility of the drug...

Pharmacokinetic-pharmacodynamic (PK-PD) modeling has emerged as a major tool in clinical pharmacology to optimize drug use by designing rational dosage forms and dosage regimes. Quantitative representation of the dose-concentration-response relationship should provide information for the prediction of the level of response to a certain level of drug dose. This paper describes the experimental details of the preformulation study, tablet manufacture, optimization, and bioanalytical methods for the estimation of dexibuprofen in human plasma...

Variations in quantity and quality of essential oil (EO) from the aerial parts of cultivated Mentha piperita were determined. The EO of air-dried sample was obtained by a hydrodistillation method and analyzed by a gas chromatography/mass spectrometry (GC/MS). The antifungal activity of the EO was investigated by broth microdilution methods as recommended by Clinical and Laboratory Standards Institute. A biofilm formation inhibition was measured by using an XTT reduction assay. Menthol (53.28%) was the major compound of the EO followed by Menthyl acetate (15...

In this paper, a new formulation of nasal spray was set up based on the extract of lemon pulp, obtained by using a new solid-liquid technology of extraction, added to pure Aloe juice, soluble propoli, and essential oils of Ravensara and Niaouly. It was tested in a clinical study in which 100 subjects were recruited for a period of one month. Nasal scraping was used for collecting samples and after the application of the May-Grünwald Giemsa standard technique, glass slides were analysed by using optical microscope with a 1000x oil immersion...

A sensitive spectrophotometric method for the determination of dopamine was carried out without any separation steps. Bromocresol green is adsorbed on Sephadex LH-20 gel but the sorption decreases in the presence of dopamine due to ion-pair formation between bromocresol green and dopamine in solution. This attenuation was used to the microdetermination of dopamine by measurement of absorbance of the solid phase (Sephadex LH-20 gel) in a 1.0 mm cell at 625 nm. Dopamine could be determined in the concentration range of 0...

Traditional drug delivery systems which are based on multiple dosing regimens usually pose many disadvantages such as poor compliance of patients and drug plasma level variation. To overcome the obstacles of traditional drug formulations, novel drug delivery system PCL-PEG-PCL hydrogels have been purposed in this study. Copolymers were synthesized by rapid microwave-assisted and conventional synthesis methods. Polymer characterizations were done using gel permeation chromatography and (1)H-NMR. Phase transition behavior was evaluated by inverting tube method and in vitro drug release profile was determined using naltrexone hydrochloride and vitamin B(12) as drug models...

The biological activity of essential oil extracted from coriander, Coriandrum sativum L. (Apiaceae), seeds against adults of Tribolium confusum Duval (Coleoptera: Tenebrionidae) and Callosobruchus maculatus F. (Coleoptera: Bruchidae) was investigated in a series of laboratory experiments. Fumigant toxicity was assessed at 27 ± 1°C and 65 ± 5% R.H., in dark condition. Dry seeds of the plant were subject to hydrodistillation using a Clevenger-type apparatus. The composition of essential oil was analyzed by gas chromatography mass spectrometry...

Degradation pathway for eplerenone is established as per ICH recommendations by validated and stability-indicating reverse phase liquid chromatographic method. Eplerenone is subjected to stress conditions of acid, base, oxidation, and thermal and photolysis. Significant degradation is observed in acid and base stress conditions. Four impurities are studied and the major degradant (RRT about 0.31) was identified by LC-MS and spectral analysis. The stress samples are assayed against a qualified reference standard and the mass balance is found close to 99...

The aim of the present work was designed to develop a model-sustained release matrix tablet formulation for Metformin hydrochloride using wet granulation technique. In the present study the formulation design was employed to statistically optimize different parameters of Metformin hydrochloride tablets at different drug-to-polymer ratios employing polymers Hydroxypropyl methylcellulose of two grades K4M and K100M as two independent variables whereas the dependent variables studied were X(60), X(120), T(50), T(90), n, and b values obtained from dissolution kinetics data...

In this study, the role of the immune system in nevirapine- (NVP-) induced subclinical liver injury was investigated by observing for changes of some immune parameters during the initial stages of NVP-induced hepatotoxicity in a rat model. In the acute phase, two test-groups of 10 Sprague-Dawley rats each were administered with bacterial lipopolysaccharide (LPS) or saline (S) intraperitoneally, followed by oral NVP, after which 5 rats from each group were sacrificed at 6 and 24 hours. For the chronic phase, two groups of 15 rats each received daily NVP, and on days 7, 14, and 21, five rats from each group were administered with either LPS or S, followed by that day's NVP dose, and were sacrificed 24 hours later...

Purpose. The objective of the proposed work is to evaluate the efficacy of Pectins to qualify them as polymers for designing an oral microsphere for the delivery of selected oral antidiabetic drug-like metformin hydrochloride. Methods. Different Microspheres formulations were prepared by the water in oil (w\o) emulsion solvent evaporation technique and subsequently evaluated for its different physical parameters as well as its in vitro and in vivo drug release study. Results. The formulations F2 (98.42) and F3 (98...

Lipid-based innovations have achieved new heights during the last few years as an essential component of drug development. The current challenge of drug delivery is liberation of drug agents at the right time in a safe and reproducible manner to a specific target site. A number of novel drug delivery systems has emerged encompassing various routes of administration, to achieve controlled and targeted drug delivery. Microparticulate lipoidal vesicular system represents a unique technology platform suitable for the oral and systemic administration of a wide variety of molecules with important therapeutic biological activities, including drugs, genes, and vaccine antigens...