ISRN Pharmaceutics The latest articles from Hindawi Publishing Corporation © 2014 , Hindawi Publishing Corporation . All rights reserved. Formulation Development and Optimization of Fast Dissolving Tablets of Aceclofenac Using Natural Superdisintegrant Thu, 08 May 2014 16:09:01 +0000 The current research work involves preparation of fast dissolving tablets of Aceclofenac by direct compression method using different concentrations of Lepidium sativum mucilage as natural superdisintegrant. A two-factor three-level (32) factorial design is being used to optimize the formulation. Nine formulation batches (D1–D9) were prepared accordingly. Two factors as independent variables (-amount of -cyclodextrin and -amount of Lepidium sativum mucilage) were taken with three levels . The levels of two factors were selected on the basis of preliminary experiments conducted and their effect on three dependent variables (disintegration time, wetting time, and in vitro drug release) was studied along with their % prediction error. All the active blends were evaluated for postcompression parameters (angle of repose, Carr’s index, Hausner ratio, etc.) and the tablets were evaluated for postcompression parameters (weight variation, hardness, and friability, wetting time, disintegration time, water absorption ratio, and in vitro drug release studies). The optimum batch was further used for SEM and stability studies. Formulation D5 was selected by the Design-Expert software which exhibited DT (15.5 sec), WT (18.94 sec), and in vitro drug release (100%) within 15 minutes. Lovleen Kaur, Rajni Bala, Neha Kanojia, Manju Nagpal, and Gitika Arora Dhingra Copyright © 2014 Lovleen Kaur et al. All rights reserved. Alginate Particles as Platform for Drug Delivery by the Oral Route: State-of-the-Art Wed, 09 Apr 2014 07:33:15 +0000 Pharmaceutical research and development aims to design products with ensured safety, quality, and efficacy to treat disease. To make the process more rational, coherent, efficient, and cost-effective, the field of Pharmaceutical Materials Science has emerged as the systematic study of the physicochemical properties and behavior of materials of pharmaceutical interest in relation to product performance. The oral route is the most patient preferred for drug administration. The presence of a mucus layer that covers the entire gastrointestinal tract has been exploited to expand the use of the oral route by developing a mucoadhesive drug delivery system that showed a prolonged residence time. Alginic acid and sodium and potassium alginates have emerged as one of the most extensively explored mucoadhesive biomaterials owing to very good cytocompatibility and biocompatibility, biodegradation, sol-gel transition properties, and chemical versatility that make possible further modifications to tailor their properties. The present review overviews the most relevant applications of alginate microparticles and nanoparticles for drug administration by the oral route and discusses the perspectives of this biomaterial in the future. Alejandro Sosnik Copyright © 2014 Alejandro Sosnik. All rights reserved. High-Amylose Sodium Carboxymethyl Starch Matrices: Development and Characterization of Tramadol Hydrochloride Sustained-Release Tablets for Oral Administration Tue, 08 Apr 2014 08:31:22 +0000 Substituted amylose (SA) polymers were produced from high-amylose corn starch by etherification of its hydroxyl groups with chloroacetate. Amorphous high-amylose sodium carboxymethyl starch (HASCA), the resulting SA polymer, was spray-dried to obtain an excipient (SD HASCA) with optimal binding and sustained-release (SR) properties. Tablets containing different percentages of SD HASCA and tramadol hydrochloride were produced by direct compression and evaluated for dissolution. Once-daily and twice-daily SD HASCA tablets containing two common dosages of tramadol hydrochloride (100 mg and 200 mg), a freely water-soluble drug, were successfully developed. These SR formulations presented high crushing forces, which facilitate further tablet processing and handling. When exposed to both a pH gradient simulating the pH variations through the gastrointestinal tract and a 40% ethanol medium, a very rigid gel formed progressively at the surface of the tablets providing controlled drug-release properties. These properties indicated that SD HASCA was a promising and robust excipient for oral, sustained drug-release, which may possibly minimize the likelihood of dose dumping and consequent adverse effects, even in the case of coadministration with alcohol. Teresa Nabais and Grégoire Leclair Copyright © 2014 Teresa Nabais and Grégoire Leclair. All rights reserved. Manilkara zapota (Linn.) Seeds: A Potential Source of Natural Gum Tue, 04 Mar 2014 06:49:05 +0000 Mucilage isolated from seeds of Manilkara zapota (Linn.) P. Royen syn. is a plant growing naturally in the forests of India. This mucilage is yet to be commercially exploited, and characterized as polymer. Various physicochemical methods like particle size analysis, scanning electron microscopy, thermal analysis, gel permeation chromatography, X-ray diffraction spectrometry, zeta potential, Fourier transform infrared spectroscopy, and nuclear magnetic resonance spectroscopy have been employed to characterize this gum in the present study. Particle size analyses suggest that mucilage has particle size in nanometer. Scanning electron microscopy analysis suggests that the mucilage has irregular particle size. The glass transition temperature of the gum was observed to be 138°C and 136°C by differential scanning calorimetry and differential thermal analysis, respectively. The thermogravimetric analysis suggested that mucilage had good thermal stability. The average molecular weight of mucilage was determined to be 379180, by gel permeation chromatography, while the viscosity of mucilage was observed to be 219.1 cP. The X-ray diffraction spectrometry pattern of the mucilage indicates a completely amorphous structure. Elemental analysis of the gum revealed the contents of carbon, hydrogen, nitrogen, and sulfur to be 80.9 (%), 10.1 (%), 1.58 (%), and 512 (mg/kg), respectively. Mucilage had specific content of calcium, magnesium, potassium, lower concentrations of aluminum, cadmium, cobalt, lead, and nickel. The major functional groups identified from FT-IR spectrum include 3441 cm−1 (–OH), 1660 cm−1 (Alkenyl C–H & C=C Stretch), 1632 cm−1 (–COO–), 1414 cm−1 (–COO–), and 1219 cm−1 (–CH3CO). Analysis of mucilage by paper chromatography and 1D NMR, indicated the presence of rhamnose, xylose, arabinose, mannose, and fructose. Sudarshan Singh and Sunil B. Bothara Copyright © 2014 Sudarshan Singh and Sunil B. Bothara. All rights reserved. Transdermal Nitroglycerin Delivery Using Acrylic Matrices: Design, Formulation, and In Vitro Characterization Mon, 06 Jan 2014 14:44:34 +0000 Nitroglycerin (TNG) transdermal drug delivery systems (TDDSs) with different acrylic pressure-sensitive adhesives (PSAs) and chemical permeation enhancers (CPEs) were prepared. The effects of PSAs and CPEs types and concentrations on skin permeation and in vitro drug release from devices were evaluated using the dissolution method as well as the modified-jacketed Franz diffusion cells fitted with excised rat abdominal skin. It was demonstrated that the permeation rate or steady state flux () of the drug through the excised rat skin was dependent on the viscosity and type of acrylic PSA as well as the type of CPE. Among different acrylic PSAs, Duro-Tak 2516 and Duro-Tak 2054 showed the highest and Duro-Tak 2051 showed the lowest . Among the various CPEs, propylene glycol and cetyl alcohol showed the highest and the lowest enhancement of the skin permeation of TNG, respectively. The adhesion properties of devices such as 180° peel strength and probe tack values were obtained. It was shown that increasing the concentration of CPE led to reduction in the adhesion property of PSA. Moreover, after optimization of the formulation, it was found that the use of 10% PG as a CPE and 25% nitroglycerin loading in Duro-Tak 2054 is an effective monolithic DIAP for the development of a transdermal therapeutic system for nitroglycerin. Houman Savoji, Amir Mehdizadeh, and Ahmad Ramazani Saadat Abadi Copyright © 2014 Houman Savoji et al. All rights reserved. Formulation Strategies to Improve the Bioavailability of Poorly Absorbed Drugs with Special Emphasis on Self-Emulsifying Systems Thu, 26 Dec 2013 14:12:26 +0000 Poorly water-soluble drug candidates are becoming more prevalent. It has been estimated that approximately 60–70% of the drug molecules are insufficiently soluble in aqueous media and/or have very low permeability to allow for their adequate and reproducible absorption from the gastrointestinal tract (GIT) following oral administration. Formulation scientists have to adopt various strategies to enhance their absorption. Lipidic formulations are found to be a promising approach to combat the challenges. In this review article, potential advantages and drawbacks of various conventional techniques and the newer approaches specifically the self-emulsifying systems are discussed. Various components of the self-emulsifying systems and their selection criteria are critically reviewed. The attempts of various scientists to transform the liquid self-emulsifying drug delivery systems (SEDDS) to solid-SEDDS by adsorption, spray drying, lyophilization, melt granulation, extrusion, and so forth to formulate various dosage forms like self emulsifying capsules, tablets, controlled release pellets, beads, microspheres, nanoparticles, suppositories, implants, and so forth have also been included. Formulation of SEDDS is a potential strategy to deliver new drug molecules with enhanced bioavailability mostly exhibiting poor aqueous solubility. The self-emulsifying system offers various advantages over other drug delivery systems having potential to solve various problems associated with drugs of all the classes of biopharmaceutical classification system (BCS). Shweta Gupta, Rajesh Kesarla, and Abdelwahab Omri Copyright © 2013 Shweta Gupta et al. All rights reserved. Design and Characterization of Double Layered Mucoadhesive System Containing Bisphosphonate Derivative Thu, 19 Dec 2013 18:01:22 +0000 The objective of this study is to evaluate the effect of formulation variables on different evaluation properties such as cumulative percentage release and swelling index in development of two layered buccal mucoadhesive system consisting of a highly water soluble drug risedronate sodium. The mucoadhesive systems were developed with varied concentrations of the polymers (1-2%) using plasticizer/permeation enhancer (25–50% w/w of polymer). Two layered films comprised of risedronate sodium with chitosan (85% deacetylated) and hydroxypropylmethyl cellulose (HPMC 4KM) interpolymer complex of different ratios were prepared by solvent casting method. An impermeable backing membrane of ethyl cellulose was incorporated into the films. The study shows the effect of multipolymeric films on the release of a bisphosphonates derivative. The optimized formulations showed films with uniform drug content (), thickness ( mm to  mm), mucoadhesivity ( g), and controlled drug release profile up to a period of 10 hours. The films were also studied for swelling index, moisture uptake, viscosity, folding endurance, water vapor transmission rate, and mucoadhesive time. Dhrubojyoti Mukherjee and Srinivasan Bharath Copyright © 2013 Dhrubojyoti Mukherjee and Srinivasan Bharath. All rights reserved. Development and Evaluation of Gastroretentive Floating Tablets of an Antihypertensive Drug Using Hydrogenated Cottonseed Oil Wed, 18 Dec 2013 17:27:05 +0000 The aim of the present work was to develop a gastroretentive floating tablet of Atenolol and investigate the effects of both hydrophilic and hydrophobic retardant on in vitro release. Atenolol is an antihypertensive drug with an oral bioavailability of only 50% because of its poor absorption from lower gastrointestinal tract. The floating tablets of Atenolol were prepared to increase the gastric retention, to extend the drug release, and to improve the bioavailability of the drug. The floating tablets were formulated using hydrophilic polymers as Hydroxy propyl methyl cellulose (HPMC K4M and HPMC K15M), hydrophobic retardant as a hydrogenated cottonseed oil (HCSO), and sodium bicarbonate as a gas generating agent to reduce floating lag time. The formulated tablets were evaluated for the quality control tests such as weight variation, hardness, friability, swelling index, floating lag time, and total floating time. The in vitro release study of the tablets was performed in 0.1 N HCl as a dissolution media. The results of the present study clearly indicates the promising potential of Atenolol floating system as an alternative to the conventional dosage and other sustained release formulations. The study also revealed the effectiveness of HCSO as retardant in combination with HPMC. Harshal Ashok Pawar, Pooja Ramchandra Gharat, Rachana Vivek Dhavale, Pooja Rasiklal Joshi, and Pushpita Pankajkumar Rakshit Copyright © 2013 Harshal Ashok Pawar et al. All rights reserved. Statistical Optimization and In Vitro Evaluation of Metformin Hydrochloride Asymmetric Membrane Capsules Prepared by a Novel Semiautomatic Manufacturing Approach Sun, 08 Dec 2013 15:06:04 +0000 Asymmetric membrane capsules (AMCs) are one of the novel osmotic delivery devices which deliver a wide range of drugs in controlled manner. In the present work, we developed and validated a semiautomatic process by fabricating a hydraulic assisted bench top model for manufacturing AMCs. The capsule walls of AMCs were prepared by dip coating phase inversion process using cellulose acetate butyrate (CAB) as coating polymer and propylene glycol (PG) as plasticizer and pore former. The comparative examination of physical parameters confirmed the consistency, efficiency, and reproducibility of the semiautomatic process over the manual procedure. The SEM studies revealed a thin dense region supported on a thicker porous membrane of the capsule shells. Formulations of AMCs were prepared based on a 23 full factorial design using metformin hydrochloride as the model drug. The effect of formulation variables such as concentration of PG and levels of fructose and potassium chloride were studied on the in vitro drug release using Design-Expert 8.0.2 (USA) software. From the in vitro release studies, it was observed that the concentration of pore former and level of osmogents had a direct effect on the drug release. From the validation studies of the optimized formulation (OPT) with the predicted response, it was observed that the drug release was independent of pH and agitation intensity but dependent on osmotic pressure of the dissolution medium. The OPT followed controlled zero-order release kinetics over a period of 13 h. Venkatesh Teja Banala, Bharath Srinivasan, Deveswaran Rajamanickam, Basavaraj Basappa Veerbadraiah, and Madhavan Varadarajan Copyright © 2013 Venkatesh Teja Banala et al. All rights reserved. Preparation of a Sustained Release Drug Delivery System for Dexamethasone by a Thermosensitive, In Situ Forming Hydrogel for Use in Differentiation of Dental Pulp Wed, 27 Nov 2013 15:10:52 +0000 In situ forming delivery systems composed of block copolymers are attracting substantial attention due to their ease of use, biocompatibility, and biodegradability. In this study, the thermoresponsive triblock copolymer PLGA-PEG-PLGA was studied as a dexamethasone delivery system. Dexamethasone, a synthetic glucocorticoid, is used clinically to improve inflammation, pain, and the hyperemesis of chemotherapy, and it is applied experimentally as a differentiation factor in tissue engineering. PLGA-PEG-PLGA was synthesised under microwave irradiation for 5 min. The obtained copolymer was characterised to determine its structure and phase transition temperature. An in vitro release study was conducted for various copolymer structures and drug concentrations. The yield of the reaction and HNMR analysis confirmed the appropriateness of the microwave-assisted method for PLGA-PEG-PLGA synthesis. Phase transition temperature was affected by the drug molecule as well as by the copolymer concentration and structure. An in vitro release study demonstrated that release occurs mainly by diffusion and does not depend on the copolymer structure or dexamethasone concentration. Elham Khodaverdi, Fatemeh Kheirandish, Farnaz Sadat Mirzazadeh Tekie, Bibi Zahra Khashyarmanesh, Farzin Hadizadeh, and Hamideh Moallemzadeh Haghighi Copyright © 2013 Elham Khodaverdi et al. All rights reserved. Validation of Simultaneous Volumetric and HPLC Methods for the Determination of Pridinol Mesylate in Raw Material Wed, 02 Oct 2013 17:37:54 +0000 Simple, sensitive, and economical simultaneous volumetric and HPLC methods for the determination of pridinol mesylate in raw material have been developed. The volumetric method is based on the reaction of pridinol with sodium lauryl sulphate in diluted sulphuric acid. Dimethyl yellow was used as indicator to detect the end point of the titration in aqueous/organic layer. The HPLC method for the determination of pridinol mesylate employs a reverse phase C18 column at ambient temperature with a mobile phase consisting of acetonitrile: 0.05 M potassium dihydrogen phosphate, pH adjusted to 5.0 (1 : 2, v/v). The flow rate was 0.8 mL/min. Quantitation was achieved with UV detection at 258 nm based on peak area. Both methods were found to be suitable for the quality control of pridinol mesylate in raw material. Laura D. Simionato, Leonardo Ferello, Sebastián Stamer, Patricia D. Zubata, and Adriana I. Segall Copyright © 2013 Laura D. Simionato et al. All rights reserved. Photoinitiated Polymerization of 2-Hydroxyethyl Methacrylate by Riboflavin/Triethanolamine in Aqueous Solution: A Kinetic Study Mon, 23 Sep 2013 15:01:19 +0000 The polymerization of 1–3 M 2-hydroxyethyl methacrylate (HEMA) initiated by riboflavin/triethanolamine system has been studied in the pH range 6.0–9.0. An approximate measure of the kinetics of the reaction during the initial stages (~5% HEMA conversion) has been made to avoid the effect of any variations in the volume of the medium. The concentration of HEMA in polymerized solutions has been determined by a UV spectrophotometric method at 208 nm with a precision of ±3%. The initial rate of polymerization of HEMA follows apparent first-order kinetics and the rates increase with pH. This may be due to the presence of a labile proton on the hydroxyl group of HEMA. The second-order rate constants for the interaction of triethanolamine and HEMA lie in the range of 2.36 to  M−1 s−1 at pH 6.0–9.0 suggesting an increased activity with pH. An increase in the viscosity of HEMA solutions from 1 M to 3 M leads to a decrease in the rate of polymerization probably as a result of the decrease in the reactivity of the flavin triplet state. The effect of pH and viscosity of the medium on the rate of reaction has been evaluated. Iqbal Ahmad, Kefi Iqbal, Muhammad Ali Sheraz, Sofia Ahmed, Tania Mirza, Sadia Hafeez Kazi, and Mohammad Aminuddin Copyright © 2013 Iqbal Ahmad et al. All rights reserved. Pharmacosomes: An Emerging Novel Vesicular Drug Delivery System for Poorly Soluble Synthetic and Herbal Drugs Mon, 09 Sep 2013 14:49:28 +0000 In the arena of solubility enhancement, several problems are encountered. A novel approach based on lipid drug delivery system has evolved, pharmacosomes. Pharmacosomes are colloidal, nanometric size micelles, vesicles or may be in the form of hexagonal assembly of colloidal drug dispersions attached covalently to the phospholipid. They act as befitting carrier for delivery of drugs quite precisely owing to their unique properties like small size, amphiphilicity, active drug loading, high entrapment efficiency, and stability. They help in controlled release of drug at the site of action as well as in reduction in cost of therapy, drug leakage and toxicity, increased bioavailability of poorly soluble drugs, and restorative effects. There has been advancement in the scope of this delivery system for a number of drugs used for inflammation, heart diseases, cancer, and protein delivery along with a large number of herbal drugs. Hence, pharmacosomes open new challenges and opportunities for improved novel vesicular drug delivery system. Archana Pandita and Pooja Sharma Copyright © 2013 Archana Pandita and Pooja Sharma. All rights reserved. Formulation Development and Evaluation of Drug Release Kinetics from Colon-Targeted Ibuprofen Tablets Based on Eudragit RL 100-Chitosan Interpolyelectrolyte Complexes Tue, 06 Aug 2013 16:12:41 +0000 Colon-targeted drug delivery systems (CTDDSs) could be useful for local treatment of inflammatory bowel diseases (IBDs). In this study, various interpolyelectrolyte complexes (IPECs), formed between Eudragit RL100 (EL) and chitosan (CS), by nonstoichiometric method, and tablets based on the IPECs, prepared by wet granulation, were evaluated as potential oral CTDDSs for ibuprofen (IBF). Results obtained showed that the tablets conformed to compendial requirements for acceptance and that CS and EL formed IPECs that showed pH-dependent swelling properties and prolonged the in vitro release of IBF from the tablets in the following descending order: 3 : 2 > 2 : 3 > 1 : 1 ratios of CS and EL. An electrostatic interaction between the carbonyl (–CO–) group of EL and amino (–) group of CS of the tablets formulated with the IPECs was capable of preventing drug release in the stomach and small intestine and helped in delivering the drug to the colon. Kinetic analysis of drug release profiles showed that the systems predominantly released IBF in a zero-order manner. IPECs based on CS and EL could be exploited successfully for colon-targeted delivery of IBF in the treatment of IBDs. Kenneth Chibuzor Ofokansi and Franklin Chimaobi Kenechukwu Copyright © 2013 Kenneth Chibuzor Ofokansi and Franklin Chimaobi Kenechukwu. All rights reserved. Nontargeted Identification of the Phenolic and Other Compounds of Saraca asoca by High Performance Liquid Chromatography-Positive Electrospray Ionization and Quadrupole Time-of-Flight Mass Spectrometry Mon, 05 Aug 2013 08:26:41 +0000 High performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometer was used for separation and identification of phenolic and other compounds in the water extracts of Saraca asoca (Roxb.), De. Wilde. The aim of the study was to identify and evaluate the distribution of phenolic compounds in the different parts of the plant. The identity of compounds was established through the comparison with standards and characteristic base peaks as well as other daughter ions. In crude extracts, 34 catechin derivatives, 34 flavonoids, and 17 other compounds were identified. Interestingly, further analysis of compounds showed plant part specific unique pattern of metabolites; that is, regenerated bark is observed to be the best source for catechin/catechin derivative while flowers were found to be the source for wide variety of flavonoids. Moreover, these plant part specific compounds can be used as biomarkers for the identification of plant material or herbal drugs. Overall, the present study provides for the first time a comprehensive analysis of the phenolic components of this herb which may be helpful not only to understand their usage but also to contribute to quality control as well. Ashwani Mittal, Preeti Kadyan, Anjum Gahlaut, and Rajesh Dabur Copyright © 2013 Ashwani Mittal et al. All rights reserved. Comparison of Various Generations of Superporous Hydrogels Based on Chitosan-Acrylamide and In Vitro Drug Release Mon, 29 Jul 2013 12:52:08 +0000 The aim of the current research work was to prepare and evaluate different generations of superporous hydrogels (SPH) of acrylamide and chitosan using gas blowing technique and evaluate them for swelling, mechanical properties, FTIR, SEM, XRD, and in vitro drug release. The ingredients used were acrylamide, N,N′-methylene bisacrylamide, chitosan, Pluronic F127, ammonium per sulfate-N,N,N′,N′-tetramethylenediamine, and sodium bicarbonate. All ingredients were mixed sequentially with thorough stirring. The effect of different drying conditions on properties of SPH was also evaluated. Ethanol treated batched showed maximum swelling properties due to uniform pores as indicated in SEM studies. Equilibrium swelling time was less than 10 min in all batches. Freeze drying led to lowering of density which is also supported by porosity and void fraction data. Maximum mechanical strength was found in superporous hydrogel interpenetrating networks due to crosslinked polymeric network. 70% drug was released at the end of 2 h, and further the release was sustained till the end of 24 h. In vitro drug release kinetics showed that drug release occurs by diffusion and follows Super Case II transport indicating that mechanism of drug release is not clear. Superporous hydrogel interpenetrating networks can be successfully used as sustained release gastroretentive devices. Shikha Bhalla and Manju Nagpal Copyright © 2013 Shikha Bhalla and Manju Nagpal. All rights reserved. Formulation Development and Evaluation of Fast Disintegrating Tablets of Salbutamol Sulphate for Respiratory Disorders Mon, 15 Jul 2013 13:33:45 +0000 Recent developments in fast disintegrating tablets have brought convenience in dosing to pediatric and elderly patients who have trouble in swallowing tablets. The objective of the present study was to prepare the fast disintegrating tablet of salbutamol sulphate for respiratory disorders for pediatrics. As precision of dosing and patient's compliance become important prerequisites for a long-term treatment, there is a need to develop a formulation for this drug which overcomes problems such as difficulty in swallowing, inconvenience in administration while travelling, and patient’s acceptability. Hence, the present investigation were undertaken with a view to develop a fast disintegrating tablet of salbutamol sulphate which offers a new range of products having desired characteristics and intended benefits. Superdisintegrants such as sodium starch glycolate was optimized. Different binders were optimized along with optimized superdisintegrant concentration. The tablets were prepared by direct compression technique. The tablets were evaluated for hardness, friability, weight variation, wetting time, disintegration time, and uniformity of content. Optimized formulation was evaluated by in vitro dissolution test, drug-excipient compatibility, and accelerated stability study. It was concluded that fast disintegrating tablets of salbutamol sulphate were formulated successfully with desired characteristics which disintegrated rapidly; provided rapid onset of action; and enhanced the patient convenience and compliance. Deepak Sharma Copyright © 2013 Deepak Sharma. All rights reserved. Suitability of Biomorphic Silicon Carbide Ceramics as Drug Delivery Systems against Bacterial Biofilms Sun, 07 Jul 2013 09:31:00 +0000 The present work is aimed at getting a new insight into biomorphic silicon carbides (bioSiCs) as bone replacement materials. BioSiCs from a variety of precursors were produced, characterized, and loaded with a broad-spectrum antibiotic. The capacity of loaded bioSiCs for preventing and/or treating preformed S. aureus biofilms has been studied. The differences in precursor characteristics are maintained after the ceramic production process. All bioSiCs allow the loading process by capillarity, giving loaded materials with drug release profiles dependent on their microstructure. The amount of antibiotic released in liquid medium during the first six hours depends on bioSiC porosity, but it could exceed the minimum inhibitory concentration of Staphylococcus aureus, for all the materials studied, thus preventing the proliferation of bacteria. Differences in the external surface and the number and size of open external pores of bioSiCs contribute towards the variations in the effect against bacteria when experiments are carried out using solid media. The internal structure and surface properties of all the systems seem to facilitate the therapeutic activity of the antibiotic on the preformed biofilms, reducing the number of viable bacteria present in the biofilm compared to controls. P. Díaz-Rodríguez, A. Pérez-Estévez, R. Seoane, P. González, J. Serra, and M. Landin Copyright © 2013 P. Díaz-Rodríguez et al. All rights reserved. Microemulsion: New Insights into the Ocular Drug Delivery Thu, 27 Jun 2013 16:07:03 +0000 Delivery of drugs into eyes using conventional drug delivery systems, such as solutions, is a considerable challenge to the treatment of ocular diseases. Drug loss from the ocular surface by lachrymal fluid secretion, lachrymal fluid-eye barriers, and blood-ocular barriers are main obstacles. A number of ophthalmic drug delivery carriers have been made to improve the bioavailability and to prolong the residence time of drugs applied topically onto the eye. The potential use of microemulsions as an ocular drug delivery carrier offers several favorable pharmaceutical and biopharmaceutical properties such as their excellent thermodynamic stability, phase transition to liquid-crystal state, very low surface tension, and small droplet size, which may result in improved ocular drug retention, extended duration of action, high ocular absorption, and permeation of loaded drugs. Further, both lipophilic and hydrophilic characteristics are present in microemulsions, so that the loaded drugs can diffuse passively as well get significantly partitioned in the variable lipophilic-hydrophilic corneal barrier. This review will provide an insight into previous studies on microemulsions for ocular delivery of drugs using various nonionic surfactants, cosurfactants, and associated irritation potential on the ocular surface. The reported in vivo experiments have shown a delayed effect of drug incorporated in microemulsion and an increase in the corneal permeation of the drug. Rahul Rama Hegde, Anurag Verma, and Amitava Ghosh Copyright © 2013 Rahul Rama Hegde et al. All rights reserved. Stability of Betaine Capsules Mon, 03 Jun 2013 10:09:39 +0000 Betaine is used to treat homocystinuria and is not available in Canada as a formulated drug. In order to facilitate the administration of this compound to patients, a capsule formulation and an evaluation of its stability were required. Capsule formulations of betaine were developed (160 mg and 625 mg of betaine per capsule). As betaine has no chromophore, an HPLC-ELSD analytical method was also developed. The critical quality attributes of these formulations were evaluated (content assay, content uniformity, and dissolution) as well as their stability. Capsules with acceptable quality attributes were produced. These capsules remained stable for 1 year when stored in airtight containers at controlled room temperature. However, shelf life decreased dramatically in nonairtight containers at 30°C (3 months for the lactose-containing capsules of 160 mg and 6 months for the capsules of 625 mg). Mirza Akram Hossain, Stéphanie Boily, Natasha Beauregard, Jean-Marc Forest, and Grégoire Leclair Copyright © 2013 Mirza Akram Hossain et al. All rights reserved. In Silico Prediction of Interactions between Site II on Human Serum Albumin and Profen Drugs Wed, 06 Mar 2013 10:21:47 +0000 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. Docking simulations using multiple template structures of HSA from three crystal structures of complexes between drugs and HSA have demonstrated that most of the currently available profen drugs should be site II binders. Hideto Isogai and Noriaki Hirayama Copyright © 2013 Hideto Isogai and Noriaki Hirayama. All rights reserved. -DTPA-Meglumine-Anionic Linear Globular Dendrimer G1: Novel Nanosized Low Toxic Tumor Molecular MR Imaging Agent Tue, 26 Feb 2013 16:59:09 +0000 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. Gadopentetate (with commercial name Magnevist) is the first magnetic resonance imaging contrast media that has been approved by the US Food and Drug Administration. In this study, gadopentetate was first synthesized and then attached to a tree-like polymer called dendrimer which is formed by polyethylene glycol core and surrounding citric acid groups. Stability studies of the drug were carried out to ensure proper synthesis. Then, the uptake of the drug into liver hepatocellular cell line and the drug cytotoxicity were evaluated. Finally, in vitro and in vivo MR imaging were performed with the new synthetic drug. Based on the findings of this research, connecting gadopentetate to dendrimer surface produces a stronger, safer, and more efficient contrast media. Gd(III)-diethylenetriamine pentaacetate-meglumine-dendrimer drug has the ability to enter cells and does not produce significant cytotoxicity. It also increases the relaxivity of tissue and enhances the MR images contrast. The obtained results confirm the hypothesis that the binding of gadopentetate to citric acid dendrimer produces a new, biodegradable, stable, and strong version of the old contrast media. Tahmineh Darvish Mohamadi, Massoud Amanlou, Negar Ghalandarlaki, Bita Mehravi, Mehdi Shafiee Ardestani, and Parichehr Yaghmaei Copyright © 2013 Tahmineh Darvish Mohamadi et al. All rights reserved. Design and Development of Novel Dual-Compartment Capsule for Improved Gastroretention Sun, 27 Jan 2013 12:12:59 +0000 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. Coating attained by the capsule shell was found to be 0.0643 mm. Depending on nature of natural polymer used, most of the formulations showed buoyancy for more than 9 hrs. Developed formulation demonstrated considerably higher drug release up to 9 hrs. The developed formulation depicted the drug release according to Korsmeyer-Peppas model. There was not any significant change in performance characteristics of developed ring caps after subjecting them to stability studies. The present study suggests that the use of NDCC for oral delivery of Ofloxacin could be an alternative to improve its systemic availability which could be regulated by the floating approach. The designed dosage system can have futuristic applications over payloads which require stomach-specific delivery. Ganesh B. Patil, Saurabh S. Singh, Ketan P. Ramani, Vivekanand K. Chatap, and Prashant K. Deshmukh Copyright © 2013 Ganesh B. Patil et al. All rights reserved. A Review of Hot-Melt Extrusion: Process Technology to Pharmaceutical Products Thu, 27 Dec 2012 14:32:02 +0000 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). This paper reviews the innumerable benefits of HME, based on a holistic perspective of the equipment, processing technologies to the materials, novel formulation design and developments, and its varied applications in oral drug delivery systems. Mohammed Maniruzzaman, Joshua S. Boateng, Martin J. Snowden, and Dennis Douroumis Copyright © 2012 Mohammed Maniruzzaman et al. All rights reserved. Evaluation of an Innovative Over-the-Counter Treatment for Symptoms of Reflux Disease: Quick-Dissolving Alginate Granules Sun, 23 Dec 2012 11:06:07 +0000 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. GDP was considered convenient and easy to use. The consumer-driven product development was also shown to form a strong alginate raft in standardised in vitro conditions that met the specifications of the BP monograph (raft strength > 7.5 g). Gastric retention of GDP and a test meal was investigated in healthy volunteers using gamma scintigraphy in comparison to Liquid Gaviscon. Both products formed an alginate raft in the stomach above the test meal and emptied after the meal. The gastric retention of the GDP product was found to be noninferior to Liquid Gaviscon. In conclusion, the innovative GDP product formed an effective raft and was well liked by consumers. Vicki Strugala, Peter W. Dettmar, and Edward C. M. Thomas Copyright © 2012 Vicki Strugala et al. All rights reserved. Effect of Chemical Enhancers in Transdermal Permeation of Alfuzosin Hydrochloride Thu, 20 Dec 2012 09:14:39 +0000 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. Among the various enhancers Transcutol 20% and tween-20 (2%) showed the highest cumulative amount (Q24) of 702.28 ± 6.97 μg/cm2 and 702.74 ± 7.49 μg/cm2, respectively. A flux rate of 31.08 ± 0.21 μg/cm2/hr by Transcutol 20% and 30.38 ± 0.18 μg/cm2/hr by tween-20 (2%) was obtained. Transcutol 20% showed decreased lag time of 0.13 ± 0.05 hr. The lowest skin content of 342.33 ± 5.30 μg/gm was seen with oleic acid 2.5%. Maximum enhancement of flux by 3.94-fold was obtained with transcutol 20%. Primary skin irritation studies were performed with rabbit. Histopathological studies of transcutol 20% showed marked changes such as degeneration and infiltration of mononuclear cells in dermis indicating the effect of transcutol on the skin. Among the different enhancers transcutol is efficient in enhancing transdermal delivery of AH. D. Prasanthi and P. K. Lakshmi Copyright © 2012 D. Prasanthi and P. K. Lakshmi. All rights reserved. Studies on the Cytotoxic Activities of Punica granatum L. var. spinosa (Apple Punice) Extract on Prostate Cell Line by Induction of Apoptosis Mon, 17 Dec 2012 10:52:03 +0000 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. Dye exclusion analysis was performed for viability rate. Our results demonstrated that the Punica granatum L. var. spinosa extract dose dependently suppressed the proliferation of PC3 cells (IC50= 250.21 μg/mL) when compared with a chemotherapeutic anticancer drug (Toxol) (Vesper Pharmaceuticals) with increased nucleosome production from apoptotic cells. The Punica granatum L. var. spinosa extract attenuated the human prostate cell proliferation in vitro possibly by inducing apoptosis. The Punica granatum L. var. spinosa is likely to be valuable for the treatment of some forms of human prostate cell line. Koushan Sineh Sepehr, Behzad Baradaran, Masoumeh Mazandarani, Vahid Khori, and Fatemeh Zare Shahneh Copyright © 2012 Koushan Sineh Sepehr et al. All rights reserved. Chemical Composition, Antifungal and Antibiofilm Activities of the Essential Oil of Mentha piperita L. Thu, 13 Dec 2012 14:44:53 +0000 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 (15.1%) and Menthofuran (11.18%). The EO exhibited strong antifungal activities against the examined fungi at concentrations ranging from 0.12 to 8.0 μL/mL. In addition, the EO inhibited the biofilm formation of Candida albicans and C. dubliniensis at concentrations up to 2 μL/mL. Considering the wide range of the antifungal activities of the examined EO, it might be potentially used in the management of fungal infections or in the extension of the shelf life of food products. Mohammad Jamal Saharkhiz, Marjan Motamedi, Kamiar Zomorodian, Keyvan Pakshir, Ramin Miri, and Kimia Hemyari Copyright © 2012 Mohammad Jamal Saharkhiz et al. All rights reserved. Itraconazole Niosomes Drug Delivery System and Its Antimycotic Activity against Candida albicans Thu, 13 Dec 2012 09:32:32 +0000 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. Permeation of the drug through the skin was affected by cholesterol content in formulation. Itraconazole niosome were having larger zone of inhibition than marketed formulation when activity was checked against C. albicans. Niosomes may be a promising carrier for topical delivery of Itraconazole especially due to their simple production. Vijay D. Wagh and Onkar J. Deshmukh Copyright © 2012 Vijay D. Wagh and Onkar J. Deshmukh. All rights reserved. Use of Response Surface Methodology in the Formulation and Optimization of Bisoprolol Fumarate Matrix Tablets for Sustained Drug Release Mon, 10 Dec 2012 14:24:51 +0000 The aim of this investigation was to develop and optimize bisoprolol fumarate matrix tablets for sustained release application by response surface methodology based on 23 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. The optimized bisoprolol fumarate matrix tablets showed prolonged sustained release of bisoprolol fumarate over 6 hours. These matrix tablets followed the first-order model with anomalous (non-Fickian) diffusion mechanism. Jadupati Malakar, Amit Kumar Nayak, and Soumita Goswami Copyright © 2012 Jadupati Malakar et al. All rights reserved.