Journal of Pharmaceutics The latest articles from Hindawi © 2017 , Hindawi Limited . All rights reserved. High-Throughput Screening of Potential Skin Penetration-Enhancers Using Stratum Corneum Lipid Liposomes: Preliminary Evaluation for Different Concentrations of Ethanol Tue, 21 Feb 2017 08:38:19 +0000 In this study, we developed a technique for high-throughput screening (HTS) of skin penetration-enhancers using stratum corneum lipid liposomes (SCLLs). A fluorescent marker, sodium fluorescein (FL), entrapped in SCLLs was prepared to provide a preliminary evaluation of the effect of different concentrations of ethanol on the disruption effect of SCLLs, which is an alternative for skin penetration-enhancing effects. In addition, SCLLs containing a fluorescent probe (DPH, TMA-DPH, or ANS) were also prepared and utilized to investigate SCLL fluidity. The results using SCLL-based techniques were compared with conventional skin permeation and skin impedance test using hairless rat skin. The obtained correlations were validated between FL leakage, SCLL fluidity with various probes, or skin impedance and increases in the skin permeation enhancement ratio (ER) of caffeine as a model penetrant. As a result, FL leakage and SCLL fluidity using ANS were considered to be good indices for the skin penetration-enhancing effect, suggesting that the action of ethanol on the SC lipid and penetration-enhancing is mainly on the polar head group of intercellular lipids. In addition, this screening method using SCLL could be utilized as an alternative HTS technique for conventional animal tests. Simultaneously, the method was found to be time-saving and sensitive compared with a direct assay using human and animal skins. Pajaree Sakdiset, Yuki Kitao, Hiroaki Todo, and Kenji Sugibayashi Copyright © 2017 Pajaree Sakdiset et al. All rights reserved. Formulation and Evaluation of New Glimepiride Sublingual Tablets Sun, 05 Feb 2017 06:38:08 +0000 Oral mucosal delivery of drugs promotes rapid absorption and high bioavailability, with a subsequent immediate onset of pharmacological effect. However, many oral mucosal deliveries are compromised by the possibility of the patient swallowing the active substance before it has been released and absorbed locally into the systemic circulation. The aim of this research was to introduce a new glimepiride formula for sublingual administration and rapid drug absorption that can be used in an emergency. The new sublingual formulation was prepared after five trials to prepare the suitable formulation. Two accepted formulations of the new sublingual product were prepared, but one of them with disintegration time of 1.45 min and searching for preferred formulation, the binder, is changed with Flulac and starch slurry to prepare formula with disintegration time of 21 seconds that supports the aim of research to be used in an emergency. The five formulations were done, after adjusting to the binder as Flulac and aerosil with disintegration time of 21 seconds and accepted hardness as well as the weight variation. The assay of a new product (subglimepiride) is 103% which is a promising result, confirming that the formula succeeded. The new product (subglimepiride) is accepted in most quality control tests and it is ready for marketing. Wafa Al-Madhagi, Ahmed Abdulbari Albarakani, Abobakr Khaled Alhag, Zakaria Ahmed Saeed, Nahlah Mansour Noman, and Khaldon Mohamed Copyright © 2017 Wafa Al-Madhagi et al. All rights reserved. Immunooncology: Can the Right Chimeric Antigen Receptors T-Cell Design Be Made to Cure All Types of Cancers and Will It Be Covered? Mon, 23 Jan 2017 00:00:00 +0000 Immunooncology (IO) is the buzz word today and it has everyone doing IO research. If we look back at the history of cancer treatment, the survival rate was measured in months which, according to oncologists, was a lot back then because the mortality rate in most cancers was 100%. However, most traditional chemotherapies were not well tolerated because they would kill both cancerous and healthy cells, which lead to major side effects such as loss of hair, nausea and vomiting, and risk of infection. Survival was better but not much better depending on the type of cancer and the patient’s own genetic and physiological make-up. IO therapies target specific receptors on the cancer cells. However, with more advance technologies, the cost to develop these types of therapies increases significantly because the biology is more complex and it is more difficult to produce. Find out why these therapies are more complex and therefore more expensive. But the enhanced efficacy of these therapies does justify the cost. Regina Au Copyright © 2017 Regina Au. All rights reserved. Self-Medication Pattern among Social Science University Students in Northwest Ethiopia Mon, 16 Jan 2017 00:00:00 +0000 Background. Inappropriate self-medication causes wastage of resources among others. Method. This survey study was conducted to determine self-medication pattern of 404 social science university students in Northwest Ethiopia, who were selected through stratified random sampling technique. Data were collected using self-administered questionnaire and analyzed with SPSS version 20 statistical software. Binary Logistic Regression analysis was employed with value < 0.05 considered statistically significant. Result. At 95.3% response rate, mean age of 21.26 ± 1.76 years, and male/female ratio of 1.26, the prevalence of self-medication during the six month recall period was 32.7%. Headache (, 69.1%) was the primary complaint that prompted the practice and hence analgesics (, 53.2%) were the mostly used drugs followed by antimicrobials (, 39.7%). The top two reasons driving the practice were nonseverity of the illness (, 32.5%) and suggestions from friends (, 26.2%). Female sex () and higher income () were associated with the practice. Conclusion. Self-medication practice, involving the use of both nonprescription and prescription drugs such as antimicrobials, among the social science university students is high. Therefore health education interventions regarding the risks of inappropriate self-medication are essential. Dessalegn Asmelashe Gelayee Copyright © 2017 Dessalegn Asmelashe Gelayee. All rights reserved. Methanolic Extract of Dill Leaves Inhibits AGEs Formation and Shows Potential Hepatoprotective Effects in CCl4 Induced Liver Toxicity in Rat Sun, 15 Jan 2017 00:00:00 +0000 The research was aimed at evaluating the antiglycation, antioxidant, and hepatoprotective properties of methanolic extract of Anethum graveolens (dill). The antioxidant properties, photochemical characteristics, and antiglycation effects of dill extract were measured. Carbon tetrachloride-induced hepatotoxic rats were used to show the hepatoprotective activity of dill leaves. Different concentration of dill extract (0.032, 0.065, 0.125, 0.25, 0.5, and 1 mg/mL) showed potential antioxidant ability. The extract of dill leaves significantly reduced AGEs formation and also fructosamine and protein carbonyl levels in rats’ liver. Thiol groups’ oxidation, amyloid cross-β, and protein fragmentation () significantly reduced in treated rats. Liver damage markers significantly reduced in dill-treated animals (). Dill with potential antioxidant, antiglycation, and hepatoprotective effects can be suggested for treatment of diabetes complications. Ebrahim Abbasi Oshaghi, Iraj Khodadadi, Fatemeh Mirzaei, Mozafar Khazaei, Heidar Tavilani, and Mohammad Taghi Goodarzi Copyright © 2017 Ebrahim Abbasi Oshaghi et al. All rights reserved. Combined Effect of Synthetic and Natural Polymers in Preparation of Cetirizine Hydrochloride Oral Disintegrating Tablets: Optimization by Central Composite Design Thu, 05 Jan 2017 00:00:00 +0000 Our aim was to employ experimental design to formulate and optimize cetirizine hydrochloride oral disintegrating tablets (ODTs) by direct compression technique, using the mutual effect of synthetic croscarmellose sodium (CCS) and natural Hibiscus rosa-sinensis mucilage (HRM) as disintegrants in the formulation. Central composite design (CCD) was applied to optimize the influence of three levels each of CCS () and HRM () concentrations (independent variables) for investigated responses: disintegration time (DT) (), % friability () (), and % cumulative drug release (DR) () (dependent variables). This face-centered second-order model’s reliability was verified by the probability and adequate precision values from the analysis of variance, while the significant factor effects influencing the studied responses were identified using multiple linear regression analysis. Perturbation and response surface plots were interpreted to evaluate the responses’ sensitivity towards the variables. During optimization, the concentrations of the processed factors were evaluated, and the resulting values were in good agreement with predicted estimates endorsing the validity. Spectral study by Fourier Transform Infrared Spectroscopy (FTIR) and thermograms from Differential Scanning Calorimetry (DSC) demonstrated the drug-excipients compatibility of the optimized formulation. The optimized formulation has concentrations of 9.05 mg and 16.04 mg of CCS and HRM each, respectively, and the model predicted DT of 13.271 sec, of 0.498, and DR of 99.768%. Chandra Sekhar Patro and Prafulla Kumar Sahu Copyright © 2017 Chandra Sekhar Patro and Prafulla Kumar Sahu. All rights reserved. Structural Alteration in Dermal Vessels and Collagen Bundles following Exposure of Skin Wound to Zeolite–Bentonite Compound Wed, 28 Dec 2016 12:12:32 +0000 Background. This study examines the impact of one-time direct application of haemostatic agent zeolite–bentonite powder to wounded skin on the healing process in rats. Materials and Methods. 24 male Sprague-Dawley rats were randomly allocated into two groups (): (1) the rats whose wounds were washed only with sterile normal saline (NS-treated) and (2) those treated with zeolite–bentonite compound (ZEO-treated). The wound was circular, full-thickness, and 2 cm in diameter. At the end of the 12th day, six animals from each group were randomly selected and terminated. The remaining rats were terminated after 21 days. Just after scarification, skin samples were excised and sent for stereological evaluation. Results. The results showed a significant difference between the two groups regarding the length density of the blood vessels and diameter of the large and small vessels on the 12th day after the wound was inflicted. Besides, volume density of both the dermis and collagen bundles was reduced by 25% in the ZEO-treated rats in comparison to the NS-treated animals after 21 days. Conclusions. One-time topical usage of zeolite–bentonite haemostatic powder on an animal skin wound might negatively affect the healing process through vasoconstriction and inhibition of neoangiogenesis. Shahram Paydar, Ali Noorafshan, Behnam Dalfardi, Shahram Jahanabadi, Seyed Mohammad Javad Mortazavi, Seyedeh-Saeedeh Yahyavi, and Hadi Khoshmohabat Copyright © 2016 Shahram Paydar et al. All rights reserved. Quantification of Warfarin in Dried Rat Plasma Spots by High-Performance Liquid Chromatography with Tandem Mass Spectrometry Mon, 12 Dec 2016 14:31:14 +0000 This paper presents the development and validation of a novel method for quantification of the oral anticoagulant drug warfarin in dried plasma spots (DPS) by high-performance liquid chromatography with tandem mass spectrometry (HPLC-MS/MS). Blood plasma was chosen as a biological fluid to preclude the influence of the hematocrit on the results of the analysis. A 30 L sample of rat plasma was placed onto Whatman 903 Protein Saver Card and was allowed to dry. A single DPS is sufficient for preparing eight 3.2 mm discs, each containing approximately 1.5–1.6 L of plasma. Warfarin extraction from one 3.2 mm disc was carried out by adding 200 L of the acetonitrile : water mixture (1 : 1, v/v) containing 10 mM NH4COOH (pH 4.0), with incubation on a shaker at 1000 rpm for 1 h at 25°C. After chromatographic separation, warfarin and coumachlor (an internal standard) were measured using negative-ion multiple-reaction monitoring with ion transitions 307 → 161 for warfarin and 341 → 161 for the internal standard. The working range of this method is 10–10,000 ng/mL. Within this range, intra- and interday variability of precision and accuracy was <13% and recovery was 82–99%. The results indicate that the new method requires only small plasma samples and may be useful for pharmacokinetic research on warfarin. Alexander Chernonosov Copyright © 2016 Alexander Chernonosov. All rights reserved. Ingestibility and Formulation Quality of Lansoprazole Orally Disintegrating Tablets Thu, 01 Dec 2016 07:43:51 +0000 Objectives. We evaluated the ingestibility and formulation quality of one branded (formulation A) and five generic (formulations B, C, D, E, and F) lansoprazole orally disintegrating (OD) tablets. Methods. Ingestibility, including the oral disintegrating time, taste, mouth feeling, and palatability, was examined by sensory testing in healthy subjects. Formulation qualities, including salivary stability, gastric acid resistance, and intestinal dissolution behavior, were examined. Results and Discussion. The oral disintegration time of formulation F (52 s) was significantly longer than that of other formulations (32–37 s). More than 90% of subjects did not experience bitterness with formulations A, E, and F, whereas 50% of subjects felt rough and powdery sensations with formulations B, C, and D. More than 80% of subjects suggested that formulations A, E, and F had good palatability. Ingestibility was different between formulations. OD tablets consist of enteric granules containing lansoprazole, which is unstable in gastric acid. Enteric granules of each formulation were stable in artificial saliva and gastric juice. No differences were observed in dissolution behaviors among the formulations, indicating that the formulation quality of the formulations was almost equivalent. Conclusions. This study provides useful information for selecting branded or generic lansoprazole OD tablets for individualized treatments. Sumio Chono, Megumi Matsui, Katsuki Nakamura, and Ryoya Kasai Copyright © 2016 Sumio Chono et al. All rights reserved. Freeze Dried Quetiapine-Nicotinamide Binary Solid Dispersions: A New Strategy for Improving Physicochemical Properties and Ex Vivo Diffusion Wed, 30 Nov 2016 11:34:42 +0000 Improving the physicochemical properties and oral bioavailability of quetiapine fumarate (QF) enabling enhanced antipsychotic attributes are the main aims of this research. The freeze dried solid dispersion strategy was adopted using nicotinamide (NIC) as highly soluble coformer. The prepared dispersions were characterized using scanning electron microscopy (SEM) differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), and X-ray diffraction (XRD). Static disc intrinsic dissolution rate and ex vivo diffusion through intestinal tissues were conducted and compared to pure quetiapine fumarate. The results demonstrated a highly soluble coamorphous system formed between quetiapine fumarate and nicotinamide at 1 : 3 molar ratio through H-bonding interactions. The results showed >14-fold increase in solubility of QF from the prepared dispersions. Increased intrinsic dissolution rate (from 0.28 to 0.603 mg cm−2 min−1) and faster flux rate through duodenum (from 0.027 to 0.041 mg cm−2 h−1) and jejunum (0.027 to 0.036 mg cm−2 h−1) were obtained. The prepared coamorphous dispersion proved to be effective in improving the drug solubility and dissolution rate and ex vivo diffusion. Therefore, binary coamorphous dispersions could be a promising solution to modify the physicochemical properties, raise oral bioavailability, and change the biopharmaceutics classification (BCS) of some active pharmaceutical ingredients. Ahmed Mahmoud Abdelhaleem Ali and Mayyas Mohammad Ahmad Al-Remawi Copyright © 2016 Ahmed Mahmoud Abdelhaleem Ali and Mayyas Mohammad Ahmad Al-Remawi. All rights reserved. Antioxidant and Antibacterial Potential of Silver Nanoparticles: Biogenic Synthesis Utilizing Apple Extract Mon, 28 Nov 2016 09:00:53 +0000 The advancement of the biological production of nanoparticles using herbal extracts performs a significant role in nanotechnology discipline as it is green and does not engage harsh chemicals. The objective of the present investigation was to extract flavonoids in the mode of apple extract and synthesize its silver nanoparticles and ultimately nanoparticles loading into hydrogels. The presence of flavonoids in apple extract was characterized by preliminary testing like dil. ammonia test and confirmatory test by magnesium ribbon test. The synthesized silver nanoparticles were characterized using UV spectroscopy, particle size and surface morphology, and zeta potential. Silver nanoparticles loaded hydrogels were evaluated for physical appearance, pH, viscosity, spreadability, porosity, in vitro release, ex vivo permeation, and antibacterial (E. coli and S. aureus) and antioxidant studies (DPPH radical scavenging assay). Well dispersed silver nanoparticles below were observed in scanning electron microscope image. Hydrogels displayed in vitro release of 98.01%  ±  0.37% up to 24 h and ex vivo permeation of 98.81  ±  0.24% up to 24 h. Hydrogel effectively inhibited the growth of both microorganism indicating good antibacterial properties. The value of percent radical inhibition was 75.16%  ±  0.04 revealing its high antioxidant properties. As an outcome, it can be concluded that antioxidant and antiageing traits of flavonoids in apple extract plus biocidal feature of silver nanoparticles can be synergistically and successfully utilized in the form of hydrogel. Upendra Nagaich, Neha Gulati, and Swati Chauhan Copyright © 2016 Upendra Nagaich et al. All rights reserved. Novel Concepts for Drug Hypersensitivity Based on the Use of Long-Time Scale Molecular Dynamic Simulation Wed, 23 Nov 2016 11:34:56 +0000 The discovery that several drug hypersensitivity reactions (DHRs) are associated with specific human leukocyte antigen (HLA) alleles has attracted increasing research interest. However, the underlying mechanisms of these HLA-induced DHRs remain unclear, especially for drug-induced immediate activation of T-cell clones (TCCs). Recently, a novel hypothesis involving partial detachment between self-peptide(s) and the HLA molecule (altered peptide-HLA (pHLA) model) has been proposed to explain these phenomena. In order to clarify this hypothesis, we performed long-timescale molecular dynamics (MD) simulations. We focused on HLA-B⁎57:01-restricted abacavir hypersensitivity reactions (AHRs), one of the most famous DHRs. One of the simulation results showed that this altered-pHLA model might be driven by an increase in the distance not only between HLA and self-peptides but also between the α1 and α2 helices of HLA. Our findings provide novel insights into abacavir-induced immediate activation of TCCs and these findings might also be applied to other DHRs, such as HLA-B⁎58:01-restricted allopurinol hypersensitivity reactions. Takahiro Murai, Norihito Kawashita, Yu-Shi Tian, and Tatsuya Takagi Copyright © 2016 Takahiro Murai et al. All rights reserved. A Comparison of the Effects of Alpha and Medical-Grade Honey Ointments on Cutaneous Wound Healing in Rats Thu, 03 Nov 2016 13:16:09 +0000 Introduction. This study compared the healing efficacy and possible adverse effects of topical Alpha and medical-grade honey ointments on cutaneous wounds in rats. Methods. To conduct the study, 22 male Sprague-Dawley rats were randomly allocated into two equal groups: (1) rats with Alpha ointment applied to the wound surface area and (2) rats with medical-grade honey ointment applied to their wounds. The ointments were applied daily during the 21-day study period. Wound contraction was examined photographically with images taken on days 0, 7, and 21 after wounding. The healing process was histopathologically assessed using skin biopsies taken from the wound sites on days 7 and 21. Results. No statistically significant difference in mean wound surface area was observed between the two study groups. According to histopathological assessment, a significant reduction in the amount of collagen deposition ( value: 0.007) and neovascularisation ( value: 0.002) was seen in the Alpha-treated rats on day 21. No tissue necrosis occurred following the application of Alpha ointment. Conclusion. Daily topical usage of Alpha ointment on a skin wound can negatively affect the healing process by inhibiting neovascularization. Topical Alpha ointment can reduce the possibility of excessive scar formation by reducing collagen deposition. Shahram Paydar, Majid Akrami, Amirreza Dehghanian, Roshanak Alavi Moghadam, Mohsen Heidarpour, Amir Bahari Khoob, and Behnam Dalfardi Copyright © 2016 Shahram Paydar et al. All rights reserved. Formulation and Evaluation of Antibacterial Creams and Gels Containing Metal Ions for Topical Application Thu, 03 Nov 2016 11:30:20 +0000 Background. Skin infections occur commonly and often present therapeutic challenges to practitioners due to the growing concerns regarding multidrug-resistant bacterial, viral, and fungal strains. The antimicrobial properties of zinc sulfate and copper sulfate are well known and have been investigated for many years. However, the synergistic activity between these two metal ions as antimicrobial ingredients has not been evaluated in topical formulations. Objective. The aims of the present study were to (1) formulate topical creams and gels containing zinc and copper alone or in combination and (2) evaluate the in vitro antibacterial activity of these metal ions in the formulations. Method. Formulation of the gels and creams was followed by evaluating their organoleptic characteristics, physicochemical properties, and in vitro antibacterial activity against Escherichia coli and Staphylococcus aureus. Results. Zinc sulfate and copper sulfate had a strong synergistic antibacterial activity in the creams and gels. The minimum effective concentration was found to be 3 w/w% for both active ingredients against the two tested microorganisms. Conclusions. This study evaluated and confirmed the synergistic in vitro antibacterial effect of copper sulfate and zinc sulfate in a cream and two gels. Mei X. Chen, Kenneth S. Alexander, and Gabriella Baki Copyright © 2016 Mei X. Chen et al. All rights reserved. Porcine Pancreatic Lipase Inhibitory Agent Isolated from Medicinal Herb and Inhibition Kinetics of Extracts from Eleusine indica (L.) Gaertner Mon, 31 Oct 2016 11:04:38 +0000 Eleusine indica (Linnaeus) Gaertner is a traditional herb known to be depurative, febrifuge, and diuretic and has been reported with the highest inhibitory activity against porcine pancreatic lipase (PPL) among thirty two plants screened in an earlier study. This study aims to isolate and identify the active components that may possess high potential as an antiobesity agent. Of the screened solvent fractions of E. indica, hexane fraction showed the highest inhibitory activity of % at 100 μg/mL. Bioactivity-guided isolation afforded three compounds from the hexane fraction of E. indica, namely, β-sitosterol, stigmasterol, and lutein. The structures of these compounds were elucidated using spectral techniques. Lutein showed an outstanding inhibitory activity against PPL (%), with activity 60% higher than that of the reference drug Orlistat. The other compounds isolated and identified were β-sitosterol (%) and stigmasterol (%). The enzyme kinetics of E. indica crude methanolic extract on PPL showed mixed inhibition mechanism. Siew Ling Ong, Siau Hui Mah, and How Yee Lai Copyright © 2016 Siew Ling Ong et al. All rights reserved. Functional Performance of Chitosan/Carbopol 974P NF Matrices in Captopril Tablets Tue, 25 Oct 2016 15:33:37 +0000 Chitosan and Carbopol have been used to form a complex through an electrostatic interaction between the protonated amine (NH3+) group of chitosan and the carboxylate (COO−) group of Carbopol. In situ polyelectrolyte complexes formations based on the physical mixture of chitosan and sodium alginate were found and could be used as an oral controlled release matrix. The aim of this work is the assessment of a possible interaction between the particles of chitosan and Carbopol 974P NF that could modify their technological performance in captopril tablets. The drug and excipients were evaluated as mixtures of powders and tablets. The mixtures with captopril contained Carbopol 974P NF, chitosan, or a 1 : 1 mixture thereof with polymer proportions of 10%, 20%, and 30%. The evaluated parameters were the powder flow rate, the powder compressibility index, and the compactibility and release behavior of the tablets. The observed technological behavior points out to a greater interaction between the particles of polymers with different charge than between particles of the individual polymers. This produces more coherent matrices restricting more efficiently the drug dissolution, more coherent tablets with higher compactibility, and less flowing powder mixtures. All this, however, requires additional investigation to confirm the current results. Yuritze Alejandra Aguilar-López and Leopoldo Villafuerte-Robles Copyright © 2016 Yuritze Alejandra Aguilar-López and Leopoldo Villafuerte-Robles. All rights reserved. Formulations of Amlodipine: A Review Sun, 16 Oct 2016 07:54:53 +0000 Amlodipine (AD) is a calcium channel blocker that is mainly used in the treatment of hypertension and angina. However, latest findings have revealed that its efficacy is not only limited to the treatment of cardiovascular diseases as it has shown to possess antioxidant activity and plays an important role in apoptosis. Therefore, it is also employed in the treatment of cerebrovascular stroke, neurodegenerative diseases, leukemia, breast cancer, and so forth either alone or in combination with other drugs. AD is a photosensitive drug and requires protection from light. A number of workers have tried to formulate various conventional and nonconventional dosage forms of AD. This review highlights all the formulations that have been developed to achieve maximum stability with the desired therapeutic action for the delivery of AD such as fast dissolving tablets, floating tablets, layered tablets, single-pill combinations, capsules, oral and transdermal films, suspensions, emulsions, mucoadhesive microspheres, gels, transdermal patches, and liposomal formulations. Muhammad Ali Sheraz, Syed Furqan Ahsan, Marium Fatima Khan, Sofia Ahmed, and Iqbal Ahmad Copyright © 2016 Muhammad Ali Sheraz et al. All rights reserved. The Genus Luehea (Malvaceae-Tiliaceae): Review about Chemical and Pharmacological Aspects Thu, 13 Oct 2016 13:00:48 +0000 Popularly known as “açoita-cavalo” (whips-horse), Luehea species (Malvaceae-Tilioideae) are native to America and are used in folk medicine as anti-inflammatory, antidiarrheal, antiseptic, expectorant, and depurative and against skin infections. Although there are studies showing the chemical constituents of some species, the active substances have not been properly identified. A systematic study was carried out through a computer search of data on CAPES journals, SciELO, ISI Bireme, PubMed, ScienceDirect, ScienceDomain Medline, and Google Scholar from published articles using key words: Luehea, açoita-cavalo, and Malvaceae. Luehea divaricata was the species with the highest number of studies observed. Triterpenes (9), flavonoids (6), and steroids (4), including saponins, organic acids (4), and one lignan, are the main types of secondary metabolites registered and the most cited flavonoids were rutin and quercetin and among triterpenes there was maslinic acid, which might be associated with the popular indication of its anti-inflammatory action. The vitexin, a C-glycosylated flavone, isolated from three different species, is cited as a possible taxonomic marker of the genus. Studies confirm in part the medicinal uses of plants named as “açoita-cavalo” species. Some pharmacological activities, not assigned to the species of the genus Luehea by populations, were observed in laboratory experiments. João Tavares Calixto-Júnior, Selene Maia de Morais, Aracélio Viana Colares, and Henrique Douglas Melo Coutinho Copyright © 2016 João Tavares Calixto-Júnior et al. All rights reserved. Application of Cerium (IV) as an Oxidimetric Agent for the Determination of Ethionamide in Pharmaceutical Formulations Thu, 13 Oct 2016 12:35:07 +0000 Two simple methods are described for the determination of ethionamide (ETM) in bulk drug and tablets using cerium (IV) sulphate as the oxidimetric agent. In both methods, the sample solution is treated with a measured excess of cerium (IV) solution in H2SO4 medium, and after a fixed standing time, the residual oxidant is determined either by back titration with standard iron (II) solution to a ferroin end point in titrimetry or by reacting with o-dianisidine followed by measurement of the absorbance of the orange-red coloured product at 470 nm in spectrophotometry. In titrimetry, the reaction proceeded with a stoichiometry of 1 : 2 (ETM : Ce (IV)) and the amount of cerium (IV) consumed by ETM was related to the latter’s amount, and the method was applicable over 1.0–8.0 mg of drug. In spectrophotometry, Beer’s law was obeyed over the concentration range of 0.5–5.0 μg/mL ETM with a molar absorptivity value of 2.66 × 104 L/(mol·cm). The limits of detection (LOD) and quantification (LOQ) calculated according to ICH guidelines were 0.013 and 0.043 μg/mL, respectively. The proposed titrimetric and spectrophotometric methods were found to yield reliable results when applied to bulk drug and tablets analysis, and hence they can be applied in quality control laboratories. Kanakapura Basavaiah, Nagib A. S. Qarah, and Sameer A. M. Abdulrahman Copyright © 2016 Kanakapura Basavaiah et al. All rights reserved. Adverse Effects of Subchronic Dose of Aspirin on Reproductive Profile of Male Rats Tue, 12 Apr 2016 06:40:09 +0000 Aspirin (acetylsalicylic acid) is widely used for cardiovascular prophylaxis and as anti-inflammatory pharmaceutical. An investigation was carried out to evaluate the influence of subchronic dose of aspirin on reproductive profile of male rats, if any. Experimental animals were divided into three groups: control and aspirin subchronic dose of 12.5 mg/kg for 30 days and 60 days, respectively, while alterations in sperm dynamics, testicular histopathological and planimetric investigations, body and organs weights, lipid profiles, and hematology were performed as per aimed objectives. Subchronic dose of aspirin reduced sperm density, count, and mobility in cauda epididymis and testis; histopathology and developing primary spermatogonial cells (primary spermatogonia, secondary spermatogonia, and mature spermatocyte) count were also significantly decreased in rats. Hematological investigations revealed hemopoietic abnormalities in 60-day-treated animals along with dysfunctions in hepatic and renal functions. The findings of the present study revealed that administration with subchronic dose of aspirin to male rats resulted in altered reproductive profiles and serum biochemistry. Archana Vyas, Heera Ram, Ashok Purohit, and Rameshwar Jatwa Copyright © 2016 Archana Vyas et al. All rights reserved. Physicochemical and Antimicrobial Properties of Cocoa Pod Husk Pectin Intended as a Versatile Pharmaceutical Excipient and Nutraceutical Mon, 14 Mar 2016 10:14:09 +0000 The physicochemical and antimicrobial properties of cocoa pod husk (CPH) pectin intended as a versatile pharmaceutical excipient and nutraceutical were studied. Properties investigated include pH, moisture content, ash values, swelling index, viscosity, degree of esterification (DE), flow properties, SEM, FTIR, NMR, and elemental content. Antimicrobial screening and determination of MICs against test microorganisms were undertaken using agar diffusion and broth dilution methods, respectively. CPH pectin had a DE of 26.8% and exhibited good physicochemical properties. Pectin had good microbiological quality and exhibited pseudoplastic, shear thinning behaviour, and high swelling capacity in aqueous media. The DE, FTIR, and NMR results were similar to those of previous studies and supported highly acetylated low methoxy pectin. CPH pectin was found to be a rich source of minerals and has potential as a nutraceutical. Pectin showed dose-dependent moderate activity against gram positive and gram negative microorganisms but weak activity against Listeria spp. and A. niger. The MICs of pectin ranged from 0.5 to 4.0 mg/mL, with the highest activity against E. coli and S. aureus (MIC: 0.5–1.0 mg/mL) and the lowest activity against A. niger (MIC: 2.0–4.0 mg/mL). The study has demonstrated that CPH pectin possesses the requisite properties for use as a nutraceutical and functional pharmaceutical excipient. Ofosua Adi-Dako, Kwabena Ofori-Kwakye, Samuel Frimpong Manso, Mariam EL Boakye-Gyasi, Clement Sasu, and Mike Pobee Copyright © 2016 Ofosua Adi-Dako et al. All rights reserved. Pharmacological Investigation of the Wound Healing Activity of Cestrum nocturnum (L.) Ointment in Wistar Albino Rats Thu, 25 Feb 2016 15:29:33 +0000 Objectives. The present study was aimed at investigating the wound healing effect of ethanolic extract of Cestrum nocturnum (L.) leaves (EECN) using excision and incision wound model. Methods. Wistar albino rats were divided into five groups each consisting of six animals; group I (left untreated) considered as control, group II (ointment base treated) considered as negative control, group III treated with 5% (w/w) povidone iodine ointment (Intadine USP), which served as standard, group IV treated with EECN 2% (w/w) ointment, and group V treated with EECN 5% (w/w) ointment were considered as test groups. All the treatments were given once daily. The wound healing effect was assessed by percentage wound contraction, epithelialization period, and histoarchitecture studies in excision wound model while breaking strength and hydroxyproline content in the incision wound model. Result. Different concentration of EECN (2% and 5% w/w) ointment promoted the wound healing activity significantly in both the models studied. The high rate of wound contraction (), decrease in the period for epithelialization (), high skin breaking strength (), and elevated hydroxyproline content were observed in animal treated with EECN ointments when compared to the control and negative control group of animals. Histopathological studies of the EECN ointments treated groups also revealed the effectiveness in improved wound healing. Conclusions. Ethanolic extract of Cestrum nocturnum (EECN) leaves possesses a concentration dependent wound healing effect. Hemant Kumar Nagar, Amit Kumar Srivastava, Rajnish Srivastava, Madan Lal Kurmi, Harinarayan Singh Chandel, and Mahendra Singh Ranawat Copyright © 2016 Hemant Kumar Nagar et al. All rights reserved. In Vitro and In Vivo Correlation of Colon-Targeted Compression-Coated Tablets Wed, 17 Feb 2016 10:48:00 +0000 This study was performed to assess and correlate in vitro drug release with in vivo absorption of prednisolone (PDL) from a colon-targeted tablet prepared by compression coating of core tablet. In vivo drug absorption study was conducted using a high performance liquid chromatographic (HPLC) method, which was developed and validated for the estimation of PDL in rabbit plasma. The calibration curve showed linearity in the concentration range of 0.05 to 50 μg/mL with the correlation coefficient () of 0.999. The method was specific and sensitive with the limit of detection (LOD) and lower limit of quantification (LLOQ) of  ng/mL and  ng/mL, respectively. The extraction recovery (ER) of PDL from three different levels of quality control (QC) samples ranged from 98.18% to 103.54%. In vitro drug release study revealed that less than 10% drug was released in 6.34 h and almost complete (98.64%) drug release was achieved in the following 6 h. In vivo drug absorption study demonstrated lower values of , , and protracted from compression-coated tablet. The results confirmed the maximum release of drug in the colon while minimizing release in the upper gastrointestinal tract (GIT). An excellent in vitro and in vivo correlation (IVIVC) was also achieved after considering the lag time. Siddhartha Maity, Amit Kundu, Sanmoy Karmakar, and Biswanath Sa Copyright © 2016 Siddhartha Maity et al. All rights reserved. Cellulose Acetate 398-10 Asymmetric Membrane Capsules for Osmotically Regulated Delivery of Acyclovir Thu, 11 Feb 2016 13:39:59 +0000 The study was aimed at developing cellulose acetate asymmetric membrane capsules (AMCs) of acyclovir for its controlled delivery at the absorption site. The AMCs were prepared by phase inversion technique using wet process. A 23 full factorial design assessed the effect of independent variables (level(s) of polymer, pore former, and osmogen) on the cumulative drug release from AMCs. The buoyant optimized formulation F7 (low level of cellulose acetate; high levels of both glycerol and sodium lauryl sulphate) displayed maximum drug release of in 8 h that was independent of variation in agitational intensity and intentional defect on the cellulose acetate AMC. The in vitro data best fitted zero-order kinetics (). SEM micrograph of the transverse section confirmed the asymmetric nature of the cellulose acetate capsular membrane. Statistical analysis by Design Expert software indicated no interaction between the independent variables confirming the efficiency of the design in estimating the effects of variables on drug release. The optimized formulation F7 (desirability = 0.871) displayed sustenance of drug release over the drug packed in AMC in pure state proving the superiority of osmotically active formulation. Conclusively the AMCs have potential for controlled release of acyclovir at its absorption site. Alka Sonkar, Anil Kumar, and Kamla Pathak Copyright © 2016 Alka Sonkar et al. All rights reserved. Xyloglucan Based In Situ Gel of Lidocaine HCl for the Treatment of Periodontosis Thu, 28 Jan 2016 08:14:46 +0000 The present study was aimed at formulating thermoreversible in situ gel of local anesthetic by using xyloglucan based mucoadhesive tamarind seed polysaccharide (TSP) into periodontal pocket. Temperature-sensitive in situ gel of lidocaine hydrochloride (LH) (2% w/v) was formulated by cold method. A full 32 factorial design was employed to study the effect of independent variables concentrations of Lutrol F127 and TSP to optimize in situ gel. The dependent variables evaluated were gelation temperature () and drug release (). The results revealed the surface pH of 6.8, similar to the pH of saliva. Viscosity study showed the marked increase in the viscosity of gel at 37°C due to sol-gel conversion. TSP was found to act as good mucoadhesive component to retain gel at the site of application in dental pocket. Gelation of formulation occurred near to body temperature. In vitro study depicted the fast onset of drug action but lasting the release (90%) till 2 h. Formulation F7 was considered as optimized batch, containing 18% Lutrol F127 and 1% tamarind seed polysaccharide. Thus, lidocaine hydrochloride thermoreversible in situ gel offered an alternative to painful injection therapy of anesthesia during dental surgery, with fast onset of anesthetic action lasting throughout the dental procedure. Ashlesha P. Pandit, Vaibhav V. Pol, and Vinit S. Kulkarni Copyright © 2016 Ashlesha P. Pandit et al. All rights reserved. Validation of a UV Spectrometric Method for the Assay of Tolfenamic Acid in Organic Solvents Thu, 10 Dec 2015 10:53:44 +0000 The present study has been carried out to validate a UV spectrometric method for the assay of tolfenamic acid (TA) in organic solvents. TA is insoluble in water; therefore, a total of thirteen commonly used organic solvents have been selected in which the drug is soluble. Fresh stock solutions of TA in each solvent in a concentration of 1 × 10−4 M (2.62 mg%) were prepared for the assay. The method has been validated according to the guideline of International Conference on Harmonization and parameters like linearity, range, accuracy, precision, sensitivity, and robustness have been studied. Although the method was found to be efficient for the determination of TA in all solvents on the basis of statistical data 1-octanol, followed by ethanol and methanol, was found to be comparatively better than the other studied solvents. No change in the stock solution stability of TA has been observed in each solvent for 24 hours stored either at room (°C) or at refrigerated temperature (2–8°C). A shift in the absorption maxima has been observed for TA in various solvents indicating drug-solvent interactions. The studied method is simple, rapid, economical, accurate, and precise for the assay of TA in different organic solvents. Sofia Ahmed, Nafeesa Mustaan, Muhammad Ali Sheraz, Syeda Ayesha Ahmed un Nabi, and Iqbal Ahmad Copyright © 2015 Sofia Ahmed et al. All rights reserved. Market Assessment and Product Evaluation of Probiotic Containing Dietary Supplements Available in Bangladesh Market Mon, 16 Nov 2015 14:27:53 +0000 Probiotics containing food supplements available in Bangladesh market were identified and collected for assessment. To assess their label claim, they were resuspended into sterile distilled water. Then, series dilutions of each sample solution were prepared and immediately plated out, in duplicate, into De Man Rogosa Sharpe (MRS) agar. These plates were then incubated at 37°C for 48 hours and colonies were counted. Viable cell numbers stated on the labels were compared with actual viable cell numbers. To assess the viability of the probiotics included in the products, probiotic strains were isolated from each of the four products and screened for inhibitory activity against six indicator strains. It was surprisingly found that although the viable cell numbers of all supplements were three to four log cycles lower than label claim of the products, however, this problem did not affect the inhibitory activity of the probiotic strains against indicator strains according to in vitro assessment. Legislation and regulation regarding prebiotic-probiotic containing products should be built up in Bangladesh to ensure quality products supply to the consumers. Moreover, manufacturers of probiotic containing products should take the responsibility for providing the consumer with scientifically and legally correct information. Anjuman Ara Begum, D. M. Jakaria, Sharif Md Anisuzzaman, Mahfuzul Islam, and Siraje Arif Mahmud Copyright © 2015 Anjuman Ara Begum et al. All rights reserved. Surface Deposition and Coalescence and Coacervation Phase Separation Methods: In Vitro Study and Compatibility Analysis of Eudragit RS30D, Eudragit RL30D, and Carbopol-PLA Loaded Metronidazole Microspheres Mon, 16 Nov 2015 13:58:05 +0000 Metronidazole (MTZ) has extremely broad spectrum of protozoal and antimicrobial activity and is clinically effective in trichomoniasis, amoebic colitis, and giardiasis. This study was performed to formulate and evaluate the MTZ loaded microspheres by coacervation phase separation and surface deposition and coalescence methods using different polymers like Gelatin, Carbopol 934P, Polylactic Acid (PLA), Eudragit RS30D, and Eudragit RL30D to acquire sustained release of drug. In vitro dissolution studies were carried out in phosphate buffer (pH 7.4) for 8 hours according to USP paddle method. The maximum and minimum release of MTZ from microspheres observed were 84.81% and 76.6% for coacervation and 95.07% and 80.07% for surface deposition method, respectively, after 8 hours. Release kinetics was studied in different mathematical release models. The SEM and FTIR studies confirm good spheres and smooth surface as well as interaction between drug and polymers. Though release kinetic is uncertain, the best fit was obtained with the Korsmeyer kinetic model with release exponent () lying between 0.45 and 0.89. In vitro studies showed that MTZ microspheres with different polymers might be a good candidate as sustained drug delivery system to treat bacterial infections. Irin Dewan, Md. Maynul Islam, Maksud Al-Hasan, Joydeb Nath, Sefat Sultana, and Md. Sohel Rana Copyright © 2015 Irin Dewan et al. All rights reserved. Enhancement of Solubility of Lamotrigine by Solid Dispersion and Development of Orally Disintegrating Tablets Using 32 Full Factorial Design Tue, 27 Oct 2015 09:56:15 +0000 Present investigation deals with the preparation and evaluation of orally disintegrating tablets (ODTs) of lamotrigine using β-cyclodextrin and PVP-K30 as polymers for the preparation of solid dispersion which help in enhancement of aqueous solubility of this BCS CLASS-II drug and sodium starch glycolate (SSG) and crospovidone as a superdisintegrating agent, to reduce disintegration time. The ODTs were prepared by direct compression method. Nine formulations were developed with different ratios of superdisintegrating agents. All the formulations were evaluated for disintegration time, weight variation, hardness, friability, drug content uniformity, wetting time, and in vitro drug release study. In vitro drug release study was performed using United States Pharmacopoeia (USP) type 2 dissolution test apparatus employing paddle stirrer at 50 rpm using 900 mL of 0.1 N HCl maintained at 37°C ± 0.5°C as the dissolution medium. On the basis of evaluation parameters formulations were prepared using β-CD 1 : 1 solid dispersion. Then 32 full factorial design was applied using SSG and crospovidone in different ratios suggested by using design expert and optimized formulation was prepared using amount of SSG and crospovidone as suggested by the software. The optimized formulation prepared had disintegrating time of 15 s, wetting time of 24 s, and % friability of 0.55. Jatinderpal Singh, Rajeev Garg, and Ghanshyam Das Gupta Copyright © 2015 Jatinderpal Singh et al. All rights reserved. Development of Budesonide Loaded Biopolymer Based Dry Powder Inhaler: Optimization, In Vitro Deposition, and Cytotoxicity Study Sun, 15 Jun 2014 11:00:36 +0000 The progress in the development of DPI technology has boosted the use of sensitive drug molecules for lung diseases. However, delivery of these molecules from conventional DPI to the active site still poses a challenge with respect to deposition efficiency in the lung. At same time, serious systemic side effects of drugs have become a cause for concern. The developed budesonide loaded biopolymer based controlled release DPI had shown maximum in vitro lung deposition with least toxicity. The subject of present study, lactose-free budesonide loaded biopolymer based DPI, further corroborates the great potential of antiasthmatic drugs. This technology is expected to revolutionize the approaches towards enhanced therapeutic delivery of prospective drugs. Ashwin J. Mali, Atmaram P. Pawar, and Ravindra N. Purohit Copyright © 2014 Ashwin J. Mali et al. All rights reserved.