Journal of Pharmaceutics The latest articles from Hindawi Publishing Corporation © 2016 , Hindawi Publishing Corporation . 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. Lipid-Based Drug Delivery Systems Mon, 19 May 2014 09:02:21 +0000 The principle objective of formulation of lipid-based drugs is to enhance their bioavailability. The use of lipids in drug delivery is no more a new trend now but is still the promising concept. Lipid-based drug delivery systems (LBDDS) are one of the emerging technologies designed to address challenges like the solubility and bioavailability of poorly water-soluble drugs. Lipid-based formulations can be tailored to meet a wide range of product requirements dictated by disease indication, route of administration, cost consideration, product stability, toxicity, and efficacy. These formulations are also a commercially viable strategy to formulate pharmaceuticals, for topical, oral, pulmonary, or parenteral delivery. In addition, lipid-based formulations have been shown to reduce the toxicity of various drugs by changing the biodistribution of the drug away from sensitive organs. However, the number of applications for lipid-based formulations has expanded as the nature and type of active drugs under investigation have become more varied. This paper mainly focuses on novel lipid-based formulations, namely, emulsions, vesicular systems, and lipid particulate systems and their subcategories as well as on their prominent applications in pharmaceutical drug delivery. Hina Shrestha, Rajni Bala, and Sandeep Arora Copyright © 2014 Hina Shrestha et al. All rights reserved. Emerging Trends in Noninvasive Insulin Delivery Wed, 14 May 2014 07:16:50 +0000 This paper deals with various aspects of oral insulin delivery system. Insulin is used for the treatment of diabetes mellitus, which is characterized by the elevated glucose level (above the normal range) in the blood stream, that is, hyperglycemia. Oral route of administration of any drug is the most convenient route. Development of oral insulin is still under research. Oral insulin will cause the avoidance of pain during the injection (in subcutaneous administration), anxiety due to needle, and infections which can be developed. Different types of enzyme inhibitors, like sodium cholate, camostat, mesilate, bacitracin, leupeptin, and so forth, have been used to prevent insulin from enzymatic degradation. Subcutaneous route has been used for administration of insulin, but pain and itching at the site of administration can occur. That is why various alternative routes of insulin administration like oral route are under investigation. In this paper authors summarized advancement in insulin delivery with their formulation aspects. Arun Verma, Nitin Kumar, Rishabha Malviya, and Pramod Kumar Sharma Copyright © 2014 Arun Verma et al. All rights reserved. Formulation and Evaluation of Multilayered Tablets of Pioglitazone Hydrochloride and Metformin Hydrochloride Mon, 12 May 2014 12:49:57 +0000 In the treatment of type 2 diabetes mellitus a continuous therapy is required which is a more complex one. As in these patients there may be a defect in both insulin secretion and insulin action exists. Hence, the treatment depends on the pathophysiology and the disease state. In the present study, multilayered tablets of pioglitazone hydrochloride 15 mg and metformin hydrochloride 500 mg were prepared in an attempt for combination therapy for the treatment of type 2 diabetes mellitus. Pioglitazone HCl was formulated as immediate release layer to show immediate action by direct compression method using combination of superdisintegrants, namely, crospovidone and avicel PH 102. Crospovidone at 20% concentration showed good drug release profile at 2 hrs. Metformin HCl was formulated as controlled release layer to prolong the drug action by incorporating hydrophilic polymers such as HPMC K4M by direct compression method and guar gum by wet granulation method in order to sustain the drug release from the tablets and maintain its integrity so as to provide a suitable formulation. The multilayered tablets were prepared after carrying out the optimization of immediate release layer and were evaluated for various precompression and postcompression parameters. Formulation F13 showed 99.97% of pioglitazone release at 2 hrs in 0.1 N HCl and metformin showed 98.81% drug release at 10 hrs of dissolution in 6.8 pH phosphate buffer. The developed formulation is equivalent to innovator product in view of in vitro drug release profile. The results of all these evaluation tests are within the standards. The procedure followed for the formulation of these tablets was found to be reproducible and all the formulations were stable after accelerated stability studies. Hence, multilayered tablets of pioglitazone HCl and metformin HCl can be a better alternative way to conventional dosage forms. Y. Ankamma Chowdary, Ramakrishna Raparla, and Muramshetty Madhuri Copyright © 2014 Y. Ankamma Chowdary et al. All rights reserved. Design and Evaluation of Voriconazole Eye Drops for the Treatment of Fungal Keratitis Wed, 30 Apr 2014 00:00:00 +0000 Voriconazole is a novel antifungal agent with excellent broad spectrum activity commercially available for oral and intravenous administration. The purpose of this study was to prepare ophthalmic formulation of hydroxypropyl beta cyclodextrin (HP--CD) based voriconazole containing benzalkonium chloride BAK and EDTA with or without viscosity modifiers and study its permeation characteristics through freshly excised goat cornea. The results were observed that viscosity and force of bioadhesion of the voriconazole HP--CD solutions containing xanthan gum (XG) are more as compared to polyvinyl alcohol. The results revealed that voriconazole drop containing PVA provided least viscosity and higher corneal permeation of drug, while drop formulated with XG had maximum viscosity and least permeation. The HP--CD based voriconazole (1.5%) ophthalmic formulation containing xanthan gum (1.5), preserved with BAK and EDTA, could provide shelf life of 2 years. The microbiological studies showed that voriconazole ophthalmic solution containing xanthan gum shows better antifungal activity as compared to voriconazole and xanthan gum alone. Thus, it can be concluded that HP--CD based voriconazole (1.5%, pH 7.0) ophthalmic solution containing BAK and EDTA with viscosity modifier XG provided maximum precorneal residence time as compared to other viscosity modifiers and polyvinyl alcohol provided less precorneal residence time than other viscosity modifiers. Sakshi Malhotra, Anubha Khare, Kanchan Grover, Inderbir Singh, and Pravin Pawar Copyright © 2014 Sakshi Malhotra et al. All rights reserved. FDA-Approved Natural Polymers for Fast Dissolving Tablets Sun, 27 Apr 2014 09:17:26 +0000 Oral route is the most preferred route for administration of different drugs because it is regarded as safest, most convenient, and economical route. Fast disintegrating tablets are very popular nowadays as they get dissolved or facilely disintegrated in mouth within few seconds of administration without the need of water. The disadvantages of conventional dosage form, especially dysphagia (arduousness in swallowing), in pediatric and geriatric patients have been overcome by fast dissolving tablets. Natural materials have advantages over synthetic ones since they are chemically inert, non-toxic, less expensive, biodegradable and widely available. Natural polymers like locust bean gum, banana powder, mango peel pectin, Mangifera indica gum, and Hibiscus rosa-sinenses mucilage ameliorate the properties of tablet and utilized as binder, diluent, and superdisintegrants increase the solubility of poorly water soluble drug, decrease the disintegration time, and provide nutritional supplement. Natural polymers are obtained from the natural origin and they are cost efficacious, nontoxic, biodegradable, eco-friendly, devoid of any side effect, renewable, and provide nutritional supplement. It is proved from the studies that natural polymers are more safe and efficacious than the synthetic polymers. The aim of the present article is to study the FDA-approved natural polymers utilized in fast dissolving tablets. Md Tausif Alam, Nayyar Parvez, and Pramod Kumar Sharma Copyright © 2014 Md Tausif Alam et al. All rights reserved. Preparation and In Vitro Evaluation of Ethylcellulose and Polymethacrylate Resins Loaded Microparticles Containing Hydrophilic Drug Thu, 10 Apr 2014 14:13:02 +0000 Objective. The purpose of the recent study was to prepare and estimate sustained release of Ethylcellulose (300 cps) and Eudragit (RS 100 and RL 100) microparticles containing Propranolol hydrochloride used as a treatment of cardiovascular system, especially hypertension. Method. Propranolol hydrochloride was microencapsulated with different polymers (Ethylcellulose, Eudragit RS, and Eudragit RL) using modified hydrophobic (O/O) solvent evaporation method using 1 : 1 combination of acetone and isopropanol as the internal phase. Obtained microparticles were showing higher batch yield with higher encapsulation efficiency. Microparticles were prepared with different ratios of 1 : 1, 1 : 3, 1 : 5, and 1 : 7 (%, wt/wt) using span 80 (%, v/v) as a surfactant. Results. The influence of formulation factors like drug: polymer ratio, internal phase, and type of polymers on obtained microparticles was characterized with respect to particle size distribution, encapsulation efficiency, percentage yield, FTIR, and FE-SEM. Higher encapsulation efficiencies were obtained with various polymers like Ethylcellulose (96.63 ± 0.5) compared to Eudragit RS 100 (83.70 ± 0.6) and RL 100 (89.62 ± 0.6). The in vitro release study was characterized by initial burst. Conclusion. The result of study displays that Ethylcellulose and Eudragit loaded microparticles of Propranolol hydrochloride can be effectively prepared using modified hydrophobic emulsification solvent evaporation technique. Therefore, the modified hydrophobic emulsion technique can also be applied to the preparation of microparticles for low molecular weight and highly water soluble drugs. Satish Pandav and Jitendra Naik Copyright © 2014 Satish Pandav and Jitendra Naik. All rights reserved. Solubility Enhancement of Budesonide and Statistical Optimization of Coating Variables for Targeted Drug Delivery Thu, 10 Apr 2014 07:41:54 +0000 The purpose of the research was to present Budesonide (BUD) as a novel formulation showing improved aqueous solubility, which may decrease variability in and found in inflammatory bowel disease (IBD) patients, and drug targeting to colon. To improve aqueous solubility, solid dispersion (SD) of the BUD with poloxamer 188 was prepared by melting method. Physical characterization of solid dispersion was performed. The SD was used to prepare tablet equivalent to 9 mg of BUD. The tablet was coated with enteric polymers Eudragit S100 and Eudragit L100 to target colon. The ratio of polymers and percentage coating was optimized using statistical design. Variables studied in design were ratio of enteric polymers and the effect of percentage coating on in vitro drug release. Dissolution at different pH showed that drug release in colon could be modified by optimizing the ratio of polymers and percentage coating. The dissolution data showed that the percentage coating and ratio of polymers are very important to get lag time and optimum formulation. The optimized batch from statistical design was kept under accelerated condition for three months. After accelerated stability study, there was no significant change in the drug release. Himanshu Bhatt, Bhargavi Naik, and Abhay Dharamsi Copyright © 2014 Himanshu Bhatt et al. All rights reserved. Recently Investigated Natural Gums and Mucilages as Pharmaceutical Excipients: An Overview Mon, 07 Apr 2014 08:19:01 +0000 Due to advances in drug delivery technology, currently, excipients are included in novel dosage forms to fulfil specific functions and in some cases they directly or indirectly influence the extent and/or rate of drug release and drug absorption. Recent trends towards use of plant based and natural products demand the replacement of synthetic additives with natural ones. Today, the whole world is increasingly interested in natural drugs and excipients. These natural materials have many advantages over synthetic ones as they are chemically inert, nontoxic, less expensive, biodegradable, and widely available. This review discusses majority of the plant-derived polymeric compounds (gums and mucilage’s), their sources, chemical constituents, uses, and some recent investigations as excipients in novel drug delivery systems. Pritam Dinesh Choudhary and Harshal Ashok Pawar Copyright © 2014 Pritam Dinesh Choudhary and Harshal Ashok Pawar. All rights reserved.