Vicki Strugala, Peter W Dettmar, Edward C M Thomas
{"title":"Evaluation of an Innovative Over-the-Counter Treatment for Symptoms of Reflux Disease: Quick-Dissolving Alginate Granules.","authors":"Vicki Strugala, Peter W Dettmar, Edward C M Thomas","doi":"10.5402/2012/950162","DOIUrl":"https://doi.org/10.5402/2012/950162","url":null,"abstract":"<p><p>Traditional antacids and alginate-based reflux suppressants are OTC products commonly used to treat reflux symptoms. There has been a lack of innovation of new formulations in this therapy area despite consumers finding established products unpalatable. Here we evaluate a novel product formulation which takes the form of quick-dissolving alginate granules in single-dose sachets (Gaviscon Direct Powder (GDP)). Market research and taste evaluation confirmed that reflux sufferers considered GDP to have good flavour and taste, no chalky aftertaste and dissolved rapidly in the mouth with 68% noting so within 10 seconds. GDP was considered convenient and easy to use. The consumer-driven product development was also shown to form a strong alginate raft in standardised in vitro conditions that met the specifications of the BP monograph (raft strength > 7.5 g). Gastric retention of GDP and a test meal was investigated in healthy volunteers using gamma scintigraphy in comparison to Liquid Gaviscon. Both products formed an alginate raft in the stomach above the test meal and emptied after the meal. The gastric retention of the GDP product was found to be noninferior to Liquid Gaviscon. In conclusion, the innovative GDP product formed an effective raft and was well liked by consumers.</p>","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":"2012 ","pages":"950162"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2012/950162","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9433088","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Jadupati Malakar, Amit Kumar Nayak, Soumita Goswami
{"title":"Use of response surface methodology in the formulation and optimization of bisoprolol fumarate matrix tablets for sustained drug release.","authors":"Jadupati Malakar, Amit Kumar Nayak, Soumita Goswami","doi":"10.5402/2012/730624","DOIUrl":"https://doi.org/10.5402/2012/730624","url":null,"abstract":"<p><p>The aim of this investigation was to develop and optimize bisoprolol fumarate matrix tablets for sustained release application by response surface methodology based on 2(3) factorial design. The effects of the amounts of calcium alginate, HPMC K4M, and Carbopol 943 in bisoprolol fumarate matrix tablets on the properties of bisoprolol fumarate sustained release matrix tablets like drug release and hardness were analyzed and optimized. The observed responses were coincided well with the predicted values by the experimental design. The optimized bisoprolol fumarate matrix tablets showed prolonged sustained release of bisoprolol fumarate over 6 hours. These matrix tablets followed the first-order model with anomalous (non-Fickian) diffusion mechanism.</p>","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":"2012 ","pages":"730624"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2012/730624","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9433093","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Dimitrios Bitounis, Raphaelle Fanciullino, Athanassios Iliadis, Joseph Ciccolini
{"title":"Optimizing Druggability through Liposomal Formulations: New Approaches to an Old Concept.","authors":"Dimitrios Bitounis, Raphaelle Fanciullino, Athanassios Iliadis, Joseph Ciccolini","doi":"10.5402/2012/738432","DOIUrl":"https://doi.org/10.5402/2012/738432","url":null,"abstract":"<p><p>Developing innovative delivery strategies remains an ongoing task to improve both efficacy and safety of drug-based therapy. Nanomedicine is now a promising field of investigation, rising high expectancies for treating various diseases such as malignancies. Putting drugs into liposome is an old story that started in the late 1960s. Because of the near-total biocompatibility of their lipidic bilayer, liposomes are less concerned with the safety issue related to the possible long-term accumulation in the body of most nanoobjects currently developed in nanomedicine. Additionally, novel techniques and recent efforts to achieve better stability (e.g., through sheddable coating), combined with a higher selectivity towards target cells (e.g., by anchoring monoclonal antibodies or incorporating phage fusion protein), make new liposomal drugs an attractive and challenging opportunity to improve clinical outcome in a variety of disease. This review covers the physicochemistry of liposomes and the recent technical improvements in the preparation of liposome-encapsulated drugs in regard to the scientific and medical stakes.</p>","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":"2012 ","pages":"738432"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2012/738432","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9375781","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Studies on the Cytotoxic Activities of Punica granatum L. var. spinosa (Apple Punice) Extract on Prostate Cell Line by Induction of Apoptosis.","authors":"Koushan Sineh Sepehr, Behzad Baradaran, Masoumeh Mazandarani, Vahid Khori, Fatemeh Zare Shahneh","doi":"10.5402/2012/547942","DOIUrl":"https://doi.org/10.5402/2012/547942","url":null,"abstract":"<p><p>The Punica granatum L. var. granatum (pomegranate) has been demonstrated to exert antitumor effects on various types of cancer cells. The present study aimed to evaluate the medicinal herbs Punica granatum L. var. spinosa (apple punice) that are native to Iran. This study was determined to test the possible cytotoxic activity and induction of apoptosis on human prostate cell lines. The effect of ethanol extracts of the herbs on the inhibition of cell proliferation was assessed by MTT colorimetric assay. PC3 cell lines treated with the extracts were analyzed for the induction of apoptosis by cell death detection (ELISA) and TUNEL assay. Dye exclusion analysis was performed for viability rate. Our results demonstrated that the Punica granatum L. var. spinosa extract dose dependently suppressed the proliferation of PC3 cells (IC(50)= 250.21 μg/mL) when compared with a chemotherapeutic anticancer drug (Toxol) (Vesper Pharmaceuticals) with increased nucleosome production from apoptotic cells. The Punica granatum L. var. spinosa extract attenuated the human prostate cell proliferation in vitro possibly by inducing apoptosis. The Punica granatum L. var. spinosa is likely to be valuable for the treatment of some forms of human prostate cell line.</p>","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":"2012 ","pages":"547942"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2012/547942","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9376767","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Microemulsion drug delivery system: for bioavailability enhancement of ampelopsin.","authors":"Shailendra Singh Solanki, Brajesh Sarkar, Rakesh Kumar Dhanwani","doi":"10.5402/2012/108164","DOIUrl":"https://doi.org/10.5402/2012/108164","url":null,"abstract":"<p><p>Ampelopsin, one of the most common flavonoids, reported to possess numerous pharmacological activities and shows poor aqueous solubility. The purpose of this study was to enhance the dissolution rate and bioavailability of this drug by developing a novel delivery system that is microemulsion (ME) and to study the effect of microemulsion (ME) on the oral bioavailability of ampelopsin. Capmul MCM-based ME formulation with Cremophor EL as surfactant and Transcutol as cosurfactant was developed for oral delivery of ampelopsin. Optimised ME was evaluated for its transparency, viscosity, percentage assay and so forth. Solubilisation capacity of the ME system was also determined. The prepared ME was compared with the pure drug solution and commercially available tablet for in vitro drug release. The optimised ME formulation containing ampelopsin, Capmul MCM (5.5%), Cremophor EL (25%), Transcutol P (8.5%), and distilled water showed higher in vitro drug release, as compared to plain drug suspension and the suspension of commercially available tablet. These results demonstrate the potential use of ME for improving the bioavailability of poor water soluble compounds, such as ampelopsin.</p>","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":"2012 ","pages":"108164"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2012/108164","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9380470","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
ISRN PharmaceuticsPub Date : 2012-01-01Epub Date: 2012-03-07DOI: 10.5402/2012/369270
Christian Jreyssaty, Qin Shi, Huijie Wang, Xingping Qiu, Françoise M Winnik, Xiaoling Zhang, Kerong Dai, Mohamed Benderdour, Julio C Fernandes
{"title":"Efficient Nonviral Gene Therapy Using Folate-Targeted Chitosan-DNA Nanoparticles In Vitro.","authors":"Christian Jreyssaty, Qin Shi, Huijie Wang, Xingping Qiu, Françoise M Winnik, Xiaoling Zhang, Kerong Dai, Mohamed Benderdour, Julio C Fernandes","doi":"10.5402/2012/369270","DOIUrl":"https://doi.org/10.5402/2012/369270","url":null,"abstract":"<p><p>Nonviral cationic polymers like chitosan can be combined with DNA to protect it from degradation. The chitosan is a biocompatible, biodegradable, nontoxic, and cheap polycationic polymer with low immunogenicity. The objective of this study was to synthesize and then assess different chitosan-DNA nanoparticles and to select the best ones for selective in vitro transfection in human epidermoid carcinoma (KB) cell lines. It revealed that different combinations of molecular weight, the presence or absence of folic acid ligand, and different plasmid DNA sizes can lead to nanoparticles with various diameters and diverse transfection efficiencies. The intracellular trafficking, nuclear uptake, and localization are also studied by confocal microscopy, which confirmed that DNA was delivered to cell nuclei to be expressed.</p>","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":" ","pages":"369270"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2012/369270","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30551402","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Elham Khodaverdi, Ali Golmohammadian, Seyed Ahmad Mohajeri, Gholamhossein Zohuri, Farnaz Sadat Mirzazadeh Tekie, Farzin Hadizadeh
{"title":"Biodegradable In Situ Gel-Forming Controlled Drug Delivery System Based on Thermosensitive Poly(ε-caprolactone)-Poly(ethylene glycol)-Poly(ε-caprolactone) Hydrogel.","authors":"Elham Khodaverdi, Ali Golmohammadian, Seyed Ahmad Mohajeri, Gholamhossein Zohuri, Farnaz Sadat Mirzazadeh Tekie, Farzin Hadizadeh","doi":"10.5402/2012/976879","DOIUrl":"https://doi.org/10.5402/2012/976879","url":null,"abstract":"<p><p>Traditional drug delivery systems which are based on multiple dosing regimens usually pose many disadvantages such as poor compliance of patients and drug plasma level variation. To overcome the obstacles of traditional drug formulations, novel drug delivery system PCL-PEG-PCL hydrogels have been purposed in this study. Copolymers were synthesized by rapid microwave-assisted and conventional synthesis methods. Polymer characterizations were done using gel permeation chromatography and (1)H-NMR. Phase transition behavior was evaluated by inverting tube method and in vitro drug release profile was determined using naltrexone hydrochloride and vitamin B(12) as drug models. The results indicated that loaded drug structure and copolymer concentration play critical roles in release profile of drugs from these hydrogels. This study also confirmed that synthesis of copolymer using microwave is the most effective method for synthesis of this kind of copolymer.</p>","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":"2012 ","pages":"976879"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2012/976879","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9729463","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Ketan T Savjani, Anuradha K Gajjar, Jignasa K Savjani
{"title":"Drug solubility: importance and enhancement techniques.","authors":"Ketan T Savjani, Anuradha K Gajjar, Jignasa K Savjani","doi":"10.5402/2012/195727","DOIUrl":"https://doi.org/10.5402/2012/195727","url":null,"abstract":"<p><p>Solubility, the phenomenon of dissolution of solute in solvent to give a homogenous system, is one of the important parameters to achieve desired concentration of drug in systemic circulation for desired (anticipated) pharmacological response. Low aqueous solubility is the major problem encountered with formulation development of new chemical entities as well as for the generic development. More than 40% NCEs (new chemical entities) developed in pharmaceutical industry are practically insoluble in water. Solubility is a major challenge for formulation scientist. Any drug to be absorbed must be present in the form of solution at the site of absorption. Various techniques are used for the enhancement of the solubility of poorly soluble drugs which include physical and chemical modifications of drug and other methods like particle size reduction, crystal engineering, salt formation, solid dispersion, use of surfactant, complexation, and so forth. Selection of solubility improving method depends on drug property, site of absorption, and required dosage form characteristics.</p>","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":"2012 ","pages":"195727"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2012/195727","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9368092","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Development and evaluation of sustained release tablet of betahistine hydrochloride using ion exchange resin tulsion t344.","authors":"Vijay D Wagh, Nilesh Pawar","doi":"10.5402/2012/438342","DOIUrl":"https://doi.org/10.5402/2012/438342","url":null,"abstract":"<p><p>An attempt was made to sustain the release of Betahistine hydrochloride by complexation technique using strong cation-exchange resin, Tulsion T344. The drug loading onto ion-exchange resin was optimized for mixing time, activation, effect of pH, swelling time, ratio of drug : resin, and temperature. The resinate was evaluated for micromeritic properties and characterized using XRPD and IR. For resinate sustained release tablets were formulated using hydoxypropyl methylcellulose K100M. The tablets were evaluated for hardness, thickness, friability, drug content, weight variation, and in vitro drug release. Tablets thus formulated (Batch T-3) provided sustained release of drug over a period of 12 h. The release of Betahistine HCl from resinate controls the diffusion of drug molecules through the polymeric material into aqueous medium. Results showed that Betahistine HCl was formulated into a sustained dosage form as an alternative to the conventional tablet.</p>","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":"2012 ","pages":"438342"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2012/438342","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9374992","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Effects of Aqueous Extract of Fresh Leaves of Abroma augusta L. on Oral Absorption of Glucose and Metformin Hydrochloride in Experimental Rats.","authors":"Tariqul Islam, Ajijur Rahman, Anwar Ul Islam","doi":"10.5402/2012/472586","DOIUrl":"https://doi.org/10.5402/2012/472586","url":null,"abstract":"<p><p>To get better control in disease conditions, many people take herbs with conventional medicines, therefore, posing a risk of potential pharmacokinetic interactions between herbs and conventional drugs. The aqueous extract of the fresh leaves of Abroma augusta L. (Family: Sterculiaceae, Bengali name: Ulatkambal, English name: Devil's cotton, DC) is viscous and used traditionally to treat diabetes mellitus. This study was done to investigate the probable mechanism by which the aqueous extract of Abroma augusta L. is beneficial in managing type 2 DM and to observe the effects of this extract on absorption of metformin hydrochloride from the gastrointestinal tract. Studies were conducted in healthy Long Evans rats using Na-carboxymethyl cellulose (CMC) as positive control. Both Na-CMC and WSF of DC significantly (P < 0.05) reduced the absorption of glucose administered orally in fasted rats. On the other hand, WSF of DC significantly (P < 0.05) reduced the absorption of metformin hydrochloride in alloxan-induced diabetic rats. The results of this study suggest that WSF of DC may be beneficial in diabetic patients to improve glycemic control but should not be coadministered with metformin HCl for management of type 2 diabetes mellitus.</p>","PeriodicalId":14802,"journal":{"name":"ISRN Pharmaceutics","volume":"2012 ","pages":"472586"},"PeriodicalIF":0.0,"publicationDate":"2012-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5402/2012/472586","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9368096","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}