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Ian P Harrison, Fabrizio Spada
Wound management, in addition to presenting a significant burden to patients and their families, also contributes significantly to a country’s healthcare costs. Treatment strategies are numerous, but in most cases not ideal. Hydrogels, three-dimensional polymeric materials that can withstand a great degree of swelling without losing structural integrity, are drawing great attention for their use as topical wound management solutions in the form of films and as vehicles for drug delivery, due to their unique properties of high water content, biocompatibility, and flexibility...
June 14, 2018: Pharmaceutics
Yuki Shirosaki, Motomasa Furuse, Takuji Asano, Yoshihiko Kinoshita, Toshihiko Kuroiwa
Burr holes in craniotomy are not self-repairing bone defects. To regenerate new bone at the sites of these defects, a good scaffold is required. Biodegradable hybrids including silica or siloxane networks have been investigated as bone tissue scaffolds. This study examined skull bone regeneration using chitosan-siloxane hybrids after long-term implantation (two and three years). After implantation of the hybrids, the surrounding cells migrated and formed fibrous tissues and blood vessels. Then, bone formation occurred from the surrounding blood vessels...
June 8, 2018: Pharmaceutics
Seok-Ho Shin, Min-Ho Park, Jin-Ju Byeon, Byeong Ill Lee, Yuri Park, Ah-Ra Ko, Mi-Ran Seong, Soyeon Lee, Mi Ra Kim, Jinwook Seo, Myung Eun Jung, Dong-Kyu Jin, Young G Shin
Fabry disease is a rare lysosomal storage disorder resulting from the lack of α-Gal A gene activity. Globotriaosylceramide (GB3, ceramide trihexoside) is a novel endogenous biomarker which predicts the incidence of Fabry disease. At the early stage efficacy/biomarker study, a rapid method to determine this biomarker in plasma and in all relevant tissues related to this disease simultaneously is required. However, the limited sample volume, as well as the various levels of GB3 in different matrices makes the GB3 quantitation very challenging...
June 7, 2018: Pharmaceutics
Sushma V Lute, Ranjit M Dhenge, Agba D Salman
Lactose and mannitol are some of the most commonly used powders in the pharmaceutical industry. The limited research published so far highlights the effects of process and formulation parameters on the properties of the granules and the tablets produced using these two types of powders separately. However, the comparison of the performance of these two types of powders during twin screw wet granulation has received no attention. The present research is focused on understanding the granulation mechanism of different grades of two pharmaceutical powders with varying properties (i...
June 2, 2018: Pharmaceutics
Sushma V Lute, Ranjit M Dhenge, Agba D Salman
This paper focuses on investigating the influence of varying barrel fill levels on the mean residence time, granule properties (median size, size distribution, and shape), and tensile strength of tablets. Specific feed load (SFL) (powder feed rate divided by screw speed) and powder feed number (PFN) (i.e., powder mass flow rate divided by the product of screw speed, screw diameter, and the material density in the denominator) were considered as surrogates for the barrel fill level. Two type of powders (lactose and microcrystalline cellulose (MCC)) were granulated separately at varying fill levels at different liquid-to-solid ratios (L/S)...
June 1, 2018: Pharmaceutics
Andrea Luaces-Rodríguez, Miguel González-Barcia, María José Blanco-Teijeiro, María Gil-Martínez, Francisco Gonzalez, Francisco Gómez-Ulla, María-Jesús Lamas, Francisco-Javier Otero-Espinar, Anxo Fernández-Ferreiro
Although intravitreal administration of anti-infectives represents the standard treatment for infectious endophthalmitis, the knowledge about their pharmacokinetics is still limited. In this review, we aimed to summarise the factors influencing the pharmacokinetics of the anti-infective agents. We have conducted a comprehensive review of the preclinical pharmacokinetic parameters obtained in different studies of intravitreal injections of anti-infectives performed on animals, mainly rabbits. The two aspects with the biggest influence on pharmacokinetics are the distribution in the vitreous humour and the elimination through the posterior segment...
May 29, 2018: Pharmaceutics
Md Emranul Karim, Kyi Kyi Tha, Iekhsan Othman, Mohammad Borhan Uddin, Ezharul Hoque Chowdhury
RNA Interference (RNAi) has brought revolutionary transformations in cancer management in the past two decades. RNAi-based therapeutics including siRNA and shRNA have immense scope to silence the expression of mutant cancer genes specifically in a therapeutic context. Although tremendous progress has been made to establish catalytic RNA as a new class of biologics for cancer management, a lot of extracellular and intracellular barriers still pose a long-lasting challenge on the way to clinical approval. A series of chemically suitable, safe and effective viral and non-viral carriers have emerged to overcome physiological barriers and ensure targeted delivery of RNAi...
May 26, 2018: Pharmaceutics
Okky Dwichandra Putra, Daiki Umeda, Eriko Fujita, Tamami Haraguchi, Takahiro Uchida, Etsuo Yonemochi, Hidehiro Uekusa
Benexate, a drug used clinically as a defensive type anti-ulcer agent, has poor solubility and a bitter taste. To improve its solubility, a crystal engineering approach was proposed with the formation of novel salts using an artificial sweetener as a salt co-former. This was also expected to address the bitter taste of the drug. In this work, we report on the preparation and evaluation of the physicochemical properties of the novel salts benexate saccharinate monohydrate and benexate cyclamate whose crystal structures were determined by single-crystal X-ray structure analysis...
May 26, 2018: Pharmaceutics
Wejdan Al-Shakarchi, Ali Alsuraifi, Anthony Curtis, Clare Hoskins
Liver cancer treatments are often hindered by poor drug physicochemical properties, hence there is a need for improvement in order to increase patient survival and outlook. Combination therapies have been studied in order to evaluate whether increased overall efficacy can be achieved. This study reports the combined treatment of liver cancer cells with a combination treatment of chemotherapeutic agent paclitaxel and pro-apoptotic protein cytochrome C. In order to administer both agents in a single formulation, a poly(allylamine)-based amphiphile has been fabricated with the incorporation of a hybrid iron oxide-gold nanoparticle into its structure...
May 26, 2018: Pharmaceutics
Yuri Park, Nahye Kim, Jangmi Choi, Min-Ho Park, Byeong Ill Lee, Seok-Ho Shin, Jin-Ju Byeon, Young G Shin
A liquid chromatography⁻quadrupole time-of-flight (Q-TOF) mass spectrometric method was developed for early-stage research on adalimumab in rats. The method consisted of immunoprecipitation followed by tryptic digestion for sample preparation and LC-QTOF-MS/MS analysis of specific signature peptides of adalimumab in the positive ion mode using electrospray ionization. This specific signature peptide is derived from the complementarity-determining region (CDR) of adalimumab. A quadratic regression (weighted 1/concentration), with an equation y = ax² + bx + c, was used to fit calibration curves over the concentration range of 1⁻100 μg/mL for adalimumab...
May 24, 2018: Pharmaceutics
Chung-Wei Kao, Po-Ting Wu, Mei-Yi Liao, I-Ju Chung, Kai-Chien Yang, Wen-Yih Isaac Tseng, Jiashing Yu
Atherosclerosis is a multifactorial inflammatory disease that may progress silently for long period, and it is also widely accepted as the main cause of cardiovascular diseases. To prevent atherosclerotic plaques from generating, imaging early molecular markers and quantifying the extent of disease progression are desired. During inflammation, circulating monocytes leave the bloodstream and migrate into incipient lipid accumulation in the artery wall, following conditioning by local growth factors and proinflammatory cytokines; therefore, monocyte accumulation in the arterial wall can be observed in fatty streaks, rupture-prone plaques, and experimental atherosclerosis...
May 24, 2018: Pharmaceutics
Hiroyuki Takabe, Zachary N Warnken, Yajie Zhang, Daniel A Davis, Hugh D C Smyth, John G Kuhn, Steve Weitman, Robert O Williams Iii
Glioblastoma multiforme (GBM) is the most common and lethal central nervous system tumor. Recently, atovaquone has shown inhibition of signal transducer and activator transcription 3, a promising target for GBM therapy. However, it is currently unable to achieve therapeutic drug concentrations in the brain with the currently reported and marketed formulations. The present study sought to explore the efficacy of atovaquone against GBM as well as develop a formulation of atovaquone that would improve oral bioavailability, resulting in higher amounts of drug delivered to the brain...
May 19, 2018: Pharmaceutics
Nataliia Melnichuk, Vladimir Zarubaev, Iaryna Iosyk, Mychaylo Andreychyn, Larisa Semernikova, Zenoviy Tkachuk
Oligoribonucleotides-D-mannitol (ORNs-D-M) complexes possess antiviral, anti-inflammatory, and immunomodulatory actions. The aim of the present study was to evaluated an antiviral effect of ORNs-D-M against parainfluenza virus type 3 (PIV3); influenza CA709, PR834; avian influenza virus H5N2 (AIV) in vitro by a TCID50 ; hemadsorption and neuraminidase activity assays; and clinical efficiency of ORNs-D-M in patients with acute respiratory infections (ARIs) of various etiologies by PCR assay and AmpliSens test systems...
May 19, 2018: Pharmaceutics
Matthias E Lauer, Reto Maurer, Anne T De Paepe, Cordula Stillhart, Laurence Jacob, Rajesh James, Yuki Kojima, Rene Rietmann, Tom Kissling, Joost A van den Ende, Sabine Schwarz, Olaf Grassmann, Susanne Page
Hot-melt extrusion is an option to fabricate amorphous solid dispersions and to enhance oral bioavailability of poorly soluble compounds. The selection of suitable polymer carriers and processing aids determines the dissolution, homogeneity and stability performance of this solid dosage form. A miniaturized extrusion device (MinEx) was developed and Hypromellose acetate succinate type L (HPMCAS-L) based extrudates containing the model drugs neurokinin-1 (NK1) and cholesterylester transfer protein (CETP) were manufactured, plasticizers were added and their impact on dissolution and solid-state properties were assessed...
May 19, 2018: Pharmaceutics
M Danaei, M Dehghankhold, S Ataei, F Hasanzadeh Davarani, R Javanmard, A Dokhani, S Khorasani, M R Mozafari
Lipid-based drug delivery systems, or lipidic carriers, are being extensively employed to enhance the bioavailability of poorly-soluble drugs. They have the ability to incorporate both lipophilic and hydrophilic molecules and protecting them against degradation in vitro and in vivo. There is a number of physical attributes of lipid-based nanocarriers that determine their safety, stability, efficacy, as well as their in vitro and in vivo behaviour. These include average particle size/diameter and the polydispersity index (PDI), which is an indication of their quality with respect to the size distribution...
May 18, 2018: Pharmaceutics
Julia Metz, Katharina Knoth, Henrik Groß, Claus-Michael Lehr, Carolin Stäbler, Udo Bock, Marius Hittinger
Hay fever is notoriously triggered when nasal mucosa is exposed to allergenic pollen. One possibility to overcome this pollen exposure may be the application of an ointment with physical protective effects. In this context, we have investigated Bepanthen® Eye and Nose Ointment and the ointment basis petrolatum as reference while using contemporary in vitro techniques. Pollen from false ragweed ( Iva xanthiifolia ) was used as an allergy-causing model deposited as aerosol using the Vitrocell® Powder Chamber (VPC) on Transwell® inserts, while being coated with either Bepanthen® Eye and Nose Ointment and petrolatum...
May 10, 2018: Pharmaceutics
Michael B Lowinger, Stephanie E Barrett, Feng Zhang, Robert O Williams
Since their introduction over 50 years ago, polyurethanes have been applied to nearly every industry. This review describes applications of polyurethanes to the development of modified release drug delivery. Although drug delivery research leveraging polyurethanes has been ongoing for decades, there has been renewed and substantial interest in the field in recent years. The chemistry of polyurethanes and the mechanisms of drug release from sustained release dosage forms are briefly reviewed. Studies to assess the impact of intrinsic drug properties on release from polyurethane-based formulations are considered...
May 9, 2018: Pharmaceutics
Tomasz M Karpiński, Artur Adamczak
Despite much progress in the diagnosis and treatment of cancer, tumour diseases constitute one of the main reasons of deaths worldwide. The side effects of chemotherapy and drug resistance of some cancer types belong to the significant current therapeutic problems. Hence, searching for new anticancer substances and medicines are very important. Among them, bacterial proteins and peptides are a promising group of bioactive compounds and potential anticancer drugs. Some of them, including anticancer antibiotics (actinomycin D, bleomycin, doxorubicin, mitomycin C) and diphtheria toxin, are already used in the cancer treatment, while other substances are in clinical trials (e...
April 30, 2018: Pharmaceutics
Disang Feng, Tingting Peng, Zhengwei Huang, Vikramjeet Singh, Yin Shi, Ting Wen, Ming Lu, Guilan Quan, Xin Pan, Chuanbin Wu
The rapid release of poorly water-soluble drugs from amorphous solid dispersion (ASD) is often associated with the generation of supersaturated solution, which provides a strong driving force for precipitation and results in reduced absorption. Precipitation inhibitors, such as polymers and surfactants, are usually used to stabilize the supersaturated solution by blocking the way of kinetic or thermodynamic crystal growth. To evaluate the combined effect of polymers and surfactants on maintaining the supersaturated state of itraconazole (ITZ), various surfactants were integrated with enteric polymer hydroxypropyl methylcellulose acetate succinate (HPMC AS) to develop polymer⁻surfactant based solid dispersion...
April 24, 2018: Pharmaceutics
Barbara Cortese, Stefania D'Amone, Ilaria Elena Palamà
Chronic myeloid leukaemia (CML) is caused by the BCR-ABL oncogene, which encodes the constitutively active BCR-ABL tyrosine kinase. Targeted therapy with tyrosine-kinase inhibitors induces a partial cytogenetic response in most patients. Nanosystems can represent an opportunity for combinatorial therapy with the capacity to simultaneously release different therapeutic agents, checking the pharmacokinetic properties. In this work, we have developed a novel poly-(ε-caprolactone) (PCL) nanosystem for combinatorial therapy in CML, composed of a biodegradable pH sensitive core releasing Nilotinib (Nil) and an enzymatic sensitive outer shell releasing Imatinib Mesylate (IM), resulting in wool-like nanoparticles (NPs)...
April 18, 2018: Pharmaceutics
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