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Joanna Szafraniec, Agata Antosik, Justyna Knapik-Kowalczuk, Karolina Gawlak, Mateusz Kurek, Jakub Szlęk, Witold Jamróz, Marian Paluch, Renata Jachowicz
The effect of solvent removal techniques on phase transition, physical stability and dissolution of bicalutamide from solid dispersions containing polyvinylpyrrolidone (PVP) as a carrier was investigated. A spray dryer and a rotavapor were applied to obtain binary systems containing either 50% or 66% of the drug. Applied techniques led to the formation of amorphous solid dispersions as confirmed by X-ray powder diffractometry and differential scanning calorimetry. Moreover, solid⁻solid transition from polymorphic form I to form II was observed for bicalutamide spray dried without a carrier...
October 18, 2018: Pharmaceutics
Yu-Lin Su, Shang-Hsiu Hu
Theranostic nanoparticles recently received great interest for uniting unique functions to amplify therapeutic efficacy and reduce side effects. Despite the enhanced permeability and retention (EPR) effect, which amplifies the accumulation of nanoparticles at the site of a tumor, tumor heterogeneity caused by the dense extracellular matrix of growing cancer cells and the interstitial fluid pressure from abnormal angiogenesis in the tumor inhibit drug/particle penetration, leading to inhomogeneous and limited treatments...
October 18, 2018: Pharmaceutics
Junzhi Yang, Bianca G Reilly, Thomas P Davis, Patrick T Ronaldson
Opioids are highly effective analgesics that have a serious potential for adverse drug reactions and for development of addiction and tolerance. Since the use of opioids has escalated in recent years, it is increasingly important to understand biological mechanisms that can increase the probability of opioid-associated adverse events occurring in patient populations. This is emphasized by the current opioid epidemic in the United States where opioid analgesics are frequently abused and misused. It has been established that the effectiveness of opioids is maximized when these drugs readily access opioid receptors in the central nervous system (CNS)...
October 18, 2018: Pharmaceutics
Vijay Mishra, Kuldeep K Bansal, Asit Verma, Nishika Yadav, Sourav Thakur, Kalvatala Sudhakar, Jessica M Rosenholm
Solid lipid nanoparticles (SLNs) are nanocarriers developed as substitute colloidal drug delivery systems parallel to liposomes, lipid emulsions, polymeric nanoparticles, and so forth. Owing to their unique size dependent properties and ability to incorporate drugs, SLNs present an opportunity to build up new therapeutic prototypes for drug delivery and targeting. SLNs hold great potential for attaining the goal of targeted and controlled drug delivery, which currently draws the interest of researchers worldwide...
October 18, 2018: Pharmaceutics
Cristina de la Torre, Valentín Ceña
Alzheimer's disease (AD) is one of the main causes of disability and dependency among elderly people. AD is a neurodegenerative disorder characterized by a progressive and irreversible cognitive impairment, whose etiology is unclear because of the complex molecular mechanisms involved in its pathophysiology. A global view of the AD pathophysiology is described in order to understand the need for an effective treatment and why nanoparticles (NPs) could be an important weapon against neurodegenerative diseases by solving the general problem of poor delivery into the central nervous system (CNS) for many drugs...
October 17, 2018: Pharmaceutics
Mario Jug, Paola Angela Mura
Among the different techniques proposed for preparing cyclodextrin inclusion complex in the solid state, mechanochemical activation by grinding appears as a fast, highly efficient, convenient, versatile, sustainable, and eco-friendly solvent-free method. This review is intended to give a systematic overview of the currently available data in this field, highlighting both the advantages as well as the shortcomings of such an approach. The possible mechanisms involved in the inclusion complex formation in the solid state, by grinding, have been illustrated...
October 16, 2018: Pharmaceutics
Jinyi Zhai, Julia Mantaj, Driton Vllasaliu
Biologics have changed the management of inflammatory bowel disease (IBD), but there are concerns with unexpected systemic toxicity and loss of therapeutic response following administration by injection. Rectal administration of biologics offers potentially reduced therapy costs, as well as safer and more effective local delivery to inflammation sites. Hydrogels are potentially useful carriers of biologics for improved delivery to the inflamed intestinal mucosa. Here, we prepared a hydrogel system based on ascorbyl palmitate (AP) and incorporated a model macromolecular drug (fluorescently-labelled dextran) into the system...
October 15, 2018: Pharmaceutics
Jeong-Soo Kim, Min-Soo Kim, In-Hwan Baek
Tadalafil is an oral selective phosphodiesterase type-5 inhibitor with demonstrated efficacy and safety that is used to treat erectile dysfunction. The purpose of this study is to compare the pharmacokinetic properties of tadalafil after conventional oral tablet administration and novel intranasal administration in beagle dogs. Fourteen 13-month-old male beagle dogs were randomly divided into two groups, and were given 5 mg tadalafil orally or intranasally in a parallel design. Blood samples were collected before and 0...
October 15, 2018: Pharmaceutics
Bremansu Osa-Andrews, Kee W Tan, Angelina Sampson, Surtaj H Iram
Multidrug resistance protein 1 (MRP1) can efflux a wide variety of molecules including toxic chemicals, drugs, and their derivatives out of cells. Substrates of MRP1 include anti-cancer agents, antibiotics, anti-virals, anti-human immunodeficiency virus (HIV), and many other drugs. To identify novel substrates and modulators of MRP1 by exploiting intramolecular fluorescence resonance energy transfer (FRET), we genetically engineered six different two-color MRP1 proteins by changing green fluorescent protein (GFP) insertion sites, while keeping the red fluorescent protein (RFP) at the C-terminal of MRP1...
October 13, 2018: Pharmaceutics
Li Key Yeo, Temidayo O B Olusanya, Cheng Shu Chaw, Amal Ali Elkordy
Novel niosomal formulations containing cinnarizine were developed to enhance its drug characteristics. In this work, niosomes (non-ionic surfactant vesicles) were prepared by conventional thin-film hydration (TFH) and microfluidic (MF) methods with sorbitan monostearate (Span® 60), cholesterol, and co-surfactants (Cremophor® ELP, Cremophor® RH40 and Solutol® HS15) as key excipients. The aim was to study the effect of cinnarizine on the characteristics of different niosomal formulations manufactured by using different methods...
October 13, 2018: Pharmaceutics
Ramon Cabiscol, Jan Henrik Finke, Harald Zetzener, Arno Kwade
Powder densification through uniaxial compaction is governed by a number of simultaneous processes taking place on a reduced time as the result of the stress gradients within the packing, as well as the frictional and adhesive forces between the powder and the die walls. As a result of that, a density and stiffness anisotropy is developed across the axial and radial directions. In this study, microindentation has been applied to assess and quantify the variation of the module of elasticity ( E m o d ) throughout the surface of cylindrical tablets...
October 12, 2018: Pharmaceutics
Ruba Malkawi, Abhishek Iyer, Anish Parmar, Daniel G Lloyd, Eunice Tze Leng Goh, Edward J Taylor, Sarir Sarmad, Annemieke Madder, Rajamani Lakshminarayanan, Ishwar Singh
Teixobactin is a highly potent cyclic depsipeptide which kills a broad range of multi-drug resistant, Gram-positive bacteria, such as Methicillin-resistant Staphylococcus aureus (MRSA) without detectable resistance. In this work, we describe the design and rapid synthesis of novel teixobactin analogues containing two cysteine moieties, and the corresponding disulfide-bridged cyclic analogues. These analogues differ from previously reported analogues, such as an Arg10 -teixobactin, in terms of their macrocyclic ring size, and feature a disulfide bridge instead of an ester linkage...
October 11, 2018: Pharmaceutics
Noriyasu Kamei, Hideyuki Tamiwa, Mari Miyata, Yuta Haruna, Koyo Matsumura, Hideyuki Ogino, Serena Hirano, Kazuhiro Higashiyama, Mariko Takeda-Morishita
Cell-penetrating peptides (CPPs) have great potential to efficiently deliver drug cargos across cell membranes without cytotoxicity. Cationic arginine and hydrophobic tryptophan have been reported to be key component amino acids for cellular internalization of CPPs. We recently found that l-arginine could increase the oral delivery of insulin in its single amino acid form. Therefore, in the present study, we evaluated the ability of another key amino acid, tryptophan, to enhance the intestinal absorption of biopharmaceuticals...
October 10, 2018: Pharmaceutics
Maria Mendes, João José Sousa, Alberto Pais, Carla Vitorino
The poor prognosis and rapid recurrence of glioblastoma (GB) are associated to its fast-growing process and invasive nature, which make difficult the complete removal of the cancer infiltrated tissues. Additionally, GB heterogeneity within and between patients demands a patient-focused method of treatment. Thus, the implementation of nanotechnology is an attractive approach considering all anatomic issues of GB, since it will potentially improve brain drug distribution, due to the interaction between the blood⁻brain barrier and nanoparticles (NPs)...
October 9, 2018: Pharmaceutics
Simona Giarra, Silvia Zappavigna, Virginia Campani, Marianna Abate, Alessia Maria Cossu, Carlo Leonetti, Manuela Porru, Laura Mayol, Michele Caraglia, Giuseppe De Rosa
This study aimed to develop nanovectors co-encapsulating doxorubicin (Doxo) and zoledronic acid (Zol) for a combined therapy against Doxo-resistant tumors. Chitosan (CHI)-based polyelectrolyte complexes (PECs) prepared by ionotropic gelation technique were proposed. The influence of some experimental parameters was evaluated in order to optimize the PECs in terms of size and polydispersity index (PI). PEC stability was studied by monitoring size and zeta potential over time. In vitro studies were carried out on wild-type and Doxo-resistant cell lines, to assess both the synergism between Doxo and Zol, as well as the restoring of Doxo sensitivity...
October 9, 2018: Pharmaceutics
Shiao-Wen Tsai, Wen-Xin Yu, Pai-An Hwang, Sheng-Siang Huang, Hsiu-Mei Lin, Yu-Wei Hsu, Fu-Yin Hsu
Hydroxyapatite (HAp) is the main inorganic component and an essential part of hard bone and teeth. Due to its excellent biocompatibility, bioactivity, and osteoconductivity, synthetic HAp has been widely used as a bone substitute, cell carrier, and therapeutic gene or drug carrier. Recently, numerous studies have demonstrated that strontium-substituted hydroxyapatite (SrHAp) not only enhances osteogenesis but also inhibits adipogenesis in mesenchymal stem cells. Mesoporous SrHAp has been successfully synthesized via a traditional template-based process and has been found to possess better drug loading and release efficiencies than SrHAp...
October 8, 2018: Pharmaceutics
Zhongzhe Cheng, Xing Zhou, Zhifeng Du, Wenyi Li, Bingying Hu, Jingkui Tian, Lin Zhang, Jiangeng Huang, Hongliang Jiang
Capilliposide B (LC-B) and Capilliposide C (LC-C), two new triterpenoid saponins extracted from Lysimachia capillipes Hemsl, exhibit potential anticancer activity both in vitro and in vivo. However, their metabolic process remains unclear. In this study, the metabolic stability of LC-B, LC-C, and Capilliposide A (LC-A, a bioactive metabolite of LC-B and LC-C) was investigated in human, rat, and mouse liver microsomes, respectively. Thereafter, their metabolites were identified and characterized after oral administration in mice...
October 8, 2018: Pharmaceutics
Hyeon Kim, Min Sun Choi, Young Seok Ji, In Sook Kim, Gi Beom Kim, In Yong Bae, Myung Chan Gye, Hye Hyun Yoo
Acetyl tributyl citrate (ATBC) is an (the Food and Drug Administration) FDA-approved substance for use as a pharmaceutical excipient. It is used in pharmaceutical coating of solid oral dosage forms such as coated tablets or capsules. However, the information of ATBC on its pharmacokinetics is limited. The aim of this study is to investigate the pharmacokinetic properties of ATBC using liquid chromatography⁻tandem mass spectrometric (LC⁻MS/MS) analysis. ATBC was rapidly absorbed and eliminated and the bioavailability was 27...
October 8, 2018: Pharmaceutics
Nihad Al-Hashimi, Nazish Begg, Raid G Alany, Hany Hassanin, Amr Elshaer
Oral modified-release multiparticulate dosage forms, which are also referred to as oral multiple-unit particulate systems, are becoming increasingly popular for oral drug delivery applications. The compaction of polymer-coated multiparticulates into tablets to produce a sustained-release dosage form is preferred over hard gelatin capsules. Moreover, multiparticulate tablets are a promising solution to chronic conditions, patients' adherence, and swallowing difficulties if incorporated into orodispersible matrices...
October 4, 2018: Pharmaceutics
Ai-Ho Liao, Ho-Chiao Chuang, Bo-Ya Chang, Wen-Chuan Kuo, Chih-Hung Wang, Hong-Wei Gao, Chien-Ping Chiang
The optodynamic process of laser-induced microbubble (MB) cavitation in liquids is utilized in various medical applications. However, how incident laser radiation interacts with MBs as an ultrasound contrast agent is rarely estimated when the liquid already contains stable MBs. The present study investigated the efficacy of the laser-mediated cavitation of albumin-shelled MBs in enhancing transdermal drug delivery. Different types and conditions of laser-mediated inertial cavitation of MBs were first evaluated...
October 3, 2018: Pharmaceutics
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