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Takehisa Nakajima, Issei Takeuchi, Hiroyuki Ohshima, Hiroshi Terada, Kimiko Makino
First, an elementary osmotic pump (EOP) with a simple structure was prepared using polyethylene oxide (PEO) and NaCl as an excipient, and the influence of the molecular-weight of PEO on drug-release was investigated. In the dissolution test of EOP, it was observed that the gelated core tablet was pushed out through the orifice. The dissolution profile of EOP was sigmoidal, and despite the short time, a zero-order release region was observed. The gel swelling rate in the zero-order region was independent of the molecular-weight of PEO...
March 13, 2018: Journal of Pharmaceutical Sciences
E Manuela P J Garrido, Ana S Cerqueira, Daniel Chavarria, Tiago Silva, Fernanda Borges, Jorge M P J Garrido
Caffeic acid phenethyl ester (CAPE) is a bioactive polyphenolic compound obtained from propolis extract. Although it has a broad therapeutic potential, the bioavailability of CAPE is limited, due to reduced solubility and poor plasmatic stability. Efforts to reduce these pharmacokinetic drawbacks resulted in the synthesis of caffeic acid phenethyl amide (CAPA). Cyclodextrins have been proved as promising excipients for the formulation of active ingredients. Herein, we report the inclusion complexation behavior and binding ability of CAPE and CAPA with hydroxypropyl-β-cyclodextrin (HP-β-CD)...
July 15, 2018: Food Chemistry
Jian Yin, Xudong Deng, Jie Zhang, Jun Lin
Adenosine triphosphate-binding cassette (ABC) transporters-mediated multidrug resistance (MDR) remains as a obstacle for effective cancer therapy. Nanoparticles (NPs)-based delivery systems are promising to overcome MDR, but only a few of them have been accepted for clinical treatment, due to characteristics such as insufficient transportation and potential toxicity. In this respect, mounting attention has been attracted towards interactions between NPs and ABC transporters, which hold a key role in the treatment of multidrug-resistant cancer and NP toxicity...
March 14, 2018: Current Medicinal Chemistry
Ayse Ipek Akyuz Unsal, Yesim Basal, Serap Birincioglu, Tolga Kocaturk, Harun Cakmak, Alparslan Unsal, Gizem Cakiroz, Nüket Eliyatkın, Ozden Yukselen, Buket Demirci
PURPOSE: To investigate the potential effects of chronic exposure to a nasal decongestant and its excipients on ocular tissues using an experimental rat model. METHODS: Sixty adult male Wistar rats were randomized into six groups. The first two groups were control (serum physiologic) and Otrivine® groups. The remaining four groups received the Otrivine excipients xylometazoline, benzalkonium chloride, sorbitol, and ethylene diamine tetra acetic acid. Medications were applied into both nostrils twice a day for 8 weeks...
January 2018: Arquivos Brasileiros de Oftalmologia
Gamal A Shazly, Sultan Alshehri, Mohamed A Ibrahim, Hesham M Tawfeek, Jelan A Razik, Yasser A Hassan, Faiyaz Shakeel
Domperidone (DOP) is extensively applied orally in the management of nausea and vomiting. Upon oral administration, its bioavailability is very poor due to its poor solubility in alkaline media. Therefore, the aim of this work was to investigate DOP-loaded solid lipid nanoparticles (DOP-SLNs) in order to sustain its release pattern and to enhance oral bioavailability. DOP-SLNs were prepared using four different lipids. Prepared DOP-SLNs were characterized for "polydispersity index (PDI), particle size, zeta potential, % entrapment efficiency (% EE), and drug release behavior...
March 12, 2018: AAPS PharmSciTech
Hojun Song, Cheol Moon, Beom-Jin Lee, Euichaul Oh
Herein, we aimed to prepare porous granules of pravastatin and evaluate their applicability to orally disintegrating tablets (ODTs). Pravastatin solid dispersion granules (PSDGs-A) were prepared by dispersing pravastatin sodium in D-mannitol (the dispersion medium) in the presence of ammonium bicarbonate (the sublimation agent) using a spray-drying process. The PSDGs-A were round, irregularly shaped, mesoporous agglomerates with appropriate particle size, bulk density, and flowability for the tableting process...
March 9, 2018: Journal of Pharmaceutical Sciences
Delphine Barnoud, Claire Pinçon, Bénédicte Bruno, Johana Béné, Sophie Gautier, Annie Lahoche, Nadine Petitpain, Michèle Vasseur, Christine Barthélémy, Bertrand Décaudin, Nicolas Simon, Pascal Odou
BACKGROUND: Etoposide phosphate (EP; single injection, 60 mg/kg) followed by total body irradiation (TBI) at 12 Gy has been used as an allogeneic stem cell transplantation (allo-SCT) conditioning regimen for children since 2010. In our institution, EP has been suspected of leading to acute nephrotoxicity. The aim of this study was to assess the potential renal toxicity of EP in this context. MATERIALS AND METHODS: A retrospective study was carried out on children hospitalized between 2007 and 2015 for allo-SCT with TBI-based myeloablative conditioning associated with cyclophosphamide (CY, 60 mg/kg/day × 2 days) or EP...
March 12, 2018: Pediatric Blood & Cancer
Andrea Arsiccio, Roberto Pisano
Biopharmaceuticals are frequently stored in the frozen state to avoid rapid degradation. Moreover, therapeutic proteins are frequently made into a dried form to provide long-term storage. However, both freezing and drying stresses can result in protein unfolding and aggregation. Thus, a proper formulation, containing suitable excipients, must be used to avoid loss of activity. Here, the conformational stability of a model protein, human growth hormone, is studied during freezing, and in the dried state as well, using molecular dynamics...
March 12, 2018: Physical Chemistry Chemical Physics: PCCP
Maria Aponte, Francesca Ungaro, Ivana d'Angelo, Carmen De Caro, Roberto Russo, Giuseppe Blaiotta, Fabrizio Dal Piaz, Antonio Calignano, Agnese Miro
This study reports novel food-grade granules for co-delivery of L. plantarum 299v and a standardized extract of Olea europaea leaves (Phenolea®) as oral carrier of probiotics and hydroxytyrosol. Different granule formulations containing either L. plantarum 299v (Lac), or the olive leave extract (Phe) or their combination (Lac-Phe) have been successfully produced through wet granulation employing excipients generally regarded as safe as granulating/binding agents. L. plantarum cells withstood the manufacturing process and were stable upon storage at 4°C for more than 6 months...
March 8, 2018: International Journal of Pharmaceutics
Maryam Alsadat Shetab Boushehri, Valentin Stein, Alf Lamprecht
Nanoparticles create exciting platforms for anticancer immunotherapy and vaccination, though their inherent immunomodulatory properties have remained underexploited. Ammonio methacrylate copolymers (AMC) are well-established excipients in pharmaceutical industry and components of controlled-release oral formulations. Here, we demonstrate that nanoscaling of type A and B AMC (Eudragit® RL and RS) endows these inactive ingredients immunostimulatory properties exploitable for cancer therapy. The particles induce the secretion of various pro-inflammatory cytokines and chemokines from the cells of innate immunity...
March 2, 2018: Biomaterials
Takashi Otaki, Yuta Tanabe, Takashi Kojima, Masaru Miura, Yukihiro Ikeda, Tatsuo Koide, Toshiro Fukami
In recent years, to guarantee a quality-by-design approach to the development of pharmaceutical products, it is important to identify properties of raw materials and excipients in order to determine critical process parameters and critical quality attributes. Feedback obtained from real-time analyses using various process analytical technology (PAT) tools has been actively investigated. In this study, in situ monitoring using low-frequency (LF) Raman spectroscopy (10-200cm-1 ), which may have higher discriminative ability among polymorphs than near-infrared spectroscopy and conventional Raman spectroscopy (200-1800 cm-1 ), was investigated as a possible application to PAT...
March 7, 2018: International Journal of Pharmaceutics
Basanth Babu Eedara, Bhamini Rangnekar, Colin Doyle, Alex Cavallaro, Shyamal C Das
Pharmacotherapy of tuberculosis is potentially more efficient when delivered by the inhaled route than by the current oral and/or parenteral routes due to the higher concentration of drug reaching the primary region of infection in the lungs. This study investigated the influence of the amino acid L-leucine alone and in combination with the phospholipid, 1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC), on the aerosolization behaviour of the anti-TB drugs, pyrazinamide and moxifloxacin HCl. Spray dried powders of pyrazinamide (P), moxifloxacin (M) alone and in combination with 10% L-leucine (PL and ML) and 10% DPPC (PLD and MLD) were produced...
March 7, 2018: International Journal of Pharmaceutics
Raul-Augustin Mitran, Cristian Matei, Daniela Berger, Laura Băjenaru, Mihaela G Moisescu
Mesoporous silica materials are promising nano-carriers for drug delivery systems. Even though there are many strategies for controlling the drug release kinetics, these must be adapted through trial and error on a case-by-case basis. Here we explore the possibility of tailoring the release kinetics of hydrophilic, water soluble therapeutic agents from mesoporous silica through addition of a hydrophobic excipient, 1-tetradecanol. In vitro drug release experiments performed at 37 °C, in phosphate buffer solution (pH 7...
March 7, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Aron H Blaesi, Nannaji Saka
At present, the most prevalent pharmaceutical dosage forms, the orally-delivered immediate-release tablets and capsules, are porous, granular solids. They disintegrate into their constituent particulates upon ingestion to release drug rapidly. The design, development, and manufacture of such granular solids, however, is inefficient due to difficulties associated with the unpredictable inter-particle interactions. Therefore, to achieve more predictable dosage form properties and processing, we have recently introduced melt-processed polymeric cellular dosage forms...
March 1, 2018: Materials Science & Engineering. C, Materials for Biological Applications
Aymeric Ousset, Pierre-François Chavez, Joke Meeus, Florent Robin, Martin Alexander Schubert, Pascal Somville, Kalliopi Dodou
The evaluation of drug-polymer miscibility in the early phase of drug development is essential to ensure successful amorphous solid dispersion (ASD) manufacturing. This work investigates the comparison of thermodynamic models, conventional experimental screening methods (solvent casting, quench cooling), and a novel atomization screening device based on their ability to predict drug-polymer miscibility, solid state properties ( T g value and width), and adequate polymer selection during the development of spray-dried amorphous solid dispersions (SDASDs)...
March 7, 2018: Pharmaceutics
Quanying Bao, Bryan Newman, Yan Wang, Stephanie Choi, Diane J Burgess
In vitro drug release testing and ex vivo transcorneal drug permeation can provide valuable information on the performance of the Q1/Q2 equivalent ointments prior to any animal studies. Good correlation between in vitro and ex vivo drug release may be indicative of good in vitro and in vivo correlation. Accordingly, it is important to investigate in vitro as well as ex vivo drug release from Q1/Q2 equivalent ophthalmic ointments and evaluate whether a correlation between these release profiles can be established...
March 5, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
Cosby A Stone, Cindy T McEvoy, Judy L Aschner, Ashudee Kirk, Christian Rosas-Salazar, Joan M Cook-Mills, Paul E Moore, William F Walsh, Tina V Hartert
Vitamin E is obtained only through the diet and has a number of important biological activities, including functioning as an antioxidant. Evidence that free radicals may contribute to pathological processes such as bronchopulmonary dysplasia (BPD), a disease of prematurity associated with increased lung injury, inflammation and oxidative stress, led to trials of the antioxidant vitamin E (α-tocopherol) to prevent BPD with variable results. These trials were all conducted at supraphysiologic doses and 2 of these trials utilized a formulation containing a potentially harmful excipient...
March 7, 2018: Neonatology
Saša Kajdič, Franc Vrečer, Petra Kocbek
Polymer nanofibers have become increasingly important for improvement of dissolution and bioavailability of poorly soluble drugs, representing a great challenge in pharmaceutical development. Here, we introduced a new concept of using amphiphilic polymers as fundamental excipients in electrospun nanofibers, which would improve drug solubilization and accelerate its release. Hydrophilic poloxamer-based nanofibers were developed as a novel drug delivery system for carvedilol. These nanofibers were electrospun from different liquid carvedilol dispersions, as carvedilol (nano)suspensions or ethanol solution...
March 4, 2018: European Journal of Pharmaceutical Sciences
Sarifuddin, Prashanta Kumar Mandal
Angioplasty with drug-coated balloons (DCBs) using excipients as drug carriers is emerging as a potentially viable strategy demonstrating clinical efficacy and proposing additional compliance for the treatment of obstructive vascular diseases. An attempt is made to develop an improved computational model where attention has been paid to the effect of interstitial flow, that is, plasma convection and internalization of bound drug. The present model is capable of capturing the phenomena of the transport of free drug and its retention, and also the internalization of drug in the process of endocytosis to atherosclerotic vessel of heterogeneous tissue composition comprising of healthy tissue, as well as regions of fibrous cap, fibro-fatty, calcified and necrotic core lesions...
March 5, 2018: Cardiovascular Engineering and Technology
Mark A Burbridge, Richard A Jaffe
Medications used in anesthesiology contain both pharmacologically active compounds and additional additives that are usually regarded as being pharmacologically inactive. These additives, called excipients, serve diverse functions. Despite being labeled inert, excipients are not necessarily benign substances. Anesthesiologists should have a clear understanding of their chemical properties and the potential for adverse reactions. This report catalogs the excipients found in drugs commonly used in anesthesiology, provides a brief description of their function, and documents examples from the literature regarding their adverse effects...
March 1, 2018: Anesthesia and Analgesia
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