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European Journal of Pharmaceutics and Biopharmaceutics

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https://www.readbyqxmd.com/read/30414990/development-of-doxorubicin-hydrochloride-loaded-ph-sensitive-liposomes-investigation-on-the-impact-of-chemical-nature-of-lipids-and-liposome-composition-on-ph-sensitivity
#1
Asad Ur Rehman, Ziad Omran, Halina Anton, Yves Mély, Salman Akram, Thierry F Vandamme, Nicolas Anton
This study investigates the impact of the chemical nature of lipids and additive on the formulation and properties of pH sensitive liposomes. The objective is to understand the respective role of the formulation parameters on the liposome properties in order to optimize the conditions for efficient encapsulation of doxorubicin (DOX). These liposomes should be stable at physiological pH, and disrupt in slightly acidic media such as the tumor microenvironment to release their DOX load. The major challenge for encapsulating DOX in pH sensitive liposomes lies in the fact that this drug is soluble at low pH (when the pH-sensitive liposomes are not stable), but the DOX aqueous solubility decreases in the pH conditions corresponding to the stability of the pH-sensitive liposomes...
November 8, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30414499/evaluation-of-chemometric-approaches-for-polymorphs-quantification-in-tablets-using-near-infrared-hyperspectral-images
#2
Vitor H da Silva, José L Soares-Sobrinho, Claudete F Pereira, Åsmund Rinnan
Near-Infrared hyperspectral image (HSI-NIR) is a useful technique for pharmaceutical research and industry alike. It can provide important surface information such as the polymorphs quantification and its distribution over the tablet. Several chemometric tools are applied for this purpose, with MCR-ALS and PLS regression being the most common approaches. In this work, a detailed comparison between these two approaches are performed. Beyond a "simple" regression comparison, a comparison of the score images (local quantification) was also evaluated...
November 7, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30414498/sirna-mediated-protein-knockdown-in-precision-cut-lung-slices
#3
Mitchel J R Ruigrok, Jia-Ling Xian, Henderik W Frijlink, Barbro N Melgert, Wouter L J Hinrichs, Peter Olinga
Small interfering RNA (siRNA) can induce RNA interference, which leads to the knockdown of messenger RNA (mRNA) and protein. As a result, siRNA is often used in vitro and in vivo to unravel the function of genes and as a therapeutic agent to disrupt excessive expression of disease-related genes. However, there is a large gap between in vitro and in vivo models in terms of simplicity, flexibility, throughput, and translatability. This gap could be bridged by using precision-cut tissue slices, which represent viable explants prepared from animal or human tissue that can be cultured ex vivo...
November 7, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30414497/betulin-silver-nanoparticles-qualify-as-efficient-antimelanoma-agents-in-in-vitro-and-in-vivo-studies
#4
Corina Danciu, Iulia Pinzaru, Dorina Coricovac, Florina Andrica, Ioana Sizemore, Cristina Dehelean, Flavia Baderca, Voichita Lazureanu, Codruta Soica, Marius Mioc, Heinfried Radeke
The current study was purported to assess the: (i) in vitro toxicity of betulin silver nanoparticles (AgNPs-B), bare and capped with polyethylene glycol (PEG), on two murine melanoma cell lines (B164A5 and B16Ova) and on healthy cell lines (keratinocytes and melanocytes), and (ii) in vivo antitumor efficacy of PEGylated AgNPs-B in an experimental melanoma model. Bare and PEG-capped AgNPs-B were synthesized by a chemical reduction method resulting in stable and non-aggregated spherical AgNPs-B and PEG-AgNPs-B, of narrow size distributions and mean hydrodynamic diameters of 25 nm and 75 nm, respectively...
November 7, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30408519/robust-mucosal-and-systemic-responses-against-htlv-1-by-delivery-of-multi-epitope-vaccine-in-plga-nanoparticles
#5
Mona Kabiri, Mojtaba Sankian, Kayvan Sadri, Mohsen Tafaghodi
In this investigation, the immunogenicity of HTLV-1 fusion epitope-loaded PLGA nanoparticles (NPs) was assessed in the absence or presence of co-encapsulated CpG ODN adjuvant, in a mice model. For this purpose, the multi-epitope chimera including Tax, env, and gag immunogenic HTLV-1 epitopes was encapsulated in biodegradable PLGA NPs with or without CpG adjuvant. PLGA nanospheres produced by a double emulsion method had a size of less than 200 nm, and encapsulation efficiency of chimera antigen was 85%. The release profile of radiolabeled chimera indicated that only 17...
November 5, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30408518/comparative-evaluation-of-dimeric-and-monomeric-forms-of-adapt-scaffold-protein-for-targeting-of-her2-expressing-tumours
#6
Javad Garousi, Sarah Lindbo, Jesper Borin, Emma von Witting, Anzhelika Vorobyeva, Maryam Oroujeni, Bogdan Mitran, Anna Orlova, Jos Buijs, Vladimir Tolmachev, Sophia Hober
ADAPTs are small engineered non-immunoglobulin scaffold proteins, which have demonstrated very promising features as vectors for radionuclide tumour targeting. Radionuclide imaging of human epidermal growth factor 2 (HER2) expression in vivo might be used for stratification of patients for HER2-targeting therapies. ADAPT6, which specifically binds to HER2, has earlier been shown to have very promising features for in vivo targeting of HER2 expressing tumours. In this study we tested the hypothesis that dimerization of ADAPT6 would increase the apparent affinity to HER2 and accordingly improve tumour targeting...
November 5, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30399400/oxcarbazepine-free-or-loaded-plga-nanoparticles-as-effective-intranasal-approach-to-control-epileptic-seizures-in-rodents
#7
Teresa Musumeci, Maria Francesca Serapide, Rosalia Pellitteri, Alessandro Dalpiaz, Luca Ferraro, Roberta Dal Magro, Angela Bonaccorso, Claudia Carbone, Francisco Veiga, Giulio Sancini, Giovanni Puglisi
The brain as a target for drug delivery is a challenge in pharmaceutical research. Among the several proposed strategies, the intranasal route represents a good strategy to deliver drugs to the brain. The goal of this study was to investigate the potential use of oxcarbazepine (OXC) to enhance brain targeting efficiency after intranasal (IN) administration. As well as attempting to use as low a dose as possible to obtain therapeutic effect. Our results showed that, after IN administrations, the dose of OXC that was effective in controlling epileptic seizures was 0...
November 3, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30385421/biorelevant-in-vitro-assessment-of-dissolution-and-compatibility-properties-of-a-novel-paediatric-hydrocortisone-drug-product-following-exposure-of-the-drug-product-to-child-appropriate-administration-fluids
#8
Erik Wollmer, Greg Neal, Martin J Whitaker, Daniel Margetson, Sandra Klein
Alkindi® is a novel oral multi-particulate taste-masked formulation of hydrocortisone for use in children with the rare disease adrenal insufficiency. The objective of the present work was to study the biorelevant dissolution and compatibility properties of Alkindi® granules following exposure to administration fluids including breast milk, artificial milk, whole milk and water. To provide in vitro data for a representative patient collective, dosing conditions in neonates, infants and pre-school children were assessed...
October 29, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30385420/incorporation-and-effects-of-mesoporous-sio-2-cao-nanospheres-loaded-with-ipriflavone-on-osteoblast-osteoclast-cocultures
#9
Laura Casarrubios, Natividad Gómez-Cerezo, María José Feito, María Vallet-Regí, Daniel Arcos, María Teresa Portolés
Mesoporous nanospheres in the system SiO2 -CaO (NanoMBGs) with a hollow core surrounded by a radial arrangement of mesopores were characterized, labeled with FITC (FITC-NanoMBGs) and loaded with ipriflavone (NanoMBG-IPs) in order to evaluate their incorporation and their effects on both osteoblasts and osteoclasts simultaneously and maintaining the communication with each other in coculture. The influence of these nanospheres on macrophage polarization towards pro-inflammatory M1 or reparative M2 phenotypes was also evaluated in basal and stimulated conditions through the expression of CD80 (as M1 marker) and CD206 (as M2 marker) by flow cytometry and confocal microscopy...
October 29, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30385419/inhalable-poly-lactic-co-glycolic-acid-plga-microparticles-encapsulating-all-trans-retinoic-acid-atra-as-a-host-directed-adjunctive-treatment-for-mycobacterium-tuberculosis-mtb-infection
#10
Gemma O'Connor, Nitya Krishnan, Aidan Fagan-Murphy, Joseph Cassidy, Seonadh O'Leary, Brian D Robertson, Joseph Keane, Mary P O'Sullivan, Sally-Ann Cryan
Ending the tuberculosis (TB) epidemic by 2030 was recently listed in the United Nations (UN) Sustainable Development Goals alongside HIV/AIDS and malaria as it continues to be a major cause of death worldwide. With a significant proportion of TB cases caused by resistant strains of Mycobacterium tuberculosis (Mtb), there is an urgent need to develop new and innovative approaches to treatment. Since 1989, researchers have been assessing the anti-bacterial effects of the active metabolite of vitamin A, all trans-Retinoic acid (ATRA) solution, in Mtb models...
October 29, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30385418/how-relevant-is-ribbon-homogeneity-in-roll-compaction-dry-granulation-and-can-it-be-influenced
#11
Raphael Wiedey, Rok Šibanc, Annika Wilms, Peter Kleinebudde
A homogeneous distribution of solid fraction in ribbons is generally assumed to be beneficial during roll compaction/dry granulation. Numerous attempts have been made to increase this homogeneity by modification of the machine, i.e. the roll design and the design of the feeding unit. It has however not been critically tested how relevant this homogeneity really is during subsequent processing. This study investigated two resulting questions: How can process parameters used to increase homogeneity in ribbons and how relevant is this homogeneity for properties of resulting tablets? For that, a statistically designed experiment were performed and ribbon homogeneity analyzed using X-ray micro-computed tomography...
October 29, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30367935/%C3%AE-casein-micelles-for-oral-delivery-of-sn-38-and-elacridar-to-overcome-bcrp-mediated-multidrug-resistance-in-gastric-cancer
#12
Maya Bar-Zeev, Daniel Kelmansky, Yehuda G Assaraf, Yoav D Livney
Gastric cancer is the third leading cause of cancer-related mortality worldwide. A dominant hindrance towards curative cancer therapy is multidrug resistance (MDR) mediated by ATP-dependent efflux pumps. We have previously demonstrated the ability of β-casein (β-CN) micelles and re-assembled casein micelles to serve as nanovehicles for oral delivery and target-activated release of hydrophobic chemotherapeutics in the stomach, and to overcome P-glycoprotein-dependent MDR in gastric cancer. Herein we investigated the modularity and versatility of this β-CN-based delivery system using a different synergistic drug duo to treat MDR gastric cancer cells overexpressing the breast cancer resistance protein (BCRP)...
October 24, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30359717/buccal-delivery-of-small-molecules-impact-of-levulinic-acid-oleic-acid-sodium-dodecyl-sulfate-and-hypotonicity-on-ex-vivo-permeability-and-spatial-distribution-in-mucosa
#13
Stine Egebro Hansen, Eva Marxen, Christian Janfelt, Jette Jacobsen
Studies of drug permeability rate and localization in buccal mucosa are essential to gain new knowledge of means such as chemical enhancers or osmolality to enhance buccal drug transport in the development of new buccal drug products. The transport of caffeine, diazepam and mannitol across porcine buccal mucosa was studied in modified Ussing chambers with a hypotonic donor solution, in the presence of levulinic acid (LA), oleic acid (OA), propylene glycol (PG) as well as sodium dodecyl sulfate (SDS). Subsequently, matrix-assisted laser desorption ionization - mass spectrometry imaging (MALDI-MSI) was applied to image the spatial distribution of caffeine, mannitol and SDS in cross-sections of porcine buccal mucosa...
October 22, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30359716/the-function-and-mechanism-of-preactivated-thiomers-in-triggering-epithelial-tight-junctions-opening
#14
Yang Zhang, Shurong Zhou, Feiyang Deng, Xianhui Chen, Xing Wang, Yaoqi Wang, Hua Zhang, Wenbing Dai, Bing He, Qiang Zhang, Xueqing Wang
As a unique macromolecular permeation enhancer, thiolated polymers (thiomers), especially the preactivated thiomers, have demonstrated great merits in oral delivery of protein/peptide drugs by triggering epithelial tight junctions (TJs) opening. However, the underlying molecular mechanism remains unclear. To clarify this issue, preactivated thiomers were synthesized and their TJs opening function as well as signaling pathways on MDCK and Caco-2 cell monolayers was investigated. The results showed that preactivated thiomers could reduce TEER and increase the permeation of Na-Flu and FITC-Insulin over 2-fold and 4-fold on MDCK monolayers, respectively, indicating their huge potential as macromolecular permeation enhancers...
October 22, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30342089/pharmacodynamical-effects-of-orally-administered-exenatide-nanoparticles-embedded-in-gastro-resistant-microparticles
#15
Liat Soudry-Kochavi, Natalya Naraykin, Rosanna Di Paola, Enrico Gugliandolo, Alessio Peritore, Salvatore Cuzzocrea, Ehud Ziv, Taher Nassar, Simon Benita
One of the major disadvantages associated with macromolecules therapy is that most of them can only be administered parenterally. Exenatide, an efficient anti-diabetic drug, incretin mimetic, is currently administered subcutaneously (SC) causing compliance issues. Nanoparticles (NPs) are considered a promising solution for oral delivery of this drug. In order to overcome exenatide's inability to cross the enterocytes and to increase its stability in the gastrointestinal (GI) tract, we encapsulated exenatide into a nano-in-micro delivery system...
October 17, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30339889/targeted-delivery-of-p-coumaric-acid-encapsulated-mannosylated-liposomes-to-the-synovial-macrophages-inhibits-osteoclast-formation-and-bone-resorption-in-the-rheumatoid-arthritis-animal-model
#16
Manoj Kumar Neog, Mahaboobkhan Rasool
The current study aimed to target the delivery of p-coumaric acid (CA), a dietary polyphenol to the synovial macrophages of AIA rats via mannose incorporated liposomal delivery system (ML) with reference to osteoclastogenesis and bone resorption. In vivo imaging and in vitro drug release study indicated the efficiency of mannosylated liposomes to localize at the site of inflammation and increased sustain drug release respectively. Morphological assessment of isolated synovial macrophages with respect to CD86 (synovial macrophages) and CD51 (pre-/osteoclast) indicated that p-coumaric acid encapsulated mannnosylated liposomes (ML-CA) inhibited the osteoclasts differentiation...
October 16, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30339888/in-situ-co-amorphisation-of-arginine-with-indomethacin-or-furosemide-during-immersion-in-an-acidic-medium-a-proof-of-concept-study
#17
Ina Petry, Korbinian Löbmann, Holger Grohganz, Thomas Rades, Claudia S Leopold
The concept of controlled in situ amorphisation of drug/polymer mixtures has been introduced previously with indomethacin-Eudragit® E and naproxen-Eudragit® E compacts. In the present study, the feasibility of in situ amorphisation of a crystalline API with the low molecular weight coformer arginine was investigated. This research was based on a previous study, which showed that a high relative humidity (75% RH) may induce co-amorphisation of indomethacin with arginine. It was assumed that an in situ co-amorphisation may be achieved, if a tablet containing a crystalline acidic API and the basic amino acid arginine, coated with a gastro-resistant but water-permeable coating, is exposed to an acidic medium...
October 16, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30316818/cross-interaction-chromatography-as-a-rapid-screening-technique-to-identify-the-stability-of-new-antibody-therapeutics
#18
Sarah H M Hedberg, Jonathan Rapley, Jonathan M Haigh, Daryl R Williams
Protein aggregation can be a major problem in the manufacturing of new biopharmaceuticals and there is a desirability for development of techniques that can predict the behaviour of new biopharmaceuticals early on in the development process. A technique that can be used to predict aggregation is self-interaction chromatography that is used to determine the second virial coefficient, B22 , but one of the limitations includes the need to immobilise every protein of interest. In this study a related technique, cross interaction chromatography (CIC), is evaluated which overcomes this limitation...
October 11, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30315863/monoolein-based-nanoparticles-for-drug-delivery-to-the-central-nervous-system-a-platform-for-lysosomal-storage-disorder-treatment
#19
Bruna Donida, Bárbara Tauffner, Marco Raabe, Maira F Immich, Marcelo A de Farias, Diego de Sá Coutinho, Andryele Zaffari Machado, Rejane Gus Kessler, Rodrigo V Portugal, Andressa Bernardi, Rudimar Frozza, Dinara J Moura, Fernanda Poletto, Carmen Regla Vargas
Lysosomal Storage Disorders (LSDs) are characterized by an abnormal accumulation of substrates within the lysosome and comprise more than 50 genetic disorders with a frequency of 1:5000 live births. Nanotechnology may be a promising way to circumvent the drawbacks of the current therapies for lysosomal diseases. The blood circulation time and bioavailability of the enzymes or drugs could be improved by inserting them in nanocarriers, which could decrease and/or avoid the need of frequent intravenous infusions along with the minimization or elimination of associated immunogenic responses...
October 10, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30312742/passive-inhalation-of-dry-powder-influenza-vaccine-formulations-completely-protects-chickens-against-h5n1-lethal-viral-challenge
#20
Jasmine Tomar, Carin Biel, Cornelis A M de Haan, Peter J M Rottier, Nikolai Petrovsky, Henderik W Frijlink, Anke Huckriede, Wouter L J Hinrichs, Ben Peeters
Bird to human transmission of high pathogenicity avian influenza virus (HPAIV) poses a significant risk of triggering a flu pandemic in the human population. Therefore, vaccination of susceptible poultry during an HPAIV outbreak might be the best remedy to prevent such transmissions. To this end, suitable formulations and an effective mass vaccination method that can be translated to field settings needs to be developed. Our previous study in chickens has shown that inhalation of a non-adjuvanted dry powder influenza vaccine formulation during normal breathing results in partial protection against lethal influenza challenge...
October 9, 2018: European Journal of Pharmaceutics and Biopharmaceutics
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