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European Journal of Pharmaceutics and Biopharmaceutics

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https://www.readbyqxmd.com/read/30633973/polyamidoamine-dendrimers-based-nanomedicine-for-combination-therapy-with-sirna-and-chemotherapeutics-to-overcome-multidrug-resistance
#1
Jiayi Pan, Livia Palmerston Mendes, Momei Yao, Nina Filipczak, Sumanta Garai, Ganesh A Thakur, Can Sarisozen, Vladimir P Torchilin
Multidrug resistance (MDR) significantly decreases the therapeutic efficiency of anti-cancer drugs. Its reversal could serve as a potential method to restore the chemotherapeutic efficiency. Downregulation of MDR-related proteins with a small interfering RNA (siRNA) is a promising way to reverse the MDR effect. Additionally, delivery of small molecule therapeutics simultaneously with siRNA can enhance the efficiency of chemotherapy by dual action in MDR cell lines. Here, we conjugated the dendrimer, generation 4 polyamidoamine (G4 PAMAM), with a polyethylene glycol (PEG)-phospholipid copolymer...
January 8, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30633972/recent-advances-in-microneedle-based-drug-delivery-special-emphasis-on-its-use-in-paediatric-population
#2
REVIEW
Sanjukta Duarah, Manisha Sharma, Jingyuan Wen
Transdermal drug delivery offers several attractive advantages over the traditional oral and parenteral routes. Particularly, in case of paediatric patients, it helps to overcome the issues specific to this population, such as difficulty in swallowing and palatability of oral medicines as well as fear and pain associated with needles. However, due to the formidable barrier characteristic of the stratum corneum, it fails in the effective systemic delivery of broad range of therapeutic molecules, especially macromolecules and genetic material...
January 8, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30630062/stability-of-lysozyme-incorporated-into-electrospun-fibrous-mats-for-wound-healing
#3
Xiaoli Liu, Line Hagner Nielsen, Haiyan Qu, Lars Porskjær Christensen, Jukka Rantanen, Mingshi Yang
In this study, we investigated the feasibility of incorporating protein drugs into electrospun fibrous mats (EFMs) for wound healing using lysozyme as a model drug. Lysozyme nanoparticles (Lyso- NPs) were first obtained by electrospray. Lysozyme solutions were prepared with a binary solvent mixture of ethanol (EtOH)-water (H2 O) at varied volume ratios. Subsequently, Lyso-NPs were suspended in poly(lactic-co-glycolic acid) (PLGA) solutions using trifluoroethanol (TFE) as a solvent. Lyso-NPs loaded EFMs were obtained by electrospinning of the aforementioned suspensions, and the bioactivity of lysozyme in the EFMs was investigated using fluorescence-based assay kit...
January 7, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30630061/edible-solid-foams-as-porous-substrates-for-inkjet-printable-pharmaceuticals
#4
Laura-Diana Iftimi, Magnus Edinger, Daniel Bar-Shalom, Jukka Rantanen, Natalja Genina
The aim of this study was to investigate new porous flexible substrates, i.e., solid foams that would serve as a carrier with a high ink absorption potential for inkjet printable pharmaceuticals. Propranolol hydrochloride was used as a model active pharmaceutical ingredient (API). Pharmaceutically approved and edible cellulose derivatives and gums together with different additives were evaluated as a base for the substrate. Different methods for preparation of a solid foam such as freeze-drying, vacuum oven drying and drying at room temperature were explored...
January 7, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30630060/imiquimod-loaded-nanocapsules-improve-cytotoxicity-in-cervical-cancer-cell-line
#5
L A Frank, R P Gazzi, P Mello, A Buffon, A R Pohlmann, S S Guterres
This paper proposes the development of imiquimod-loaded polymeric nanocapsules formulation for the treatment of cervical cancer. The mechanism of death involved in the reduction of the cell viability as well as the production of an inflammation marker (IL-6) after the treatment in cell line SiHa have been evaluated. The formulation has significantly decreased the viability of the cells in a time-dependent manner, after 24, 48 and 72 hours. Additionally, results showed a cellular decrease of almost 80% of the cells after 72 hours of treatment...
January 7, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30615927/polymeric-nanoparticles-for-the-delivery-of-mirna-to-treat-chronic-obstructive-pulmonary-disease-copd
#6
Adel Mohamed, Nitesh K Kunda, Kehinde Ross, Gillian A Hutcheon, Imran Y Saleem
RNA interference (RNAi) based therapeutics are considered an endogenous mechanism for modulating gene expression. In addition, microRNAs (miRNAs) may be tractable targets for the treatment of Chronic Obstructive Pulmonary Disease (COPD). In this study miR146a was adsorbed onto poly (glycerol adipate-co-ω-pentadecalactone), PGA-co-PDL, nanoparticles (NPs) to reduce target gene IRAK1 expression. NPs were prepared using an oil-in-water single emulsion solvent evaporation method incorporating cationic lipid dioleoyltrimethylammoniumpropane (DOTAP)...
January 4, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30590107/lipodendriplexes-a-promising-nanocarrier-for-enhanced-gene-delivery-with-minimal-cytotoxicity
#7
Imran Tariq, Shashank Reddy Pinnapireddy, Lili Duse, Muhammad Yasir Ali, Sajid Ali, Muhammad Umair Amin, Nathalie Goergen, Jarmila Jedelská, Jens Schäfer, Udo Bakowsky
Non-viral vectors are a safe, efficient and non-toxic alternative to viral vectors for gene therapy against many diseases ranging from genetic disorders to cancers. Polyamidoamine (PAMAM), a positively charged dendrimer has a tendency to complex with nucleic acids (to form dendriplexes) like plasmid DNA (pDNA) and small interfering RNA (siRNA) and can shield them from enzymatic degradation, thereby facilitating endocytosis and endosomal release. In this study, we developed an advanced variant of the dendriplexes by encapsulating them within liposomes to enhance their gene delivery efficiency...
December 24, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30582960/bioanalytical-method-development-and-validation-for-determination-of-fibroblast-growth-factor-peptide-and-its-application-to-pharmacokinetic-studies
#8
Ing-Orn Prasanchaimontri, Hardik Chandasana, Mohammad A Akbar, Steven Swarts, Paul Okuneiff, Hartmut Derendorf
Fibroblast growth factor peptide (FGF-P) is a polypeptide analog of FGF-2 that could be a potential mitigation and treatment agent for radiation syndromes. Prior to conducting preclinical pharmacokinetics, we developed and validated the LC-MS/MS bioanalytical method for determination of FGF-P in rat plasma for the first time. FGF-P was extracted from rat plasma using the protein precipitation technique followed liquid-liquid extraction using dichloromethane as a solvent. The mobile phases consisted of two components: (a) 0...
December 21, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30582959/managing-active-pharmaceutical-ingredient-raw-material-variability-during-twin-screw-blend-feeding
#9
F Stauffer, V Vanhoorne, G Pilcer, Pierre-François Chavez, M A Schubert, C Vervaet, T De Beer
Continuous powder feeding is a critical step in continuous manufacturing of solid dosage forms, as this unit operation should ensure the mass flow consistency at the desired powder feed rate to guarantee the process throughput and final product consistency. In this study, twin-screw feeding of a pharmaceutical formulation (i.e., blend) existing of a highly dosed very poorly flowing active pharmaceutical ingredient (API) leading to insufficient feeding capacity was investigated. Furthermore, the API showed very high batch-to-batch variability in raw material properties dominating the formulation blend properties...
December 21, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30579852/-temporary-plasticiser-a-novel-solution-to-fabricate-3d-printed-patient-centred-cardiovascular-polypill-architectures
#10
Beatriz C Pereira, Abdullah Isreb, Robert T Forbes, Filipa Dores, Rober Habashy, Jean-Baptiste Petit, Mohamed A Alhnan, Enoche Oga
Hypertension and dyslipidaemia are modifiable risk factors associated with cardiovascular diseases (CVDs) and often require a complex therapeutic regimen. The administration of several medicines is commonly associated with poor levels of adherence among patients, to which World Health Organisation (WHO) proposed a fixed-dose combination unit (polypill) as a strategy to improve adherence. In this work, we demonstrate the fabrication of patient-specific polypills for the treatment of CVDs by fused deposition modelling (FDM) 3D printing and introduce a novel solution to meet critical quality attributes...
December 20, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30579851/in-vitro-models-for-the-prediction-of-in-vivo-performance-of-oral-dosage-forms-recent-progress-from-partnership-through-the-imi-orbito-collaboration
#11
James Butler, Bart Hens, Maria Vertzoni, Joachim Brouwers, Philippe Berben, Jennifer Dressman, Cord J Andreas, Kerstin Julia Schaefer, James Mann, Mark McAllister, Masoud Jamei, Edmund Kostewicz, Filippos Kesisoglou, Peter Langguth, Mans Minekus, Anette Müllertz, Ronald Schilderink, Mirko Koziolek, Philipp Jedamzik, Werner Weitschies, Christos Reppas, Patrick Augustijns
The availability of in vitro tools that are constructed on the basis of a detailed knowledge of key aspects of gastrointestinal (GI) physiology and their impact on formulation performance and subsequent drug release behaviour is fundamental to the success and efficiency of oral drug product development. Over the last six years, the development and optimization of improved, biorelevant in vitro tools has been a cornerstone of the IMI OrBiTo (Oral Biopharmaceutics Tools) project. By bringing together key industry and academic partners, and by linking tool development and optimization to human studies to understand behaviour at the formulation / GI tract interface, the collaboration has enabled innovation, optimization and implementation of the requisite biorelevant in vitro tools...
December 20, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30576708/evaluation-of-the-effects-of-spray-drying-parameters-for-producing-cubosome-powder-precursors
#12
Christoffer von Halling Laier, Tommy Sonne Alstrøm, Mia Travers Bargholz, Pernille Bjerg Sjøltov, Thomas Rades, Anja Boisen, Line Hagner Nielsen
Vaccines provide great benefit for global health, but are insufficiently distributed in developing countries due to high costs of manufacturing and limited storage stability. Spray drying formulations of peptide-based vaccines offer a promising strategy to reduce production costs and improve unrefrigerated storage stability. This design of experiments investigated how adjusting spray drying parameters (inlet temperature, atomization pressure, feed rate and aspiration rate) affects residual moisture and reconstitution properties of the powder product, and morphology and size of the rehydrated particles...
December 18, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30552972/sustained-release-of-recombinant-thrombomodulin-from-cross-linked-gelatin-hyaluronic-acid-hydrogels-potentiate-wound-healing-in-diabetic-mice
#13
Yun-Yan Hsu, Kuan-Lin Liu, Hsun-Hua Yeh, Hong-Ru Lin, Hua-Lin Wu, Jui-Chen Tsai
Thrombomodulin (TM) is a type-I transmembrane glycoprotein expressed on the surfaces of endothelial cells and epidermal keratinocytes. It is known to regulate blood coagulation, inflammation, and cell-cell adhesion. A recombinant TM, which contains an epidermal growth factor - like domain and serine/threonine-riches domain, has been demonstrated to stimulate cell proliferation and migration of keratinocytes and wound healing. In this study, we developed the biodegradable hydrogels and evaluated the efficacy of sustained release of rhTM from the hydrogel for the treatment of diabetic wounds...
December 12, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30550923/redox-responsive-prodrug-like-pegylated-macrophotosensitizer-nanoparticles-for-enhanced-near-infrared-imaging-guided-photodynamic-therapy
#14
Zheng Ruan, Pan Yuan, Tuanwei Li, Youliang Tian, Quan Cheng, Lifeng Yan
Efficient delivery of hydrophobic photosensitizer (PS) into tumor cells is a key step for photodynamic therapy (PDT). Redox-responsive polymeric nanoparticles of amphiphilic macro-photosensitizer has designed and prepared as a prodrug-like pro-photosensitizer (pro-PS) for PDT. PEG works as the hydrophilic block and the near infrared (NIR) brominated BODIPY derivative (BDP) works as the hydrophobic PS, and they were linked via the disulfide bond as PEG-SS-BDP, which could be broken for drug release owing to the high GSH concentration inside tumor cells...
December 11, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30543948/elastic-recovery-of-filler-binders-to-safeguard-viability-of-lactobacillus-rhamnosus-gg-during-direct-compression
#15
Eline Byl, Sarah Lebeer, Filip Kiekens
Tablets are increasingly explored as dosage form for oral probiotics, especially for applications such as pharyngitis and dental health. In such tablets, the dry form increases the stability and the shelf life of the product. In addition, the probiotic cells are entrapped in the tablet matrix, which protects them against the environmental factors in the human body. However, the development of a probiotic tablet with an adequate number of viable cells remains a challenge due to the stress of the compression process...
December 10, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30529296/individualized-in-vitro-and-in-silico-methods-for-predicting-in-vivo-performance-of-enteric-coated-tablets-containing-a-narrow-therapeutic-index-drug
#16
Frank Karkossa, Sandra Klein
The efficacy of narrow therapeutic index (NTI) drugs is closely related to their plasma concentration-time profile. Particularly for these compounds interindividual variability of gastrointestinal (GI) parameters relevant to in vivo drug release may result in fluctuations of the plasma concentration. The present study focused on assessing the influence of individual GI pH- and transit profiles on drug release of enteric valproate tablet formulations by means of individualized in vitro dissolution experiments...
December 5, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30529295/chemically-identical-but-physically-different-a-comparison-of-spray-drying-hot-melt-extrusion-and-cryo-milling-for-the-formulation-of-high-drug-loaded-amorphous-solid-dispersions-of-naproxen
#17
Sien Dedroog, Christophe Huygens, Guy Van den Mooter
In spite of the large research efforts in the past two decades, it is still difficult, if possible at all, to predict what manufacturing technology will lead to the best amorphous solid dispersions (ASDs) in terms of drug to polymer ratio ("drug loading") and physical stability. In general, ASDs can be prepared by solvent based methods, heat based methods and mechanochemical activation. In the current study, one manufacturing technique per category was selected: spray drying, hot melt extrusion and cryo-milling, respectively...
December 5, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30529294/hydroxycamptothecin-nanoparticles-based-on-poly-oligo-ethylene-glycol-architecture-effects-of-nanocarriers-on-antitumor-efficacy
#18
Yifei Guo, Ting Wang, Hanhong Qiu, Meihua Han, Zhengqi Dong, Xiangtao Wang, Yanhong Wang
Nanoparticles decorated with hydrophilic PEG chains had been emerged as effective drug delivery system due to their biocompatibility and biodegradability, while, the influence of their architecture on antitumor efficacy remained challenging. In this study, the linear poly(ethylene glycol) (PEG45 ), brush oligo(triethylene glycol) (TEG10 ), and oligo(ethylene glycol) dendron (G2), which showed the similar molar mass but different architecture, were utilized as nanocarriers to prepare 10-hydroxycamptothecin (HCPT) nanoparticles...
December 5, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30529434/freeze-thaw-of-igg-solutions
#19
Jacqueline Horn, Sampeeti Jena, Alptekin Aksan, Wolfgang Friess
In this communication, the effect of mannitol and trehalose crystallization on the unfolding of IgG1 , a monoclonal antibody, in the frozen state with repeat freeze/thaw under different pH conditions was explored. Formulations were annealed at -20°C for 20hours five times (interrupted by freeze/thaw). This was done to induce excipient crystallization. Characterization of the frozen-thawed samples was performed by circular dichroism, particle analysis, and size exclusion chromatography. At a pH of 3, formation of insoluble and soluble aggregates was observed however, these could be reduced by the use of a surfactant...
December 4, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/30481559/development-of-a-flow-through-usp-4-apparatus-drug-release-assay-for-the-evaluation-of-amphotericin-b-liposome
#20
Jie Tang, Santhanakrishnan Srinivasan, Wenmin Yuan, Ran Ming, Yayuan Liu, Zhipeng Dai, Charles O Noble, Mark E Hayes, Nan Zheng, Wenlei Jiang, Francis C Szoka, Anna Schwendeman
AmBisome® is a liposomal formulation of amphotericin B (Amp B), a complex parenteral antifungal product with no US FDA approved generic version available to date. For generic Amp B liposomal product development, examination of the drug release profile is important for product quality control and analytical comparability evaluation with the reference listed drug. Yet, there is no standardized in vitro drug release (IVR) assay currently available for Amp B liposomes. In this study, we describe the development of a USP-4 apparatus-based IVR assay capable of discriminating liposomal Amp B formulations based on the drug release profile...
November 24, 2018: European Journal of Pharmaceutics and Biopharmaceutics
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