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European Journal of Pharmaceutics and Biopharmaceutics

Yuchen Wang, Maureen R Newman, Danielle S W Benoit
Impaired fracture healing is a major clinical problem that can lead to patient disability, prolonged hospitalization, and significant financial burden. Although the majority of fractures heal using standard clinical practices, approximately 10% suffer from delayed unions or non-unions. A wide range of factors contribute to the risk for nonunions including internal factors, such as patient age, gender, and comorbidities, and external factors, such as the location and extent of injury. Current clinical approaches to treat nonunions include bone grafts and low-intensity pulsed ultrasound (LIPUS), which realizes clinical success only to select patients due to limitations including donor morbidities (grafts) and necessity of fracture reduction (LIPUS), respectively...
February 19, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Manuel Gregoritza, Kathrin Abstiens, Moritz Graf, Achim M Goepferich
Reducing burst effects, providing controlled release, and safeguarding biologics against degradation are a few of several highly attractive applications for microgels in the field of controlled release. However, the incorporation of proteins into microgels without impairing stability is highly challenging. In this proof of concept study, the combination of microfluidics and thiol-ene photoclick chemistry was evaluated for the fabrication of antibody-loaded microgels with narrow size distribution. Norbornene-modified eight-armed poly(ethylene glycol) with an average molecular mass of 10,000 Da, 20,000 Da, or 40,000 Da were prepared as macromonomers for microgel formation...
February 19, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Taro Shimizu, Amr S Abu Lila, Risako Fujita, Mizuki Awata, Munehira Kawanishi, Yosuke Hashimoto, Keiichiro Okuhira, Yu Ishima, Tatsuhiro Ishida
Surface decoration of liposomes with polyethylene glycol (PEG), PEGylation, is recognized as a method to bestow liposomes with a prolonged circulation time following intravenous administration. However, many reports have emphasized that a first dose of PEGylated liposomes (PL) elicits an anti-PEG IgM antibody response that can trigger a rapid systemic clearance of a second dose of PL via a phenomenon that is referred to as "accelerated blood clearance (ABC)." Such a phenomenon is usually observed with PL that has been modified with methoxy-PEG...
February 17, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Xunan Zhang, Wei Zong, Hongmei Bi, Kunming Zhao, Thomas Fuhs, Ying Hu, Wenlong Cheng, Xiaojun Han
As promising drug delivery vehicles, previous investigations of liposomes as carriers are primarily focused on insertion and modification of lipid membrane interfaces. The utility of inner core seems to be overlooked. Herein, we developed PSLs containing aqueous two phase system (ATPS), and intriguingly discovered their hierarchical release under acidic stimuli. ATPS containing two polymers (poly(ethylene glycol) (PEG) and dextran) is homogeneous beyond phase transition temperature when producing ATPS-liposomes, and separated into PEG-rich phase and dextran-rich phase after cooling down to room temperature...
February 17, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Déborah Simões, Sónia P Miguel, Maximiano P Ribeiro, Paula Coutinho, António G Mendonça, Ilídio J Correia
Skin and soft tissue infections (SSTIs) have high rates of morbidity and mortality associated. Despite the successful treatment of some SSTIs, those affecting the subcutaneous tissue, fascia, or muscle delay the healing process and can lead to life-threatening conditions. Therefore, more effective treatments are required to deal with such pathological situations. Recently, wound dressings loaded with antimicrobial agents emerged as viable options to reduce wound bacterial colonization and infection, in order to improve the healing process...
February 17, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Elisa Boanini, Paola Torricelli, Francesca Bonvicini, Maria Cristina Cassani, Milena Fini, Giovanna Angela Gentilomi, Adriana Bigi
The development of new biomaterials able to favor bone formation and to inhibit bone abnormal resorption is mandatory to face the increasing number of age-related musculo-skeletal disorders. Moreover, the increasing antibiotic resistance of clinically important bacteria, which is among the main causes of implant failure, requires new antimicrobial systems. In this study, we prepared multifunctional materials consisting of hydroxyapatite-zoledronate composite crystals decorated with Ag Nanoparticles (AgNPs)...
February 15, 2018: European Journal of Pharmaceutics and Biopharmaceutics
F Stauffer, V Vanhoorne, G Pilcer, P-F Chavez, S Rome, M A Schubert, L Aerts, T De Beer
Active Pharmaceutical Ingredients (API) raw material variability is not always thoroughly considered during pharmaceutical process development, mainly due to low quantities of drug substance available. However, synthesis, crystallization routes and production sites evolve during product development and product life cycle leading to changes in physical material attributes which can potentially affect their processability. Recent literature highlights the need for a global approach to understand the link between material synthesis, material variability, process and product quality...
February 13, 2018: European Journal of Pharmaceutics and Biopharmaceutics
M De Bardi, R Müller, C Grünzweig, D Mannes, M Rigollet, F Bamberg, T A Jung, K Yang
Staked-in needle pre-fillable syringes (SIN-PFS) are a convenient delivery system widely established in the growing pharmaceutical market. Under specific storage conditions, the needle of PFS containing high concentration drug product (DP) solution is prone to clogging, which prevents administration of the liquid. The purpose of this study is to clarify the clogging phenomenon of SIN-PFS and to elucidate the role of water vapor transmission via the needle shield. The presence of liquid within needles is a prerequisite condition for clogging and was investigated non-invasively by neutron imaging (NI) to confirm that liquid can migrate into the needle under certain processing conditions...
February 12, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Li-Ping Zhang, Xue-Xia Tan, Yan-Ping Huang, Zhao-Sheng Liu
Liquid crystalline molecularly imprinted polymers (LC-MIPs) were low cross-linking MIPs (5-20 mol %) by introducing a LC monomer into the MIP polymerization system to keep the shape of the imprinted cavities due to additional interactions between the mesogenic groups. The multiwalled carbon nanotubes (MWCNTs) coated LC-MIP (MWCNT@LC-MIP) was the first fabricated as a novel floating interaction-controlled DDS. The synthesis was achieved by adding 9-vinylanthracene to obtain the high-density vinyl group functionalized MWCNTs firstly, and then polymerization of LC MIPs was performed on the surface of MWCNTs using a mixture of methacrylic acid, ethylene glycol dimethacrylate, and 4-methyl phenyl dicyclohexyl ethylene (LC monomer) with levofloxacin (LVF) as model template drug...
February 10, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Hye-Rin Jeong, Ji-Yeon Kim, Sang-Nyun Kim, Jung-Hwan Park
Dissolving microneedles (MN) containing cyclosporin A (CyA) were prepared for local delivery of CyA into the dermal layer. The efficacy of using MN to deliver CyA, an insoluble and high molecular weight drug, was observed and compared with oral administration of solubilized CyA. Microneedles containing CyA (CyA MN) were prepared using a closed, low-temperature molding process. The mechanical properties of CyA MN and phase separation were studied regarding the content of CyA. CyA MN were inserted into porcine skin for a predetermined time, and the dissolution and delivered amount of CyA were measured in vitro with an optical microscope and high-performance liquid chromatography (HPLC) analysis of the extracted CyA...
February 9, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Marcela Araújo Pereira, Juliana de Souza Rebouças, Rafaela de Siqueira Ferraz Carvalho, Inés Luis de Redín, Priscila Valera Guerra, Carlos Gamazo, Claudia Ida Brodskyn, Juan M Irache, Nereide Stela Santos-Magalhães
Cashew nut allergy is the second most commonly reported tree nut allergy. Traditional allergen immunotherapy presents several clinical drawbacks that can be reduced by using nanoparticles-basedallergen-delivery systems, modulating the immune response towards a protective one. In this context, the goal of this work was to assess the potential of poly(anhydride) nanoparticles (NP) for cashew nut oral immunization. Cashew nut allergens-loaded nanoparticles (CNE-NP) were prepared by solvent displacement method...
February 8, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Marina P Abuçafy, Bruno L Caetano, Bruna G Chiari-Andréo, Bruno Fonseca-Santos, Aline M do Santos, Marlus Chorilli, Leila A Chiavacci
Drug delivery systems have been used to reduce adverse effects and improve the efficacy of therapies. Drug carriers have been developed over the years, but they have limitations. γ-cyclodextrin-based metal-organic frameworks (γ-CD-MOF) have significant advantages due to their biocompatibility and environmental safety, besides crystallinity and porosity. Herein, γ-CD-MOFs were synthesised with different metals as nodes and investigated. Uniform mesoporous γ-CD-MOFs were obtained and showed an absence of toxicity in HepG2 and Caco-2 cells...
February 8, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Ziwei Zhang, Dominique Jasmin Lunter
The purpose of this study was to investigate the impact of emulsifiers and formulations on intercellular lipids of porcine stratum corneum (SC) and evaluate confocal Raman microscopy (CRM) as an alternative method in this research context. To this end, four different formulations were used: three conventional creams that contained ionic and/or non-ionic emulsifiers and one surfactants-free emulsion stabilized by a polymeric emulsifier. Additionally, all emulsifiers were tested in aqueous solution/dispersion in the respective concentrations as present in the formulations...
February 8, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Yuki Sato, Tatsuru Joumura, Shunsuke Nashimoto, Sayaka Yokoyama, Yoh Takekuma, Hideto Yoshida, Mitsuru Sugawara
Lutein is located in the macula lutea in the human eye. Since humans cannot synthesize lutein de novo, it must be digested as food. Some studies including our previous study showed very low absorption of lutein after oral administration. Those studies also suggested that the absorption route of lutein from the small intestine involves not only the blood but also the lymph. The aim of this study was to clarify the transfer of lutein into lymph and the tissue distribution after oral administration of a solid dispersion (SD) and a self-microemulsifying drug delivery system (SMEDDS) for improvement of the absorption...
February 8, 2018: European Journal of Pharmaceutics and Biopharmaceutics
R M de Kruijff, A J G M van der Meer, C A A Windmeijer, J J M Kouwenberg, A Morgenstern, F Bruchertseifer, P Sminia, A G Denkova
Alpha emitters have great potential in targeted tumour therapy, especially in destroying micrometastases, due to their high linear energy transfer (LET). To prevent toxicity caused by recoiled daughter atoms in healthy tissue, alpha emitters like 225Ac can be encapsulated in polymeric nanocarriers (polymersomes), which are capable of retaining the daughter atoms to a large degree. In the translation to a (pre-)clinical setting, it is essential to evaluate their therapeutic potential. As multicellular tumour spheroids mimic a tumour microenvironment more closely than a two-dimensional cellular monolayer, this study has focussed on the interaction of the polymersomes with U87 human glioma spheroids...
February 8, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Guoliang Wu, Shujing Wang, Zhou Tian, Ning Zhang, Han Sheng, Weiguo Dai, Feng Qian
No abstract text is available yet for this article.
February 8, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Giacomo Russo, Lucia Grumetto, Roman Szucs, Francesco Barbato, Frederic Lynen
The Blood-Brain Barrier (BBB) plays an essential role in protecting the brain tissues against possible injurious substances. In the present work, 79 neutral, basic, acidic and amphoteric structurally unrelated analytes were considered and their chromatographic retention coefficients on immobilized artificial membrane (IAM) stationary phase were determined employing a mass spectrometry (MS) -compatible buffer based on ammonium acetate. Their BBB passage predictive strength was evaluated and the statistical models based on IAM indexes and in silico physico-chemical descriptors showed solid statistics (r2 (n-1) = 0...
February 7, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Cheng Du, Gregory Barnett, Ameya Borwankar, Angela Lewandowski, Nripen Singh, Sanchayita Ghose, Michael Borys, Zheng Jian Li
As macromolecules, biologics are susceptible to light exposure, which induces oxidation of multiple amino acid residues including tryptophan, tyrosine, phenylalanine, cysteine and methionine. Pertaining to safety, efficacy and potency, light-induced oxidation of biologics has been widely studied and necessary precautions need to be taken during biologics manufacturing process, drug substance and products handling and storage. Proteins will degrade to varying extents depending on the protein properties, degradation pathways, formulation compositions and type of light source...
February 7, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Arnold Duralliu, Paul Matejtschuk, Daryl R Williams
Maintaining low moisture content is seen as crucial to sustaining long term stability in freeze dried (FD) cakes as higher moisture could lead to cake collapse, degradation and loss in biological potency. Using a combination of gravimetric data and video images captured from a Dynamic Vapour Sorption instrument the onset humidity Collapse Point (RHcp), the humidity Onset Crystallisation (RHc) and Onset Glass Transition (RHg) points for a series of freeze dried cakes at 10, 25 and 40°C have been determined...
February 3, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Safrina Dyah Hardiningtyas, Rie Wakabayashi, Momoko Kitaoka, Yoshiro Tahara, Kosuke Minamihata, Masahiro Goto, Noriho Kamiya
Phycocyanin (PC), a water-soluble protein-chromophore complex composed of hexameric (αβ)6 subunits, has important biological functions in blue-green algae as well as pharmacological activities in biomedicine. We have previously developed a solid-in-oil (S/O) nanodispersion method to deliver biomacromolecules through the skin, although the transcutaneous mechanism has not yet been fully elucidated. To study the mechanism of transcutaneous protein delivery, we therefore enabled S/O nanodispersion by coating PC with hydrophobic surfactants and evaluated how the proteinaceous macromolecules formulated in an oil phase might permeate the skin...
February 3, 2018: European Journal of Pharmaceutics and Biopharmaceutics
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