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European Journal of Pharmaceutics and Biopharmaceutics

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https://read.qxmd.com/read/31004790/effect-of-implantation-site-on-outcome-of-tissue-engineered-vascular-grafts
#1
Tornike Sologashvili, Shahrul A Saat, Jean-Christophe Tille, Sarra De Valence, Damiano Mugnai, Jean Pierre Giliberto, Jeswant Dillon, Azhari Yakub, Zamrin Dimon, Robert Gurny, Beat H Walpoth, Michael Moeller
OBJECTIVE: Vascular prostheses for small caliber bypass grafts in cardiac and vascular diseases or for access surgery are still missing. Poly (Ɛ-caprolactone) (PCL) has been previously investigated by our group and showed good biocompatibility and mechanical properties in vitro and rapid endothelialisation, cellular infiltration and vascularisation in vivo yielding optimal patency in the abdominal aortic position. The aim of the present study is to evaluate our PCL graft in the carotid position and to compare its outcome to the grafts implanted in the abdominal aortic position...
April 17, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://read.qxmd.com/read/31002864/vancomycin-ocular-delivery-systems-based-on-glycerol-monooleate-reversed-hexagonal-and-reversed-cubic-liquid-crystalline-phases
#2
Spomenka Milak, Angela Chemelli, Otto Glatter, Andreas Zimmer
Lyotropic bulk reversed hexagonal and reversed cubic liquid crystalline phases (hexagonal and cubic phases) composed of glycerol monooleate (GM) were used to design the vancomycin hydrochloridés (VHCl) delivery systems aiming to maintain VHCĺs therapeutic concentration during 24 h in the eye, locally (as an insert) and/or intravitreally (as a bulk phase injection). Bulk VHCĺs hexagonal and cubic phases were successfully prepared by melted homogenization and solvent evaporation method, and then an insert was prepared...
April 16, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://read.qxmd.com/read/31002863/infrared-spectroscopic-study-of-the-coil-helix-transition-of-highly-concentrated-gelatin-formulations
#3
Fabian Polyak, Gabriele Reich
The aim of this study was to investigate the applicability of ATR-FTIR spectroscopy as an analytical tool to monitor the gel formation of highly concentrated gelatin formulations. Spectral changes induced by the coil-helix transition have been studied and related to the elasticity parameter G' obtained by oscillatory rheology in simultaneous measurements. A principal component analysis of the amide I band allowed the evaluation of triple helix formation kinetics. It was found that the key frequencies of the amide I band at 1657 and 1612 cm-1 represent the transition of the gelatin molecules from the random coil to the triple helical conformation in the emerging gel...
April 16, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://read.qxmd.com/read/30991089/liposomes-containing-biosurfactants-isolated-from-lactobacillus-gasseri-exert-antibiofilm-activity-against-methicillin-resistant-staphylococcus-aureus-strains
#4
Barbara Giordani, Paolo Emidio Costantini, Stefano Fedi, Martina Cappelletti, Angela Abruzzo, Carola Parolin, Claudio Foschi, Giulia Frisco, Natalia Calonghi, Teresa Cerchiara, Federica Bigucci, Barbara Luppi, Beatrice Vitali
Staphylococcus aureus is the major causative agent of skin and soft tissue infections, whose prevention and treatment have become more difficult due to the emergence of antibiotic-resistant strains. In this regard, the development of an effective treatment represents a challenge that can be overcome by delivering new antibiofilm agents with appropriate nanocarriers. In this study, a biosurfactant (BS) isolated from Lactobacillus gasseri BC9 and subsequently loaded in liposomes (LP), was evaluated for its ability to prevent the development and to eradicate the biofilm of different methicillin resistant S...
April 13, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://read.qxmd.com/read/30981947/development-of-resiquimod-loaded-modified-pla-based-nanoparticles-for-cancer-immunotherapy-a-kinetic-study
#5
Cédric Thauvin, Jérôme Widmer, Inès Mottas, Sandra Hocevar, Eric Allémann, Carole Bourquin, Florence Delie
Resiquimod (R848), a member of the imidazoquinoline family, is a Toll-like receptor 7/8 agonist with high potency for cancer immunotherapy. However, tolerance induction and adverse effects limit its development as a drug. Encapsulation in a polymer matrix can circumvent these limitations, as shown in our formerly published approach where R848 was loaded into polylactic acid (PLA)-based nanoparticles (NP). Although the results were encouraging, low rates of encapsulation and rapid release of the drug were observed...
April 11, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://read.qxmd.com/read/30981946/development-and-in-vitro-evaluation-of-pressure-sensitive-adhesive-patch-for-the-transdermal-delivery-of-galantamine-effect-of-penetration-enhancers-and-crystallization-inhibition
#6
Dina Ameen, Bozena Michniak-Kohn
The transdermal route offers an attractive alternative route of drug administration especially for Alzheimer's disease patients through eliminating gastrointestinal side effects and ultimately improving compliance. In this study, we prepared an optimized matrix -type patches for the transdermal delivery of galantamine free base with ex vivo and in vitro evaluation. Four pressure sensitive adhesives with different functional groups, ten penetration enhancers and four drug loadings were tested to determine the optimized patch...
April 11, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://read.qxmd.com/read/30959180/targeted-chemo-sonodynamic-therapy-treatment-of-breast-tumours-using-ultrasound-responsive-microbubbles-loaded-with-paclitaxel-doxorubicin-and-rose-bengal
#7
Keiran Logan, Federica Foglietta, Heather Nesbitt, Yingjie Sheng, Thomas McKaig, Sukanta Kamila, Jinhui Gao, Nikolitsa Nomikou, Bridgeen Callan, Anthony P McHale, John F Callan
Mastectomy is a common surgical treatment used in the management of breast cancer but has associated physical and psychological consequences for the patient. Breast conservation surgery (BCS) is an alternative to mastectomy but is only possible when the tumour is of an appropriate size. Neo-adjuvant chemotherapy has been successfully used to downstage tumours and increase the number of patients eligible for BCS. However, the chemotherapies used in this approach are non-targeted and often result in significant side effects to the patient...
April 5, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://read.qxmd.com/read/30954659/studying-the-effect-of-solubilizing-agents-on-drug-diffusion-through-the-unstirred-water-layer-uwl-by-localized-spectroscopy
#8
Massimiliano Pio di Cagno, Paul C Stein
An experimental/computational approach has been successfully applied in order to study the effect of solubilizing vehicles (cyclodextrins and liposomes) on the passive diffusion of four active pharmaceutical ingredients (API) of different nature (hydrophilic, ionizable and lipophilic) through an unstirred water layer (UWL) model. This approach allowed the measurement of flux changes through the UWL and the computational calculation of different parameters relevant to interpret the interplay within solubilizing vehicles and UWL diffusion...
April 4, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://read.qxmd.com/read/30954658/ultrafast-in-situ-forming-poly-ethylene-glycol-poly-amido-amine-hydrogels-with-tunable-drug-release-properties-via-controllable-degradation-rates
#9
Sytze J Buwalda, Audrey Bethry, Sylvie Hunger, Sofian Kandoussi, Jean Coudane, Benjamin Nottelet
Fast in situ forming, chemically crosslinked hydrogels were prepared by the amidation reaction between N-succinimidyl ester end groups of multi-armed poly(ethylene glycol) (PEG) and amino surface groups of poly(amido amine) (PAMAM) dendrimer generation 2.0. To control the properties of the PEG/PAMAM hydrogels, PEGs were used with different arm numbers (4 or 8) as well as different linkers (amide or ester) between the PEG arms and their terminal N-succinimidyl ester groups. Oscillatory rheology measurements showed that the hydrogels form within seconds after mixing the PEG and PAMAM precursor solutions...
April 4, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://read.qxmd.com/read/30951820/pharmacological-characterization-of-the-3d-mucilair%C3%A2-nasal-model
#10
Clément Mercier, Elodie Jacqueroux, Zhiguo He, Sophie Hodin, Samuel Constant, Nathalie Perek, Delphine Boudard, Xavier Delavenne
The preclinical evaluation of nasally administered drug candidates requires screening studies based on in vitro models of the nasal mucosa. The aim of this study was to evaluate the morpho-functional characteristics of the 3D MucilAir™ nasal model with a pharmacological focus on [ATP]-binding cassette (ABC) efflux transporters. We initially performed a phenotypic characterization of the MucilAir™ model and assessed its barrier properties by immunofluorescence (IF), protein mass spectrometry and examination of histological sections...
April 2, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://read.qxmd.com/read/30951819/targeted-brain-delivery-of-methotrexate-by-glutathione-pegylated-liposomes-how-can-the-formulation-make-a-difference
#11
Yang Hu, Pieter J Gaillard, Elizabeth C M de Lange, Margareta Hammarlund-Udenaes
The purpose of this study was to quantitatively investigate how conjugation of GSH to different liposomal formulations influence the brain delivery of methotrexate (MTX) in rats. GSH-PEG liposomal MTX based on hydrogenated soy phosphatidylcholine (HSPC) or egg yolk phosphatidylcholine (EYPC) and their corresponding PEG control liposomes were prepared. The brain delivery of MTX after intravenously administering free MTX, four liposomal formulations or free MTX + empty GSH-PEG-HSPC liposomes was evaluated by performing microdialysis in brain interstitial fluid and blood...
April 2, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://read.qxmd.com/read/30946916/ultra-fast-disintegrating-odts-comprising-viable-probiotic-bacteria-and-hpmc-as-a-mucoadhesive
#12
Anja Hoffmann, Rolf Daniels
Orodispersible tablets (ODTs) are a convenient dosage form and a recent trend in formulation development. The fast disintegration is accompanied by rapid removal of the active principle and the excipients from the mouth due to saliva flow and swallowing. Probiotic bacteria are a promising strategy to fight disease with bacterial aetiology in the mouth, but a certain residence time in the oral cavity is inevitable to exert their positive effects. The addition of a mucoadhesive polymer, like hydroxypropyl methylcellulose (HPMC), is an auspicious strategy to prolong this residence time...
April 1, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://read.qxmd.com/read/30940541/antibody-drug-conjugates-stability-and-formulation
#13
REVIEW
Corinna Duerr, Wolfgang Friess
The number of antibody-drug conjugates (ADCs) on the market is expected to multiply in the upcoming years. The main reason: this novel drug delivery system combines the benefits of the selectivity of the antibody and the potency of the cytotoxic agent. The interplay of the antibody, linker and payload, however, calls for a stable and unique formulation. In this review, the literature on the stability of marketed ADCs and the respective formulations are summarized and used as a basis to give general formulation considerations for ADCs...
March 30, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://read.qxmd.com/read/30910731/exploring-the-use-of-spray-congealing-to-produce-solid-dispersions-with-enhanced-indomethacin-bioavailability-in-vitro-characterization-and-in-vivo-study
#14
Serena Bertoni, Beatrice Albertini, Luca Ferraro, Sarah Beggiato, Alessandro Dalpiaz, Nadia Passerini
The current study proposes an original oral delivery system for the bioavailability enhancement of indomethacin (IND), a BCS class II drug, with the aim to overcome the common limitations of amorphous solid dispersion. In fact, the potential risk of drug re-crystallization is a serious concern for the stability of amorphous systems and represents, despite the great bioavailability, one of the primary causes of their limited clinical applications. IND-loaded microparticles (MPs) were prepared by spray congealing using oral-approved excipients (Gelucire 50/13 and the recently marketed Gelucire 48/16)...
March 22, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://read.qxmd.com/read/30905779/comprehensive-characterization-of-nanostructured-lipid-carriers-using-laboratory-and-synchrotron-x-ray-scattering-and-diffraction
#15
Carolin Tetyczka, Aden Hodzic, Manfred Kriechbaum, Krunoslav Juraić, Christina Spirk, Sonja Hartl, Elisabeth Pritz, Gerd Leitinger, Eva Roblegg
The development of lipid nanoparticles requires knowledge on the crystalline structure, polymorphic transitions and lipid-drug interactions. This study aimed at introducing advanced techniques to characterize nanostructured lipid carriers (NLC) comprising palmitic acid, oleic acid, stabilizer and Domperidone. Crystallinity of single components and mixtures was investigated by laboratory Small Angle X-ray Scattering (SAXS). NLC were studied with laboratory Small and Wide Angle X-ray Scattering (SWAXS). Photon Correlation Spectroscopy and Freeze Fracture Transmission Electron Microscopy were used to monitor particle size, zeta potential and shape...
March 21, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://read.qxmd.com/read/30905778/n-glycans-of-complex-glycosylated-biopharmaceuticals-and-their-impact-on-protein-clearance
#16
Fabian Higel, Theresa Sandl, Chi-Ya Kao, Nicole Pechinger, Fritz Sörgel, Wolfgang Friess, Florian Wolschin, Andreas Seidl
N-glycosylation is a common post-translational modification of biopharmaceutical products. Certain types of N-glycans have been shown to influence important properties of monoclonal antibody products including pharmacokinetics and effector functions. Complex biopharmaceuticals e.g. Fc fusion proteins may contain several N- and O-glycosylation sites. Domain specific characterization of two Fc fusion proteins showed an Fc N-glycosylation pattern comparable to IgG molecules. The receptor N-glycosylation was found to contain some larger and more complex N-glycans compared to the Fc part...
March 21, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://read.qxmd.com/read/30905777/biorelevant-release-testing-of-biodegradable-microspheres-intended-for-intra-articular-administration
#17
Giulia Magri, Francesca Selmin, Francesco Cilurzo, Nikoletta Fotaki
Characterization of controlled release formulations used for intra-articular (IA) drug administration is challenging. Bio-relevant synovial fluids (BSF), containing physiologically relevant amounts of hyaluronic acid, phospholipids and proteins, were recently proposed to simulate healthy and osteoarthritic conditions. This work aims to evaluate the performance of different controlled release formulations of methylprednisolone (MP) for IA administration, under healthy and disease states simulated conditions...
March 21, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://read.qxmd.com/read/30902733/polymer-degradation-induced-drug-precipitation-in-plga-implants-why-less-is-sometimes-more
#18
Christin Zlomke, Martin Barth, Karsten Mäder
Nifedipine and nicardipine loaded PLGA extrudates have a great potential to prevent cerebral vasospasms after subarachnoid hemorrhage or surgical clipping of aneurysm. A constant release over approx. two weeks is desired. Although in vivo studies on humans have been reported, there is limited knowledge about the release kinetics and the underlying mechanisms. Therefore, Nifedipine and Nicardipine loaded PLGA implants with different drug loads were manufactured by extrusion and investigated. In addition to the measurements of the release kinetics, GPC, DSC, X-ray diffraction and light microscopic investigations were performed for a detailed characterization...
March 19, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://read.qxmd.com/read/30902732/designing-robust-immediate-release-tablet-formulations-avoiding-food-effects-for-bcs-class-3-drugs
#19
Kamran Zaheer, Peter Langguth
Food induced viscosity in the gastrointestinal tract is reported to reduce the bioavailability of tablets containing BCS class 3 drugs, mainly by retarding their disintegration and dissolution of the active pharmaceutical ingredient. The role of formulation factors in minimizing this negative food effect is largely unknown. Combinations of disintegrants were studied together with soluble and insoluble fillers and trospium chloride as model drug substance. Different batches of tablets were compressed at 10 KN and 30 KN, by incorporating different combinations of croscarmellose sodium (CSS), cross-linked polyvinylpolypyrrolidone (CPD) and sodium starch glycolate (SSG) at low level i...
March 19, 2019: European Journal of Pharmaceutics and Biopharmaceutics
https://read.qxmd.com/read/30898541/covalently-binding-mucoadhesive-polymers-n-hydroxysuccinimide-grafted-polyacrylates
#20
Claudia Menzel, Moritz Hauser, Amelie Frey, Max Jelkmann, Flavia Laffleur, Sina K Götzfried, Ronald Gust, Andreas Bernkop-Schnürch
AIM: The aim of the study was to establish a novel type of covalently mucus-binding polymers by targeting selectively amino groups within mucus glycoproteins. METHODS: N-Hydroxysuccinimide (NHS) was attached to carboxylic groups of polyacrylic acid (PAA). The reaction was mediated by the coupling reagent N,N'-dicyclohexylcarbodiimide (DCC) achieving polymeric NHS esters being able to form amide bonds with free amino groups. The chemical structure of the obtained conjugates was characterized via FTIR- and UV spectroscopy...
March 18, 2019: European Journal of Pharmaceutics and Biopharmaceutics
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