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European Journal of Pharmaceutics and Biopharmaceutics

V Gervasi, R Dall Agnol, S Cullen, T McCoy, S Vucen, A Crean
The study presented is a comprehensive overview of commercial parenteral protein formulations, approved by the European Medicines Agency (EMA), 1995-2018. The objective of this overview was to analyse current trends in the design of commercial parenteral protein products and thereby support formulation scientists in the design of new formulations. The main data source was the publicly available European Public Assessment Reports (EPARs) published by the EMA for each authorised product. An analysis of the percentage of formulations in a liquid and lyophilised form was conducted...
July 10, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Jonas Van Dingenen, Christoph Steiger, Markus Zehe, Lorenz Meinel, Romain A Lefebvre
Endogenously produced carbon monoxide (CO) has antioxidant and anti-inflammatory effects which is why CO has been investigated as a possible therapeutic agent for inflammatory disorders in different body systems, including the gastrointestinal (GI) tract. In an effort to develop an easy to use platform for CO delivery to the GI tract, we recently introduced the Oral CO Release System (OCORS) and demonstrated its preventive effect for experimental colitis in a rodent model. Building off on a comprehensive preclinical dataset on efficacy of inhaled and intraperitoneal CO in reducing postoperative ileus (POI), which is being defined as GI transit retardation after abdominal surgery, we evaluated an adapted OCORS platform to ameliorate POI by local CO delivery to the murine small intestine...
July 10, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Angela Fabiano, Anna Maria Piras, Gloria Uccello-Barretta, Federica Balzano, Andrea Cesari, Lara Testai, Valentina Citi, Ylenia Zambito
Nanoparticles (NP) only different in mucoadhesivity are compared for impact on drug oral bioavailability. Two polymeric NP types based on quaternary ammonium-chitosan (NP QA-Ch) and S-protected thiolated derivative thereof (NP QA-Ch-S-pro), respectively, containing the macromolecular drug model, FD4, were prepared by crosslinking each polymer with reduced MW hyaluronic acid. The structure of basic polymers was determined by H1 NMR analysis. NP were similar in size (371±38 vs. 376±82 nm); polydispersity index (0...
July 10, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Lisa Binder, Eva Maria Kulovits, Romana Petz, Johanna Ruthofer, Dieter Baurecht, Victoria Klang, Claudia Valenta
Vibrational spectroscopy is a useful tool for analysis of skin properties and to confirm the penetration of drugs and other formulation compounds into the skin. In particular, attenuated total reflection Fourier transform infrared (ATR-FTIR) spectroscopy and confocal Raman spectroscopy (CRS) have been optimised for skin analysis. Despite an impressive amount of data on these techniques, a comparative methodological assessment for skin penetration monitoring of model substances is still amiss. Thus, in vitro skin penetration studies were conducted in parallel using the same porcine material and four model substances, namely sodium laureth sulfate (SLES), sodium dodecyl sulfate (SDS), sulfathiazole sodium (STZ) and dimethyl sulfoxide (DMSO)...
July 5, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Kapilkumar Vithani, Adrian Hawley, Vincent Jannin, Colin Pouton, Ben J Boyd
Lipid based-formulations can enhance the bioavailability of poorly water-soluble lipophilic drugs through enhanced solubilisation of drugs in the gastrointestinal (GI) tract during digestion. This study investigates the solubilisation behaviour of poorly water-soluble drugs upon digestion of solid self-microemulsifying drug delivery system (S-SMEDDS). The S-SMEDDS were prepared using two different core lipids, Gelucire® 44/14 (GEL) or glyceryl monooleate (GMO), and were loaded with two model drugs, fenofibrate (FEN) and cinnarizine (CINN)...
July 4, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Manisha Kumari, Mahaveer Prasad Purohit, Satyakam Patnaik, Yogeshwer Shukla, Pradeep Kumar, Kailash Chand Gupta
Doxorubicin (DOX) has been extensively used to treat a wide range of cancers in free and nanotized form. Nanotization of Doxorubicin (DOX) has alleviated its toxicity and efflux-mediated resistance. However, frequent upregulation of anti-apoptotic pathways, chemotherapy-enhanced inflammation, and epithelial-mesenchymal transition (EMT), present additional aspects of cellular DOX résistance. Nanoparticle-mediated combination therapy of DOX with additional anticancer agents is expected to offer greater therapeutic benefit by alleviating the overall drug résistance...
June 30, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Dalia M Kabary, Maged W Helmy, Elsayeda-Zeinab A Abdelfattah, Jia-You Fang, Kadria A Elkhodairy, Ahmed O Elzoghby
Pulmonary delivery of drug nanocarriers can overcome the shortcomings of systemic cancer therapy via the enhanced permeability and retention (EPR) based-nanomedicine. Herein, inhalable multi-compartmental nanocomposites with the capability for both localized and modulated release of the hydrophobic mTOR inhibitor, rapamycin (RAP) and the hydrophilic herbal drug, berberine (BER) have been developed for lung cancer therapy. Two types of multi-compartmental nanocarriers were fabricated by enveloping BER hydrophobic ion pair-lipid nanocore within a shell of RAP-phospholipid complex bilayer to reduce the delivery gap between the two drugs...
June 28, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Rute Nunes, Francisca Araújo, Joana Tavares, Bruno Sarmento, José das Neves
Dense surface modification with short chain polyethylene glycol (PEG) has been previously demonstrated as favoring the transport of nanoparticles (NPs) across mucus. However, the ability of such approach to influence the distribution and retention of NPs along the length of the colorectum after rectal delivery has not been previously established. Herein, the distribution and retention of poly(lactic-co-glycolic acid) NPs modified with PEG in a non-covalent fashion are reckoned in a mouse model. Despite overall rapid depletion, both PEG-modified and non-modified NPs are able to reach the middle segment of the colon...
June 27, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Christina Apfelthaler, Katharina Skoll, Raphaela Ciola, Franz Gabor, Michael Wirth
Non-muscle invasive bladder cancer is one of the most frequent forms of cancer. Commonly, the superficial tumor is removed by a minimal invasive surgery, mostly followed by the intravesical instillation of cytostatic agents. Although the initial treatment is usually successful, the recurrence rate is extraordinary high, which might be grounded in limiting factors during instillation, such as the high resistance of the bladder wall and the constant dilution with the permanently produced urine reducing the probability of interaction between the drug and the target cell...
June 27, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Sergey Deyev, Galina Proshkina, Olga Baryshnikova, Anastasiya Ryabova, Gavriel Avishai, Liat Katrivas, Clelia Giannini, Yael Levi-Kalisman, Alexander Kotlyar
Since their discovery, liposomes have been widely employed in biomedical research. These nano-size spherical vesicles consisting one or few phospholipid bilayers surrounding an aqueous core are capable of carrying a wide variety of bioactive compounds, including drugs, peptides, nucleic acids, proteins and others. Despite considerable success achieved in synthesis of liposome constructs containing bioactive compounds, preparation of ligand-targeted liposomes comprising large quantities of encapsulated proteins and capable of affecting pathological cell still remains a big challenge...
June 26, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Philippe Berben, Jef Stappaerts, Matthias J A Vink, Elena Domínguez-Vega, Govert W Somsen, Joachim Brouwers, Patrick Augustijns
In a previously performed small-scale clinical study, healthy volunteers were asked to ingest an oral solution of itraconazole (Sporanox® ) containing 40% 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) (i) with or (ii) without a standardized volume of water (240 mL) after which gastrointestinal and blood samples were collected. Although omitting water during the administration of Sporanox® resulted in noticeable higher duodenal concentrations of itraconazole, systemic exposure was almost unaffected. It is assumed that this discrepancy can be explained by differences in the extent of entrapment of itraconazole in the duodenum caused by differential complexation depending on the concentration of cyclodextrins...
June 26, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Myoung Jin Ho, Dae Ro Lee, Sung Hyun Im, Jeong A Yoon, Chang Yong Shin, Hyun Jung Kim, Sun Woo Jang, Young Wook Choi, Young Taek Han, Myung Joo Kang
The objectives of this study were to formulate microcrystals of entecavir-3-palmiate (EV-P), a palmitic acid ester of entecavir (EV), and evaluate the influence of particle size on its pharmacokinetic behavior following subcutaneous (SC) injection. Systemic toxicity and local tolerability of the hepatitis B anti-viral suspension were further evaluated in normal rats. EV-P microcrystals possessing median diameters of 2.1, 6.3, and 12.7 µm were fabricated using anti-solvent crystallization technique with polysorbate 20 and polyethylene glycol 4000 as steric stabilizer...
June 22, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Geoff Smith, Yowwares Jeeraruangrattana, Irina Ermolina
Through vial impedance spectroscopy (TVIS) is a product non-invasive process analytical technology which exploits the frequency dependence of the complex impedance spectrum of a composite object (i.e. the freeze-drying vial and its contents) in order to track the progression of the freeze-drying cycle. This work demonstrates the use of a dual electrode system, attached to the external surface of a type I glass tubing vial (nominal capacity 10 mL) in the prediction of (i) the ice interface temperatures at the sublimation front and at the base of the vial, and (ii) the primary drying rate...
June 22, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Enrico Miceli, Stefanie Wedepohl, Ernesto Rafael Osorio Blanco, Guido Noé Rimondino, Marisa Martinelli, Miriam Strumia, Maria Molina, Mrityunjoy Kar, Marcelo Calderón
The use of thermoresponsive nanogels (NGs) allows the controlled release of therapeutic molecules upon a thermal switch. Usually, this strategy involves the use of temperature increase to activate cargo expulsion from shrinking NGs. In this study, poly(N-isopropylacrylamide) (pNIPAM)-based NGs were involved in the release of a therapeutic protein corona by temperature decrease. NGs based on dendritic polyglycerol (dPG) and thermoresponsive pNIPAM were semi-interpenetrated with poly(4-acryloylamine-4-(carboxyethyl)heptanodioic acid) (pABC)...
June 19, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Aron H Blaesi, Nannaji Saka
Recently, we have introduced fibrous dosage forms prepared by 3D-micro-patterning of drug-laden viscous melts. Such dosage forms enable predictable microstructures and increased drug release rates, and they can be manufactured continuously. However, melt processing is not applicable if the melting temperature of the formulation is greater than the degradation temperature of the drug or of the excipient. In this work, therefore, a continuous wet micro-patterning process that operates at ambient temperature is presented...
June 19, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Song Huang, Qian Zhang, Hao Li, Yaqing Sun, Gang Cheng, Meijuan Zou, Hongyu Piao
The aim of this study was to improve the oral bioavailability of a practically insoluble drug, efonidipine hydrochloride (EFH), by agglomeration in acid solution/gastric fluid. The EFH nanosuspension was prepared by the wet-milling method with F68 as a dispersing agent, SDS as an auxiliary stabilizer and L-arginine as a pH adjusting agent. The EFH nanosuspension have been prepared in industrial scale-up. The dissolution rate of the EFH nanosuspension was greater than that of bulk EFH. An in vitro intestinal permeability study showed a clear increase in the apparent permeability of different intestinal segments compared with bulk EFH...
June 18, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Annelies Smeets, Robin Koekoekx, Christian Clasen, Guy Van den Mooter
The interest in using electrospraying as a manufacturing method for amorphous solid dispersions has grown remarkably. However, the impact of formulation and process parameters needs further clarification. In this study, amorphous solid dispersions of darunavir and hydroxypropyl methylcellulose (HPMC), hydroxypropyl methylcellulose acetate succinate (HPMC AS) and polyvinylpyrrolidone K-30 (PVP) were prepared with electrospraying and spray drying, in order to compare both solvent based manufacturing techniques...
June 18, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Chiara Setti, Giulia Suarato, Giovanni Perotto, Athanassia Athanassiou, Ilker S Bayer
Emulsions are known to be effective carriers of hydrophobic drugs, and particularly injectable emulsions have been successfully implemented for in vivo controlled drug release. Recently, high internal phase emulsions have also been used to produce porous polymeric templates for pharmaceutical applications. However, emulsions containing dissolved biopolymers both in the oil and water phases are very scarce. In this study, we demonstrate such an emulsion, in which the oil phase contains a hydrophobic biodegradable polymer, MaterBi® , and the water phase is aqueous sodium alginate dispersion...
June 18, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Jinlong Zhao, Xueyan Zhang, Xiangshi Sun, Menghui Zhao, Changhui Yu, Robert J Lee, Fengying Sun, Yulin Zhou, Youxin Li, Lesheng Teng
Methotrexate (MTX), as a disease modifying antirheumatic drug (DMARD), was first line drug to treat rheumatoid arthritis. However, the severe side effect during long term and high dosage usage limit its application. The aim of this study was to develop dual-functional lipid polymeric hybrid pH-responsive nanoparticles to deliver MTX to inflamed joints selectively. The designed MTX loaded stearic acid-octa-arginine and folic acid decorated poly lactic-co-glycolic acid (PLGA) -PK3-based lipid polymeric hybrid nanoparticles (Sta-R8-FA-PPLPNs/MTX) were composed of PK3, Folate-PEG-PLGA, egg PC, and Sta-R8...
June 18, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Juliana Valencia-Serna, Hamidreza M Aliabadi, Adam Manfrin, Mahsa Mohseni, Xiaoyan Jiang, Hasan Uludag
Therapies for the treatment of Chronic Myeloid Leukemia and other leukemias are still limited for patients at advanced stages, which allow development of point mutations in the BCR-ABL fusion gene that render CML cells insensitive to therapies. An effective non-viral delivery system based on lipopolymers is described in this study to deliver specific siRNAs to CML cells for therapeutic gene silencing. The lipopolymer, based on the lipid α-linolenic acid (αLA) substitution on low molecular weight polyethyleneimine (PEI), was used to deliver siRNA against the BCR-ABL gene and, the resultant therapeutic effect was evaluated in in vitro and in vivo CML models...
June 15, 2018: European Journal of Pharmaceutics and Biopharmaceutics
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