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European Journal of Pharmaceutics and Biopharmaceutics

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https://www.readbyqxmd.com/read/28633956/a-time-adjustable-pulsatile-release-system-for-ketoprofen-in-vitro-and-in-vivo-investigation-in-a-pharmacokinetic-study-and-an-ivivc-evaluation
#1
Haiying Wang, Lizhen Cheng, Haoyang Wen, Caiyan Li, Yuenan Li, Xiaoyu Zhang, Yongfei Wang, Yanyan Wang, Tuanjie Wang, Weisan Pan, Xinggang Yang
A time-adjustable pulsatile release system (TAPS) containing ketoprofen (KF) as an active pharmaceutical agent was developed having been designed for bedtime dosing and releasing drug in the early morning to control the symptoms of rheumatoid arthritis (RA). The formulation involved a tablet core (KF) and a control-release layer, and the coating membrane was composed of EC and Eudragit L100. A single-factor study, a central composite design and a response surface method were selected to optimize the formula and the optimum prescription was as follows: tablet core (KF 50mg, MCC 70mg, lactose 40mg, L-HPC 38mg), and film (EC 7...
June 17, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28629719/alpha-ketoglutarate-nanoparticles-a-potentially-effective-treatment-for-cyanide-poisoning
#2
Shaheen Sultana, Sushma Talegaonkar, Dhruv Kumar Nishad, Gaurav Mittal, F J Ahmad, Aseem Bhatnagar
The purpose of this research work was to prepare nanosized formulation of alpha ketoglutarate as dry powder inhaler for cyanide poisoning. Nanosizing can be approached by solid phase and liquid phase method. The different conditions encountered in both these approaches can greatly affect the particle characteristics. In this study milling and precipitation technique were compared to study their effect on α-KG particles characteristics. Differences in choice of stabilizers were observed between the two processing techniques...
June 16, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28625688/electrically-atomised-formulations-of-timolol-maleate-for-direct-and-on-demand-ocular-lens-coatings
#3
Prina Mehta, Ali Al-Kinani, Rita Haj-Ahmad, Muhammad Sohail Arshad, Ming-Wei Chang, G Raid Alany, Zeeshan Ahmad
Advances in nanotechnology have enabled solutions for challenging drug delivery targets. While the eye presents numerous emerging opportunities for delivery, analysis and sensing; issues persist for conventional applications. This includes liquid phase formulation localisation on the ocular surface once administered as formulated eye-drops; with the vast majority of dosage (>90%) escaping from the administered site due to tear production and various drainage mechanisms. The work presented here demonstrates a single needle electrohydrodynamic (EHD) engineering process to nano-coat (as an on demand and controllable fiber depositing method) the surface of multiple contact lenses rendering formulations to be stationary on the lens and at the bio-interface...
June 15, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28627400/improved-tacrolimus-skin-permeation-by-co-encapsulation-with-clobetasol-in-lipid-nanoparticles-study-of-drug-effects-in-lipid-matrix-by-electron-paramagnetic-resonance
#4
Lígia Marquez Andrade, Luis Antônio Dantas Silva, Anna Paula Krawczyk-Santos, Isabella Cristina de S M Amorim, Priscila Bianca Rodrigues da Rocha, Eliana Martins Lima, Jorge Luiz V Anjos, Antonio Alonso, Ricardo Neves Marreto, Stephânia Fleury Taveira
Combined therapy with corticosteroids and immunosuppressant-loaded nanostructured lipid carriers (NLC) could be useful in the treatment of skin diseases. To circumvent NLC loading capacity problems, loaded drugs should have different physicochemical characteristics, such as tacrolimus (TAC) and clobetasol (CLO). Therefore, in the present study, TAC and CLO were encapsulated in NLC (TAC-NLC, CLO-NLC and TAC+CLO-NLC), coated or otherwise with chitosan. Electron paramagnetic resonance (EPR) spectroscopy of different spin labels was used to investigate the impact of drug and oil incorporation on the lipid dynamic behavior of the lipid matrices...
June 13, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28627399/elucidation-of-the-impact-of-cell-culture-conditions-of-caco-2-cell-monolayer-on-barrier-integrity-and-intestinal-permeability
#5
Anna Lechanteur, Andreia Almeida, Bruno Sarmento
No abstract text is available yet for this article.
June 13, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28619610/forecasting-gastrointestinal-precipitation-and-oral-pharmacokinetics-of-dantrolene-in-dogs-using-an-in-vitro-precipitation-testing-coupled-with-in-silico-modeling-and-simulation
#6
Atsushi Kambayashi, Jennifer B Dressman
The aim of the current research was to determine the precipitation kinetics of dantrolene sodium using canine biorelevant in vitro testing and to model the precipitation kinetics by appropriately coupling the data with an in silico tool adapted for dogs. The precipitation profiles of dantrolene sodium solutions were obtained with the in vitro paddle apparatus at a revolution rate of 50 rpm. The in silico prediction tool was designed using STELLA software and the predicted plasma concentration profiles of dantrolene using the in vitro precipitation data were compared with the observed in vivo pharmacokinetics in beagle dogs...
June 12, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28610879/preactivated-thiolated-glycogen-as-mucoadhesive-polymer-for-drug-delivery
#7
Mara Perrone, Antonio Lopalco, Angela Lopedota, Annalisa Cutrignelli, Valentino Laquintana, Justin Douglas, Massimo Franco, Elisa Liberati, Vincenzo Russo, Serena Tongiani, Nunzio Denora, Andreas Bernkop-Schnürch
The purpose of this study was to synthesize and characterize a novel thiolated glycogen, so-named S-preactivated thiolated glycogen, as a mucosal drug delivery systems and the assessment of its mucoadhesive properties. In this regard, glycogen-cysteine and glycogen-cysteine-2-mercaptonicotinic acid conjugates were synthesized. Glycogen was activated by an oxidative ring opening with sodium periodate resulting in reactive aldehyde groups to which cysteine was bound via reductive amination. The obtained thiolated polymer displayed 2203...
June 10, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28610878/electrospraying-of-polymer-solutions-study-of-formulation-and-process-parameters
#8
Annelies Smeets, Christian Clasen, Guy Van den Mooter
Over the past decade, electrospraying has proven to be a promising method for the preparation of amorphous solid dispersions, an established formulation strategy to improve the oral bioavailability of poorly soluble drug compounds. Due to the lack of fundamental knowledge concerning adequate single nozzle electrospraying conditions, a trial-and-error approach is currently the only option. The objective of this paper is to study/investigate the influence of the different formulation and process parameters, as well as their interplay, on the formation of a stable cone-jet mode as a prerequisite for a reproducible production of monodisperse micro- and nanoparticles...
June 10, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28606596/mini-review-recombinant-production-of-tailored-bio-pharmaceuticals-in-different-bacillus-strains-and-future-perspectives
#9
REVIEW
Antonia Lakowitz, Thibault Godard, Rebekka Biedendieck, Rainer Krull
Bio-pharmaceuticals like antibodies, hormones and growth factors represent about one-fifth of commercial pharmaceuticals. Host candidates of growing interest for recombinant production of these proteins are strains of the genus Bacillus, long being established for biotechnological production of homologous and heterologous proteins. Bacillus strains benefit from development of efficient expression systems in the last decades and emerge as major industrial workhorses for recombinant proteins due to easy cultivation, non-pathogenicity and their ability to secrete recombinant proteins directly into extracellular medium allowing cost-effective downstream processing...
June 9, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28602870/ultrasound-mediated-nanoparticle-delivery-across-ex-vivo-bovine-retina-after-intravitreal-injection
#10
Di Huang, Ying-Shan Chen, Ilva D Rupenthal
Intravitreal injection is the most common administration route for the treatment of retinal diseases. However, the vitreous and some of the retinal layers themselves act as significant barriers to efficient delivery of drugs administered intravitreally. This study aimed to improve the diffusive mobility of nanoparticles (NPs) in the vitreous and enhance their permeation across the retina after intravitreal injection by application of ultrasound (US). Ex vivo posterior bovine eye cups were used and the vitreous was either left intact or removed gently from the neural retina...
June 8, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28602869/solid-state-properties-and-drug-release-behavior-of-co-amorphous-indomethacin-arginine-tablets-coated-with-kollicoat%C3%A2-protect
#11
Ina Petry, Korbinian Löbmann, Holger Grohganz, Thomas Rades, Claudia S Leopold
A promising approach to improve the solubility of poorly water-soluble drugs and to overcome the stability issues related to the plain amorphous form of the drugs, is the formulation of drugs as co-amorphous systems. Although polymer coatings have been proven very useful with regard to tablet stability and modifying drug release, there is little known on coating co-amorphous formulations. Hence, the aim of the present study was to investigate whether polymer coating of co-amorphous formulations is possible without inducing recrystallization...
June 8, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28600224/enhancement-of-transdermal-protein-delivery-by-photothermal-effect-of-gold-nanorods-coated-on-polysaccharide-based-hydrogel
#12
Aung Thu Haine, Yuki Koga, Yuta Hashimoto, Taishi Higashi, Keiichi Motoyama, Hidetoshi Arima, Takuro Niidome
Transdermal protein delivery is a useful and attractive method for protein therapy and dermal vaccination. However, this delivery method is restricted by the low permeability of the stratum corneum. The purpose of this study was to develop a transdermal delivery system for enhancement of protein permeability into the skin. First, we prepared a transparent gel patch made of polysaccharides with gold nanorods on the gel surface and fluorescein isothiocyanate-modified ovalbumin (FITC-OVA) inside. Next, the gel patch was placed on mouse skin to allow contact with the coated gold nanorods, and irradiated by a continuous-wave laser...
June 6, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28600223/-nano-in-nano-hybrid-liposomes-increase-target-specificity-and-gene-silencing-efficiency-in-breast-cancer-induced-scid-mice
#13
Dhiraj Bhavsar, Krishnakumar Subramanian, Swaminathan Sethuraman, Uma Maheswari Krishnan
Gene silencing has immense potential in the treatment of cancer. However, enhancement of its efficiency requires the development of specifically targeted and safe carrier systems. Cationic carriers are generally limited by their immunogenicity. Hence, in this study, we report hybrid liposomes encapsulating Poly (L-lysine)-siRNA complex to silence epithelial cell adhesion molecule (EpCAM), highly expressed in epithelial cancers. The hybrid liposomes LL1 (Egg PC:DSPE-PEG, 10:0) and hybrid immunoliposomes LL2 (Egg PC:DSPE-PEG, 8:2) linked with EpCAM antibody as the targeting ligand showed an encapsulation efficiency of 70% and 86%, respectively...
June 6, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28596036/the-oriented-processes-for-extraction-and-recovery-of-paracetamol-compound-across-different-affinity-polymer-membranes-parameters-and-mechanisms
#14
E H El Atmani, A Benelyamani, H Mouadili, S Tarhouchi, S Majid, K Touaj, L Lebrun, M Hlaibi
Membrane processes represent one of the most promising technologies for separation and extraction in modern industries, because they have several advantages. Today these processes are an important research topic, including affinity polymer membranes that are highly efficient for oriented processes. Three affinity polymer membrane types containing lipophilic compounds, methyl cholate (MC) and cholic acid (CA) as extractive agents were prepared and characterized. They have been used to extract active ingredient paracetamol (acetaminophen), from concentrated solutions (0...
June 6, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28596037/development-and-evaluation-of-an-oral-fast-disintegrating-anti-allergic-film-using-hot-melt-extrusion-technology
#15
Manjeet B Pimparade, Anh Vo, Abhijeet S Maurya, Jungeun Bae, Joseph T Morott, Xin Feng, Dong Wuk Kim, Vijay I Kulkarni, Roshan Tiwari, K Vanaja, Reena Murthy, H N Shivakumar, D Neupane, S R Mishra, S N Murthy, Michael A Repka
The main objective of this novel study was to develop chlorpheniramine maleate orally disintegrating films (ODF) using hot-melt extrusion technology and evaluate the characteristics of the formulation using in vitro and in vivo methods. Modified starch with glycerol was used as a polymer matrix for melt extrusion. Sweetening and saliva-simulating agents were incorporated to improve palatability and lower the disintegration time of film formulations. A standard screw configuration was applied, and the last zone of the barrel was opened to discharge water vapors, which helped to manufacture non-sticky, clear, and uniform films...
June 5, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28596035/the-pharmacokinetic-and-pharmacodynamic-properties-of-site-specific-pegylated-genetically-modified-recombinant-human-interleukin-11-in-normal-and-thrombocytopenic-monkeys
#16
Shan-Shan Ma, Seong-Hyun Ho, Su-Yong Ma, Yue-Juan Li, Kai-Tong Li, Xiao-Chuang Tang, Guang-Rong Zhao, Song-Shan Xu
In order to improve the pharmacokinetic and pharmacodynamic properties of recombinant human interleukin-11 mutein (mIL-11) and to reduce the frequency of administration, we examined the feasibility of chemical modification of mIL-11 by methoxy polyethylene glycol succinimidyl carbonate (mPEG-SC). PEG-mIL-11 was prepared by a pH controlled amine specific method. Bioactivity of the protein was determined in a IL-11-dependent in vitro bioassay, its pharmacodynamic and pharmacokinetic properties were investigated by using normal and thrombocytopenic monkey models...
June 5, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28583590/combined-treatment-of-thymus-vulgaris-l-rosmarinus-officinalis-l-and-myrtus-communis-l-essential-oils-against-salmonella-typhimurium-optimization-of-antibacterial-activity-by-mixture-design-methodology
#17
Mouhcine Fadil, Kawtar Fikri-Benbrahim, Saad Rachiq, Bouchaib Ihssane, Sara Lebrazi, Marwa Chraibi, Taoufik Haloui, Abdellah Farah
To increase the sensibility of Salmonella typhimurium strain, a mixture of Thymus vulgaris L. (T. vulgaris L.), Rosmarinus officinalis L. (R. officinalis L.) and Myrtus communis L. (M. communis L.) essential oils (EOs) was used in combined treatment by experimental design methodology (mixture design). The chemical composition of EOs was firstly identified by GC and GC/MS and their antibacterial activity was evaluated. The results of this first step have shown that thymol and borneol were the major compounds in T...
June 2, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28583589/a-comparative-assessment-of-nanocomposites-vs-amorphous-solid-dispersions-prepared-via-nanoextrusion-for-drug-dissolution-enhancement
#18
Meng Li, Nicolas Ioannidis, Costas Gogos, Ecevit Bilgili
Nanoextrusion was used to produce extrudates of griseofulvin, a poorly water-soluble drug, with the objective of examining the impact of drug particle size and polymeric matrix type-size of the extrudates on drug dissolution enhancement. Hydroxypropyl cellulose (HPC) and Soluplus® were used to stabilize wet-milled drug suspensions and form matrices of the extrudates. The wet-milled suspensions along with additional polymer (HPC/Soluplus®) were fed to a co-rotating twin-screw extruder, which dried the suspensions and formed various extrudates...
June 2, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28583588/processing-thermally-labile-drugs-by-hot-melt-extrusion-the-lesson-with-gliclazide
#19
Siyuan Huang, Kevin P O'Donnell, Sophie M Delpon de Vaux, John O'Brien, John Stutzman, Robert O Williams Iii
The formation of molecularly dispersed amorphous solid dispersions by the hot-melt extrusion technique relies on the thermal and mechanical energy inputs, which can cause chemical degradation of drugs and polymeric carriers. Additionally, drug degradation may be exacerbated as drugs convert from a more stable crystalline form to a higher energy amorphous form. Therefore, it is imperative to study how drug degrades and evaluate methods to minimize drug degradation during the extrusion process. In this work, gliclazide was used as a model thermally labile drug for the degradation kinetics and process optimization studies...
June 2, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28559112/investigation-of-polymorphic-transitions-of-piracetam-induced-during-wet-granulation
#20
Catherine B Potter, Gayathri Kollamaram, Jacek Zeglinski, Darren A Whitaker, Denise M Croker, Gavin M Walker
Piracetam was investigated as a model API which is known to exhibit a number of different polymorphic forms. It is freely soluble in water so the possibility exists for polymorphic transformations to occur during wet granulation. Analysis of the polymorphic form present during lab-scale wet granulation, using water as a granulation liquid, was studied with powder X-ray diffraction and Raman spectroscopy as off-line and inline analysis tools respectively. Different excipients with a range of hydrophilicities, aqueous solubilities and molecular weights were investigated to examine their influence on these solution-mediated polymorphic transitions and experimental results were rationalised using molecular modelling...
May 27, 2017: European Journal of Pharmaceutics and Biopharmaceutics
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