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European Journal of Pharmaceutics and Biopharmaceutics

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https://www.readbyqxmd.com/read/28427956/curcumin-poly-2-methyl-2-oxazoline-b-tetrahydrofuran-b-2-methyl-2-oxazoline-formulation-an-improved-penetration-and-biological-effect-of-curcumin-in-f508del-cftr-cell-lines
#1
Cristine Gonçalves, Jean-Pierre Gomez, William Même, Bazoly Rasolonjatovo, David Gosset, Steven Nedellec, Philippe Hulin, Cécile Huin, Tony Le Gall, Tristan Montier, Pierre Lehn, Chantal Pichon, Philippe Guégan, Hervé Cheradame, Patrick Midoux
Neutral amphiphilic triblock ABA copolymers are of great interest to solubilize hydrophobic drugs. We reported that a triblock ABA copolymer consisting of methyl-2-oxazoline (MeOx) and tetrahydrofuran (THF) (MeOx6-THF19-MeOx6) (TBCP2) can solubilize curcumin (Cur) a very hydrophobic molecule exhibiting multiple therapeutic effects but whose insolubility and low stability in water is a major drawback for clinical applications. Here, we provide evidences by flow cytometry and confocal microscopy that Cur penetration in normal and ΔF508-CFTR human airway epithelial cell lines is facilitated by TBCP2...
April 17, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28414191/instant-odfs-development-of-an-intermediate-nanoparticle-based-product-platform-for-individualized-medication
#2
Denise Steiner, Jan Henrik Finke, Arno Kwade
The individualization of solid dosage forms to realize a flexible therapy for all patient groups is a topic which increasingly gains importance in pharmaceutical research. The goal of this study was to develop a nanoparticulate, instant orodispersible film (iODF) powder which can easily be reconstituted in water to cast ODFs containing an individualized concentration of an active pharmaceutical ingredient (API). It was shown that the processing of the film casing mass to iODF powders by spray drying provides the same advantageous film properties, particles sizes redispersed from the ODF and dissolution profiles as compared to the common production route...
April 13, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28414190/engineered-polymeric-microspheres-obtained-by-multi-step-method-as-potential-systems-for-transarterial-embolization-and-intraoperative-imaging-of-hcc-preliminary-evaluation
#3
Elena Piera Porcu, Andrea Salis, Giovanna Rassu, Marcello Maestri, Jacopo Galafassi, Giovanna Bruni, Paolo Giunchedi, Elisabetta Gavini
The aim of this study was the development of novel fluorescent microspheres as embolic agent for transarterial embolization (TAE) of advanced stages of hepatocellular carcinoma (HCC). TAE is a minimally invasive procedure that induces tumour regression blocking the blood flow by injection of microparticles. The microspheres currently used in clinical application cannot be visualized in vivo. Surgeon could exploit the intraoperative detection of embolic agents during resection of the malignant mass. Biocompatible indocyanine green (ICG)-loaded microspheres (CAB-CS-ICG) were prepared using a multi-step method...
April 13, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28414189/radioiodinated-hypericin-disulfonic-acid-sodium-salts-as-a-dna-binding-probe-for-early-imaging-of-necrotic-myocardium
#4
Xinghua Duan, Zhiqi Yin, Cuihua Jiang, Qiaomei Jin, Dongjian Zhang, Ziping Sun, Wencai Ye, Jian Zhang
Necrotic myocardium imaging can provide great indicators of salvaged myocardial areas for clinical guidances to patients with myocardial infarction (MI). One of the key challenges in necrotic myocardium imaging however, is lack of ideal necrotic imaging tracers for exactly and timely depicting the necrotic myocardium. (131)I-hypericin ((131)I-Hyp) is a promising tracer in exact necrotic myocardium delineation. However, it can't clearly image necrotic myocardium until 9 h post injection (p.i.) for the high background signals in blood and lung due to the strong lipophilicity...
April 13, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28412473/nanoformulations-for-dimethyl-fumarate-physicochemical-characterization-and-in-vitro-in-vivo-behavior
#5
Elisabetta Esposito, Rita Cortesi, Markus Drechsler, Jie Fan, Bingmei M Fu, Laura Calderan, Silvia Mannucci, Federico Boschi, Claudio Nastruzzi
Dimethyl fumarate has been demonstrated useful in relapsing remitting multiple sclerosis treatment (Tecfidera®). Nevertheless, since Tecfidera® capsules induce flushing, gastro-intestinal events and other more serious drawbacks, in this investigation a nanoparticle based system to be administered by an alternative way is proposed. In particular this study describes the preparation and characterization of dimethyl fumarate-containing solid lipid nanoparticles (SLN). Namely SLN based on tristearin, tristearin SLN treated with polysorbate 80 and cationic SLN constituted of tristearin in mixture with dimethyldioctadecylammonium chloride were investigated...
April 12, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28412472/preparation-and-characterization-of-dutasteride-loaded-nanostructured-lipid-carriers-coated-with-stearic-acid-chitosan-oligomer-for-topical-delivery
#6
Norhayati Mohamed Noor, Khalid Sheikh, Satyanarayana Somavarapu, Kevin Mg Taylor
Dutasteride, used for treating benign prostate hyperplasia (BPH), promotes hair growth. To enhance delivery to the hair follicles and reduce systemic effects, in this study dutasteride has been formulated for topical application, in a nanostructured lipid carrier (NLC) coated with chitosan oligomer-stearic acid (CSO-SA). CSO-SA has been successfully synthesized, as confirmed using (1)H NMR and FTIR. Formulation of dutasteride-loaded nanostructured lipid carriers (DST-NLCs) was optimised using 2(3) full factorial design...
April 12, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28412471/surface-modification-of-solid-lipid-nanoparticles-for-oral-delivery-of-curcumin-improvement-of-bioavailability-through-enhanced-cellular-uptake-and-lymphatic-uptake
#7
Jong-Suep Baek, Cheong-Weon Cho
Curcumin has been reported to exhibit potent anticancer effects. However, poor solubility, bioavailability and stability of curcumin limit its in vivo efficacy for the cancer treatment. Solid lipid nanoparticles (SLN) are a promising delivery system for the enhancement of bioavailability of hydrophobic drugs. However, burst release of drug from SLN in acidic environment limits its usage as oral delivery system. Hence, we prepared N-carboxymethyl chitosan (NCC) coated curcumin-loaded SLN (NCC-SLN) to inhibit the rapid release of curcumin in acidic environment and enhance the bioavailability...
April 12, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28411057/microwave-assisted-microemulsion-technique-for-production-of-miconazole-nitrate-and-econazole-nitrate-loaded-solid-lipid-nanoparticles
#8
Rohan M Shah, Daniel S Eldridge, Enzo A Palombo, Ian H Harding
The microwave-assisted production of solid lipid nanoparticles (SLNs) is a novel technique reported recently by our group. The small particle size, solid nature and use of physiologically well-tolerated lipid materials make SLNs an interesting and potentially efficacious drug carrier. The main purpose of this research work was to investigate the suitability of microwave-assisted microemulsion technique to encapsulate selected ionic drug substances such as miconazole nitrate and econazole nitrate. The microwave-produced SLNs had a small size (250-300 nm), low polydispersity (<0...
April 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28411056/development-and-evaluation-of-resveratrol-vitamin-e-and-epigallocatechin-gallate-loaded-lipid-nanoparticles-for-skin-care-applications
#9
Jin Chen, Ning Wei, Maria Lopez-Garcia, Dianna Ambrose, Jason Lee, Colin Annelin, Teresa Peterson
Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) have been studied as potential carriers for both dermal and transdermal drug delivery. SLN contain lipid droplets that are fully crystallized and have a highly-ordered crystalline structure. NLC are modified SLN in which the lipid phase contains both solid and liquid lipids at room temperature. SLN and NLC are thought to combine the advantages of polymeric particles, liposomes and emulsions. Therefore they provide high encapsulation percentages, better protection for incorporated actives and allow for control of desired release profile...
April 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28396280/high-oral-bioavailability-of-2-methoxyestradiol-in-peg-plga-micelles-microspheres-for-cancer-therapy
#10
XinHong Guo, CaiPing Chen, Xin Liu, PanPan Hou, XiaoNan Guo, Fang Ding, ZhiHao Wang, YuRong Hu, Zhi Li, ZhenZhong Zhang
The development of effective oral preparations of 2-methoxyestradiol (2-ME) has been a worldwide problem. In this study, breakthrough progress has been made in oral delivery of 2-ME by encapsulating 2-ME micelles in pH-responsive microspheres. 2-ME micelles with small particle size (58 nm) and high drug loading (7.94±0.23%) were successfully prepared and showed slower release characteristics and 12.8 times higher cytotoxicity on 4T1 cells than free 2-ME. The pH-sensitive microspheres could slowly release 82% of 2-ME micelles for 10 h in PBS (7...
April 7, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28396279/extracellular-vesicles-a-promising-avenue-for-the-detection-and-treatment-of-infectious-diseases
#11
Gregor Fuhrmann, Anna Lena Neuer, Inge K Herrmann
Extracellular vesicles (EVs) have gained increasing attention as novel disease biomarkers and as promising therapeutic agents. These cell-derived, phospholipid-based particles are present in many - if not all - physiological fluids. They have been shown to govern several physiological processes, such as cell-cell communication, but also to be involved in pathological conditions, for example tumour progression. In infectious diseases, EVs have been shown to induce host immune responses and to mediate transfer of virulence or resistance factors...
April 7, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28396278/transport-of-curcumin-derivatives-in-caco-2-cell-monolayers
#12
Zhen Zeng, Zhe L Shen, Shuo Zhai, Jia L Xu, Hui Liang, Qin Shen, Qing Y Li
Curcumin (Cur) is a strong natural antioxidant, who can prevent multiple diseases such as anti-cancer, anti-inflammatory, have a resistance to alzheimer's disease and various malignant diseases. But it has poor oral bioavailability due to its poor aqueous solubility, as well as instability. While its novel derivatives (CB and FE), showed better anti-tumor activity, better anti-oxidant activity and better stability than the original drug (Cur). The aim of this study was to study the intestinal transport of Cur, CB and FE using an in vitro Caco-2 cell monolayer model...
April 7, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28392414/micro-flow-imaging-as-a-quantitative-tool-to-assess-size-and-agglomeration-of-plga-microparticles
#13
Miranda M C van Beers, Cees Slooten, Jelte Meulenaar, Ahmad S Sediq, Ruud Verrijk, Wim Jiskoot
The purpose of this study was to explore the potential of flow imaging microscopy to measure particle size and agglomeration of poly(D,L-lactic-co-glycolic acid) (PLGA) microparticles. The particle size distribution of pharmaceutical PLGA microparticle products is routinely determined with laser diffraction. In our study, we performed a unique side-by-side comparison between MFI 5100 (flow imaging microscopy) and Mastersizer 2000 (laser diffraction) for the particle size analysis of two commercial PLGA microparticle products, i...
April 6, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28389342/use-of-mesoporous-cellular-foam-mcf-in-preparation-of-polymeric-microspheres-for-long-acting-injectable-release-formulations-of-paliperidone-antipsychotic-drug
#14
Stavroula Nanaki, Maria Tseklima, Zoe Terzopoulou, Maria Nerantzaki, Dimitrios J Giliopoulos, Konstantinos Triantafyllidis, Margaritis Kostoglou, Dimitrios N Bikiaris
In this study, high surface area mesoporous silica foam with cellular pore morphology (MCF) was used for injectable delivery of paliperidone, an antipsychotic drug used in patients suffering from bipolar disorder. The aim was to enhance paliperidone solubility and simultaneously to prepare long active intractable microspheres. For this reason paliperidone was first loaded in MCF silica and whole system was further encapsulated into PLA and PLGA 75/25 w/w copolymer in the form of microspheres. It was found that paliperidone after its adsorption into MCF was transformed in its amorphous state, thus leading to enhanced in vitro dissolution profile...
April 4, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28385617/antioxidant-based-topical-formulations-influence-on-the-inflammatory-response-of-japanese-skin-a-clinical-study-using-non-invasive-techniques
#15
Tais A L Wagemaker, Patrícia M B G Maia Campos, Kenji Shimizu, Daiki Kyotani, Daisuke Yoshida
Cutaneous irritants exposure induces an excess of ROS in the skin and can ensue an inflammatory response. Topical antioxidant-based formulations can help to counteract ROS generation. This study evaluated the influence of antioxidant-based topical formulations on the inflammatory response of skin, using a combination of in vivo real-time non-invasive techniques. Nine test areas were defined on each volar forearm of the 25 Japanese volunteers. Measurements were performed before and after treatment with 15µL of a 5% sodium dodecyl sulfate solution and 15µL of the same based formulation or the vehicle with 1% of the antioxidants...
April 3, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28385616/hydroxyl-versus-permethylated-glycopolymers-as-gene-carriers
#16
Juan Alfonso Redondo, Enrique Martínez-Campos, Rodrigo Navarro, Mónica Pérez-Perrino, Helmut Reinecke, Alberto Gallardo, Guillermo Corrales, Alfonso Fernández-Mayoralas, Carlos Elvira
The main parameters that contribute to non-viral gene delivery are chemical structure and charge distribution. Indeed, saccharide units have been reported to have specific interactions with proteins located in the outer leaflet of the plasma cell membrane that facilitate the cellular internalization of plasmid-DNA vector complexes. In this work, glycopolymers based on statistical copolymers were synthesized through radical copolymerization of a cationic unit, N-ethyl pyrrolidine methacrylamide (EPA), with two styrenic monomers derived from the hydroxylated and permethylated forms of α-glucose...
April 3, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28385615/identification-and-characterisation-of-a-salt-form-of-danirixin-with-reduced-pharmacokinetic-variability-in-patient-populations
#17
Jackie C Bloomer, Claire Ambery, Bruce E Miller, Paul Connolly, Helen Garden, Nick Henley, Neil Hodnett, Sarah Keel, James L Kreindler, Richard S Lloyd, Wayne Matthews, John Yonchuk, Aili L Lazaar
The natural variability of gastric pH or gastric acid reducing medications can result in lower and more variable clinical pharmacokinetics for basic compounds in patient populations. Progressing alternative salt forms with improved solubility and dissolution properties can minimise this concern. This manuscript outlines a nonclinical approach comprising multiple biopharmaceutical, in vitro and physiologically based pharmacokinetic model (PBPK) modelling studies to enable selection of an alternative salt form for danirixin (DNX, GSK1325756), a pharmaceutical agent being developed for chronic obstructive pulmonary disease (COPD)...
April 3, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28377274/dynamites-a-dynamic-cell-culture-platform-for-in-vitro-drug-testing-part-2-ocular-dynamites-for-drug-absorption-studies-of-the-anterior-eye
#18
Nicole Beißner, Kai Mattern, Andreas Dietzel, Stephan Reichl
In the present study, a formerly designed Dynamic Micro Tissue Engineering System (DynaMiTES) was applied with our prevalidated human hemicornea (HC) construct to obtain a test platform for improved absorption studies of the anterior eye (Ocular DynaMiTES). First, the cultivation procedure of the classic HC was slightly adapted to the novel DynaMiTES design. The obtained inverted HC was then compared to classic HC regarding cell morphology using light and scanning electron microscopy, cell viability using MTT dye reaction and epithelial barrier properties observing transepithelial electrical resistance and apparent permeation coefficient of sodium fluorescein...
April 1, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28377273/biotechnological-production-of-hyperforin-for-pharmaceutical-formulation
#19
REVIEW
Mariam Gaid, Eline Biedermann, Jendrik Füller, Paul Haas, Sönke Behrends, Rainer Krull, Stephan Scholl, Ute Wittstock, Christel Müller-Goymann, Ludger Beerhues
Hyperforin is a major active constituent of Hypericum perforatum (St. John's wort). It has amazing pharmacological activities, such as antidepressant properties, but it is labile and difficult to synthesize. Its sensitivity and lipophilicity are challenges for processing and formulation. Its chemical complexity provokes approaches of biotechnological production and modification. Dedifferentiated H. perforatum cell cultures lack appropriate storage sites and hence appreciable hyperforin levels. Shoot cultures are capable of forming hyperforin but less suitable for biomass up-scaling in bioreactors...
April 1, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28377272/interactions-and-release-of-two-palmitoyl-peptides-from-phytantriol-cubosomes
#20
Seyedeh Parinaz Akhlaghi, Watson Loh
Phytantriol cubosomes loaded with two palmitoyl peptides (Palpepcubes), namely GHKcube and GQPRcube, were prepared using an ultrasonication protocol. The Palpepcubes dimensions were characterized by dynamic light scattering (DLS) and cryo-transmission electron microscopy (cryo-TEM). Small-angle X-ray scattering (SAXS) analyses revealed that the bicontinuous cubic structure remained even at palmitoyl peptide contents as high as 5 wt.%, with an increase in the cell parameter from approximately 6.5 to 7.2 nm. Isothermal titration calorimetry (ITC) was used to elucidate the interactions between the blank cubosomes and the palmitoyl peptides, revealing an exothermic process of interaction...
April 1, 2017: European Journal of Pharmaceutics and Biopharmaceutics
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