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European Journal of Pharmaceutics and Biopharmaceutics

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https://www.readbyqxmd.com/read/28104440/twin-screw-extruded-lipid-implants-containing-trp2-peptide-for-tumour-therapy
#1
Marie-Paule Even, Sharan Bobbala, Blake Gibson, Sarah Hook, Gerhard Winter, Julia Engert
Much effort has been put in the development of specific anti-tumour immunotherapies over the last few years, and several studies report on the use of liposomal carriers for tumour-associated antigens. In this work, the use of lipid implants, prepared using two different extruders, was investigated for sustained delivery in tumour therapy. The implants consisted of cholesterol, soybean lecithin, Dynasan 114, trehalose, ovalbumin (OVA) or a TRP2 peptide, and Quil-A. Implants were first produced on a Haake Minilab extruder, and then a scale-down to minimal quantities of material on a small scale ZE mini extruder was performed...
January 16, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28093351/in-vitro-uptake-and-transport-studies-of-peg-plga-polymeric-micelles-in-respiratory-epithelial-cells
#2
Xiao Hu, Fei-Fei Yang, Chun-Yu Liu, Carsten Ehrhardt, Yong-Hong Liao
Polymeric micelles are considered promising carriers for pulmonary drug delivery. Their interaction with the respiratory epithelium, however, is mostly unknown. In the present study, methoxypoly (ethylene glycol) (mPEG)-poly (lactic-co-glycolic acid) (PLGA) micelles containing curcumin acetate (CA) or a mixture of CA and Nile Red (NR) were prepared using the solvent evaporation method. Calu-3 and NCI-H441 human respiratory epithelial cell monolayers were used as in vitro models of upper and lower respiratory tract epithelium barrier, respectively, to study the cellular uptake and transport of the vesicles...
January 13, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28089914/arachidonic-acid-with-taurine-enhances-pulmonary-absorption-of-macromolecules-without-any-serious-histopathological-damages
#3
Masateru Miyake, Takanori Minami, Hiroyuki Yamazaki, Chie Emoto, Tadashi Mukai, Hajime Toguchi
Therapeutic peptides and protein are being used in several indications; however, their poor permeability still remains to be solved. This study focused on the pulmonary route of macromolecules. First, the effects of arachidonic acid (AA) as an absorption enhancer on drug serum concentration, after intratracheal administration, were investigated in rats. Second, the safety of AA was assessed in rats in an acute toxicity study for 7 days. AA enhanced the exposure of both interferon-α (IFN-α) and fluorescein isothiocyanate 4000 (FD-4)...
January 13, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28089916/stable-curcumin-loaded-polymeric-micellar-formulation-for-enhancing-cellular-uptake-and-cytotoxicity-to-flt3-overexpressing-eol-1-leukemic-cells
#4
Singkome Tima, Songyot Anuchapreeda, Chadarat Ampasavate, Cory Berkland, Siriporn Okonogi
The present study aims to develop a stable polymeric micellar formulation of curcumin (CM) with improved solubility and stability, and that is suitable for clinical applications in leukemia patients. CM-loaded polymeric micelles (CM-micelles) were prepared using poloxamers. The chemical structure of the polymers influenced micellar properties. The best formulation of CM-micelles, namely CM-P407, was obtained from poloxamer 407 at drug to polymer ratio of 1:30 and rehydrated with phosphate buffer solution pH 7...
January 12, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28089915/dendrimers-as-nanocarriers-for-nucleoside-analogues
#5
REVIEW
Michał Gorzkiewicz, Barbara Klajnert-Maculewicz
Dendrimers constitute a class of hyperbranched macromolecules with several potential applications due to their unique properties such as a well-defined structure, multivalency and biocompatibility. These polymers became one of the most promising drug nanocarriers, providing improved solubility of therapeutics, high loading capacity and controllable biodistribution pattern. In addition, the use of dendrimers as drug delivery devices in cancer therapies may help to overcome the resistance mechanisms by transporting activated drug molecules directly to cancer cells...
January 12, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28089786/3-carboxyphenylboronic-acid-modified-carboxymethyl-chitosan-nanoparticles-for-improved-tumor-targeting-and-inhibitory
#6
Xin Wang, Bing Wei, Xu Cheng, Jun Wang, Rupei Tang
Carboxymethyl chitosan-based nanoparticles (CM NPs) were prepared, and were further modified with a tumor-homing ligand (3-carboxyphenylboronic acid, 3-CPBA) to give tumor-targeting nanoparticles (CB NPs). Particle sizes were measured by dynamic light scattering, while the morphology was observed via transmission electron microscopy and scanning electronic microscope. The results show that CM and CB NPs are spherical-like, and kinetically stable in various conditions. Doxorubicin (DOX) as a model drug was successfully encapsulated to give CM-DOX and CB-DOX NPs...
January 12, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28089785/mechanistic-modelling-of-infrared-mediated-energy-transfer-during-the-primary-drying-step-of-a-continuous-freeze-drying-process
#7
Pieter-Jan Van Bockstal, Séverine Thérèse F C Mortier, Laurens De Meyer, Jos Corver, Chris Vervaet, Ingmar Nopens, Thomas De Beer
Conventional pharmaceutical freeze-drying is an inefficient and expensive batch-wise process, associated with several disadvantages leading to an uncontrolled end product variability. The proposed continuous alternative, based on spinning the vials during freezing and on optimal energy supply during drying, strongly increases process efficiency and improves product quality (uniformity). The heat transfer during continuous drying of the spin frozen vials is provided via non-contact infrared (IR) radiation. The energy transfer to the spin frozen vials should be optimised to maximise the drying efficiency while avoiding cake collapse...
January 12, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28088636/comparison-of-mucoadhesive-and-cohesive-features-of-poly-acrylic-acid-conjugates-respective-their-molecular-mass
#8
Flavia Laffleur, Kathrin Knapp, Wongsakorn Suchaoin, Alexandra Partenhauser, Kesinee Netsomboon, Andreas Bernkop-Schnürch
OBJECTIVES: This study aimed to assess the impact of molecular mass as well as the differences between poly(acrylic acid)-thiol-conjugates (PAA100,250,450 KDa) on their mucoadhesive and cohesive qualities. METHODS: Covalent attachment of cysteine (CYS), cysteamine (CYSM) and L-gluthathione (GSH) to poly(acrylic acid) was achieved by formation of amide bonds between primary amino group of the amino acid (in the case of cysteine and glutathione), respectively the amino group of the aminothiol cysteamine and carboxylic acid group of the polymer...
January 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28088635/mucoadhesive-amorphous-solid-dispersions-for-sustained-release-of-poorly-water-soluble-drugs
#9
Justin S LaFountaine, Leena Kumari Prasad, Dave A Miller, James W McGinity, Robert O Williams
The oral delivery of mucoadhesive patches has been shown to enhance the absorption of large molecules such as peptides. We hypothesized that this mechanism could have utility for poorly soluble small molecules by utilizing a mucoadhesive polymer as the matrix for an amorphous solid dispersion. Binary dispersions of itraconazole and carbomer (Carbopol 71G) were prepared utilizing a thermokinetic mixing process (KinetiSol Dispersing) and the physicochemical properties were investigated by powder x-ray diffraction, calorimetry, and liquid chromatography...
January 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28088634/chitosan-g-poly-n-isopropylacrylamide-copolymers-as-delivery-carriers-for-intracameral-pilocarpine-administration
#10
Jui-Yang Lai, Li-Jyuan Luo
This study reports, for the first time, the development of a chitosan-g-poly(N-isopropylacrylamide) (Chi-PN) biodegradable in situ gelling delivery system for ocular pilocarpine administration through intracameral injection. The number of thermo-responsive polymer segments grafted onto the chitosan via carbodiimide-mediated formation of amide linkages was greatly affected by varying the feeding amount of carboxyl-terminated poly(N-isopropylacrylamide) in the synthesis, thereby determining the phase transition temperature and enzymatic degradability of Chi-PN materials...
January 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28088633/quantitative-analysis-of-lab-to-lab-variability-in-caco-2-permeability-assays
#11
Jong Bong Lee, Atheer Zgair, Dhiaa A Taha, Xiaowei Zang, Leonid Kagan, Tae Hwan Kim, Min Gi Kim, Hwi-Yeol Yun, Peter M Fischer, Pavel Gershkovich
In this study, Caco-2 permeability results from different laboratories were compared. Six different sets of apparent permeability coefficient (Papp) values reported in the literature were compared to experimental Papp obtained in our laboratory. The differences were assessed by determining the root mean square error (RMSE) values between the datasets, which reached levels as high as 0.581 for the training set compounds, i.e. ten compounds with known effective human permeability (Peff). The consequences of these differences in Papp for prediction of oral drug absorption were demonstrated by introducing the Papp into the absorption and pharmacokinetics simulation software application GastroPlus(TM) for prediction of the fraction absorbed (Fa) in humans using calibrated "user-defined permeability models"...
January 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28088632/nanosized-complexation-assemblies-housed-inside-reverse-micelles-churn-out-monocytic-delivery-cores-for-bendamustine-hydrochloride
#12
Yuvraj Singh, Anumandla Chandrashekhar, Jaya Gopal Meher, K K Durga Rao Viswanadham, Vivek K Pawar, Kavit Raval, Komal Sharma, Pankaj K Singh, Animesh Kumar, Manish K Chourasia
OBJECTIVE: We explore a plausible method of targeting bendamustine hydrochloride (BM) to circulatory monocytes by exploiting their intrinsic endocytic/phagocytic capability. METHODS: We do so by complexation of sodium alginate and chitosan inside dioctyl sulfo succinate sodium (AOT) reverse micelles to form bendamustine hydrochloride loaded nanoparticles (CANPs). Dynamic light scattering, electrophoretic mobility and UV spectroscopy were used to detail intra-micellar complexation dynamics and to prove that drug was co-captured during interaction of carbohydrate polymers...
January 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28088005/nicotine-hydrogen-tartrate-loaded-chitosan-nanoparticles-formulation-characterization-and-in-vitro-delivery-from-dry-powder-inhaler-formulation
#13
Hui Wang, Graeme George, Selena Bartlett, Changyou Gao, Nazrul Islam
This study reports the development of nanoparticles in the form of inhalable micro-aggregates of biodegradable chitosan (CS) loaded with nicotine hydrogen tartrate (NHT) for potential pulmonary delivery of nicotine from dry powder inhaler (DPI) formulations with prolonged release profile. The NHT-loaded CS particles were prepared using a water-in-oil emulsion crosslinking method. The prepared particles were characterized using scanning electron microscopy (SEM) and transmission electron microscopy (TEM) for morphological studies; Zetasizer and Mastersizer were applied for particle size analysis...
January 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28088004/a-catechin-nanoformulation-inhibits-wm266-melanoma-cell-proliferation-migration-and-associated-neo-angiogenesis
#14
Nicoletta di Leo, Matteo Battaglini, Liron Berger, Martina Giannaccini, Luciana Dente, Silke Hampel, Orazio Vittorio, Giuseppe Cirillo, Vittoria Raffa
We validated the anticancer potential of a nanoformulation made by (+)-catechin, gelatin and carbon nanotubes in terms of inhibition of cancer cell proliferation, migration and associated neo-angiogenesis. Gelatin was selected to stabilize the catechin without compromising its anti-oxidant potential and the carbon nanotubes were used to increase its intracellular bioavailability. The anticancer potential of the resulting nanohybrid was validated on an aggressive melanoma cell line, in vitro and in zebrafish xenotransplants...
January 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28088003/the-effect-of-the-antioxidant-on-the-properties-of-thiolated-poly-aspartic-acid-polymers-in-aqueous-ocular-formulations
#15
Mária Budai-Szűcs, Gabriella Horvát, Benjámin Gyarmati, Barnabás Áron Szilágyi, András Szilágyi, Szilvia Berkó, Rita Ambrus, Piroska Szabó-Révész, Giuseppina Sandri, Maria Cristina Bonferoni, Carla Caramella, Erzsébet Csányi
Thiolated polymers are a promising new group of excipients, but their stability against atmospheric oxidation has not been investigated in detail, and only a few efforts have been made to improve their stability. The oxidation of the thiol groups in solutions of thiolated polymers may result in a decrease of mucoadhesion and unpredictable in situ gelation. The aims of our work were to study the stability of aqueous solutions of thiolated polymers and the effects of stabilizing agents. We investigated thiolated poly(aspartic acid) polymers stabilized with dithiothreitol, glutathione or acetylcysteine...
January 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28087377/in-vivo-biodistribution-and-imaging-studies-with-a-99m-tc-radiolabeled-derivative-of-the-c-terminus-of-prothymosin-alpha-in-mice-bearing-experimentally-induced-inflammation
#16
Chrysoula-Evangelia Karachaliou, Charalampos Triantis, Christos Liolios, Lazaros Palamaris, Christos Zikos, Ourania E Tsitsilonis, Hubert Kalbacher, Wolfgang Voelter, George Loudos, Minas Papadopoulos, Ioannis Pirmettis, Evangelia Livaniou
Prothymosin alpha (ProTα) is a highly conserved mammalian polypeptide (109 amino acids in man) exerting in vitro and in vivo immunoenhancing activities. Recently, our team has developed a (99m)Tc-radiolabeled derivative of the C-terminal bioactive decapeptide of ProTα ([(99m)Tc]C1) and employed it in in vitro studies, the results of which support the existence of binding sites on human neutrophils that recognize [(99m)Tc]C1, intact ProTα as well as the C-terminal decapeptide of ProTα and presumably involve Toll-like receptor 4...
January 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28087376/ir780-loaded-tpgs-tos-micelles-for-breast-cancer-photodynamic-therapy
#17
Cleide Pais-Silva, Duarte de Melo-Diogo, Ilídio J Correia
IR780 iodide is a near-infrared (NIR) dye with a huge potential for cancer imaging and phototherapy. However, its biomedical application is strongly impaired by its lipophilic character. Herein, amphiphilic micelles based on d-α-tocopheryl polyethylene glycol succinate (TPGS) and d-α-tocopheryl succinate (TOS), two vitamin E derivatives with intrinsic anticancer activity, are explored to load IR780. IR780-loaded micelles with suitable sizes are obtained by using specific TPGS and TOS weight feed ratios during micelles formulation and these are able to encapsulate IR780 with high efficiency...
January 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28087380/polymeric-mixed-micelles-as-nanomedicines-achievements-and-perspectives
#18
REVIEW
Maximiliano Cagel, Fiorella C Tesan, Ezequiel Bernabeu, Maria J Salgueiro, Marcela B Zubillaga, Marcela A Moretton, Diego A Chiappetta
During the past few decades, polymeric micelles have raised special attention as novel nano-sized drug delivery systems for optimizing the treatment and diagnosis of numerous diseases. These nanocarriers exhibit several in vitro and in vivo advantages as well as increased stability and solubility to hydrophobic drugs. An interesting approach for optimizing these properties and overcoming some of their disadvantages is the combination of two or more polymers in order to assemble polymeric mixed micelles. This review article gives an overview on the current state of the art of several mixed micellar formulations as nanocarriers for drugs and imaging probes, evaluating their ongoing status (preclinical or clinical stage), with special emphasis on type of copolymers, physicochemical properties, in vivo progress achieved so far and toxicity profiles...
January 10, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28087379/pegylated-liposomes-for-topical-vaginal-therapy-improve-delivery-of-interferon-alpha
#19
May Wenche Jøraholmen, Purusotam Basnet, Ganesh Acharya, Nataša Škalko-Basnet
Recent studies regarding mucosal drug delivery indicate that nanosystems with surface-available polyethylene glycol (PEG) are able to penetrate mucus barrier, assure closer contact with the epithelium, and improve drug delivery to vagina. In the present work, we developed the mucus-penetrating PEGylated liposomes containing interferon alpha-2b (IFN α-2b), destined to provide localized therapy for human papilloma virus (HPV) vaginal infections. The PEGylated liposomes were of a mean size of 181 ± 8 nm, bearing a negative zeta potential of - 13 mV and an entrapment efficiency of 81 ± 10 %...
January 10, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28087378/new-scaffolds-encapsulating-tgf-%C3%AE-3-bmp-7-combinations-driving-strong-chondrogenic-differentiation
#20
Jose Crecente-Campo, Erea Borrajo, Anxo Vidal, Marcos Garcia-Fuentes
The regeneration of articular cartilage remains an unresolved question despite the current access to a variety of tissue scaffolds activated with growth factors relevant to this application. Further advances might result from combining more than one of these factors; here, we propose a scaffold composition optimized for the dual delivery of BMP-7 and TGF-β3, two proteins with described chondrogenic activity. First, we tested in a mesenchymal stem cell micromass culture with TGF-β3 whether the exposure to microspheres loaded with BMP-7 would improve cartilage formation...
January 10, 2017: European Journal of Pharmaceutics and Biopharmaceutics
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