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International Journal of Pharmaceutics

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https://www.readbyqxmd.com/read/28533175/dendrimer-encapsulated-and-conjugated-delivery-of-berberine-a-novel-approach-mitigating-toxicity-and-improving-in-vivo-pharmacokinetics
#1
Lokesh Gupta, Ashok Kumar Sharma, Avinash Gothwal, Mohammed Shahid Khan, Mahaveer Prasad Khinchi, Arem Qayum, Shashank Kumar Singh, Umesh Gupta
Berberine (BBR) is a nitrogenous cyclic natural alkaloid with potential anticancer activity. However it has been less explored due to its poor pharmacokinetic profile. Dendrimers (e.g. PAMAM) have promising potential to deliver anticancer drugs/bio-actives because of their well-defined architecture, monodispersity and tailor-made surface functionality. In the present study it was attempted to deliver berberine through G4 PAMAM dendrimers by conjugation (BPC) as well as encapsulation (BPE) approach. The developed encapsulated and conjugated berberine formulations were found to have size in the approximate range of 100-200nm while zeta potential was almost same as PAMAM G4 dendrimer...
May 19, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28533174/how-should-we-plan-the-future-of-nanomedicine-for-cancer-diagnosis-and-therapy
#2
EDITORIAL
Khair Alhareth, Lucie Sancey, Nicolas Tsapis, Nathalie Mignet
No abstract text is available yet for this article.
May 19, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28528851/microstructure-evaluation-of-dermally-applicable-liquid-crystals-as-a-function-of-water-content-and-temperature-can-electron-paramagnetic-resonance-provide-complementary-data
#3
Mirjam Gosenca Matjaž, Janez Mravljak, Marija Bešter Rogač, Marjeta Šentjurc, Mirjana Gašperlin, Alenka Zvonar Pobirk
Insight into the microstructure of lyotropic liquid crystals (LCs) is of crucial importance for development of novel dermal delivery systems. Our aim was to evaluate the phase behaviour of dermally applicable LCs composed of isopropyl myristate/Tween 80/lecithin/water, along the dilution line, where phase transitions are predominantly driven by increased water content. Additionally, identification of LC temperature dependence is of great importance for skin application. Selected LCs were evaluated using electron paramagnetic resonance (EPR) plus conventionally used methods of polarization microscopy, small-angle X-ray scattering, differential scanning calorimetry, and rheological measurements...
May 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28528850/overview-of-solidification-techniques-for-self-emulsifying-drug-delivery-systems-from-industrial-perspective
#4
J Mandić, A Zvonar Pobirk, F Vrečer, M Gašperlin
Self-emulsifying drug delivery systems (SEDDS) are lipid formulations that improve solubility and oral bioavailability of the incorporated drug with poor biopharmaceutical properties. As liquids they are traditionally filled into soft or hard capsules. Transformation of SEDDS into solid dosage form has been extensively investigated in the recent years because solid dosage forms improve stability, handling and patient compliance. By using different solidification techniques selfemulsifying powders, granules, pellets and tablets can be produced...
May 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28528212/targeted-co-delivery-of-polypyrrole-and-rapamycin-by-trastuzumab-conjugated-liposomes-for-combined-chemo-photothermal-therapy
#5
Hanh Thuy Nguyen, Tuan Hiep Tran, Raj Kumar Thapa, Cao Dai Phung, Beom Soo Shin, Jee-Heon Jeong, Han-Gon Choi, Chul Soon Yong, Jong Oh Kim
Trastuzumab is a therapeutic monoclonal antibody that selectively recognizes HER2/neu receptor for targeting breast cancers. In this study, we aimed to present a strategy to combine chemo and phototherapy and targeted delivery via monoclonal antibody for enhanced anticancer effects. We co-loaded a chemotherapeutic agent, rapamycin, and a photosensitizer, polypyrrole, in trastuzumab-conjugated liposomes (LRPmAb) for combined chemo-photothermal therapy. LRPmAb had small size (172.2±9.6nm), narrow distribution, and negative ζ-potential (-12...
May 17, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28522428/characterization-of-new-crystalline-forms-of-hydroxyprogesterone-caproate
#6
Jeffrey Caplette, Timothy Frigo, Michael Jozwiakowski, Helene Shea, Mahmoud Mirmehrabi, Peter Müller
A systematic polymorph screening process was conducted on the steroid hydroxyprogesterone caproate, which had only one previously described orthorhombic crystalline form (A), in order to fully elucidate its solid state properties. Cooling, anti-solvent and evaporative techniques largely reproduced the same polymorph, but slurries in various solvents over two days produced a new triclinic form (B). Experiments at different temperatures in ethyl acetate or isopropyl alcohol confirmed this was an enantiotropic system with a transition temperature of approximately 30°C...
May 15, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28522427/association-of-chitosan-and-aluminium-as-a-new-adjuvant-strategy-for-improved-vaccination
#7
F Lebre, D Bento, J Ribeiro, M Colaço, G Borchard, M C Pedroso de Lima, O Borges
The use of particulate adjuvants offers an interesting possibility to enhance and modulate the immune responses elicited by vaccines. Aluminium salts have been extensively used as vaccine adjuvants, but they lack the capacity to induce a strong cellular and mucosal immune response. Taking this into consideration, in this study we designed a new antigen delivery system combining aluminium salts with chitosan. Chitosan-aluminium nanoparticles (CH-Al NPs) exhibited a mean diameter of 280nm and a positive surface charge...
May 15, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28522426/polymer-coated-mucoadhesive-liposomes-intended-for-the-management-of-xerostomia
#8
Małgorzata I Adamczak, Ørjan G Martinsen, Gro Smistad, Marianne Hiorth
The aim of this work was to prepare and test different pharmaceutical formulations in respect of their potential in relieving dry mouth symptom. Since many of the products available on the market provide only temporary relief to the patients, there is need for new formulations able to retain on the oral mucosa. The prolonged moisture protection could be achieved by combining mucoadhesive materials, such as polymers containing hydrogen bonding groups, with vesicles capable of releasing hydration medium from the inner compartment...
May 15, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28522425/development-and-characterization-of-fast-dissolving-tablets-of-oxaprozin-based-on-hybrid-systems-of-the-drug-with-cyclodextrins-and-nanoclays
#9
Francesca Maestrelli, Paola Mura, Marzia Cirri, Natascia Mennini, Carla Ghelardini, Lorenzo Di Cesare Mannelli
Previous studies highlighted an increase of the randomly-methylated-ß-cyclodextrin (RAMEB) solubilizing power towards oxaprozin when used in combination with L-arginine (ARG) or sepiolite nanoclay (SV). Therefore, the aim of this work was to investigate the possibility of maximising the RAMEB solubilizing efficacy by a joined approach based on the entrapment in SV of the drug-RAMEB-ARG complex. The quaternary nanocomposite was prepared by different techniques and characterized for solid state and dissolution properties, compared to ternary drug combinations with RAMEB-ARG, RAMEB-SV or ARG-SV...
May 15, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28522424/cyclodextrin-based-nanocarriers-containing-a-synergic-drug-combination-a-potential-formulation-for-pulmonary-administration-of-antitubercular-drugs
#10
Giuseppina Salzano, Jitendra Wankar, Stefano Ottani, Baptiste Villemagne, Alain R Baulard, Nicolas Willand, Priscille Brodin, Ilse Manet, Ruxandra Gref
Tuberculosis (TB) remains a major global health problem. The use of ethionamide (ETH), a main second line drug, is associated to severe toxic side-effects due to its low therapeutic index. In this challenging context, "booster" molecules have been synthetized to increase the efficacy of ETH. However, the administration of ETH/booster pair is mostly hampered by the low solubility of these drugs and the tendency of ETH to crystallize. Here, ETH and a poorly water-soluble booster, so-called BDM43266, were simultaneously loaded in polymeric β-cyclodextrin nanoparticles (pβCyD NPs) following a "green" protocol...
May 15, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28522423/sertaconazole-nitrate-loaded-nanovesicular-systems-for-targeting-skin-fungal-infection-in-vitro-ex-vivo-and-in-vivo-evaluation
#11
Menna M Abdellatif, Islam A Khalil, Mahmoud A F Khalil
The aim of this study was to develop different vesicular systems for sertaconazole nitrate and evaluate the ability of targeting deep skin layers to treat dermal fungal infection. Therefore, different phospholipid based nanovesicles, namely liposomes, glycerosomes, transferosmes and ethosomes were prepared and in-vitro evaluated for morphology, entrapment efficiency, vesicle size and zeta potential value, followed by ex-vivo evaluation through skin penetration and permeation. The selected vesicular formula was incorporated into gel base system and assessed by ex-vivo permeation visualization study using confocal laser scanning microscopy (CLSM)...
May 15, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28506803/peg-coated-and-doxorubicin-loaded-multimodal-gadolinium-oxide-nanoparticles-for-simultaneous-drug-delivery-and-imaging-applications
#12
Shailja Kumar, Virendra Kumar Meena, Puja Panwar Hazari, Rakesh Kumar Sharma
We report water-in-oil microemulsion mediated synthesis of polyethylene glycol (PEG(1)) coated Gd2O3 nanoparticles (NPs(2)) loaded with fluorescent anti-cancer drug doxorubicin (dox(3)) for synchronous drug delivery, optical and magnetic resonance (MR(4)) imaging applications. These PEG covered Gd2O3 NPs loaded with dox (Gd-PEG-dox NPs) were found to possess spherical morphology with 13nm size as measured from TEM and the hydrodynamic diameter comes out to be 37nm as determined from DLS. Fluorescence spectra and fluorescence microscopy images confirmed optical activity of the NPs...
May 12, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28506802/stealth-magnetic-nanocarriers-of-sirna-as-platform-for-breast-cancer-theranostics
#13
J Bruniaux, S Ben Djemaa, K Hervé-Aubert, H Marchais, I Chourpa, S David
The endogenous mechanism of RNA interference is more and more used in research to obtain specific down-regulation of gene expression in diseases such as breast cancer. Currently, despite the new fields of study open up by RNA interference, the rapid degradation of siRNA by nucleases and their negative charges prevent them from crossing cell membranes. To overcome these limitations, superparamagnetic iron oxide nanoparticles (SPIONs) represent a promising alternative for nucleic acid delivery. Previously, we reported the magnetic siRNA nanovectors (MSN) formulation using electrostatic assembly of (1) SPIONs, also able to act as contrast agents for magnetic resonance imaging (MRI), (2) siRNA and (3) chitosan aiming at their protection and enhancing their transfection efficacy...
May 12, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28506801/old-drug-new-wrapping-a-possible-comeback-for-chloramphenicol
#14
Sveinung G Ingebrigtsen, Alena Didriksen, Mona Johannessen, Nataša Škalko-Basnet, Ann Mari Holsæter
The antimicrobial drug chloramphenicol (CAM) exhibits activity against resistant bacteria, such as methicillin-resistant Staphylococcus aureus (MRSA). However, its use has been limited due to its toxicity. As the threat of antibiotic resistance continues to grow, a promising approach might be to increase the use of historical antimicrobial agents that demonstrate clinical efficacy, but are hampered by toxicity. We therefore aimed to prepare a liposome-in-hydrogel system for dermal delivery of CAM. Chitosan (CS) was used as the hydrogel vehicle due to its antimicrobial activity and excellent biocompatibility...
May 12, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28506800/behaviour-of-silver-nanoparticles-in-simulated-saliva-and-gastrointestinal-fluids
#15
Lucie Pinďáková, Věra Kašpárková, Kristina Kejlová, Markéta Dvořáková, Daniel Krsek, Dagmar Jírová, Lucie Kašparová
Continuously increasing application of silver nanoparticles (AgNPs) requires information on their safety and performance under biological conditions. Assessment of AgNPs in biological systems is also related to availability of robust toxicological methods for evaluation of toxic potential of AgNPs and information on their physicochemical state. Silver nanoparticles were subjected to action of simulated saliva, gastric and intestinal fluids, appropriately supplemented with digestive enzymes pepsin or pancreatin...
May 12, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28502898/development-of-modified-release-3d-printed-tablets-printlets-with-pharmaceutical-excipients-using-additive-manufacturing
#16
Alvaro Goyanes, Fabrizio Fina, Annalisa Martorana, Daniel Sedough, Simon Gaisford, Abdul W Basit
The aim of this study was to manufacture 3D printed tablets (printlets) from enteric polymers by single filament fused deposition modeling (FDM) 3D printing (3DP). Hot melt extrusion was used to generate paracetamol-loaded filaments from three different grades of the pharmaceutical excipient hypromellose acetate succinate (HPMCAS), grades LG, MG and HG. One-step 3DP was used to process these filaments into enteric printlets incorporating up to 50% drug loading with two different infill percentages (20 and 100%)...
May 11, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28502897/a-multifunctional-%C3%AE-cyclodextrin-conjugate-photodelivering-nitric-oxide-with-fluorescence-reporting
#17
Gábor Benkovics, Marta Perez-Lloret, Damien Afonso, András Darcsi, Szabolcs Béni, Éva Fenyvesi, Milo Malanga, Salvatore Sortino
This contribution reports the design, synthesis and photochemical properties of a novel cationic, water soluble, β-cyclodextrin (βCD) conjugate integrating an anthracene moiety and a nitroaniline derivative within the primary side of the βCD scaffold. Photoinduced energy transfer between the anthracene and the nitroaniline chromophores effectively suppresses the fluorescence of the anthracene unit. Excitation with visible light triggers the release of nitric oxide (NO) from the nitroaniline chromophore, accompanied to the concomitant revival of the anthracene fluorescence, which acts as an optical reporter for detecting the amount of the NO released...
May 11, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28502896/a-quality-by-design-qbd-twin-screw-extrusion-wet-granulation-approach-for-processing-water-insoluble-drugs
#18
Mohammed Maniruzzaman, Steven A Ross, Tumpa Dey, Arun Nair, Martin J Snowden, Dennis Douroumis
In this study, a Quality by Design (QbD) approach was used to identify the effect of formulation parameters in a twin screw wet extrusion granulation process for the manufacturing of ibuprofen (IBU) granules with increased dissolution rates. A fractional factorial Design of Experiment (DoE) was used to investigate the effect of the excipient composition, binder amount and liquid to solid (L/S) ratio (independent variables) on drug dissolution rates, median particle size diameter and specific surface area (dependent variables)...
May 11, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28502895/nanostructured-lipid-carriers-employing-polyphenols-as-promising-anticancer-agents-quality-by-design-qbd-approach
#19
Ketki Bhise, Sushil Kumar Kashaw, Samaresh Sau, Arun K Iyer
Cancer is one of the leading causes of death worldwide. There are several hurdles in cancer therapy because of side-effects which limits its usage. Nanoparticulate drug delivery systems have been tested against cancer in a range of scientific studies. In the recent years, advanced research on Nanostructured Lipid Carriers (NLCs) has garnered considerable attention owing to the advantages over their first-generation counterparts, Solid Lipid Nanoparticles (SLN). NLCs facilitate efficient loading of poorly water soluble drugs with simple methods of drug loading...
May 11, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28502894/soluble-1-1-complexes-and-insoluble-3-2-complexes-understanding-the-phase-solubility-diagram-of-hydrocortisone-and-%C3%AE-cyclodextrin
#20
Christian Schönbeck, Tobias L Madsen, Günther H Peters, René Holm, Thorsteinn Loftsson
The molecular mechanisms underlying the drug-solubilizing properties of γ-cyclodextrin were explored using hydrocortisone as a model drug. The BS-type phase-solubility diagram of hydrocortisone with γ-cyclodextrin was thoroughly characterized by measuring the concentrations of hydrocortisone and γ-cyclodextrin in solution and the solid phase. The drug-solubilizer interaction was also studied by isothermal titration calorimetry from which a precise value of the 1:1 binding constant (K11=4.01mM(-1) at 20°C) was obtained...
May 11, 2017: International Journal of Pharmaceutics
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