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P-Glycoprotein in skin contributes to transdermal absorption of topical corticosteroids
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Naoto Hashimoto, Noritaka Nakamichi, Erina Yamazaki, Masashi Oikawa, Yusuke Masuo, Alfred H. Schinkel, Yukio Kato ATP binding cassette transporters, P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), are expressed in skin, but their involvement in transdermal absorption of clinically used drugs remains unknown. Here, we examined their role in transdermal absorption of corticosteroids. Skin and plasma concentrations of dexamethasone after dermal application were reduced in P-gp and BCRP tri...
Source: International Journal of Pharmaceutics - March 17, 2017 Category: Drugs & Pharmacology Source Type: research

A study of the aggregation of cyclodextrins: Determination of the critical aggregation concentration, size of aggregates and thermodynamics using isodesmic and K2 –K models
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Thao Thi Do, Rob Van Hooghten, Guy Van den Mooter The aggregation of three different cyclodextrins (CDs): 2-hydroxypropyl-β-cyclodextrin (HP-β-CD), 2-hydroxypropyl-γ-cyclodextrin (HP-γ-CD) and sulfobutylether-β-cyclodextrin (SBE-β-CD) was studied. The critical aggregation concentration (cac) of these three CDs is quite similar and is situated at ca. 2% (m/v). There was only a small difference in the cac values determined by DLS and 1H NMR. DLS measurements revealed that CDs...
Source: International Journal of Pharmaceutics - March 17, 2017 Category: Drugs & Pharmacology Source Type: research

A pH-responsive glycolipid-like nanocarrier for optimising the time-dependent distribution of free chemical drugs in focal cells
Publication date: 30 April 2017 Source:International Journal of Pharmaceutics, Volume 522, Issues 1–2 Author(s): Bolin Cheng, Binbin Lu, Xuan Liu, Tingting Meng, Yanan Tan, Yun Zhu, Na Liu, Hong Yuan, Xuan Huang, Fuqiang Hu Though Drug delivery systems have achieved accumulation at tumor sites via passive targeting and active targeting, the therapeutic effects are far from perfect. The unsatisfactory results are mainly due to limited drug release from the nanocarriers at tumor sites, while the pharmacological activities of the drug are attributed to the concentration of the free drug and the time maintained at the p...
Source: International Journal of Pharmaceutics - March 17, 2017 Category: Drugs & Pharmacology Source Type: research

Modifying plasmid-loaded HSA-nanoparticles with cell penetrating peptides – Cellular uptake and enhanced gene delivery
Publication date: 30 April 2017 Source:International Journal of Pharmaceutics, Volume 522, Issues 1–2 Author(s): J. Mesken, A. Iltzsche, D. Mulac, K. Langer Gene therapy bears great potential for the cure of a multitude of human diseases. Research efforts focussed on the use of viral delivery vectors in the past decades, neglecting non-viral gene therapies of physical or chemical origin due to low transfection efficiency. However, side effects such as activation of oncogenes and inflammatory reactions upon immune cell activation are major obstacles impeding the clinical applicability of viral gene therapy vectors. T...
Source: International Journal of Pharmaceutics - March 17, 2017 Category: Drugs & Pharmacology Source Type: research

Protein-based nanoparticles: From preparation to encapsulation of active molecules
Publication date: 30 April 2017 Source:International Journal of Pharmaceutics, Volume 522, Issues 1–2 Author(s): Mohamad Tarhini, Hélène Greige-Gerges, Abdelhamid Elaissari Nowadays, nanotechnology has become very integrated in the domain of pharmaceutical sciences since nanoparticle dispersions show various advantages as drug carriers. Among nanoparticles, the protein-based ones are of paramount importance. In fact, protein nanoparticles show many advantages over other types of nanoparticles, they are often non-toxic and biodegradable. In this review, the most common preparation methods of protein nan...
Source: International Journal of Pharmaceutics - March 17, 2017 Category: Drugs & Pharmacology Source Type: research

Preparation and characterization of gastrointestinal wafer formulations
In this study gastrointestinal, twolayered wafers containing a water-insoluble backing layer and a drug-loaded, mucoadhesive layer were fabricated by casting solvent technique. The backing layer consists of Ethocel™ Standard 10 Premium and the mucoadhesive layer was prepared using a mixture of Methocel™ E15 Premium LV, polyvinyl alcohol and Macrogol 400. The wafers were characterized regarding their appearance, mechanical properties and dissolution profiles as well as the influence of backing layer thickness on drug transfer and their ability of unidirectional drug release. The wafers with backing layer thickne...
Source: International Journal of Pharmaceutics - March 17, 2017 Category: Drugs & Pharmacology Source Type: research

Surface functionalization of methotrexate-loaded chitosan nanoparticles with hyaluronic acid/human serum albumin: Comparative characterization and in vitro cytotoxicity
Publication date: 30 April 2017 Source:International Journal of Pharmaceutics, Volume 522, Issues 1–2 Author(s): Rania A. Hashad, Rania A.H. Ishak, Ahmed S. Geneidi, Samar Mansour The active tumor targeting ligands, hyaluronic acid (HA) and human serum albumin (HSA), are considered promising targeting moieties of drug carriers for cancer therapy. The chitosan nanoparticles loaded with methotrexate (MTX-CsNPs) were employed as the core for subsequent coating process. HA and HSA coating solutions were used at different concentrations. The effect of different HA Mw (1000, 360, 10kDa) was also investigated. The coated M...
Source: International Journal of Pharmaceutics - March 14, 2017 Category: Drugs & Pharmacology Source Type: research

Plant-expressed Hepatitis B core antigen virus-like particles: Characterization and investigation of their stability in simulated and pig gastro-intestinal fluids
Publication date: 30 April 2017 Source:International Journal of Pharmaceutics, Volume 522, Issues 1–2 Author(s): Alberto Berardi, George P. Lomonossoff, David J. Evans, Susan A. Barker Virus-like particles (VLPs) are potential oral vaccine candidates, as their highly compact structure may allow them to withstand the harsh conditions of the gastro-intestinal (GI) environment. Hepatitis B core antigen (HBcAg) is an immunogenic protein that assembles into 30 or 34nm diameter VLPs. Here, the stabilities of both the HBcAg polypeptide itself and the three-dimensional structure of the VLPs upon exposure to in vitro and ex ...
Source: International Journal of Pharmaceutics - March 14, 2017 Category: Drugs & Pharmacology Source Type: research

Real life dose emission characterization using COPD patient inhalation profiles when they inhaled using a fixed dose combination (FDC) of the medium strength Symbicort ® Turbuhaler®
Publication date: 30 April 2017 Source:International Journal of Pharmaceutics, Volume 522, Issues 1–2 Author(s): Golshan Bagherisadeghi, El Hassane Larhrib, Henry Chrystyn The dose emitted from dry powder inhalers (DPI) is inhalation flow dependent and so varies with the peak inhalation flow (PIF) of a patient’s inhalation maneuver (IM). Dose emission could also be affected by other IM parameters-the inhaled volume (Vin) and the initial acceleration rate of the IM (ACIM). We have adapted the compendial method for in-vitro DPI determinations so that inhalation profiles replace the inhalation square profile gene...
Source: International Journal of Pharmaceutics - March 14, 2017 Category: Drugs & Pharmacology Source Type: research

Gambogic acid grafted low molecular weight heparin micelles for targeted treatment in a hepatocellular carcinoma model with an enhanced anti-angiogenesis effect
In this study, GA grafted low molecular weight heparin (GA-LMWH) was prepared and self-assembled into micelles in aqueous solution to improve the solubility and antitumor effects against hepatocellular carcinoma. The substitution of GA-LMWH is 27.5±0.2%. The micelles had a mean size of 190.4±10.8nm, a low critical micelle concentration of 2.4±0.2μgmL−1, and the highest area under the concentration-time curve and mean retention time in the liver compared to the heart, spleen, lung and kidney (p< 0.05). The targeting efficiency of micelles to the liver is 2.1-times higher than that of the...
Source: International Journal of Pharmaceutics - March 11, 2017 Category: Drugs & Pharmacology Source Type: research

Characterisation of aggregates of cyclodextrin-drug complexes using Taylor Dispersion Analysis
Publication date: 30 April 2017 Source:International Journal of Pharmaceutics, Volume 522, Issues 1–2 Author(s): Hadar Zaman, Andrew G. Bright, Kevin Adams, David M. Goodall, Robert T. Forbes There is a need to understand the nature of aggregation of cyclodextrins (CDs) with guest molecules in increasingly complex formulation systems. To this end an innovative application of Taylor dispersion analysis (TDA) and comparison with dynamic light scattering (DLS) have been carried out to probe the nature of ICT01-2588 (ICT-2588), a novel tumor-targeted vascular disrupting agent, in solvents including a potential buffered ...
Source: International Journal of Pharmaceutics - March 11, 2017 Category: Drugs & Pharmacology Source Type: research

The diffusion dynamics of PEGylated liposomes in the intact vitreous of the ex vivo porcine eye: A fluorescence correlation spectroscopy and biodistribution study
Publication date: 30 April 2017 Source:International Journal of Pharmaceutics, Volume 522, Issues 1–2 Author(s): Anne Z. Eriksen, Jonathan Brewer, Thomas L. Andresen, Andrew J. Urquhart The diffusion dynamics of nanocarriers in the vitreous and the influence of nanocarrier physicochemical properties on these dynamics is an important aspect of the efficacy of intravitreal administered nanomedicines for the treatment of posterior segment eye diseases. Here we use fluorescence correlation spectroscopy (FCS) to determine liposome diffusion coefficients in the intact vitreous (DVit) of ex vivo porcine eyes using a modifi...
Source: International Journal of Pharmaceutics - March 10, 2017 Category: Drugs & Pharmacology Source Type: research

Pharmaceutical properties of two ethenzamide-gentisic acid cocrystal polymorphs: Drug release profiles, spectroscopic studies and theoretical calculations
Publication date: 30 April 2017 Source:International Journal of Pharmaceutics, Volume 522, Issues 1–2 Author(s): Agnieszka Sokal, Edyta Pindelska, Lukasz Szeleszczuk, Waclaw Kolodziejski The aim of this study was to evaluate the stability and solubility of the polymorphic forms of the ethenzamide (ET) – gentisic acid (GA) cocrystals during standard technological processes leading to tablet formation, such as compression and excipient addition. In this work two polymorphic forms of pharmaceutical cocrystals (ETGA) were characterized by 13C and 15N solid-state nuclear magnetic resonance and Fourier transformed i...
Source: International Journal of Pharmaceutics - March 10, 2017 Category: Drugs & Pharmacology Source Type: research

Amorphous is not always better —A dissolution study on solid state forms of carbamazepine
In this study the dissolution properties of different solid state forms of carbamazepine, crystalline or amorphous drug, with or without either polyvinylpyrrolidone (PVP) or hydroxypropylmethylcellulose (HPMC) and glass solutions of the drug with both polymers (2:1, 4:1 and 10:1 (w/w) drug-to-polymer ratio) were tested with respect to their dissolution behaviour in a biorelevant gastric medium (for 30min) and subsequently in intestinal conditions (for 2h). Carbamazepine form III in the absence of polymer dissolved to a drug concentration of 540μg/ml, but the concentration decreased after around 70min due to precipitatio...
Source: International Journal of Pharmaceutics - March 10, 2017 Category: Drugs & Pharmacology Source Type: research

The application of novel nano-thermal and imaging techniques for monitoring drug microstructure and distribution within PLGA microspheres
In this study, we investigate the feasibility of applying the aforementioned technique combined with other thermal, imaging and structural techniques for monitoring the drug microstructure and spatial distribution within bovine serum albumin (BSA) loaded and nimodipine loaded PLGA microspheres, with a view to better predicting the in vitro drug release performance. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - March 7, 2017 Category: Drugs & Pharmacology Source Type: research

Enhanced ocular efficacy of topically-delivered dorzolamide with nanostructured mucoadhesive microparticles
Publication date: 30 April 2017 Source:International Journal of Pharmaceutics, Volume 522, Issues 1–2 Author(s): Chun Gwon Park, Young Kook Kim, Se-Na Kim, Seung Ho Lee, Beom Kang Huh, Min-A Park, Hyein Won, Ki Ho Park, Young Bin Choy Dorzolamide eye drops are widely prescribed to reduce intraocular pressure (IOP) in the treatment of ocular hypertension and glaucoma. However, in an eye drop formulation, dorzolamide is rapidly cleared from the preocular space, hence requiring multiple daily administrations. Here, we sought to increase the preocular retention of dorzolamide using nanostructured, mucoadhesive micropart...
Source: International Journal of Pharmaceutics - March 7, 2017 Category: Drugs & Pharmacology Source Type: research

Mathematical model to analyze the dissolution behavior of metastable crystals or amorphous drug accompanied with a solid-liquid interface reaction
In this study, a novel mathematical model that can represent the dissolution behavior of the solid-liquid interface reaction for metastable crystals or amorphous drug was developed and its validity was evaluated. The theory for this model was based on the Noyes-Whitney equation and assumes that the precipitation of stable crystals at the solid-liquid interface occurs through a first-order reaction. Moreover, two models were developed, one assuming that the surface area of the drug remains constant because of the presence of excess drug in the bulk and the other that the surface area changes in time-dependency because of ag...
Source: International Journal of Pharmaceutics - March 7, 2017 Category: Drugs & Pharmacology Source Type: research

Evaluation of a dynamic dissolution/permeation model: Mutual influence of dissolution and barrier-flux under non-steady state conditions
Publication date: 30 April 2017 Source:International Journal of Pharmaceutics, Volume 522, Issues 1–2 Author(s): Daniel Sironi, Mette Christensen, Jörg Rosenberg, Annette Bauer-Brandl, Martin Brandl Combined dissolution/permeation testing is gaining increasing attention as an in vitro tool for predictive performance ranking of enabling oral formulations. The current aim was to study how in vitro drug permeation evolves under conditions, where the donor concentration is changing (non-steady state). To this end, a model case was construed: compacts of pure crystalline hydrocortisone methanolate (HC·MeOH) o...
Source: International Journal of Pharmaceutics - March 7, 2017 Category: Drugs & Pharmacology Source Type: research

Triphenylphosphonium-modified poly(ethylene glycol)-poly( ε-caprolactone) micelles for mitochondria- targeted gambogic acid delivery
In conclusion, the GA-TPP micelle system shows great promise for lung cancer treatment by inducing an apoptotic effect via the mitochondrial signaling pathway. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - March 6, 2017 Category: Drugs & Pharmacology Source Type: research

Cell based therapeutics in type 1 diabetes mellitus
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Fernanda Zamboni, Maurice N. Collins This review focuses on Type 1 diabetes mellitus (T1DM) and the role of bioengineering, nanotechnology and cell therapy in its treatment. T1DM is discussed in terms of its prevalence as well as the role of the extra cellular matrix (ECM) of the pancreas in its development and mode of action. Surface engineering strategies and the chemistries behind important cell encapsulation techniques, which are emerging from recent research in immunosuppression, are described. Key e...
Source: International Journal of Pharmaceutics - March 5, 2017 Category: Drugs & Pharmacology Source Type: research

Powder properties and compaction parameters that influence punch sticking propensity of pharmaceuticals
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Shubhajit Paul, Lisa J. Taylor, Brendan Murphy, Joseph F. Krzyzaniak, Neil Dawson, Matthew P. Mullarney, Paul Meenan, Changquan Calvin Sun Punch sticking is a frequently occurring problem that challenges successful tablet manufacturing. A mechanistic understanding of the punch sticking phenomenon facilitates the design of effective strategies to solve punch sticking problems of a drug. The first step in this effort is to identify process parameters and particle properties that can profoundly affect sticki...
Source: International Journal of Pharmaceutics - March 5, 2017 Category: Drugs & Pharmacology Source Type: research

Development of an inducible platform for intercellular protein delivery
Publication date: 30 April 2017 Source:International Journal of Pharmaceutics, Volume 522, Issues 1–2 Author(s): Richard Siller, Eric Dufour, Max Lycke, Ian Wilmut, Yong-Wook Jung, In Hyun Park, Gareth J. Sullivan A challenge to protein based therapies is the ability to produce biologically active proteins and their ensured delivery. Various approaches have been utilised including fusion of protein transduction domains with a protein or biomolecule of interest. A compounding issue is lack of specificity, efficiency and indeed whether the protein fusions are actually translocated into the cell and not merely an artef...
Source: International Journal of Pharmaceutics - March 5, 2017 Category: Drugs & Pharmacology Source Type: research

Development of advanced biantibiotic loaded bone cement spacers for arthroplasty associated infections
Publication date: 30 April 2017 Source:International Journal of Pharmaceutics, Volume 522, Issues 1–2 Author(s): F.J. Parra-Ruíz, A. González-Gómez, M. Fernández-Gutiérrez, J. Parra, J. García-García, G. Azuara, B. De la Torre, J. Buján, B. Ibarra, L. Duocastella-Codina, M. Molina-Crisol, B. Vázquez-Lasa, J. San Román The incidence increase of infections in patients with hip or knee implants with resistant pathogens (mainly some S. coagulase-negative and gram positive bacteria) demands advanced antibiotic loaded formulations. In this paper, we rep...
Source: International Journal of Pharmaceutics - March 5, 2017 Category: Drugs & Pharmacology Source Type: research

Ligand peptide-grafted PEGylated liposomes using HER2 targeted peptide-lipid derivatives for targeted delivery in breast cancer cells: The effect of serine-glycine repeated peptides as a spacer
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Tadaharu Suga, Yuki Fuchigami, Masayori Hagimori, Shigeru Kawakami Ligand peptide-grafted PEGylated liposomes have been widely studied for targeted drug delivery systems. Because ligand peptides are commonly grafted using PEG as a spacer on the surface of PEGylated liposomes, the interaction between ligand peptides and their corresponding receptors can be interrupted by steric hindrance of the PEG layer. Therefore, we aimed to develop ligand peptide-lipid derivatives to enhance the targeting efficiency of...
Source: International Journal of Pharmaceutics - March 1, 2017 Category: Drugs & Pharmacology Source Type: research

One-week in vivo sustained release of a peptide formulated into in situ forming implants
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Marianne Parent, Igor Clarot, Sébastien Gibot, Marc Derive, Philippe Maincent, Pierre Leroy, Ariane Boudier The LR12 peptide has been reported to reduce the size of infarct and improve both cardiac function and survival in myocardial infarction in murine models, after daily repeated intraperitoneal injections. In order to protect peptide from degrading and to prolong its release, in situ implants based on biocompatible biodegradable polymers were prepared and both in vitro and in vivo releases were...
Source: International Journal of Pharmaceutics - March 1, 2017 Category: Drugs & Pharmacology Source Type: research

High-throughput screening and scale-up of cocrystals using resonant acoustic mixing
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Karthik Nagapudi, Evelyn Yanez Umanzor, Colin Masui This paper explores the effectiveness of resonant acoustic mixing RAM for screening and scale up of cocrystals. 16 cocrystal systems were selected as test cases based on previous literature precedent. A 96 well plate set up in conjunction with zirconia beads was used for cocrystal screening using RAM. A success rate of 80% was obtained in the screen for plates containing solvent or solvent plus Zirconia beads. A proof of concept production of hydrated an...
Source: International Journal of Pharmaceutics - March 1, 2017 Category: Drugs & Pharmacology Source Type: research

New gonadotropin-releasing hormone glycolipids with direct antiproliferative activity and gonadotropin-releasing potency
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Pegah Varamini, Friederike M. Mansfeld, Ashwini Kumar Giddam, Frederik Steyn, Istvan TothGraphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - March 1, 2017 Category: Drugs & Pharmacology Source Type: research

Design of novel injectable in-situ forming scaffolds for non-surgical treatment of periapical lesions: In-vitro and in-vivo evaluation
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Rehab N. Shamma, Nermeen A. Elkasabgy, Azza A. Mahmoud, Shaimaa I. Gawdat, Mohamed M. Kataia, Mohamed A. Abdel Hamid Periapical lesions are considered one of the common pathological conditions affecting alveolar bone. The primary focus of this study was to investigate the effectiveness of formulating an injectable in-situ forming scaffold-loaded with risedronate (bone resorption inhibitor) and with lornoxicam (anti-inflammatory drug) for the non-surgical treatment of periapical lesions. The scaffolds were...
Source: International Journal of Pharmaceutics - February 28, 2017 Category: Drugs & Pharmacology Source Type: research

Physical key properties of antibiotic-free, PLGA/HPMC-based in-situ forming implants for local periodontitis treatment
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): K. Agossa, M. Lizambard, T. Rongthong, E. Delcourt-Debruyne, J. Siepmann, F. Siepmann In-situ forming implants (ISFI) offer an interesting potential for the treatment of periodontitis, allowing for time-controlled drug release directly at the site of action (which is difficult to reach). For this purpose, ISFI loaded with antibiotics have been reported in the literature. But the use of antibiotic drugs at low doses over prolonged periods of time can lead to the development of bacterial resistances. This r...
Source: International Journal of Pharmaceutics - February 28, 2017 Category: Drugs & Pharmacology Source Type: research

Computational fluid dynamics (CFD) studies of a miniaturized dissolution system
In this study we used computational fluid dynamics to simulate and investigate the hydrodynamics in a novel miniaturized dissolution method for parenteral formulations. The dissolution method is based on a rotating disc system and uses a rotating sample reservoir which is separated from the remaining dissolution medium by a nylon screen. Sample reservoirs of two sizes were investigated (SR6 and SR8) and the hydrodynamic studies were performed at rotation rates of 100, 200 and 400rpm. The overall fluid flow was similar for all investigated cases, with a lateral upward spiraling motion and central downward motion in the form...
Source: International Journal of Pharmaceutics - February 26, 2017 Category: Drugs & Pharmacology Source Type: research

Patients ’ appropriateness, acceptability, usability and preferences for pharmaceutical preparations: Results from a literature review on clinical evidence
In conclusion, more interdisciplinary scientific efforts are required to develop and increase research in understanding patient needs and preferences. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 26, 2017 Category: Drugs & Pharmacology Source Type: research

Application of halloysite clay nanotubes as a pharmaceutical excipient
This study reports the development composite tablets based on 50wt.% of the drug loaded halloysite mixed with 45wt.% of microcrystalline cellulose. Powder flow and compressibility properties of halloysite (angle of repose, Carr’s index, Hausner ratio, Brittle Fracture Index, tensile strength) indicate that halloysite is an excellent tablet excipient. Halloysite tubes can also be filled with nifedipine with ca. 6wt.% loading efficiency and sustained release from the nanotubes. Tablets prepared with drug loaded halloysite allowed for almost zero order nifedipine release for up to 20h. Nifedipine trapped in the nanotube...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

Cytotoxicity of polycations: Relationship of molecular weight and the hydrolytic theory of the mechanism of toxicity
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Bryn D. Monnery, Michael Wright, Rachel Cavill, Richard Hoogenboom, Sunil Shaunak, Joachim H.G. Steinke, Maya Thanou The mechanism of polycation cytotoxicity and the relationship to polymer molecular weight is poorly understood. To gain an insight into this important phenomenon a range of newly synthesised uniform (near monodisperse) linear polyethylenimines, commercially available poly(l-lysine)s and two commonly used PEI-based transfectants (broad 22kDa linear and 25kDa branched) were tested for their c...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

Modulation mechanism of the stratum corneum structure during permeation of surfactant-based rigid and elastic vesicles
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Tomonobu Uchino, Ichiro Hatta, Yasunori Miyazaki, Tomoya Onai, Takuto Yamazaki, Fuyoko Sugiura, Yoshiyuki Kagawa We evaluated the interaction between human stratum corneum (SC) and surfactant-based rigid or elastic vesicles during permeation using synchrotron X-ray diffraction to obtain the mechanism action of surfactant-based vesicles for enhanced skin permeation. The effects of vesicle elasticity on the interaction with SC were also investigated. Changes in the small-angle X-ray diffraction peaks of the...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

Improving the dissolution rate of hydrophobic drugs through encapsulation in porous lactose as a new biocompatible porous carrier
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Amirali Ebrahimi, Morteza Saffari, Timothy Langrish T he dissolution rates of indomethacin (IMC) and nifedipine (NIF) as poorly water-soluble model drugs have been significantly improved by encapsulating their molecules in the porous structure of engineered-particles of lactose as a new biocompatible porous carrier. The formulation method used in this study utilized a template-based spray-drying technique for in-situ production of porous lactose followed by two solvent-based drug-loading methods: (i) adso...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

In situ hybrid nano drug delivery system (IHN-DDS) of antiretroviral drug for simultaneous targeting to multiple viral reservoirs: An in vivo proof of concept
In conclusion, IHN-DDS systems could be a promising approach for simultaneous multisite targeting and could provide therapeutic benefits in complete eradication of HIV infections. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

In situ determination of the saturation solubility of nanocrystals of poorly soluble drugs for dermal application
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Miriam Colombo, Sven Staufenbiel, Eckart Rühl, Roland Bodmeier The aim of this study was to determine, in situ, the saturation solubility and dissolution rate of nanocrystals of three poorly water-soluble drugs for dermal application. The nanocrystals were prepared by wet bead milling. Their size could be controlled by various process parameters. The saturation solubility was measured in water or in the presence of surfactant at 32°C with a Sirius® inForm based on in situ UV–vis spectro...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

An equation for the prediction of human skin permeability of neutral molecules, ions and ionic species
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Keda Zhang, Michael H. Abraham, Xiangli Liu Experimental values of permeability coefficients, as log Kp, of chemical compounds across human skin were collected by carefully screening the literature, and adjusted to 37°C for the effect of temperature. The values of log Kp for partially ionized acids and bases were separated into those for their neutral and ionic species, forming a total data set of 247 compounds and species (including 35 ionic species). The obtained log Kp values have been regressed ag...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

Improving the dissolution properties of curcumin using dense gas antisolvent technology
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Firman Kurniawansyah, Lisa Quachie, Raffaella Mammucari, Neil R. Foster The dissolution properties of curcumin are notoriously poor and hinder its bioavailability. To improve its dissolution properties, curcumin has been formulated with methyl-β-cyclodextrin and polyvinylpyrrolidone by the atomized rapid injection solvent extraction (ARISE) system. The compounds were co-precipitated from organic solutions using carbon dioxide at 30°C and 95bar as the antisolvent. Curcumin formulations were also p...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

Influence of preparation pathway on the glass forming ability
This study investigates the correlation of the GFA between these two pathways. Eighteen compounds were chosen and their GFA was investigated by determining the critical cooling rate and the minimal milling time. It was observed that drugs, which turned amorphous upon cooling from the melt at slow cooling rates also had a low minimal milling time and vice versa. It was found that the GFA of the studied set of drugs was inherent and independent of the preparation method. It can be concluded that a drug with low critical cooling rate will also have a low minimal milling time and is thus a good glass former. Graphical abstract...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

Laser deposition of poly(3-hydroxybutyric acid-co-3-hydroxyvaleric acid) – lysozyme microspheres based coatings with anti-microbial properties
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): V. Grumezescu, A.M. Holban, L.E. Sima, M.B. Chiritoiu, G.N. Chiritoiu, A.M. Grumezescu, L. Ivan, F. Safciuc, F. Antohe, C. Florica, C.R. Luculescu, M.C. Chifiriuc, G. Socol The purpose of this study was to obtain, characterize and evaluate the cytotoxicity and antimicrobial activity of coatings based on poly(3-hydroxybutyric acid-co-3-hydroxyvaleric acid) – Lysozyme (P(3HB-3HV)/Lys) and P(3HB-3HV) – Polyethylene glycol – Lysozyme (P(3HB-3HV)/PEG/Lys) spheres prepared by Matrix Assisted P...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

Parameters affecting the transscleral delivery of two positively charged proteins of comparable size
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Maria Aurora Grimaudo, Elena Tratta, Silvia Pescina, Cristina Padula, Patrizia Santi, Sara Nicoli Apart from molecular weight and net surface charge, there are other macromolecule-related factors that could, in principle, influence their diffusion across biological tissues, such as shape, conformability, water solubility and surface charge distribution. Lysozyme and cytochrome c, proteins with comparable molecular weight, isoelectric point and net surface charge in physiological conditions (approx. +7.8),...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

Potential of single cationic amino acid molecule “Arginine” for stimulating oral absorption of insulin
In this study, we found that arginine is a key cationic amino acid for delivering insulin across intestinal epithelial barriers and hopefully accelerating the clinical development of oral insulin delivery systems. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

Exosomes as novel bio-carriers for gene and drug delivery
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Xin-Chi Jiang, Jian-Qing Gao Clinical treatments have stalled in certain diseases due to a lack of proper therapeutic delivery systems. Recent studies have identified exosomes for their potential use as cell-free therapies, which may provide a novel mechanism for solving this problem. Exosomes are nanoscale extracellular vesicles that can transport rich cargos of proteins, lipids, DNA, and RNA. It is increasingly recognized that exosomes play a complex role in not only the physiological conditions but als...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

Increased intestinal permeation and modulation of presystemic metabolism of resveratrol formulated into self-emulsifying drug delivery systems
In conclusion, our data suggests that oil-in-water nanoemulsions prepared from SEDDS dispersions of medium-chain lipids could be promising formulations for enhancing oral delivery of resveratrol. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 23, 2017 Category: Drugs & Pharmacology Source Type: research

Non-viral vectors based on magnetoplexes, lipoplexes and polyplexes for VEGF gene delivery into central nervous system cells
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Ilia Villate-Beitia, Gustavo Puras, Cristina Soto-Sánchez, Mireia Agirre, Edilberto Ojeda, Jon Zarate, Eduardo Fernández, José Luis Pedraz Nanotechnology based non-viral vectors hold great promise to deliver therapeutic genes into the central nervous system (CNS) in a safe and controlled way. Vascular endothelial growth factor (VEGF) is a potential therapeutic gene candidate for CNS disorders due to its specific roles in brain angiogenesis and neuroprotection. In this work, we elabora...
Source: International Journal of Pharmaceutics - February 23, 2017 Category: Drugs & Pharmacology Source Type: research

PEGylation prolongs the pulmonary retention of an anti-IL-17A Fab ’ antibody fragment after pulmonary delivery in three different species
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Danielle Freches, Harshad P. Patil, Maria Machado Franco, Catherine Uyttenhove, Sam Heywood, Rita Vanbever The PEGylation of antibody fragments has been shown to greatly prolong their residence time in the lungs in mice. The purpose of this research was to confirm the effect of PEGylation in higher animal species, that is, the rat and the rabbit. An anti-IL-17A Fab’ antibody fragment was conjugated to a two-armed 40kDa polyethylene glycol (PEG) via site-selective thiol PEGylation. PEGylation did not...
Source: International Journal of Pharmaceutics - February 23, 2017 Category: Drugs & Pharmacology Source Type: research

Effects of storage conditions on the stability of spray dried, inhalable bacteriophage powders
This study aimed to develop inhalable powders containing phages active against antibiotic-resistant Pseudomonas aeruginosa for pulmonary delivery. A Pseudomonas phage, PEV2, was spray dried into powder matrices comprising of trehalose (0–80%), mannitol (0–80%) and l-leucine (20%). The resulting powders were stored at various relative humidity (RH) conditions (0, 22 and 60% RH) at 4°C. The phage stability and in vitro aerosol performance of the phage powders were examined at the time of production and after 1, 3 and 12 months storage. After spray drying, a total of 1.3 log titer reduction in phage was observ...
Source: International Journal of Pharmaceutics - February 23, 2017 Category: Drugs & Pharmacology Source Type: research

Design and evaluation of antibiotic releasing self- assembled scaffolds at room temperature using biodegradable polymer particles
Publication date: 30 March 2017 Source:International Journal of Pharmaceutics, Volume 520, Issues 1–2 Author(s): Prasad Admane, Jatin Gupta, Ancy I.J., Robin Kumar, Amulya K. Panda Biodegradable polymer-based drug-eluting implants offer many advantages such as predictable drug release kinetics, safety, and acceptable drug loading under ambient conditions. Herein, we describe fabrication and evaluation of antibiotic loaded scaffolds for localized delivery and tissue engineering applications. PDLLA particles entrapping gentamycin were formulated using solvent evaporation method and used for scaffold fabrication. Optim...
Source: International Journal of Pharmaceutics - February 20, 2017 Category: Drugs & Pharmacology Source Type: research

Multiwalled carbon nanotubes for drug delivery: Efficiency related to length and incubation time
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Niccolò Sciortino, Stefano Fedeli, Paolo Paoli, Alberto Brandi, Paola Chiarugi, Mirko Severi, Stefano Cicchi Batches of oxidized multiwalled carbon nanotubes differing in length were adopted to prepare two drug delivery systems (DDS) loaded with doxorubicin. The different internalization of the two batches, verified by atomic emission spectroscopy onto cell lysates, was also confirmed by the different toxicity of the same DDS loaded with doxorubicin. In vitro experiments evidenced, after 48h of inc...
Source: International Journal of Pharmaceutics - February 20, 2017 Category: Drugs & Pharmacology Source Type: research