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Improved control over MSCs behavior within 3D matrices by using different cell loads in both in vitro and in vivo environments
In conclusion, these results demonstrate how the final outcome of a cell-based drug delivery system may be tuned by just modifying the initial cell load, always taking into account the surrounding microenvironment. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 28, 2017 Category: Drugs & Pharmacology Source Type: research

Application of feedback control and in situ milling to improve particle size and shape in the crystallization of a slow growing needle-like active pharmaceutical ingredient
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): Yang Yang, Kanjakha Pal, Andy Koswara, Qingqing Sun, Yuqi Zhang, Justin Quon, Rahn McKeown, Charles Goss, Zoltan K. Nagy Control of crystal size and shape is crucially important for crystallization process development in the pharmaceutical industries. In general crystals of large size and low aspect ratio are desired for improved downstream manufacturability. It can be extremely challenging to design crystallization processes that achieve these targets for active pharmaceutical ingredients (APIs) that have very...
Source: International Journal of Pharmaceutics - September 27, 2017 Category: Drugs & Pharmacology Source Type: research

Host –guest interaction and structural ordering in polymeric nanoassemblies: Influence of molecular design
This study, centered on the influence of the molecular design on the host–guest interactions and structural ordering in polymeric nanoassemblies, will help to tailor host–guest nanoassemblies with attractive drug delivery profiles. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 26, 2017 Category: Drugs & Pharmacology Source Type: research

Cyclodextrin-based metal-organic frameworks particles as efficient carriers for lansoprazole: Study of morphology and chemical composition of individual particles
Publication date: 15 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 2 Author(s): Xue Li, Tao Guo, Laurent Lachmanski, Francesco Manoli, Mario Menendez-Miranda, Ilse Manet, Zhen Guo, Li Wu, Jiwen Zhang, Ruxandra Gref Cyclodextrin-based metal-organic frameworks (CD-MOFs) represent an environment-friendly and biocompatible class of MOFs drawing increasing attention in drug delivery. Lansoprazole (LPZ) is a proton-pump inhibitor used to reduce the production of acid in the stomach and recently identified as an antitubercular prodrug. Herein, LPZ loaded CD-MOFs were successfully synthesized upon ...
Source: International Journal of Pharmaceutics - September 26, 2017 Category: Drugs & Pharmacology Source Type: research

Cyclodextrins and topical drug delivery to the anterior and posterior segments of the eye
Publication date: 15 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 2 Author(s): Thorsteinn Loftsson, Einar Stefánsson It is generally believed that it is virtually impossible to obtain therapeutic drug concentrations in the posterior segment of the eye after topical application of aqueous, low viscosity eye drops. Thus, intravitreal drug injections and drug implants are currently used to treat diseases in the posterior segment such as macular edema. Here it is described how, through proper analysis of the drug permeation barriers and application of well-known pharmaceutical excipient...
Source: International Journal of Pharmaceutics - September 26, 2017 Category: Drugs & Pharmacology Source Type: research

Editorial Special edition of International Journal of Pharmaceutics in honor of Professor Dominique Duch êne
Publication date: 15 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 2 Author(s): Ruxandra Gref, Patrick Couvreur, Thorsteinn Loftsson (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 26, 2017 Category: Drugs & Pharmacology Source Type: research

Preparation and investigation of P28GST-loaded PLGA microparticles for immunomodulation of experimental colitis
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): T.H. Hoang Thi, P.A. Priemel, Y. Karrout, V. Driss, M. Delbeke, A. Dendooven, M.P. Flament, M. Capron, J. Siepmann The aim of this work was to prepare and characterize (in vitro and in vivo) PLGA-based microparticles loaded with an enzymatic protein derived from the helminth parasite Schistosoma haematobium: glutathione S-transferase P28GST (P28GST). This protein is not only a promising candidate vaccine against schistosomiasis, it also exhibits interesting immunomodulating effects, which can be helpful for the...
Source: International Journal of Pharmaceutics - September 25, 2017 Category: Drugs & Pharmacology Source Type: research

Kaolinite in pharmaceutics and biomedicine
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): Mahmoud E. Awad, Alberto López-Galindo, Massimo Setti, Mahmoud M. El-Rahmany, César Viseras Iborra Kaolinite Al2Si2O5(OH)4 is an abundant and inexpensive geomaterial regarded as one of the most common clay minerals in the earth's crust and the most widespread phase among the other kaolin polymorphs (halloysite, dickite and nacrite). Structurally, it is a hydrous aluminum phyllosilicate member belonging to the dioctahedral 1:1 kaolin mineral group. The particle size of the pseudohexagonal kaolinite...
Source: International Journal of Pharmaceutics - September 25, 2017 Category: Drugs & Pharmacology Source Type: research

Design and pharmaceutical applications of a low-flow-rate single-nozzle impactor
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): Hui Wang, Pallavi Bhambri, James Ivey, Reinhard Vehring A new low-flow-rate (0.5L/min) single-nozzle impactor for the concentration of dilute aerosol particles with selected pharmaceutical applications is described in this paper. The impactor can be configured up to 11 stages with a wide range of cutoff diameters from 0.6μm to 21.1μm, enabling convenient sampling of inhalable drug particles from inhalation devices and drug production processes. Its unique single-nozzle design and removable impaction plate...
Source: International Journal of Pharmaceutics - September 24, 2017 Category: Drugs & Pharmacology Source Type: research

Levetiracetam+nonsteroidal anti-inflammatory drug binary systems: A contribution to the development of new solid dosage forms
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): Sara M.T. Machado, Ricardo A.E. Castro, Teresa M.R. Maria, João Canotilho, M. Ermelinda S. Eusébio A study has been carried out of binary solid systems made up of the antiepileptic drug levetiracetam, LEV, and a nonsteroidal anti-inflammatory drug, NSAID, capable of managing the inflammation that accompanies epileptic activity. One aim of this research was to identify eutectic mixtures and co-crystals, which are able to impact positively on their biopharmaceutical properties. The NSAIDs studied ar...
Source: International Journal of Pharmaceutics - September 24, 2017 Category: Drugs & Pharmacology Source Type: research

Folate-targeted amphiphilic cyclodextrin nanoparticles incorporating a fusogenic peptide deliver therapeutic siRNA and inhibit the invasive capacity of 3D prostate cancer tumours
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): James C. Evans, Meenakshi Malhotra, Katrina Sweeney, Raphael Darcy, Colleen C. Nelson, Brett G. Hollier, Caitriona M. O’Driscoll The main barrier to the development of an effective RNA interference (RNAi) therapy is the lack of a suitable delivery vector. Modified cyclodextrins have emerged in recent years for the delivery of siRNA. In the present study, a folate-targeted amphiphilic cyclodextrin was formulated using DSPE-PEG5000-folate to target prostate cancer cells. The fusogenic peptide GALA was includ...
Source: International Journal of Pharmaceutics - September 22, 2017 Category: Drugs & Pharmacology Source Type: research

Modeling drug release through stimuli responsive polymer hydrogels
We present a mathematical model that couples Nernst–Planck, Poisson and force balance equations to incorporate diffusion of ionic species and drug along with deformation of hydrogel under osmotic pressure. The model can be used to simulate swelling behaviour of the hydrogel along with the kinetics of drug release. It has been validated with published experimental data for swelling of polyhydroxyl methacrylate-co-methacrylic acid (pHEMA-co-MA) gels and release kinetics of Phenylpropanolamine from these gels. Effect of formulation parameters such as polymer concentration and cross-linker concentration has also been eva...
Source: International Journal of Pharmaceutics - September 22, 2017 Category: Drugs & Pharmacology Source Type: research

Synthesis and preparation of biodegradable hybrid dextran hydrogel incorporated with biodegradable curcumin nanomicelles for full thickness wound healing
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Mona Alibolandi, Marzieh Mohammadi, Seyed Mohammad Taghdisi, Khalil Abnous, Mohammad Ramezani There is a clinical need for a novel, more efficient therapy for full thickness wound healing. In the current study, curcumin encapsulated PEG-PLA [poly(lactide)-block-poly(ethylene glycol)] nanomicelles were incorporated into dextran hydrogel for a full thickness dermal wound healing application. To assess the application of the hydrogel as a therapeutic wound dressing, its morphology, swelling pattern, kinetics of deg...
Source: International Journal of Pharmaceutics - September 21, 2017 Category: Drugs & Pharmacology Source Type: research

Leachable diphenylguanidine from rubber closures used in pre-filled syringes: A case study to understand solid and solution interactions with oxytocin
This study investigated the mechanism and kinetics of this interaction in both solid and solution states through in-vitro tests and spectroscopic methods For solid state interaction, the protein-adducts with DPG were characterized using SEM, XRD, DSC, FTIR, 13C ss NMR, and dissolution analysis. For solution state interaction, LC–HRMS was used to assess stability of Oxytocin solutions in presence of various concentrations of DPG at 25°C and 40°C for 4 weeks. Moreover, molecular docking analysis was used to identify possible molecular configurations of the interaction.Results were consistent with the formation ...
Source: International Journal of Pharmaceutics - September 21, 2017 Category: Drugs & Pharmacology Source Type: research

Reconstitutable spray dried ultra-fine dispersion as a robust platform for effective oral delivery of an antihyperlipidemic drug
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Mona Basha, Alaa H. Salama, Sally El Awdan The current article highlights the application of spray drying technique to produce an ultra-fine powder encapsulating the antihyperlipidemic drug, atorvastatin calcium (ATV). First, ATV was dissolved in an emulsion formulation, and different carriers (pectin, alginate, chitosan HCl and hydroxypropylmethyl cellulose) in two concentrations (1.5 and 3%) were added. Then, these carrier-containing formulations were subjected to spray drying, whereby ultra-fine ATV-loaded sp...
Source: International Journal of Pharmaceutics - September 21, 2017 Category: Drugs & Pharmacology Source Type: research

Glycerosomes: Investigation of role of 1,2-dimyristoyl-sn-glycero-3-phosphatidycholine (DMPC) on the assembling and skin delivery performances
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Maria Letizia Manca, Maria Manconi, Marco Zaru, Donatella Valenti, Jose Esteban Peris, Pietro Matricardi, Anna Maria Maccioni, Anna Maria Fadda Glycerosomes were formulated using 1,2-dimyristoyl-sn-glycero-3-phosphatidycholine (DMPC), diclofenac sodium salt and 10, 20 or 30% glycerol in the water phase, while corresponding liposomes were prepared with the same amount of DMPC and diclofenac, without glycerol. The aim of the present work was to evaluate the effect of the used phospholipid on vesicle features and a...
Source: International Journal of Pharmaceutics - September 20, 2017 Category: Drugs & Pharmacology Source Type: research

Carboxymethyl chitosan/phospholipid bilayer-capped mesoporous carbon nanoparticles with pH-responsive and prolonged release properties for oral delivery of the antitumor drug, Docetaxel
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Yanzhuo Zhang, Wufu Zhu, Heran Zhang, Jin Han, Lihua Zhang, Qisi Lin, Fengwei Ai In this article, a new type of carboxymethyl chitosan/phospholipid bilayer-capped mesoporous carbon nanomatrix (CCS/PL/MC) was fabricated as a potential nano-drug delivery system. In this drug delivery system, a mesoporous carbon nanomatrix (MC) acts as the support for loading drug molecules, a positively charged phospholipid (PL) layer works as the inner shell for prolonged drug release and a negatively charged carboxymethyl chitos...
Source: International Journal of Pharmaceutics - September 20, 2017 Category: Drugs & Pharmacology Source Type: research

Solvent-responsive floating liquid crystalline-molecularly imprinted polymers for gastroretentive controlled drug release system
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Li-Ping Zhang, Xiao-Lin Wang, Qian-Qian Pang, Yan-Ping Huang, Lei Tang, Meng Chen, Zhao-Sheng Liu Liquid crystalline-molecularly imprinted polymer (LC-MIP) particles were first found to possess the floating behavior on the aqueous medium. Combined with molecular recognition, the LC-MIP was fabricated as a novel class of the controlled-release gastric retentive DDS. The LC-MIP was made using co-polymerization of methacrylic acid, 4-methyl phenyl dicyclohexyl ethylene (LC monomer with vinyl group), and ethylene gl...
Source: International Journal of Pharmaceutics - September 20, 2017 Category: Drugs & Pharmacology Source Type: research

Facile formation of co-amorphous atenolol and hydrochlorothiazide mixtures via cryogenic-milling: Enhanced physical stability, dissolution and pharmacokinetic profile
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Sakib M. Moinuddin, Sida Ruan, Yuting Huang, Qin Gao, Qin Shi, Baochang Cai, Ting Cai The development of poorly water-soluble drugs faces the risk of low bioavailability and therapeutic efficacy. The co-amorphous drug delivery system has recently gained considerable interest because it offers an alternative approach to modify properties of poorly water-soluble drugs. Herein, we developed a co-amorphous system of atenolol (ATE) and poorly water-soluble hydrochlorothiazide (HCT) by means of cryogenic milling. The ...
Source: International Journal of Pharmaceutics - September 20, 2017 Category: Drugs & Pharmacology Source Type: research

Development of novel double-decker microneedle patches for transcutaneous vaccine delivery
This study aims to develop novel double-decker MN patches which have not only high safety and efficacy but also broad applicability to various vaccine antigens. We developed two types of MN patches (PGA-MN and Nylon-MN) that are made from polyglycolic acid and Nylon-6. In pre-clinical studies, both MN patches could demonstrably deliver antigens into resected human dermal tissue, prolong antigen deposition and increase antigen-specific IgG levels after vaccination compared with conventional injections. We demonstrated both MN patches could be safely applied to human skin because no broken MNs or significant skin irritation ...
Source: International Journal of Pharmaceutics - September 20, 2017 Category: Drugs & Pharmacology Source Type: research

The influence of hydroalcoholic media on the performance of Grewia polysaccharide in sustained release tablets
This study evaluates effect of varying alcohol concentrations on theophylline release from two grades of Grewia mollis polysaccharides. X-ray microtomography showed that native polysaccharide formulation compacts were not homogenous after the mixing process resulting in its failure in swelling studies. Removal of starch from the native polysaccharide resulted in homogenous formulation compacts resistant to damage in high alcoholic media in pH 6.8 (40%v/v absolute ethanol). Destarched polymer compacts had a significantly higher hardness (375N) than that of the native polysaccharide (82N) and HPMC K4M (146N). Dissolution stu...
Source: International Journal of Pharmaceutics - September 20, 2017 Category: Drugs & Pharmacology Source Type: research

The in vivo transformation and pharmacokinetic properties of a liquid crystalline drug delivery system
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Andrew Otte, Yahira M. Báez-Santos, Ellina A. Mun, Bong-Kwan Soh, Young-nam Lee, Kinam Park A liquid crystalline (LC) system, composed of phosphatidylcholine, sorbitan monoleate, and tocopherol acetate, was investigated to understand the in vivo transformation after subcutaneous injection, coupled with the physicochemical and pharmacokinetic properties of the formulation. The rat model was utilized to monitor a pseudo-time course transformation from a precursor LC formulation to the LC matrix, coupled wit...
Source: International Journal of Pharmaceutics - September 20, 2017 Category: Drugs & Pharmacology Source Type: research

Effect of the pulmonary deposition and in vitro permeability on the prediction of plasma levels of inhaled budesonide formulation
This study aims to assess the efficiency of simulation by applying experimental permeability and deposition values, using budesonide as a model substance. The lung deposition values were obtained from the literature, the lung permeability data were experimentally determined by culturing Calu-3 cells under air-liquid interface and submersed conditions to morphologically resemble bronchial and alveolar epithelial cells, respectively. A two-compartment PK model was created for i.v. administration and used as a background for the in silico simulation of the plasma profile of budesonide after inhalation. The predicted plasma pr...
Source: International Journal of Pharmaceutics - September 16, 2017 Category: Drugs & Pharmacology Source Type: research

Spray drying of poorly soluble drugs from aqueous arginine solution
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Rami Ojarinta, Louise Lerminiaux, Riikka Laitinen Co-amorphous drug-amino acid mixtures have shown potential for improving the solid-state stability and dissolution behavior of amorphous drugs. In previous studies, however these mixtures have been produced mainly with small-scale preparation methods, or with methods that have required the use of organic solvents or other dissolution enhancers. In the present study, co-amorphous ibuprofen-arginine and indomethacin-arginine mixtures were spray dried from water. Th...
Source: International Journal of Pharmaceutics - September 15, 2017 Category: Drugs & Pharmacology Source Type: research

Modeling of the burst release from PLGA micro- and nanoparticles as function of physicochemical parameters and formulation characteristics
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Cristiana Rodrigues de Azevedo, Moritz von Stosch, Mariana S. Costa, A.M. Ramos, M. Margarida Cardoso, Fabienne Danhier, Véronique Préat, Rui Oliveira A substantial drug release from poly(lactic-co-glycolic) acid (PLGA) micro- and nanoparticles can occur in the first hours of immersion, which is referred to as burst release. A strong burst release (when not intentional) is to be avoided as it decreases the efficacy of the treatment and could be dangerous to the host. In this work we analyze the tot...
Source: International Journal of Pharmaceutics - September 15, 2017 Category: Drugs & Pharmacology Source Type: research

Particle interactions of fluticasone propionate and salmeterol xinafoate detected with single particle aerosol mass spectrometry (SPAMS)
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Martin W. Jetzer, Bradley D. Morrical, David P. Fergenson, Georgios Imanidis Particle co-associations between the active pharmaceutical ingredients fluticasone propionate and salmeterol xinafoate were examined in dry powder inhaled (DPI) and metered dose inhaled (MDI) combination products. Single Particle Aerosol Mass Spectrometry was used to investigate the particle interactions in Advair Diskus® (500/50 mcg) and Seretide® (125/25 mcg). A simple rules tree was used to identify each compound, either alon...
Source: International Journal of Pharmaceutics - September 15, 2017 Category: Drugs & Pharmacology Source Type: research

Fabrication of drug-loaded hydrogels with stereolithographic 3D printing
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Pamela Robles Martinez, Alvaro Goyanes, Abdul W. Basit, Simon Gaisford 3D printing (3DP) technologies have been attracting much recent interest as new methods of fabricating medicines and medical devices. Of the many types of 3DP available, stereolithographic (SLA) printing offers the unique advantage of being able to fabricate objects by cross-linking resins to form networked polymer matrices. Because water can be entrapped in these matrices, it is possible in principle to fabricate pre-wetted, drug-loaded hydr...
Source: International Journal of Pharmaceutics - September 15, 2017 Category: Drugs & Pharmacology Source Type: research

Spray drying of silica microparticles for sustained release application with a new sol-gel precursor
In conclusion, the new precursor TMEOS presents a promising alternative sol-gel technology based carrier material for sustained release application of high molecular weight biopharmaceutical drugs. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 15, 2017 Category: Drugs & Pharmacology Source Type: research

Nanofibrillar cellulose hydrogels and reconstructed hydrogels as matrices for controlled drug release
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Heli Paukkonen, Mikko Kunnari, Patrick Laurén, Tiina Hakkarainen, Vili-Veli Auvinen, Timo Oksanen, Raili Koivuniemi, Marjo Yliperttula, Timo Laaksonen Concentrated 3% and 6.5% anionic nanofibrillar cellulose (ANFC) hydrogels were introduced as matrix reservoirs for controlled delivery applications of small molecules and proteins. A further aim was to study how the freeze-drying and subsequent rehydration of ANFC hydrogel affects the rheological properties and drug release of selected model compounds from ...
Source: International Journal of Pharmaceutics - September 15, 2017 Category: Drugs & Pharmacology Source Type: research

Levofloxacin-loaded bone cement delivery system: Highly effective against intracellular bacteria and Staphylococcus aureus biofilms
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Magda Ferreira, Olena Rzhepishevska, Liliana Grenho, Danila Malheiros, Lídia Gonçalves, António J. Almeida, Luisa Jordão, Isabel A. Ribeiro, Madeleine Ramstedt, Pedro Gomes, Ana Bettencourt Staphylococcus aureus is a major pathogen in bone associated infections due to its ability to adhere and form biofilms on bone and/or implants. Moreover, recrudescent and chronic infections have been associated with S. aureus capacity to invade and persist within osteoblast cells. With the growing ...
Source: International Journal of Pharmaceutics - September 15, 2017 Category: Drugs & Pharmacology Source Type: research

Simple nanophotosensitizer fabrication using water-soluble chitosan for photodynamic therapy in gastrointestinal cancer cells
In this study, water-soluble chitosan (WSC) was used to fabricate Ce6-incorporated nanophotosensitizers (Abbreviated as ChitoCe6 nanophotosensitizer) via a self-assembling process. This was accomplished by dissolving WSC in pure water and then directly mixing the solution with solid Ce6 causing ion complex formation between WSC and Ce6. The resulting nanophotosensitizer was spherical in shape and had a particle size of less than 300nm. The photodynamic effect of ChitoCe6 nanophotosensitizer was evaluated using gastrointestinal (GI) cancer cells. At in vitro study using SNU478 cholangiocarcinoma cells, ChitoCe6 nanophotosen...
Source: International Journal of Pharmaceutics - September 15, 2017 Category: Drugs & Pharmacology Source Type: research

Modelling the primary drying step for the determination of the optimal dynamic heating pad temperature in a continuous pharmaceutical freeze-drying process for unit doses
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Laurens De Meyer, Joris Lammens, Séverine Thérèse F.C. Mortier, Brecht Vanbillemont, Pieter Jan Van Bockstal, Jos Corver, Ingmar Nopens, Chris Vervaet, Thomas De Beer In the pharmaceutical industry, traditional freeze-drying of unit doses is a batch-wise process associated with many disadvantages. To overcome these disadvantages and to guarantee a uniform product quality and high process efficiency, a continuous freeze-drying process is developed and evaluated. The main differences between t...
Source: International Journal of Pharmaceutics - September 15, 2017 Category: Drugs & Pharmacology Source Type: research

Emerging technologies for the non-invasive characterization of physical-mechanical properties of tablets
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Vivek S. Dave, Hend I. Shahin, Susanne R. Youngren-Ortiz, Mahavir B. Chougule, Rahul V. Haware The density, porosity, breaking force, viscoelastic properties, and the presence or absence of any structural defects or irregularities are important physical-mechanical quality attributes of popular solid dosage forms like tablets. The irregularities associated with these attributes may influence the drug product functionality. Thus, an accurate and efficient characterization of these properties is critical for succes...
Source: International Journal of Pharmaceutics - September 15, 2017 Category: Drugs & Pharmacology Source Type: research

Polymeric micelles: Basic research to clinical practice
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Anand S. Deshmukh, Pratik N. Chauhan, Malleshappa N. Noolvi, Kiran Chaturvedi, Kuntal Ganguly, Shyam S. Shukla, Mallikarjuna N. Nadagouda, Tejraj M. Aminabhavi Rapidly developing polymeric micelles as potential targeting carriers has intensified the need for better understanding of the underlying principles related to the selection of suitable delivery materials for designing, characterizing, drug loading, improving stability, targetability, biosafety and efficacy. The emergence of advanced analytical tools such...
Source: International Journal of Pharmaceutics - September 15, 2017 Category: Drugs & Pharmacology Source Type: research

Designing lipid nanoparticles for topical ocular drug delivery
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Jesus Alvarez-Trabado, Yolanda Diebold, Alejandro Sanchez Topically-applied dosage forms, such eye drops, are the most used formulations in the treatment of ocular diseases. Nonetheless, because of the special protection of the eye associated with the ocular surface, drug bioavailability and subsequent therapeutic efficiency obtained with these conventional dosage forms are very low. Recently, novel drug delivery systems have been proposed to solve the main drawbacks of conventional formulations. Nanotechnology,...
Source: International Journal of Pharmaceutics - September 15, 2017 Category: Drugs & Pharmacology Source Type: research

Protease-functionalized mucus penetrating microparticles: In-vivo evidence for their potential
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Arshad Mahmood, Flavia Laffleur, Gintare Leonaviciute, Andreas Bernkop-Schnürch The focus of the current study was to explore whether immobilization of proteases to microparticles could result in their enhanced penetration into mucus. The proteases papain (PAP) and bromelain (BROM) were covalently attached to a polyacrylate (PAA; Carbopol 971P) via amide bond formation based on carbodiimide reaction. Microparticles containing these conjugates were generated via ionic gelation with calcium chloride and were ...
Source: International Journal of Pharmaceutics - September 12, 2017 Category: Drugs & Pharmacology Source Type: research

Erlotinib-loaded albumin nanoparticles: A novel injectable form of erlotinib and its in vivo efficacy against pancreatic adenocarcinoma ASPC-1 and PANC-1 cell lines
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): M. Noorani, N. Azarpira, K. Karimian, H. Heli Erlotinib was loaded on albumin nanoparticles for the first time and the cytotoxic effect of the resulting nanoparticles against ASPC-1 and PANC-1 pancreatic adenocarcinoma cell lines was evaluated. The carrier (albumin nanoparticles, ANPs) was synthesized by desolvation method using a mixed solvent followed by thermal crosslinking for stabilization. ANPs and the drug-loaded ANPs were characterized by field emission scanning and transmission electron microscopies, par...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Voriconazole-loaded nanostructured lipid carriers (NLC) for drug delivery in deeper regions of the nail plate
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): Kamilla Amaral David Rocha, Anna Paula Krawczyk-Santos, Lígia Marquez Andrade, Luana Clara de Souza, Ricardo Neves Marreto, Tais Gratieri, Stephânia Fleury Taveira Voriconazole-loaded nanostructured lipid carriers (VOR-NLC) were developed and drug penetration evaluated in porcine hooves in vitro. Synergistic effect of urea (Ur), selected among other known chemical enhancers according to hoof hydration potential, was also evaluated. VOR-NLC presented a high encapsulation efficiency (74.52±2.13%...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Increasing the affinity of cationized polyacrylamide-paclitaxel nanoparticles towards colon cancer cells by a surface recognition peptide
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): Sanjay Tiwari, Boaz Tirosh, Abraham Rubinstein Nanoparticles of cationized polyacrylamide (CPAA NP), decorated with the recognition peptide VRPMPLQ (to produce CPAA-Pep NP), were prepared, characterized and tested biologically. They were designed to target dysplasia regions in the colon, characterized by overexpressed sialic acid. This targetability was augmented by the addition of VRPMPLQ. Their mean hydrodynamic size was 137nm with narrow size distribution and positive zeta potential. When incubated with three ...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Nanosuspensions of a new compound, ER- β005, for enhanced oral bioavailability and improved analgesic efficacy
In conclusion, by using β-CN as a stabilizer, nanosuspensions of ER-β005 were developed and oral absorption was enhanced. Moreover, ER-β005 is a powerful drug that inhibits pain reactions, and its therapeutic efficacy was markedly increased in the Nano-ER-β005. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Antibacterial and anti-encrustation biodegradable polymer coating for urinary catheter
In this study, the strategy used to resist bacterial adhesion and encrustation represents a combination of the antibacterial effects of norfloxacin and silver nanoparticles and the PLGA-based neutralisation of alkali products of urea hydrolysis gained through the degradation of the polymer in an aqueous milieu. Silver nanoparticles were coated with tetraether lipids (TEL) to avoid aggregation when dispersed in acetone and during the film formation. The polymer films loaded with the two antibacterial agents were applied on Polyurethane (PUR) and Silicon sheets. We demonstrated the antibacterial and anti-adhesion effectivene...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Development and evaluation of long-circulating nanoparticles loaded with betulinic acid for improved anti-tumor efficacy
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): Ankit Saneja, Robin Kumar, Amarinder Singh, Ravindra Dhar Dubey, Mubashir J. Mintoo, Gurdarshan Singh, Dilip M. Mondhe, Amulya K. Panda, Prem N. Gupta The clinical application of betulinic acid (BA), a natural pentacyclic triterpenoid with promising antitumor activity, is hampered due to its extremely poor water solubility and relatively short half-life in the systemic circulation. In order to address these issues, herein, we developed betulinic acid loaded polylactide-co-glycolide- monomethoxy polyethylene glyco...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Electrospun collagen-based nanofibres: A sustainable material for improved antibiotic utilisation in tissue engineering applications
In this study, the effects of collagen type I in polylactic acid-drug electrospun scaffolds for tissue engineering applications are examined. The samples produced were subsequently characterised using a range of techniques. Scanning electron microscopy analysis shows that the fibre morphologies varied across PLA-drug and PLA-collagen-drug samples − the addition of collagen caused a decrease in average fibre diameter by nearly half, and produced nanofibres. Atomic force microscopy imaging revealed collagen-banding patterns which show the successful integration of collagen with PLA. Solid-state characterisation suggest...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Integrated hot-melt extrusion – injection molding continuous tablet manufacturing platform: Effects of critical process parameters and formulation attributes on product robustness and dimensional stability
This study provides a framework for robust tablet development using an integrated hot-melt extrusion-injection molding (IM) continuous manufacturing platform. Griseofulvin, maltodextrin, xylitol and lactose were employed as drug, carrier, plasticizer and reinforcing agent respectively. A pre-blended drug-excipient mixture was fed from a loss-in-weight feeder to a twin-screw extruder. The extrudate was subsequently injected directly into the integrated IM unit and molded into tablets. Tablets were stored in different storage conditions up to 20 weeks to monitor physical stability and were evaluated by polarized light micros...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Impact of Eudragit EPO and hydroxypropyl methylcellulose on drug release rate, supersaturation, precipitation outcome and redissolution rate of indomethacin amorphous solid dispersions
In conclusion, the concentration-time profiles achieved from indomethacin ASD dissolution are a complex interplay of drug release rate, precipitation kinetics and outcome, and precipitate redissolution rate, whereby each of these processes is highly dependent on the polymer(s) employed in the formulation. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

In vitro and in vivo release of dinalbuphine sebacate extended release formulation: Effect of the oil ratio on drug release
In this study, we found that the in vitro release profile of DNS could be affected by adjusting the weight ratio of benzyl benzoate to sesame oil (the solvent/oil ratio). A longer release period could be attained by increasing the solvent/oil ratio in the formulation. A pharmacokinetic study was conducted in beagle dogs to verify the relationship between the in vitro release and the drug release from the formulations in vivo. The pharmacokinetic study confirmed that the formulation with a higher benzyl benzoate to oil ratio exhibits a longer drug release profile with a lower maximum concentration (Cmax) and a longer time t...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Effects of crystal habit on the sticking propensity of ibuprofen —A case study
This study demonstrates the effect of active pharmaceutical ingredient (API) particle habit on the sticking propensity of ibuprofen. Four diverse crystal habits with similar physico chemical properties are reported and the sticking propensity was found to increase with shape regularity. The surface energy of the extreme habits were shown to be different where particles that were more regular in shape exhibited surface energies of 9mJ/m2 higher than those that were needle-like in habit. Computational and experimental data reveals that the increase in surface energy of the regular shaped particles can be attributed to the in...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Bilayered buccal films as child-appropriate dosage form for systemic administration of propranolol
The objective of the present study was to develop bilayered buccal films for the release of propranolol hydrochloride. A primary polymeric layer was prepared by casting and drying of solutions of film-forming polymers, such as polyvinylpyrrolidone (PVP) or polyvinylalcohol (PVA), added with different weight ratios of gelatin (GEL) or chitosan (CH). In order to achieve unidirectional drug delivery towards buccal mucosa, a secondary ethylcellulose layer was applied onto the primary layer. Bilayered films were characterized for their physico-chemical (morphology, thickness, drug content and solid state) and functional (water ...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Downstream processing from hot-melt extrusion towards tablets: A quality by design approach
This study was designed to screen the influence of process parameters and drug load during HME on both extrudate properties and tableting behaviour of an amorphous solid dispersion formulation using a quality-by-design (QbD) approach. A full factorial experimental design with 19 experiments was used to evaluate the effect of several process variables (barrel temperature: 160–200°C, screw speed: 50–200rpm, throughput: 0.2-0.5kg/h) and drug load (0–20%) as formulation parameter on the hot-melt extrusion (HME) process, extrudate and tablet quality of Soluplus®-Celecoxib amorphous solid dispersions. A...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research

Poly(glycerol adipate) – indomethacin drug conjugates – synthesis and in vitro characterization
Publication date: 5 October 2017 Source:International Journal of Pharmaceutics, Volume 531, Issue 1 Author(s): T. Wersig, M.C. Hacker, J. Kressler, K. Mäder The linear biodegradable polyester poly(glycerol adipate) (PGA) was synthesized via enzymatic polycondensation using lipase B from Candida antarctica (CAL-B). Every monomer unit of PGA possesses a pendant hydroxyl group which is responsible for the hydrophilic character and moisture swelling. These OH groups were esterified to different degrees with the anti-inflammatory drug indomethacin in order to create a prodrug with a pH-sensitive linker for modified drug r...
Source: International Journal of Pharmaceutics - September 11, 2017 Category: Drugs & Pharmacology Source Type: research