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Design and evaluation of surface functionalized superparamagneto-plasmonic nanoparticles for cancer therapeutics
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): M. Ravichandran, Goldie Oza, S. Velumani, Jose Tapia Ramirez, A. Vera, L. Leija Designing a multifunctional nanomaterial is always considered as a biggest concern in the field of nanomedicine which aims to promote versatile action in a single use from tracking to therapeutics. Therefore, metallic nanoparticles are well exploited as a major platform with the assemblage of surface modifications which can be effectively engaged for plenty of applications. Here, in this work, we have successfully amalgamated go...
Source: International Journal of Pharmaceutics - April 2, 2017 Category: Drugs & Pharmacology Source Type: research

Surfactants from itaconic acid: Toxicity to HaCaT keratinocytes in vitro, micellar solubilization, and skin permeation enhancement of hydrocortisone
In this study, two anionic surfactants, named C12-OPK and C18-OPK, were synthesized via condensation of itaconic acid and fatty amines, with C12 and C18 alkyl chains, respectively. Assessment of impacts on HaCaT keratinocyte cell viability was used as indicator of their potential to cause skin irritation 24h post exposure (Alamar Blue assay). The LC50 values of C12-OPK and C18-OPK (144 and 85mg/L, respectively) were lower than LC50 values of the most used commercial surfactants (e.g. SDS). The effect of different surfactant concentrations (up to ten times the critical micellar concentration, CMC) on hydrocortisone (HC) sol...
Source: International Journal of Pharmaceutics - April 2, 2017 Category: Drugs & Pharmacology Source Type: research

In vitro evaluation of the genotoxicity of poly(anhydride) nanoparticles designed for oral drug delivery
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): T. Iglesias, M. Dusinska, N. El Yamani, J.M. Irache, A. Azqueta, A. López de Cerain In the last years, the development of nanomaterials has significantly increased due to the immense variety of potential applications in technological sectors, such as medicine, pharmacy and food safety. Focusing on the nanodevices for oral drug delivery, poly(anhydride) nanoparticles have received extensive attention due to their unique properties, such as their capability to develop intense adhesive interactions within the gu...
Source: International Journal of Pharmaceutics - April 1, 2017 Category: Drugs & Pharmacology Source Type: research

Supercritical anti-solvent technique assisted synthesis of thymoquinone liposomes for radioprotection: Formulation optimization, in-vitro and in-vivo studies
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Iqbal Ahmad, Sohail Akhter, Mohammed Anwar, Sobiya Zafar, Rakesh Kumar Sharma, Asgar Ali, Farhan Jalees Ahmad The aim of this study was to develop Thymoquinone (TQ) loaded PEGylated liposomes using supercritical anti-solvent (SAS) process for enhanced blood circulation, and greater radioprotection. The SAS process of PEGylated liposomes synthesis was optimized by Box-Behnken design. Spherical liposomes with a particle size of 195.6±5.56nm and entrapment efficiency (%EE) of 89.4±3.69% were obtained. Opt...
Source: International Journal of Pharmaceutics - April 1, 2017 Category: Drugs & Pharmacology Source Type: research

Core/shell poly(ethylene oxide)/Eudragit fibers for site-specific release
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Dong Jia, Yanshan Gao, Gareth R. Williams Electrospinning was used to prepare core/shell fibers containing the active pharmaceutical ingredients indomethacin (IMC) or mebeverine hydrochloride (MB-HCl). The shell of the fibers was fabricated from the pH sensitive Eudragit S100 polymer, while the drug-loaded core was based on the mucoadhesive poly(ethylene oxide) (PEO). Three different drug loadings (from 9 to 23% (w/w) of the core mass) were prepared, and for MB-HCl two different molecular weights of PEO were explore...
Source: International Journal of Pharmaceutics - April 1, 2017 Category: Drugs & Pharmacology Source Type: research

Solubility and thermodynamics of apremilast in different mono solvents: Determination, correlation and molecular interactions
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Faiyaz Shakeel, Nazrul Haq, Fars K. Alanazi, Ibrahim A. Alsarra The solubility data of recently launched poorly soluble antipsoriatic drug apremilast (APM) in any mono solvent or cosolvent mixtures with respect to temperature are not available in literature. Hence, in this research work, the solubility of APM in twelve different mono solvents namely “water, methanol, ethanol, isopropanol (IPA), ethylene glycol (EG), propylene glycol (PG), 1-butanol, 2-butanol, ethyl acetate (EA), dimethyl sulfoxide (DMSO), pol...
Source: International Journal of Pharmaceutics - April 1, 2017 Category: Drugs & Pharmacology Source Type: research

Exploring the structure-permeation relationship of topical tricyclic antidepressants used for skin analgesia
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Kuo-Sheng Liu, Tse-Hung Huang, Ibrahim A. Aljuffali, En-Li Chen, Jhi-Joung Wang, Jia-You Fang The purpose of this study was to evaluate the skin permeation of tricyclic antidepressants (TCAs) with propamine moiety to select candidates for the development of topical analgesics to treat cutaneous pain. We sought to establish the structure-permeation relationship (SPR) of topical TCAs. The lipophilicity, melting point, and aqueous solubility were determined to develop the physicochemical characterization. The TCA perme...
Source: International Journal of Pharmaceutics - April 1, 2017 Category: Drugs & Pharmacology Source Type: research

Nile red nanosuspensions as investigative model to study the follicular targeting of drug nanocrystals
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Francesco Corrias, Michele Schlich, Chiara Sinico, Rosa Pireddu, Donatella Valenti, Anna Maria Fadda, Salvatore Marceddu, Francesco Lai The strategy of formulating poorly soluble actives as nanosuspension has been explored by more than a thousand research papers, with some medicinal products for oral and intravenous use having reached the market or advanced clinical trials. Interestingly, there is a limited number of reports of nanosuspensions formulated for dermal and transdermal drug delivery. In the pres...
Source: International Journal of Pharmaceutics - April 1, 2017 Category: Drugs & Pharmacology Source Type: research

Analytical ultracentrifugation for analysis of doxorubicin loaded liposomes
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Dora Mehn, Patrizia Iavicoli, Noelia Cabaleiro, Sven Even Borgos, Fanny Caputo, Otmar Geiss, Luigi Calzolai, François Rossi, Douglas Gilliland Analytical ultracentrifugation (AUC) is a powerful tool for the study of particle size distributions and interactions with high accuracy and resolution. In this work, we show how the analysis of sedimentation velocity data from the AUC can be used to characterize nanocarrier drug delivery systems used in nanomedicine. Nanocarrier size distribution and the ratio of free...
Source: International Journal of Pharmaceutics - March 31, 2017 Category: Drugs & Pharmacology Source Type: research

Prediction of solid fraction from powder mixtures based on single component compression analysis
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Robert Schmidtke, Daniela Schröder, Judith Menth, Andrea Staab, Michael Braun, Karl G. Wagner The aim of this study was to provide a systematic evaluation of various compression models (Percolation, Kawakita, Exponential model) in respect to predict tablet́s solid fraction for direct compression mixtures, based on single component compression analysis. Four mixtures were compressed over a wide pressure range at various fractions of microcrystalline cellulose (MCC) and pre-agglomerated lactose monohydrate (LAC)...
Source: International Journal of Pharmaceutics - March 31, 2017 Category: Drugs & Pharmacology Source Type: research

Comparison of the protective effect of self-emulsifying peptide drug delivery systems towards intestinal proteases and glutathione
Conclusion SEDDS can provide a 100% protective effect towards protease degradation and deactivation by GSH. According to this, SEDDS might be promising tools for oral delivery of peptide drugs. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - March 30, 2017 Category: Drugs & Pharmacology Source Type: research

Nanohydrogel with N,N ′-bis(acryloyl)cystine crosslinker for high drug loading
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Marcin Mackiewicz, Jan Romanski, Ewa Drozd, Beata Gruber-Bzura, Piotr Fiedor, Zbigniew Stojek, Marcin Karbarz Substantially improved hydrogel particles based on poly(N-isopropylacrylamide) (pNIPA) have been obtained. First, as a result of replacing commercially available N,N′-bis(acryloyl)cystamine (BAC), the crosslinker, with acryloyl derivative of cystine containing a carboxylic group (BISS), the hydrogel particles acquired improved stability vs. ionic strength and allowed further chemical modification of th...
Source: International Journal of Pharmaceutics - March 30, 2017 Category: Drugs & Pharmacology Source Type: research

Design of fixed dose combination and physicochemical characterization of enteric-coated bilayer tablet with circadian rhythmic variations containing telmisartan and pravastatin sodium
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Daoqi Luo, Joo Hee Kim, Chulhun Park, Euichaul Oh, Jun-Bom Park, Jing-Hao Cui, Qing-Ri Cao, Beom-Jin Lee The aim of this study was to investigate a fixed dose combination (FDC) of telmisartan (TEL) and pravastatin sodium (PRA) in enteric-coated bilayer tablets, which was designed for once-daily bedtime dose in order to match circadian rhythmic variations of hypertension and cholesterol synthesis and optimize the patient friendly dosing treatment. Due to the poor aqueous solubility of TEL, ternary solid dispersions (...
Source: International Journal of Pharmaceutics - March 30, 2017 Category: Drugs & Pharmacology Source Type: research

Orodispersible films: Towards drug delivery in special populations
This article reviews the current strides of ODF technology and some of its unmet quality and manufacturing aspects. A topic highlights opportunities and limitations of inkjet printed ODF as a population-specific drug delivery. Overall, this article aims to stimulate further research to fill the current knowledge gap between manufacturing and administration requirements of ODF targeting specific patient subpopulations such as geriatrics. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - March 30, 2017 Category: Drugs & Pharmacology Source Type: research

Synergistic inhibition of migration and invasion of breast cancer cells by dual docetaxel/quercetin-loaded nanoparticles via Akt/MMP-9 pathway
In this study, an Akt inhibitor (quercetin, Qu) was co-delivered with a chemotherapeutic agent (docetaxel, DTX) by using hyaluronic acid (HA)-modified nanoparticles (NPs) as vectors to block metastasis. Dual DTX/Qu-loaded HA/polylactic-co-glycolic acid–polyethyleneimine NPs (PP-HA/NPs) were prepared through a modified emulsion solvent evaporation technique. The particle size of PP-HA/NPs with narrow polydispersity was 209.8±10.8nm. Wound healing assay revealed that Qu co-delivery and HA modification elicited synergistic inhibitory effects on cell motility. The downregulation of p-Akt and matrix metalloproteina...
Source: International Journal of Pharmaceutics - March 29, 2017 Category: Drugs & Pharmacology Source Type: research

Physicochemical attributes and dissolution testing of ophthalmic ointments
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Quanying Bao, Rajan Jog, Jie Shen, Bryan Newman, Yan Wang, Stephanie Choi, Diane J. Burgess The investigation of semisolid ophthalmic ointments is challenging due to their complex physicochemical properties and the unique anatomy of the human eye. Using Lotemax® as a model ophthalmic ointment, three different manufacturing processes and two excipient sources (Fisher® (OWP) and Fougera® (NWP)) were used to prepare loteprednol etabonate ointments that were qualitatively and quantitatively the same across t...
Source: International Journal of Pharmaceutics - March 29, 2017 Category: Drugs & Pharmacology Source Type: research

The absorption enhancer sodium deoxycholate promotes high gene transfer in skeletal muscles
We report that sodium deoxycholate (DOC) and derivatives thereof increase after intramuscular injection by more than 100-fold the levels of the reporter gene luciferase compared to naked DNA. Using a LacZ expression cassette, we found that more than 20% of the muscle fibers expressed the reporter gene. Prolonged expression of a secreted reporter gene derived from a natural murine alkaline phosphatase enzyme could be documented. Altogether, our results demonstrate that bile salts belong to the most efficient chemicals identified so far for skeletal muscle gene transfer. Importantly, since these compounds are naturally found...
Source: International Journal of Pharmaceutics - March 29, 2017 Category: Drugs & Pharmacology Source Type: research

Docetaxel-loaded RIPL peptide (IPLVVPLRRRRRRRRC)-conjugated liposomes: Drug release, cytotoxicity, and antitumor efficacy
In this study, docetaxel-loaded RIPL-L (DTX-RIPL-L) were prepared and evaluated for in vitro drug release, cytotoxicity, and in vivo antitumor efficacy. DTX was successfully encapsulated by pre-loading, with an average encapsulation efficiency and drug loading capacity of 32.4% and 21.39±2.05 (μg/mg), respectively. A DTX release study using dialysis showed a biphasic release pattern, i.e., rapid release for 6h, followed by sustained release up to 72h. The first-order equation provided the best fit for drug release (r2 =0.9349). In vitro cytotoxicity was dose-dependent, resulting in IC50 values of 36.10 (SK-OV-3) ...
Source: International Journal of Pharmaceutics - March 28, 2017 Category: Drugs & Pharmacology Source Type: research

Enhanced cellular uptake and gene silencing activity of siRNA using temperature-responsive polymer-modified liposome
In this study, to develop the temperature-responsive liposome as a novel carrier for siRNA delivery, we prepared lipoplexes and assessed cellular uptake of siRNA and gene silencing activity of target genes, compared with those of a commercial transfection reagent, Lipofectamine RNAiMAX, and non-modified or PEGylated liposomes. The temperature-responsive polymer, N-isopropylacrylamide-co-N,N’-dimethylaminopropylacrylamide [P(NIPAAm-co-DMAPAAm)]-modified liposome induced faster intracellular delivery because P(NIPAAm-co-DMAPAAm) exhibits a lower critical solution temperature (LCST) changing its nature from hydrophilic ...
Source: International Journal of Pharmaceutics - March 28, 2017 Category: Drugs & Pharmacology Source Type: research

Targeted delivery of epirubicin to tumor-associated macrophages by sialic acid-cholesterol conjugate modified liposomes with improved antitumor activity
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Songlei Zhou, Ting Zhang, Bo Peng, Xiang Luo, Xinrong Liu, Ling Hu, Yang Liu, Donghua Di, Yanzhi Song, Yihui Deng With the knowledge that the receptors of sialic acid are overexpressed on the surface of tumor-associated macrophages (TAMs), which play a crucial role in the tumor's progression and metastasis, a sialic acid-cholesterol conjugate (SA-CH) was synthesized and modified on the surface of epirubicin (EPI)-loaded liposomes (EPI-SAL) to improve the delivery of EPI to the TAMs. The liposomes were developed usin...
Source: International Journal of Pharmaceutics - March 28, 2017 Category: Drugs & Pharmacology Source Type: research

Vancomycin-loaded nanobubbles: A new platform for controlled antibiotic delivery against methicillin-resistant Staphylococcus aureus infections
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Monica Argenziano, Giuliana Banche, Anna Luganini, Nicole Finesso, Valeria Allizond, Giulia Rossana Gulino, Amina Khadjavi, Rita Spagnolo, Vivian Tullio, Giuliana Giribaldi, Caterina Guiot, Anna Maria Cuffini, Mauro Prato, Roberta Cavalli Vancomycin (Vm) currently represents the gold standard against methicillin-resistant Staphylococcus aureus (MRSA) infections. However, it is associated with low oral bioavailability, formulation stability issues, and severe side effects upon systemic administration. These drawbacks...
Source: International Journal of Pharmaceutics - March 28, 2017 Category: Drugs & Pharmacology Source Type: research

Hyperspectral imaging using near infrared spectroscopy to monitor coat thickness uniformity in the manufacture of a transdermal drug delivery system
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Naresh Pavurala, Xiaoming Xu, Yellela S.R. Krishnaiah Hyperspectral imaging using near infrared spectroscopy (NIRS) integrates spectroscopy and conventional imaging to obtain both spectral and spatial information of materials. The non-invasive and rapid nature of hyperspectral imaging using NIRS makes it a valuable process analytical technology (PAT) tool for in-process monitoring and control of the manufacturing process for transdermal drug delivery systems (TDS). The focus of this investigation was to develop and ...
Source: International Journal of Pharmaceutics - March 28, 2017 Category: Drugs & Pharmacology Source Type: research

Insights into Caco-2 cell culture structure using coherent anti-Stokes Raman scattering (CARS) microscopy
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Jukka Saarinen, Erkan Sözeri, Sara J. Fraser-Miller, Leena Peltonen, Hélder A. Santos, Antti Isomäki, Clare J. Strachan We have used coherent anti-Stokes Raman scattering (CARS) microscopy as a novel and rapid, label-free and non-destructive imaging method to gain structural insights into live intestinal epithelial cell cultures used for drug permeability testing. Specifically we have imaged live Caco-2 cells in (bio)pharmaceutically relevant conditions grown on membrane inserts. Imaging conditions ...
Source: International Journal of Pharmaceutics - March 28, 2017 Category: Drugs & Pharmacology Source Type: research

Preparation of core-crosslinked linear-dendritic copolymer micelles with enhanced stability and their application for drug solubilisation
In this study we explore the preparation of core-crosslinked micelles of linear-dendritic methoxy-poly(ethylene glycol) (MPEG)-co-poly(ester-sulfide) (PES) polymers to improve the stability of such polymeric micelle systems against premature disintegration and drug release. A series of MPEG-PES copolymers were synthesised via stepwise reactions of acetylation and thiol-ene photoreaction. Surface tension measurement showed that the copolymers with ethenyl surface groups could self-associate in dilute aqueous solutions to form micelles. Crosslinking within the micelle cores in the presence of dithioerythritol (DTT) linker wa...
Source: International Journal of Pharmaceutics - March 28, 2017 Category: Drugs & Pharmacology Source Type: research

Mixtures of hyaluronic acid and liposomes for drug delivery: Phase behavior, microstructure and mobility of liposomes
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Naila El Kechai, Sandrine Geiger, Arianna Fallacara, Ingrid Cañero Infante, Valérie Nicolas, Evelyne Ferrary, Nicolas Huang, Amélie Bochot, Florence Agnely Hyaluronic acid liposomal gels have previously demonstrated in vivo their great potential for drug delivery. Elucidating their phase behavior and structure would provide a better understanding of their use properties. This work evaluates the microstructure and the phase behavior of mixtures of hyaluronic acid (HA) and liposomes and their impa...
Source: International Journal of Pharmaceutics - March 28, 2017 Category: Drugs & Pharmacology Source Type: research

Correlation between calculated molecular descriptors of excipient amino acids and experimentally observed thermal stability of lysozyme
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Helena Meng-Lund, Natascha Friis, Marco van de Weert, Jukka Rantanen, Antti Poso, Holger Grohganz, Lene Jorgensen A quantitative structure-property relationship (QSPR) between protein stability and the physicochemical properties of excipients was investigated to enable a more rational choice of stabilizing excipients than prior knowledge. The thermal transition temperature and aggregation time were determined for lysozyme in combination with 13 different amino acids using high throughput fluorescence spectroscopy an...
Source: International Journal of Pharmaceutics - March 28, 2017 Category: Drugs & Pharmacology Source Type: research

Enhanced gastric stability of esomeprazole by molecular interaction and modulation of microenvironmental pH with alkalizers in solid dispersion
In this study, we prepared new gastric fluid resistant solid dispersions (SDs) containing alkalizers. Then, new mechanistic evidence regarding the effects of pharmaceutical alkalizers on the aqueous stability of EPM in simulated gastric fluid was investigated. The alkalizer-loaded SD were prepared by dissolving or dispersing EPM, hydroxypropyl methylcellulose (HPMC) 6 cps, and an alkalizer, in ethanol 50% (v/v) followed by spray drying. Nine different alkalizers were assessed for in vitro stability in two media, simulated gastric fluid (pH 1.2 buffer) and simulated intestinal fluid (pH 6.8 buffer). The microenvironmental p...
Source: International Journal of Pharmaceutics - March 28, 2017 Category: Drugs & Pharmacology Source Type: research

Nanoincorporation of bioactive compounds from red grape pomaces: In vitro and ex vivo evaluation of antioxidant activity
In this study, the active components of grape pomaces were first extracted by maceration in ethanol and propylene glycol, then in extra virgin olive oil. The main components of the hydrophilic extractive solutions were flavonoids, while monounsaturated fatty acids were the most abundant constituents of the extractive oil, with high levels of oleic acid, which were identified by HPLC/DAD and GC/MS, respectively. The hydrophilic extractive solutions and the lipophilic extractive oil were used to prepare phospholipid vesicles, avoiding the energetically and economically expensive steps required to obtain solid matrixes or pur...
Source: International Journal of Pharmaceutics - March 27, 2017 Category: Drugs & Pharmacology Source Type: research

Nanostructured monolinolein miniemulsions as delivery systems: Role of the internal mesophase on cytotoxicity and cell internalization
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Samuel Guillot, Fabienne Méducin, Kristina Poljak, Virginie Malard, Alexandra Foucault-Collet, Sébastien Serieye, Chantal Pichon Recent advances in nanoparticle systems for improved drug delivery display a great potential for the administration of active molecules. Here, lipid miniemulsions with various internal nanostructures were loaded with the chemotherapeutic agent Paclitaxel. The goal is to assess the impact of internal structures on their efficiency. Previously the structure, the stability and t...
Source: International Journal of Pharmaceutics - March 27, 2017 Category: Drugs & Pharmacology Source Type: research

An innovative method for the preparation of high API-loaded hollow spherical granules for use in controlled-release formulation
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Takumi Asada, Mitsuaki Kobiki, Yasushi Ochiai, Yasunori Iwao, Shigeru Itai The aim of this study was to prepare controlled-release (CR) granules with suitable particle strength, flowability, particle size distribution (PSD) and density characteristics for blending with other excipients. We also wanted these CR granules to contain large quantities of active pharmaceutical ingredient (API). A high shear mixer was used to mix an API with various polymers at various feed ratios, and the resulting granulated materials we...
Source: International Journal of Pharmaceutics - March 27, 2017 Category: Drugs & Pharmacology Source Type: research

In vitro and in silico characterization of fibrous scaffolds comprising alternate colistin sulfate-loaded and heat-treated polyvinyl alcohol nanofibrous sheets
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): István Sebe, Eszter Ostorházi, Zsolt Bodai, Zsuzsanna Eke, József Szakács, Norbert Krisztián Kovács, Romána Zelkó A multilayer mat for dispensing colistin sulfate through a body surface was prepared by electrospinning. The fabricated system comprised various polyvinyl alcohol fibrous layers prepared with or without the active ingredient. One of the electrospun layers contained water-soluble colistin sulfate and the other was prepared from the same polymer type ...
Source: International Journal of Pharmaceutics - March 27, 2017 Category: Drugs & Pharmacology Source Type: research

Engineered particles demonstrate improved flow properties at elevated drug loadings for direct compression manufacturing
This study demonstrated that flow properties of a powder blend can be improved through API particle engineering, without critically impacting blend tabletability at elevated drug loadings. In studying a jet milled API (D50 =24μm) and particle engineered wet milled API (D50 =70μm and 90μm), flow functions of all API lots were similarly poor despite the vast difference in average particle size (ffc < 4). This finding strays from the common notion that powder flow properties are directly correlated to particle size distribution. Upon adding excipients, however, clear trends in flow functions based on API parti...
Source: International Journal of Pharmaceutics - March 27, 2017 Category: Drugs & Pharmacology Source Type: research

Reflectometric monitoring of the dissolution process of thin polymeric films
In conclusion, it was demonstrated that a traditional optical reflection method can provide valuable information about the dissolution characteristics of thin polymeric films in low liquid volume surroundings. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - March 23, 2017 Category: Drugs & Pharmacology Source Type: research

Sustained release ophthalmic dexamethasone: In vitro in vivo correlations derived from the PK-Eye
We describe dexamethasone loaded poly-DL-lactide-co-glycolide (PLGA) microparticles that were fabricated by thermally induced phase separation (TIPS). The dexamethasone loaded microparticles were evaluated using a two-compartment, in vitro aqueous outflow model of the eye (PK-Eye) that estimates drug clearance time from the back of the eye via aqueous outflow by the anterior route. A dexamethasone dose of 0.20±0.02mg in a 50μL volume of TIPS microparticles resulted in a clearance t 1/2 of 9.6±0.3days using simulated vitreous in the PK-Eye. Since corticosteroids can also clear through the retina, it is nece...
Source: International Journal of Pharmaceutics - March 22, 2017 Category: Drugs & Pharmacology Source Type: research

Direct comparison between millifluidic and bulk-mixing platform in the synthesis of amorphous drug-polysaccharide nanoparticle complex
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Bingxue Dong, Kunn Hadinoto Amorphous drug-polysaccharide nanoparticle complex (or drug nanoplex) had emerged as an ideal supersaturating delivery system of poorly-soluble drugs attributed to its many attractive characteristics. Herein we presented for the first time direct comparison between two nanoplex synthesis platforms, i.e. millifluidics and bulk mixing, representing continuous and batch production modes, respectively. They were compared by the resultant nanoplex’s (1) physical characteristics (size, ze...
Source: International Journal of Pharmaceutics - March 20, 2017 Category: Drugs & Pharmacology Source Type: research

Critical material attributes (CMAs) of strip films loaded with poorly water-soluble drug nanoparticles: III. Impact of drug nanoparticle loading
This study explores the ability to achieve high loadings of poorly water-soluble drug nanoparticles in strip films while retaining good mechanical properties and enhanced dissolution rate. Aqueous suspensions containing up to 30wt% griseofulvin nanoparticles were prepared via wet stirred media milling and incorporated into hydroxypropyl methylcellulose (HPMC) films. Griseofulvin loading in films was adjusted to be between 9 and 49wt% in HPMC-E15 films and 30 and 73wt% in HPMC-E4M films by varying the mixing ratio of HPMC solution-to-griseofulvin suspension. All films exhibited good content uniformity and nanoparticle redis...
Source: International Journal of Pharmaceutics - March 20, 2017 Category: Drugs & Pharmacology Source Type: research

Denatured protein-coated docetaxel nanoparticles: Alterable drug state and cytosolic delivery
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Li Zhang, Qingqing Xiao, Yiran Wang, Chenshuang Zhang, Wei He, Lifang Yin Many lead compounds have a low solubility in water, which substantially hinders their clinical application. Nanosuspensions have been considered a promising strategy for the delivery of water-insoluble drugs. Here, denatured soy protein isolate (SPI)-coated docetaxel nanosuspensions (DTX-NS) were developed using an anti-solvent precipitation-ultrasonication method to improve the water-solubility of DTX, thus improving its intracellular deliver...
Source: International Journal of Pharmaceutics - March 20, 2017 Category: Drugs & Pharmacology Source Type: research

Electrospun protein nanofibers in healthcare: A review
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): S. Babitha, Lakra Rachita, K. Karthikeyan, Ekambaram Shoba, Indrakumar Janani, Balan Poornima, K. Purna Sai Electrospun nanofibers are being utilized for a wide range of healthcare applications. A plethora of natural and synthetic polymers are exploited for their ability to be electrospun and replace the complex habitat provided by the extracellular matrix for the cells. The fabrication of nanofibers can be tuned to act as a multicarrier system to deliver drugs, growth factors and health supplements etc. in a sustai...
Source: International Journal of Pharmaceutics - March 20, 2017 Category: Drugs & Pharmacology Source Type: research

Tensile and shear methods for measuring strength of bilayer tablets
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Shao-Yu Chang, Jian-xin Li, Changquan Calvin Sun Both shear and tensile measurement methods have been used to quantify interfacial bonding strength of bilayer tablets. The shear method is more convenient to perform, but reproducible strength data requires careful control of the placement of tablet and contact point for shear force application. Moreover, data obtained from the shear method depend on the orientation of the bilayer tablet. Although more time-consuming to perform, the tensile method yields data that are...
Source: International Journal of Pharmaceutics - March 20, 2017 Category: Drugs & Pharmacology Source Type: research

Nanoparticles as safe and effective delivery systems of antifungal agents: Achievements and challenges
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Ghareb M. Soliman Invasive fungal infections are becoming a major health concern in several groups of patients leading to severe morbidity and mortality. Moreover, cutaneous fungal infections are a major cause of visits to outpatient dermatology clinics. Despite the availability of several effective agents in the antifungal drug arena, their therapeutic outcome is less than optimal due to limitations related to drug physicochemical properties and toxicity. For instance, poor aqueous solubility limits the formulation...
Source: International Journal of Pharmaceutics - March 20, 2017 Category: Drugs & Pharmacology Source Type: research

Megalin-targeted enhanced transfection efficiency in cultured human HK-2 renal tubular proximal cells using aminoglycoside-carboxyalkyl- polyethylenimine -containing nanoplexes
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Fatemeh Oroojalian, Ali Hossein Rezayan, Wayne Thomas Shier, Khalil Abnous, Mohammad Ramezani Non-viral vectors are of interest as therapeutic gene delivery agents in gene therapy, because they are simple to prepare, easy to modify and have definable safety profiles compared to viral vectors. The potential of gene therapy in the treatment of renal diseases is limited by a lack of effective kidney-targeted gene delivery systems. Aminoglycoside antibiotics gentamicin and neomycin were connected by amide linkages to ca...
Source: International Journal of Pharmaceutics - March 20, 2017 Category: Drugs & Pharmacology Source Type: research

Multifractal and mechanical analysis of amorphous solid dispersions
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Camille Adler, Alexandra Teleki, Martin Kuentz The formulation of lipophilic and hydrophobic compounds is a challenge for the pharmaceutical industry and it requires the development of complex formulations. Our first aim was to investigate hot-melt extrudate microstructures by means of multifractal analysis using scanning electron microscopy imaging. Since the microstructure can affect solid dosage form performance such as mechanical properties, a second objective was to study the influence of the type of adsorbent ...
Source: International Journal of Pharmaceutics - March 20, 2017 Category: Drugs & Pharmacology Source Type: research

Identifying overarching excipient properties towards an in-depth understanding of process and product performance for continuous twin-screw wet granulation
Publication date: 30 April 2017 Source:International Journal of Pharmaceutics, Volume 522, Issues 1–2 Author(s): N. Willecke, A. Szepes, M. Wunderlich, J.P. Remon, C. Vervaet, T. De Beer The overall objective of this work is to understand how excipient characteristics influence the process and product performance for a continuous twin-screw wet granulation process. The knowledge gained through this study is intended to be used for a Quality by Design (QbD)-based formulation design approach and formulation optimization. A total of 9 preferred fillers and 9 preferred binders were selected for this study. The selected ...
Source: International Journal of Pharmaceutics - March 19, 2017 Category: Drugs & Pharmacology Source Type: research

NMR and ESR study of amphotericin B interactions with various binary phosphatidylcholine/phosphatidylglycerol membranes
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): J.C. Debouzy, L. Mehenni, D. Crouzier, M. Lahiani-Skiba, G. Nugue, M. Skiba Several biologically relevant phospholipids are considered as potential excipients for IV administration liposome’s formulation of AMB (Biopharmaceututics Classification System Class IV). On the basis of in vivo bioavaibility studies, DMPC and DMPG were ranked as the first potent encapsulation enhancers for this model drug, especially if one expects to target DMPG rich systems as pulmonary surfactant. Subsequently, dispersio...
Source: International Journal of Pharmaceutics - March 17, 2017 Category: Drugs & Pharmacology Source Type: research

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