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Formulation of carbapenems loaded gold nanoparticles to combat multi-antibiotic bacterial resistance: In vitro antibacterial study
In this study, we focused on evaluating the surface conjugation of carbapenems (imipenem and meropenem) with gold nanoparticles as a delivering strategy to specifically and safely maximize their therapeutic efficacy while destroying the developing resistance of the pathogens. Different particle size formulae (35, 70 and 200nm) were prepared by citrate reduction method. The prepared nanoparticles were functionalized with imipenem (Ipm) or meropenem (Mem) and physico-chemically characterized for loading efficiency, particle size, morphology, and in-vitro release. The antibacterial efficacy was also evaluated against carbapen...
Source: International Journal of Pharmaceutics - April 21, 2017 Category: Drugs & Pharmacology Source Type: research

Optics-based compressibility parameter for pharmaceutical tablets obtained with the aid of the terahertz refractive index
The objective of this study is to propose a novel optical compressibility parameter for porous pharmaceutical tablets. This parameter is defined with the aid of the effective refractive index of a tablet that is obtained from non-destructive and contactless terahertz (THz) time-delay transmission measurement. The optical compressibility parameter of two training sets of pharmaceutical tablets with a priori known porosity and mass fraction of a drug was investigated. Both pharmaceutical sets were compressed with one of the most commonly used excipients, namely microcrystalline cellulose (MCC) and drug Indomethacin. The opti...
Source: International Journal of Pharmaceutics - April 21, 2017 Category: Drugs & Pharmacology Source Type: research

Novel dabigatran etexilate hemisuccinate-loaded polycap: Physicochemical characterisation and in vivo evaluation in beagle dogs
Publication date: 15 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 1 Author(s): Jung Hyun Cho, Jin Cheul Kim, Hyung-Seo Kim, Dong Shik Kim, Kyeong Soo Kim, Yong Il Kim, Chul Soon Yong, Jong Oh Kim, Yu Seok Youn, Kyung Taek Oh, Jong Soo Woo, Han-Gon Choi The purpose of this study was to develop a novel dabigatran etexilate hemisuccinate (DEH) salt-loaded polycap with bioequivalence to the dabigatran etexilate mesylate (DEM)-loaded commercial product. DEH prepared with dabigatran etexilate base (DE) and succinic acid was less hygroscopic but less soluble than DEM. Numerous micronized DEHs and DE...
Source: International Journal of Pharmaceutics - April 21, 2017 Category: Drugs & Pharmacology Source Type: research

PEGylated doxorubicin nanoparticles mediated by HN-1 peptide for targeted treatment of oral squamous cell carcinoma
In conclusion, our study demonstrated for the first time that HN-1 could be used for mediating the OSCC-targeted delivery of nanoparticles. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - April 19, 2017 Category: Drugs & Pharmacology Source Type: research

Pressure-temperature phase diagram of the dimorphism of the anti-inflammatory drug nimesulide
Publication date: 15 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 1 Author(s): M. Barrio, J. Huguet, B. Robert, I.B. Rietveld, R. Céolin, J.Ll. Tamarit Understanding the phase behavior of active pharmaceutical ingredients is important for formulations of dosage forms and regulatory reasons. Nimesulide is an anti-inflammatory drug that is known to exhibit dimorphism; however up to now its stability behavior was not clear, as few thermodynamic data were available. Therefore, calorimetric melting data have been obtained, which were found to be T I-L =422.4±1.0K, ΔI→L H =...
Source: International Journal of Pharmaceutics - April 19, 2017 Category: Drugs & Pharmacology Source Type: research

Targeted intracorneal delivery —Biodistribution of triamcinolone acetonide following topical iontophoresis of cationic amino acid ester prodrugs
Publication date: 15 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 1 Author(s): Verena Santer, Sergio del Río Sancho, Maria Lapteva, Yogeshvar N. Kalia The aim was to investigate intracorneal iontophoresis of biolabile triamcinolone acetonide (TA) amino acid ester prodrugs (TA-AA). Arginine and lysine esters of TA (TA-Arg and TA-Lys, respectively) were synthesized and characterized; quantification was performed by HPLC-UV and UHPLC–MS/MS. The aqueous solubility of the prodrugs (at pH 5.5) was ∼1000-fold greater than TA. Anodal iontophoresis (10min at 3mA/cm2) of TA-AA was inve...
Source: International Journal of Pharmaceutics - April 19, 2017 Category: Drugs & Pharmacology Source Type: research

Targeted drug delivery system to neural cells utilizes the nicotinic acetylcholine receptor
Publication date: 15 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 1 Author(s): Rachel Huey, Barry O’Hagan, Paul McCarron, Susan Hawthorne Drug delivery to the brain is still a major challenge in the field of therapeutics, especially for large and hydrophilic compounds. In order to achieve drug delivery of therapeutic concentration in the central nervous system, the problematic blood brain barrier (BBB) must be overcome. This work presents the formulation of a targeted nanoparticle-based drug delivery system using a specific neural cell targeting ligand, rabies virus derived peptide (RDP...
Source: International Journal of Pharmaceutics - April 19, 2017 Category: Drugs & Pharmacology Source Type: research

Enhancement of dissolution rate through eutectic mixture and solid solution of posaconazole and benznidazole
Publication date: 15 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 1 Author(s): Camila Bezerra Melo Figueirêdo, Daniela Nadvorny, Amanda Carla Quintas de Medeiros Vieira, José Lamartine Soares Sobrinho, Pedro José Rolim Neto, Ping I. Lee, Monica Felts de La Roca Soares Benznidazole (BNZ), the only commercialized antichagasic drug, and the antifungal compound posaconazole (PCZ) have shown synergistic action in the therapy of Chagas disease, however both active pharmaceutical ingredients (APIs) exhibit low aqueous solubility potentially limiting their bioavailability and ther...
Source: International Journal of Pharmaceutics - April 19, 2017 Category: Drugs & Pharmacology Source Type: research

Investigation of in vitro PDT activities of zinc phthalocyanine immobilised TiO2 nanoparticles
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Fatma Yurt, Mine Ince, Suleyman Gokhan Colak, Kasim Ocakoglu, Ozge Er, Hale Melis Soylu, Cumhur Gunduz, Cigir Biray Avci, Cansu Caliskan Kurt Phthalocyanines (Pcs) are commonly used as Photosensors (PSs) in Photodynamic Therapy (PDT) applications due to their intense absorption in the far red-near IR spectral region with a high extinction coefficient and high ability for generating singlet oxygen. Pcs targetspecifically tumors, and do not show any considerable toxic effects under the absence of light. In pa...
Source: International Journal of Pharmaceutics - April 18, 2017 Category: Drugs & Pharmacology Source Type: research

Preparation and investigation of controlled-release glipizide novel oral device with three-dimensional printing
Publication date: 15 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 1 Author(s): Qijun Li, Haoyang Wen, Danyang Jia, Xiaoying Guan, Hao Pan, Yue Yang, Shihui Yu, Zhihong Zhu, Rongwu Xiang, Weisan Pan The purpose of this study was to explore the feasibility of combining fused deposition modeling (FDM) 3D printing technology with hot melt extrusion (HME) to fabricate a novel controlled-release drug delivery device. Glipizide used in the treatment of diabetes was selected as model drug, and was successfully loaded into commercial polyvinyl alcohol (PVA) filaments by HME method. The drug-loaded fil...
Source: International Journal of Pharmaceutics - April 18, 2017 Category: Drugs & Pharmacology Source Type: research

Oil-in-water microemulsions stabilized by 3-(N,N- dimethylalkylammonio)propanesulfonate surfactants of varying alkyl chain length: Solubilisation of testos-terone propionate
Publication date: 15 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 1 Author(s): Chien-Ming Hsieh, Warangkana Warisnoicharoen, Raju K. Patel, Farnoosh Kianfar, M. Jayne Lawrence Solubilisation of the poorly-water soluble drug, testosterone propionate, in co-surfactant-free, dilutable, oil-in-water microemulsions stabilized by zwitterionic surfactants of varying alkyl chain length, namely 3-(N,N-dimethyloctylammonio)propanesulfonate and 3-(N,N-dimethyldodecylammonio)propanesulfonate and containing one of four ethyl ester oils, has been investigated. Both 3-(N,N-dimethyloctylammonio)propanesulfon...
Source: International Journal of Pharmaceutics - April 18, 2017 Category: Drugs & Pharmacology Source Type: research

Polymer sutures for simultaneous wound healing and drug delivery – A review
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Blessy Joseph, Anne George, Sreeraj Gopi, Nandakumar Kalarikkal, Sabu Thomas Drug delivery using suitable polymeric devices has gathered momentum in the recent years due to their remarkable properties. The versatility of polymeric materials makes them reliable candidates for site targeted drug release. Among them biodegradable sutures has received considerable attention because they offer great promises in the realm of drug delivery. Sutures have been found to be an effective strategy for the delivery of an...
Source: International Journal of Pharmaceutics - April 17, 2017 Category: Drugs & Pharmacology Source Type: research

Down-stream drug product processing of itraconazole nanosuspension: Factors influencing drug particle size and dissolution from nanosuspension-layered beads
This study focuses on bead layering as one approach to solidify nanosuspensions. The aim was to systematically investigate the influence of type of coating polymer (HPMC VLV vs. copovidone), bead material and bead size (sugar vs. MCC, and small vs. large) and coating thickness (50%–150% layering level) on the properties of a dried itraconazole nanosuspension. A stable itraconazole nanosuspension with a mean particle size below 200nm was prepared and a ratio of itraconazole and coating polymer of around 1:1 was identified. XRD and DSC scans revealed that itraconazole remained mostly crystalline after the bead layering...
Source: International Journal of Pharmaceutics - April 16, 2017 Category: Drugs & Pharmacology Source Type: research

Elaboration and evaluation of alginate foam scaffolds for soft tissue engineering
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Ceccaldi Caroline, Bushkalova Raya, Cussac Daniel, Duployer Benjamin, Tenailleau Christophe, Bourin Philippe, Parini Angelo, Sallerin Brigitte, Girod Fullana Sophie Controlling microarchitecture in polymer scaffolds is a priority in material design for soft tissue applications. This paper reports for the first time the elaboration of alginate foam-based scaffolds for mesenchymal stem cell (MSC) delivery and a comparative study of various surfactants on the final device performance. The use of surfactants pe...
Source: International Journal of Pharmaceutics - April 16, 2017 Category: Drugs & Pharmacology Source Type: research

Dropwise additive manufacturing of pharmaceutical products for amorphous and self emulsifying drug delivery systems
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Elçin Içten, Hitesh S. Purohit, Chelsey Wallace, Arun Giridhar, Lynne S. Taylor, Zoltan K. Nagy, Gintaras V. Reklaitis The improvements in healthcare systems and the advent of the precision medicine initiative have created the need to develop more innovative manufacturing methods for the delivery and production of individualized dosing and personalized treatments. In accordance with the changes observed in healthcare systems towards more innovative therapies, this paper presents dropwise addit...
Source: International Journal of Pharmaceutics - April 15, 2017 Category: Drugs & Pharmacology Source Type: research

Application of a handheld NIR spectrometer in prediction of drug content in inkjet printed orodispersible formulations containing prednisolone and levothyroxine
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Hossein Vakili, Henrika Wickström, Diti Desai, Maren Preis, Niklas Sandler Quality control tools to assess the quality of printable orodispersible formulations are yet to be defined. Four different orodispersible dosage forms containing two poorly soluble drugs, levothyroxine and prednisolone, were produced on two different edible substrates by piezoelectric inkjet printing. Square shaped units of 4cm2 were printed in different resolutions to achieve an escalating drug dose by highly accurate and unifo...
Source: International Journal of Pharmaceutics - April 15, 2017 Category: Drugs & Pharmacology Source Type: research

Probing the dynamics of complexed local anesthetics via neutron scattering spectroscopy and DFT calculations
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Murillo L. Martins, Juergen Eckert, Henrik Jacobsen, Éverton C. dos Santos, Rosanna Ignazzi, Daniele Ribeiro de Araujo, Marie-Claire Bellissent-Funel, Francesca Natali, Michael Marek Koza, Aleksander Matic, Eneida de Paula, Heloisa N. Bordallo Since potential changes in the dynamics and mobility of drugs upon complexation for delivery may affect their ultimate efficacy, we have investigated the dynamics of two local anesthetic molecules, bupivacaine (BVC, C18H28N2O) and ropivacaine (RVC, C17H26N2O), ...
Source: International Journal of Pharmaceutics - April 13, 2017 Category: Drugs & Pharmacology Source Type: research

Modeling of feed-forward control using the partial least squares regression method in the tablet compression process
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Yusuke Hattori, Makoto Otsuka In the pharmaceutical industry, the implementation of continuous manufacturing has been widely promoted in lieu of the traditional batch manufacturing approach. More specially, in recent years, the innovative concept of feed-forward control has been introduced in relation to process analytical technology. In the present study, we successfully developed a feed-forward control model for the tablet compression process by integrating data obtained from near-infrared (NIR) spectra a...
Source: International Journal of Pharmaceutics - April 13, 2017 Category: Drugs & Pharmacology Source Type: research

PEGylated composite nanoparticles of PLGA and polyethylenimine for safe and efficient delivery of pDNA to lungs
This study demonstrates that a multidisciplinary approach may enable the local delivery of pDNA to lung tissue for effective treatment of deadly lung diseases. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - April 13, 2017 Category: Drugs & Pharmacology Source Type: research

Targeted delivery of anticancer drugs to tumor vessels by use of liposomes modified with a peptide identified by phage biopanning with human endothelial progenitor cells
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Tatsuya Fukuta, Tomohiro Asai, Yuri Kiyokawa, Takashi Nakada, Koji Bessyo-Hirashima, Natsuki Fukaya, Kenji Hyodo, Kazuma Takase, Hiroshi Kikuchi, Naoto Oku As tumor angiogenic vessels are critical for tumor growth and express different molecules on their surface from those on normal vessels, these vessels are expected to be an ideal target for anticancer drug delivery systems. It was previously reported that endothelial progenitor cells (EPCs) are involved in angiogenesis, tumor growth, and metastasis, and ...
Source: International Journal of Pharmaceutics - April 12, 2017 Category: Drugs & Pharmacology Source Type: research

Tablet compression tooling – Impact of punch face edge modification
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Parthiban Anbalagan, Paul Wan Sia Heng, Celine Valeria Liew The influence of punch face edge geometry modification on tablet compression and the properties of the resultant tablets produced on a rotary press were investigated. The results revealed that tablets produced from the punches with radius edge face geometry consistently displayed better physical quality; higher tensile strength and lower capping tendency. Modification of the angled edge of the bevel face to the curved edge of the radius face, enabl...
Source: International Journal of Pharmaceutics - April 12, 2017 Category: Drugs & Pharmacology Source Type: research

Dry powder inhaler performance of spray dried mannitol with tailored surface morphologies as carrier and salbutamol sulphate
This study utilises particle-engineered mannitol as an alternative carrier to discover the effect of mannitol carrier particle properties like particle shape, surface roughness, flowability or particle size on aerodynamic performance during inhalation. Spray drying as a technique to accurately control those properties was chosen for the generation of carrier sizes between 50 and 80 μm and different morphologies and therefore various carrier flowabilities. A set of these carriers has then been blended with different spray dried and jet-milled qualities of salbutamol sulphate as model drug to examine the influence of carr...
Source: International Journal of Pharmaceutics - April 12, 2017 Category: Drugs & Pharmacology Source Type: research

Computational and experimental approaches for development of methotrexate nanosuspensions by bottom-up nanoprecipitation
In this study, methotrexate (MTX) nanosuspensions were prepared using a bottom-up process based on acid-base neutralization reactions. Computational studies were performed to determine structural and electronic properties for isolated molecules and molecular clusters in order to evaluate the mechanism of MTX nanoparticle formation. Computational results indicated that the clusters in zwitterionic and cationic states presented larger dimensions and higher energies of interaction between MTX molecules, which favored aggregation. In contrast, the clusters in the anionic state exhibited lower energies of interaction, indicatin...
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Dermal absorption behavior of fluorescent molecules in nanoparticles on human and porcine skin models
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Nir Debotton, Amit Badihi, Mano Robinpour, Claes D. Enk, Simon Benita The percutaneous passage of poorly skin absorbed molecules can be improved using nanocarriers, particularly biodegradable polymeric nanospheres (NSs) or nanocapsules (NCs). However, penetration of the encapsulated molecules may be affected by other factors than the nanocarrier properties. To gain insight information on the skin absorption of two fluorescent cargos, DiIC18(5) and coumarin-6 were incorporated in NSs or NCs and topically app...
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

The effect of thermosensitive liposomal formulations on loading and release of high molecular weight biomolecules
The objective of this study was to investigate the influence of the thermosensitive liposomal formulation on the encapsulation and release of low and high molecular weight hydrophilic drugs, in order to identify the key parameters to control during nanocarrier design, depending on the specific drug delivery application. Thermosensitive liposomes with different formulations were prepared through the combinations of different lipids, including dipalmitoylphosphatidylcholine (DPPC), distearoylphosphatidylcholine (DSPC), cholesterol (Chol), 1-palmitoyl-2-hydroxy-sn-glycero-3-phosphocholine (P-Lyso-PC), and the PEGylated lipid ...
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Rapamycin nanoparticles localize in diseased lung vasculature and prevent pulmonary arterial hypertension
This study demonstrates the potential for nanoparticles to significantly impact PAH through site-specific delivery of therapeutics. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Nanocrystal formulations of a poorly soluble drug. 2. Evaluation of nanocrystal liver uptake and distribution after intravenous administration to mice
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Kalle Sigfridsson, Pia Skantze, Urban Skantze, Lena Svensson, Lars Löfgren, Pär Nordell, Erik Michaëlsson, Bård Smedsrød, Britt Fuglesteg, Kjetil Elvevold, Lennart Lindfors A stabilized high drug load intravenous formulation could allow compounds with less optimal pharmacokinetic profiles to be developed. Polyethylene glycol (PEG)-ylation is a frequently used strategy for particle delivery systems to avoid the liver, thereby extending blood circulation time. The present work repo...
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Effect of surfactant chain length on drug release kinetics from microemulsion-laden contact lenses
This study revealed the correlation between the stability of microemulsion and the release kinetics of drugs from contact lenses. Thus, it was inferred that the stable microemulsion batches sustained the release of hydrophobic drugs, such as cyclosporine from contact lenses for an extended period of time without altering critical lens properties. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

A microhydrodynamic rationale for selection of bead size in preparation of drug nanosuspensions via wet stirred media milling
This study aims to establish such rationale by investigating the impact of bead size at various stirrer speeds on the drug breakage kinetics via a microhydrodynamic model. To this end, stable suspensions of griseofulvin, a model BCS Class II drug, were prepared using hydroxypropyl cellulose and sodium dodecyl sulfate. The suspensions were milled at four different stirrer speeds (1000–4000rpm) using various sizes (50–1500μm) of zirconia beads. Laser diffraction, SEM, and XRPD were used for characterization. Our results suggest that there is an optimal bead size that achieves fastest breakage at each stirrer s...
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Development of extended-voyaging anti-oxidant Linked Amphiphilic Polymeric Nanomicelles for Anti-Tuberculosis Drug Delivery
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Rajendran Amarnath Praphakar, Murugan A. Munusamy, Mariappan Rajan Amphiphilic chitosan-graft-poly(caprolactone)/(ferulic acid) (CS-g-PCL/FA) multi-co-polymers were fabricated by microwave-assisted ring opening polymerization followed by an 1-ethyl-3-(3-dimethyl-aminopropyl) carbodiimide (EDC)-mediated coupling reaction and characterized by Fourier transformed infrared (FTIR) spectroscopy. Graft copolymers self-assembled into nanomicelles, and were able to incorporate rifampicin (RF) into their hydrophobic ...
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Production and characterization of a PEGylated derivative of recombinant human deoxyribonuclease I for cystic fibrosis therapy
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Marie-Julie Guichard, Harshad P. Patil, Salome Juliette Koussoroplis, Ruddy Wattiez, Teresinha Leal, Rita Vanbever Recombinant human deoxyribonuclease I (rhDNase) is the mucolytic agent most widely used for the treatment of respiratory disease in cystic fibrosis. However, rhDNase is rapidly cleared from the lungs which implies a high dosing frequency and limited patient adherence. The aim of this study was to produce a long-acting PEGylated derivative of rhDNase presenting a preserved enzymatic activity. Si...
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Ganoderma lucidum polysaccharide loaded sodium alginate micro-particles prepared via electrospraying in controlled deposition environments
In this study, GLP loaded sodium alginate (NaAlg) micro-particles (size range 225–355μm) were generated using the electrospray (ES) process. The loading capacity and encapsulation efficiency of GLP for composite particles (collected at different temperatures) were ∼23% and 71%, respectively. The collection substrate (CaCl2, 1–20w/v%) concentration was explored and preliminary findings indicated a 10w/v% solution to be optimal. The process was further modified by manipulating the collection environment temperature (∼25 to 50°C). Based on this, NaAlg/GLP micro-particles were engineered with variabl...
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Solid-state transformations of ribavirin as a result of high-shear mechanical processing
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Dipy M. Vasa, Peter L.D. Wildfong Ribavirin (C8H12N4O5; anti-viral agent) was crystallized as two unique, phase-pure polymorphs (R-I and R-II). Calorimetrically determined isobaric heat capacities and heat of transition data were utilized to determine the solid-state transition temperature (Ttr ), confirming enantiotropism, while R-I was determined to be kinetically stable at ambient temperature. Unprocessed samples of the low Tm polymorph, R-II, did not convert into R-I when held isothermally well above Tt...
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Effects of amine modification of mesoporous magnesium carbonate on controlled drug release
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Maria Vall, Peng Zhang, Ao Gao, Sara Frykstrand, Ocean Cheung, Maria Strømme (3-Aminopropyl)triethoxysilane (APTES) was used to modify the surface of mesoporous magnesium carbonate (MMC). The as-synthesized MMC had an average pore diameter of ∼5nm, but amine grafting occurred preferentially on the walls of the largest MMC pores. Analysis of ibuprofen (IBU) loading and release showed that IBU remained stable in the amorphous phase in all the MMC and modified MMC samples. The kinetics of IBU releas...
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Effects of wet-granulation process parameters on the dissolution and physical stability of a solid dispersion
This study investigated how the process parameters of wet-granulation affect the properties of solid dispersions (SDs), such as dissolution and physical stability. SDs of nilvadipine (NIL) and hypromellose prepared by spray-drying were wet-granulated and dried under various conditions. The NIL concentration at 4h and area under the curve from dissolution tests were taken to indicate dissolution. Then, the NIL crystallinity calculated from powder X-ray diffraction patterns of SD granules stored at 60°C for 3 months was evaluated to indicate physical stability. A statistical analysis revealed that the amount of granulati...
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Indomethacin-containing interpolyelectrolyte complexes based on Eudragit ® E PO/S 100 copolymers as a novel drug delivery system
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Rouslan I. Moustafine, Alexander Y. Sitenkov, Alexandra V. Bukhovets, Shamil F. Nasibullin, Bernard Appeltans, Tatiana V. Kabanova, Vitaliy V. Khutoryanskiy, Guy Van den Mooter Potential applications of a novel system composed of two oppositely-charged (meth)acrylate copolymers, Eudragit® ЕРО (EPO) and Eudragit® S100 (S100), loaded with indomethacin (IND) in oral drug delivery were evaluated. The particles based on drug-interpolyelectrolyte complexes (DIPEC), (EPO-IND)/S100, were prepared by mixi...
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Efficient transfection of Xenobiotic Responsive Element-biosensor plasmid using diether lipid and phosphatidylcholine liposomes in differentiated HepaRG cells
In conclusion, we established a new efficient lipofection-mediated gene transfer in hepatocyte-like HepaRG cells opening new perspectives in drug evaluation relying on xenobiotic inducible biosensor plasmids. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Rational approach for design and evaluation of anti-aggregation agents for protein stabilization: A case study of trehalose phenylalaninate
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Smita S. Kale, Krishnacharya G. Akamanchi The present work introduces new anti-aggregation agent (AAA) derived through our new approach for design and evaluation of anti-aggregation agent as a multi-purpose excipient to combat protein aggregation. Therapeutic proteins undergo aggregation due to even minor changes in environmental conditions like temperature, pH, shear and stress. Excipients play a vital role in prevention of aggregation. To stabilize a protein formulation different classes of excipients are...
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Dehydroascorbate-derivatized chitosan particles for targeting antimalarial agents to infected erythrocytes
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Hasham Shafi, D.V. Siva Reddy, Tabassum Khan, Rajeev Ranjan, Ashish Srivastava, Suniti Vaishya, Tanuj Sharma, Mohammad Imran Siddiqui, Saman Habib, Amit Misra The mammalian glucose transporter GLUT-1 and Plasmodium falciparum hexose transporter PfHT1 are overexpressed on human RBC infected with the parasite (iRBC), presumably for enhanced glucose uptake. Dehydroascorbic acid (DHA) competes out glucose in GLUT-1 binding. We prepared particles containing chloroquine phosphate using novel derivatives of chitos...
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Delivery of doxorubicin-loaded PLGA nanoparticles into U87 human glioblastoma cells
The objective of the present study is the elucidation of the mechanism by which the poloxamer 188-coated nanoparticles then enter the brain tumor cells. Their intracellular fate, therefore, was investigated using the U87 human glioma cell line. The main mechanism of the PLGA nanoparticle internalization by U87 cells was clathrin-mediated endocytosis. Within 1h free doxorubicin was released from late endosomes and could reach its target site, i.e. the DNA in the nuclei without degradation, whereas the PLGA nanoparticles, which were labeled with Cy5.5, still were observed in the endo-lysosomal compartment. These results demo...
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Influence of controlled ice nucleation on the freeze-drying of pharmaceutical products: the secondary drying step
In conclusion, the control of freezing was beneficial to the total drying time reduction, vial-to-vial homogeneity and allowed a better control of product inhomogeneity. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Gaining insight into tablet capping tendency from compaction simulation
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Shubhajit Paul, Changquan Calvin Sun Capping or lamination is an unsolved common problem in tablet manufacturing. Knowledge gaps remain despite an enormous amount of effort made in the past to better understand the tablet capping/lamination phenomenon. Using acetaminophen – containing formulations, we examined the potential use of a compaction simulator as a material-sparing tool to predict capping occurrence under commercial tableting conditions. Systematical analyses of the in-die compaction data le...
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Tandem-multimeric F3-gelonin fusion toxins for enhanced anti-cancer activity for prostate cancer treatment
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Meong Cheol Shin, Kyoung Ah Min, Heesun Cheong, Cheol Moon, Yongzhuo Huang, Huining He, Victor C. Yang Despite significant progress in prostate cancer treatment, yet, it remains the leading diagnosed cancer and is responsible for high incidence of cancer related deaths in the U.S. Because of the insufficient efficacy of small molecule anti-cancer drugs, significant interest has been drawn to more potent macromolecular agents such as gelonin, a plant-derived ribosome inactivating protein (RIP) that efficient...
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Experimental determination of residence time distribution in continuous dry granulation
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Haress Mangal, Peter Kleinebudde With increasing importance of continuous manufacturing, the interest in integrating dry granulation into a continuous manufacturing line is growing. Residence time distribution measurements are of importance as they provide information about duration of materials within the process. These data enable traceability and are highly beneficial for developing control strategies. A digital image analysis system was used to determine the residence time distribution of two materials ...
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Development of medicated foams that combine incompatible hydrophilic and lipophilic drugs for psoriasis treatment
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Janja Mirtič, Foteini Papathanasiou, Žane Temova Rakuša, Mirjam GosencaMatjaž, Robert Roškar, Julijana Kristl The focus was on the development of medicated foam for incorporation of two incompatible active agents for psoriasis treatment; i.e., lipophilic cholecalciferol, and hydrophilic salicylic acid. Emphasis was given to formulation of a propellant-free foam, with sufficient foaming properties, physical and chemical stability, and low irritancy potential to maintain relevance for later t...
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

An approach for chemical stability during melt extrusion of a drug substance with a high melting point
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Abbe Haser, Siyuan Huang, Tony Listro, David White, Feng Zhang Poorly water-soluble drug substances that exhibit high melting points are difficult to process by melt extrusion due to chemical instability at high temperatures required for processing. The purpose of this study was to extrude meloxicam (melting point 255°C) by optimizing processing parameters and formulation composition. Five extrusion studies were performed: 1) design space, 2) impact of moisture, 3) impact of melt residence time, 4) spec...
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Prospects of siRNA applications in regenerative medicine
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Fatemeh Mottaghitalab, Ali Rastegari, Mehdi Farokhi, Rassoul Dinarvand, Hossein Hosseinkhani, Keng-Liang Ou, Daniel W. Pack, Chuanbin Mao, Meshkat Dinarvand, Yousef Fatahi, Fatemeh Atyabi Small interfering RNA (siRNA) has established its reputation in the field of tissue engineering owing to its ability to silence the proteins that inhibit tissue regeneration. siRNA is capable of regulating cellular behavior during tissue regeneration processes. The concept of using siRNA technology in regenerative medicine...
Source: International Journal of Pharmaceutics - April 11, 2017 Category: Drugs & Pharmacology Source Type: research

Deferoxamine-conjugated AgInS2 nanoparticles as new nanodrug for synergistic therapy for hepatocellular carcinoma
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Isara Phiwchai, Titipun Thongtem, Somchai Thongtem, Chalermchai Pilapong Herein, a new nanodrug that exhibits multi-therapeutic modalities for synergistic treatment of hepatocellular carcinoma is reported. The nanodrug is composed of carboxymethyl cellulose modified silver indium sulfide nanoparticle (CMC-AgInS2 NP, served as a source of reactive oxygen species) covalently linked with deferoxamine (DFO, served as iron chelating agent). The DFO/CMC-AgInS2 nanodrug was taken up by the HepG2 cell and accumulat...
Source: International Journal of Pharmaceutics - April 5, 2017 Category: Drugs & Pharmacology Source Type: research

Functionalized single-walled carbon nanotubes: cellular uptake, biodistribution and applications in drug delivery
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Zixian Li, Andre Luis Branco de Barros, Daniel Cristian Ferreira Soares, Sara Nicole Moss, Laleh Alisaraie The unique properties of single-walled carbon nanotubes (SWNTs) enable them to play important roles in many fields. One of their functional roles is to transport cargo into cell. SWNTs are able to traverse amphipathic cell membranes due to their large surface area, flexible interactions with cargo, customizable dimensions, and surface chemistry. The cargoes delivered by SWNTs include peptides, proteins...
Source: International Journal of Pharmaceutics - April 5, 2017 Category: Drugs & Pharmacology Source Type: research

Insight into the role of dual-ligand modification in low molecular weight heparin based nanocarrier for targeted delivery of doxorubicin
Publication date: 15 May 2017 Source:International Journal of Pharmaceutics, Volume 523, Issue 1 Author(s): Hongliang Du, Mengrui Liu, Aihua Yu, Jianbo Ji, Guangxi Zhai Low molecular weight heparin nanoparticles (LMWH) modified by glycyrrhetinic acid (GA) (LMWH-GA) and further decorated by lactobionic acid (LA) (LA-LMWH-GA) were reported as novel hepatocellular carcinoma (HPC)-targeted carriers to overcome multidrug resistance (MDR) of doxorubicin (DOX). The drug-loaded nanoparticles had negative charge of around −25mV and average size range of 70–170nm. These nanoparticles performed sustained drug release in ...
Source: International Journal of Pharmaceutics - April 2, 2017 Category: Drugs & Pharmacology Source Type: research