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Limiting the level of tertiary amines on polyamines leads to biocompatible nucleic acid vectors
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Margarida Isabel Simão Carlos, Kai Zheng, Natalie Garrett, Natrah Arifin, David G. Workman, Ilona Kubajewska, Abdulrahman A. Halwani, Julian Moger, Qi Zhang, Andreas G. Schätzlein, Ijeoma F. Uchegbu We have designed an efficient, synthetic nucleic acid vector, which is relatively non-toxic. [N-(2-ethylamino)-6-O-glycolchitosan – EAGC] polymers were 10–50 fold less toxic than Lipofectamine 2000, able to complex DNA, mRNA and siRNA into positively charged (zeta potential=+40 − 5...
Source: International Journal of Pharmaceutics - May 7, 2017 Category: Drugs & Pharmacology Source Type: research

Enhanced adhesion and in situ photothermal ablation of cancer cells in surface-functionalized electrospun microfiber scaffold with graphene oxide
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Nicolò Mauro, Cinzia Scialabba, Giovanna Pitarresi, Gaetano Giammona The physicochemical characteristics of a biomaterial surface highly affect the interaction with living cells. Recently, much attention has been focused on the adhesion properties of functional biomaterials toward cancer cells, since is expected to control metastatic spread of a tumor, which is related to good probability containing the progression of disease burden. Here, we designed an implantable poly(caprolactone)-based electros...
Source: International Journal of Pharmaceutics - May 7, 2017 Category: Drugs & Pharmacology Source Type: research

Formulation and characterisation of dissolving microneedles for the transdermal delivery of therapeutic peptides
This study presents a dissolving MN system composed of polyvinylpyrrolidone (PVP) and trehalose to encapsulate active pharmaceutical peptides within the MN matrix. Rapid systemic delivery is then achieved once the needles have penetrated the SC and dissolved in the interstitial fluid of the skin. A variety of characterisation techniques were carried out to determine the optimum formulation. A model peptide, polymyxin B, was then incorporated into the MN system and delivered through porcine skin. In addition, the activity of the model drug was monitored during all stages of the formulation process. Graphical abstract (Sourc...
Source: International Journal of Pharmaceutics - May 7, 2017 Category: Drugs & Pharmacology Source Type: research

Montmorillonite-lipid hybrid carriers for ionizable and neutral poorly water-soluble drugs: Formulation, characterization and in vitro lipolysis studies
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Tahnee J. Dening, Shasha Rao, Nicky Thomas, Clive A. Prestidge Lipid-based formulations (LBFs) are a popular strategy for enhancing the gastrointestinal solubilization and absorption of poorly water-soluble drugs. In light of this, montmorillonite-lipid hybrid (MLH) particles, composed of medium-chain triglycerides, lecithin and montmorillonite clay platelets, have been developed as a novel solid-state LBF. Owing to the unique charge properties of montmorillonite, whereby the clay platelet surfaces carry a...
Source: International Journal of Pharmaceutics - May 5, 2017 Category: Drugs & Pharmacology Source Type: research

Improvement of the physicochemical properties of Co-amorphous naproxen-indomethacin by naproxen-sodium
In conclusion, the physical stability as well as the dissolution rate was significantly improved if partial or full exchange of naproxen by its sodium salt was performed, which may present a general optimization method to improve co-amorphous systems. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 5, 2017 Category: Drugs & Pharmacology Source Type: research

Use of acidifier and solubilizer in tadalafil solid dispersion to enhance the in vitro dissolution and oral bioavailability in rats
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Jin-Seok Choi, Soon-Hyung Kwon, Sang-Eun Lee, Woo Suk Jang, Jong Chan Byeon, Hyeong Mo Jeong, Jeong-Sook Park The purpose of this study is to improve the solubility, in vitro dissolution, and oral bioavailability in rats of tadalafil (TDF) by using SD technique with a weak acid and a copolymer. TDF-SD was prepared via solvent evaporation, coupled with the incorporation of an acidifier and solubilizer. Tartaric acid enhanced the solubility of TDF over 5-fold in DW, and Soluplus® enhanced the solubility ...
Source: International Journal of Pharmaceutics - May 4, 2017 Category: Drugs & Pharmacology Source Type: research

In vivo distribution of zoledronic acid in a bisphosphonate-metal complex-based nanoparticle formulation synthesized by a reverse microemulsion method
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Xu Li, Youssef W. Naguib, Zhengrong Cui Bisphosphonates are used to treat bone diseases such as osteoporosis and cancer-induced bone pain and fractures. It is thought that modifying the pharmacokinetics and biodistribution profiles of bisphosphonates (i.e. rapid renal clearance and extensive bone absorption) will not only reduce their side effects, but also expand their clinical applications to extraskeletal tissues. In the present work, using zoledronic acid (Zol) and calcium as model bisphosphonate and m...
Source: International Journal of Pharmaceutics - May 4, 2017 Category: Drugs & Pharmacology Source Type: research

Improvement of skin whitening agents efficiency through encapsulation: Current state of knowledge
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Elissa Ephrem, Hamid Elaissari, Hélène Greige-Gerges Hyperpigmentation is one of the most common skin disorder that affects both men and women of all ethnic groups, caused by several factors, such as UV exposure and skin inflammation. Topical whitening agents were found to be the best and the least aggressive therapy for treating hyperpigmentation compared to instrumental approaches. However, topical treatment faces several obstacles due to the low stability of the whitening agents. Therefore...
Source: International Journal of Pharmaceutics - May 4, 2017 Category: Drugs & Pharmacology Source Type: research

Towards Hypoxia-responsive Drug-eluting Embolization Beads
Publication date: 30 May 2017 Source:International Journal of Pharmaceutics, Volume 524, Issues 1–2 Author(s): Koorosh Ashrafi, Clare L. Heaysman, Gary J. Phillips, Andrew W. Lloyd, Andrew L. Lewis Drug release from chemoembolization microspheres stimulated by the presence of a chemically reducing environment may provide benefits for targeting drug resistant and metastatic hypoxic tumours. A water-soluble disulfide-based bifunctional cross-linker bis(acryloyl)-(l)-cystine (BALC) was synthesised, characterised and incorporated into a modified poly(vinyl) alcohol (PVA) hydrogel beads at varying concentrations using re...
Source: International Journal of Pharmaceutics - May 3, 2017 Category: Drugs & Pharmacology Source Type: research

Non-destructive prediction of enteric coating layer thickness and drug dissolution rate by near-infrared spectroscopy and X-ray computed tomography
Publication date: 15 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 1 Author(s): Aoi Ariyasu, Yusuke Hattori, Makoto Otsuka The coating layer thickness of enteric-coated tablets is a key factor that determines the drug dissolution rate from the tablet. Near-infrared spectroscopy (NIRS) enables non-destructive and quick measurement of the coating layer thickness, and thus allows the investigation of the relation between enteric coating layer thickness and drug dissolution rate. Two marketed products of aspirin enteric-coated tablets were used in this study, and the correlation between the predic...
Source: International Journal of Pharmaceutics - May 3, 2017 Category: Drugs & Pharmacology Source Type: research

Inhibitory effect of emulsifiers in sedds on protease activity: Just an illusion?
Conclusion The present study revealed that commonly used emulsifiers in SEDDS do not have inhibitory properties on the proteolytic activity of trypsin and α-chymotrypsin. Moreover, it was demonstrated that the incorporation of emulsifiers with inhibitory properties towards trypsin and α-chymotrypsin in SEDDS play a minor role in the protection of embedded drugs from enzymatic degradation. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - May 3, 2017 Category: Drugs & Pharmacology Source Type: research

Mathematical modelling of liquid transport in swelling pharmaceutical immediate release tablets
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Daniel Markl, Samy Yassin, D. Ian Wilson, Daniel J. Goodwin, Andrew Anderson, J. Axel Zeitler Oral dosage forms are an integral part of modern health care and account for the majority of drug delivery systems. Traditionally the analysis of the dissolution behaviour of a dosage form is used as the key parameter to assess the performance of a drug product. However, understanding the mechanisms of disintegration is of critical importance to improve the quality of drug delivery systems. The disintegration perf...
Source: International Journal of Pharmaceutics - May 3, 2017 Category: Drugs & Pharmacology Source Type: research

A novel approach to study the pMDI plume using an infrared camera and to evaluate the aerodynamic properties after varying the time between actuations
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Nitesh K. Kunda, Julia Hautmann, Sebastián E. Godoy, Patricia Marshik, Ramesh Chand, Sanjay Krishna, Pavan Muttil Plume characteristics, such as temperature and velocity, emitted from pMDIs could significantly affect the dose delivered to the lung. Currently, high speed cameras and thermocouples are used separately to evaluate these parameters. We used a low-noise infrared camera to evaluate both the temperature and velocity of the emitted plume from pMDIs. Additionally, we investigated whether the ...
Source: International Journal of Pharmaceutics - May 2, 2017 Category: Drugs & Pharmacology Source Type: research

Introducing a novel gravitation-based high-velocity compaction analysis method for pharmaceutical powders
Publication date: 30 June 2017 Source:International Journal of Pharmaceutics, Volume 526, Issues 1–2 Author(s): Timo Tanner, Osmo Antikainen, Henrik Ehlers, Jouko Yliruusi With modern tableting machines large amounts of tablets are produced with high output. Consequently, methods to examine powder compression in a high-velocity setting are in demand. In the present study, a novel gravitation-based method was developed to examine powder compression. A steel bar is dropped on a punch to compress microcrystalline cellulose and starch samples inside the die. The distance of the bar is being read by a high-accuracy laser...
Source: International Journal of Pharmaceutics - May 2, 2017 Category: Drugs & Pharmacology Source Type: research

EXCI-CEST: Exploiting pharmaceutical excipients as MRI-CEST contrast agents for tumor imaging
Publication date: 15 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 1 Author(s): Dario Livio Longo, Fatima Zzahra Moustaghfir, Alexandre Zerbo, Lorena Consolino, Annasofia Anemone, Martina Bracesco, Silvio Aime Chemical Exchange Saturation Transfer (CEST) approach is a novel tool within magnetic resonance imaging (MRI) that allows visualization of molecules possessing exchangeable protons with water. Many molecules, employed as excipients for the formulation of finished drug products, are endowed with hydroxyl, amine or amide protons, thus can be exploitable as MRI-CEST contrast agents. Their h...
Source: International Journal of Pharmaceutics - April 30, 2017 Category: Drugs & Pharmacology Source Type: research

Optimization of critical quality attributes in continuous twin-screw wet granulation via design space validated with pilot scale experimental data
In this study, the influence of key process variables (screw speed, throughput and liquid to solid (L/S) ratio) of a continuous twin screw wet granulation (TSWG) was investigated using a central composite face-centered (CCF) experimental design method. Regression models were developed to predict the process responses (motor torque, granule residence time), granule properties (size distribution, volume average diameter, yield, relative width, flowability) and tablet properties (tensile strength). The effects of the three key process variables were analyzed via contour and interaction plots. The experimental results have dem...
Source: International Journal of Pharmaceutics - April 30, 2017 Category: Drugs & Pharmacology Source Type: research

Self-assembled liposomes of dual paclitaxel-phospholipid prodrug for anticancer therapy
In this report, a newly liposomal formulation of paclitaxel (PTX) based on dual paclitaxel succinate glycerophosphorylcholine (Di-PTX-GPC) prodrug was developed. The Di-PTX-GPC prodrug was synthesized by conjugating PTX with GPC through esterification under N,N′-carbonyldiimidazole (CDI) and 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) catalytic system. Di-PTX-GPC liposomes were prepared by thin film method and characterized by dynamic light scattering (DLS) and transmission electron microscope (TEM). The results indicated that the liposomes have an average diameter of 157.9nm with well-defined spherical morphology. In v...
Source: International Journal of Pharmaceutics - April 30, 2017 Category: Drugs & Pharmacology Source Type: research

Dual-functional nanoparticles for precise drug delivery to Alzheimer ’s disease lesions: Targeting mechanisms, pharmacodynamics and safety
In conclusion, TQNP was a valuable nanodevice for the precise delivery for biotechnological drugs to treat AD. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - April 29, 2017 Category: Drugs & Pharmacology Source Type: research

Development and physicochemical characterization of acetalated dextran aerosol particle systems for deep lung delivery
In this study, we developed and characterized pulmonary drug delivery aerosol microparticle systems based on spray-dried Ac-Dex with capabilities of (1) delivering therapeutics to the deep lung, (2) targeting the particles to a desired location within the lungs, and (3) releasing the therapeutics in a controlled fashion. Two types of Ac-Dex, with either rapid or slow degradation rates, were synthesized. Nanocomposite microparticle (nCmP) and microparticle (MP) systems were successfully formulated using both kinds of Ac-Dex as excipients and curcumin as a model drug. The resulting MP were collapsed spheres approximately 1&m...
Source: International Journal of Pharmaceutics - April 29, 2017 Category: Drugs & Pharmacology Source Type: research

Improved release of triamcinolone acetonide from medicated soft contact lenses loaded with drug nanosuspensions
Publication date: 15 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 1 Author(s): Eva García-Millán, Mónica Quintáns-Carballo, Francisco Javier Otero-Espinar Drug nanosuspensions (NSs) show a significant potential to improve loading and release properties of the poorly water soluble drug triamcinolone acetonide (TA) from poly(hydroxyethyl methacrylate) (pHEMA) soft contact lenses. In this work, TA NSs were developed by a controlled precipitation method using a fractional factorial Plackett–Burmann design. Poloxamer 407 (PL) and polyvinyl alcohol (PVA) as stabili...
Source: International Journal of Pharmaceutics - April 29, 2017 Category: Drugs & Pharmacology Source Type: research

Development of light-driven gas-forming liposomes for efficient tumor treatment
In this study, we report a gas-forming liposome containing 1H-1H-2H-perfluoro-1-hexene (PFH) and gold nanoparticles (AuNPs). These liposomes were rapidly destabilized by external near-infrared (NIR) light, as a result of the vaporization of PFH influenced by an AuNPs-mediated photothermal event. In particular, these liposomes showed the triggered release of the encapsulated d-(KLAKLAK)2 peptide drug. The experimental results demonstrated that the light-irradiated liposomes significantly enhanced in vitro photothermal and d-(KLAKLAK)2 peptide-mediated cell death of CAOV-3 tumor cells. Graphical abstract (Source: Internation...
Source: International Journal of Pharmaceutics - April 27, 2017 Category: Drugs & Pharmacology Source Type: research

Chitosan and hyaluronan coated liposomes for pulmonary administration of curcumin
Publication date: 15 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 1 Author(s): Maria Manconi, Maria Letizia Manca, Donatella Valenti, Elvira Escribano, Hervé Hillaireau, Anna Maria Fadda, Elias Fattal Aiming at improving the nebulization performances and lung antioxidant protection of curcumin, chitosan or hyaluronan-coated liposomes were prepared and their characteristics and performances were compared with that of uncoated liposomes. Curcumin loaded liposomes displayed a diameter lower than 100nm, the coating with both polymers led to a small increase of vesicle size around 130nm and...
Source: International Journal of Pharmaceutics - April 27, 2017 Category: Drugs & Pharmacology Source Type: research

Gastrointestinal behavior of itraconazole in humans – Part 1: Supersaturation from a solid dispersion and a cyclodextrin-based solution
This study evaluated the fasted state gastrointestinal behavior of the lipophilic drug itraconazole, orally administered to healthy volunteers as either a solid dispersion (Sporanox® capsules) or a cyclodextrin-based solution (Sporanox® solution). Following intake of the drug products, gastric and duodenal fluids were aspirated and analyzed for itraconazole concentration, total content and solubilizing capacity. Release of itraconazole from the solid dispersion generated high and metastable supersaturated levels in the stomach, but the dissolved fraction in the duodenum remained extremely low (median 2.5%). After i...
Source: International Journal of Pharmaceutics - April 27, 2017 Category: Drugs & Pharmacology Source Type: research

Tailoring the supramolecular structure of amphiphilic glycopolypeptide analogue toward liver targeted drug delivery systems
In this study, lactosylated pullulan-graft-arginine dendrons (LP-g-G3P) was synthesized using Huisgen azide-alkyne 1,3-dipolar cycloaddition between lactosylated pullulan and generation 3 arginine dendrons bearing Pbf and Boc groups on the periphery. Hydrophilic lactosylated pullulan was selected for amphiphilic modification, aiming at specific lectin recognition. Macromolecular structure of LP-g-G3P combined alkyl, aromatic, and peptide dendritic hydrophobic moieties and was able to self-assemble spontaneously into core-shell nanoarchitectures with small particle sizes and low polydispersity in the aqueous media, which wa...
Source: International Journal of Pharmaceutics - April 27, 2017 Category: Drugs & Pharmacology Source Type: research

Enhanced release of poorly water-soluble drugs from synergy between mesoporous magnesium carbonate and polymers
In this study, amorphous mesoporous magnesium carbonate (MMC) was used as a drug carrier to achieve supersaturation of tolfenamic acid and rimonabant, two drug compounds with low aqueous solubility. The potential synergy between MMC and hydroxypropyl methylcellulose (HPMC), a polymer commonly included as a precipitation inhibitor in drug delivery systems, was explored with the aim of extending the time that high supersaturation levels were maintained. Release was studied under physiological conditions using USP-2 dissolution baths. A new small-scale method was developed to enable measurement of the initial drug release occ...
Source: International Journal of Pharmaceutics - April 25, 2017 Category: Drugs & Pharmacology Source Type: research

Highly efficient treatment of aerobic vaginitis with simple acidic buffered gels: The importance of pH and buffers on the microenvironment of vaginas
Publication date: 15 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 1 Author(s): Xiaodong Sun, Haiying Qiu, Yiguang Jin Aerobic vaginitis (AV) leads to uterus deep infection or preterm birth. Antibacterial agents are not optimal therapeutics of AV. Here, we report a series of temperature-sensitive in situ forming acidic buffered gels for topical treatment of AV, involving lactate, acetate, and citrate gels at pH 3.5, 5.0, and 6.5. AV rat models were prepared following vaginal infection with Staphylococcus aureus and Escherichia coli. In vitro/in vivo studies of the buffered gels were performed ...
Source: International Journal of Pharmaceutics - April 25, 2017 Category: Drugs & Pharmacology Source Type: research

Surface modification of acetaminophen particles by atomic layer deposition
Publication date: 15 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 1 Author(s): Tommi O. Kääriäinen, Marianna Kemell, Marko Vehkamäki, Marja-Leena Kääriäinen, Alexandra Correia, Hélder A. Santos, Luis M. Bimbo, Jouni Hirvonen, Pekka Hoppu, Steven M. George, David C. Cameron, Mikko Ritala, Markku Leskelä Active pharmaceutical ingredients (APIs) are predominantly organic solid powders. Due to their bulk properties many APIs require processing to improve pharmaceutical formulation and manufacturing in the preparation for various drug dosage forms. Im...
Source: International Journal of Pharmaceutics - April 23, 2017 Category: Drugs & Pharmacology Source Type: research

Unmet clinical needs in the treatment of systemic fungal infections: The role of amphotericin B and drug targeting
Publication date: 15 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 1 Author(s): Raquel Fernández-García, Esther de Pablo, María Paloma Ballesteros, Dolores R. Serrano Recently an increase in both the prevalence and incidence of invasive fungal infections have been reported. The number of fungal species that can cause systemic mycoses are higher and current antifungal therapies are still far from ideal. The emergence of antifungal resistances has a major clinical impact when using azoles and echinocandins leading to possible treatment failure and ultimately putting the pati...
Source: International Journal of Pharmaceutics - April 23, 2017 Category: Drugs & Pharmacology Source Type: research

Feasibility of mini-tablets as a flexible drug delivery tool
Publication date: 15 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 1 Author(s): Biplob Mitra, Jessica Chang, Sy-Juen Wu, Chad N. Wolfe, Robert L. Ternik, Thomas Z. Gunter, Michael C. Victor Mini-tablets have potential applications as a flexible drug delivery tool in addition to their generally perceived use as multi-particulates. That is, mini-tablets could provide flexibility in dose finding studies and/or allow for combination therapies in the clinic. Moreover, mini-tablets with well controlled quality attributes could be a prudent choice for administering solid dosage forms as a single unit...
Source: International Journal of Pharmaceutics - April 23, 2017 Category: Drugs & Pharmacology Source Type: research

A novel serum-stable liver targeted cytotoxic system using valerate-conjugated chitosan nanoparticles surface decorated with glycyrrhizin
Publication date: 15 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 1 Author(s): Eman M. El-Marakby, Rania M. Hathout, Ismail Taha, Samar Mansour, Nahed D. Mortada The aim of this study was to target a naturally chemotherapeutic agent: ferulic acid to the liver using a biocompatible and an in vivo stable carrier. Accordingly, chitosan as a biopolymer was modified using a hydrophobic moiety and valeric acid in order to increase its in vivo stability. The structure of the newly synthesized product was confirmed using FT-IR and NMR techniques together with the ninhydrin assay. Ferulic acid was con...
Source: International Journal of Pharmaceutics - April 22, 2017 Category: Drugs & Pharmacology Source Type: research

Preparation and characterization of lipid nanoparticle/pDNA complexes for STAT3 downregulation and overcoming chemotherapy resistance in lung cancer cells
Publication date: 15 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 1 Author(s): Mustafa Kotmakçı, Vildan Bozok Çetintaş, A. Gülten Kantarcı Developments in the field of molecular oncology have revealed that resistance to chemotherapeutics is acqured through several mechanisms including overexpression of common oncogenic proteins. Signal Transducer and Activator of Transcription 3 (STAT3) is one of these oncogenes that is overexpressed in many cancer types. RNA interference (RNAi) is proven powerful tool for downregulating STAT3, allowing re-sensitization of resistant canc...
Source: International Journal of Pharmaceutics - April 22, 2017 Category: Drugs & Pharmacology Source Type: research

Laser-treated electrospun fibers loaded with nano-hydroxyapatite for bone tissue engineering
Publication date: 15 June 2017 Source:International Journal of Pharmaceutics, Volume 525, Issue 1 Author(s): Javier Aragon, Nuria Navascues, Gracia Mendoza, Silvia Irusta Core-shell polycaprolactone/polycaprolactone (PCL/PCL) and polycaprolactone/polyvinyl acetate (PCL/PVAc) electrospun fibers loaded with synthesized nanohydroxyapatite (HAn) were lased treated to create microporosity. The prepared materials were characterized by XRD, FTIR, TEM and SEM. Uniform and randomly oriented beadless fibrous structures were obtained in all cases. Fibers diameters were in the 150–300nm range. Needle-like HAn nanoparticles with...
Source: International Journal of Pharmaceutics - April 22, 2017 Category: Drugs & Pharmacology Source Type: research

Enhanced anti-rheumatic activity of methotrexate-entrapped ultradeformable liposomal gel in adjuvant-induced arthritis rat model
In conclusion, the developed MTX-UDLs-gel has a great potential for effective delivery of MTX into the inflamed joints in rheumatoid arthritis. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - April 22, 2017 Category: Drugs & Pharmacology Source Type: research

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