Lipid- and polymer-based plexes as therapeutic carriers for bioactive molecules
Publication date: Available online 12 January 2019Source: International Journal of PharmaceuticsAuthor(s): Pravin Shende, Narayan Ture, R.S. Gaud, F. TrottaAbstractRecently, promising strategies of plexes include the complexation of nucleic acids with lipids (lipoplexes) and different kinds of polymers (polyplexes) for delivery of actives and genetic material in abnormal conditions like cancer, cystic fibrosis and genetic disorders. The present review article focuses on the comparative aspects of lipoplexes and polyplexes associated with molecular structure, cellular transportation and formulation aspects. The major advant...
Source: International Journal of Pharmaceutics - January 12, 2019 Category: Drugs & Pharmacology Source Type: research

Effects of pH of processing-medium on re-dispersion of spray dried, crystalline nanoparticles of pure naproxen
Publication date: Available online 12 January 2019Source: International Journal of PharmaceuticsAuthor(s): Veronika Braig, Christoph Konnerth, Wolfgang Peukert, Geoffrey LeeAbstractCrystalline nanodispersions of naproxen stabilized with hydroxypropyl cellulose were prepared at different pHs both below and above the pKa of the drug. After spray drying together with lactose, the measured particle size of the rehydrated dispersions using laser light scattering/Mie analysis was found to depend strongly on the pH of the original, processed nanodispersion. The pH-dependent solubility of this weak acid resulted in formation of a ...
Source: International Journal of Pharmaceutics - January 12, 2019 Category: Drugs & Pharmacology Source Type: research

Tunable Sustained Release Drug Delivery System Based on Mononuclear Aqueous Core-Polymer Shell Microcapsules
Publication date: Available online 12 January 2019Source: International Journal of PharmaceuticsAuthor(s): Samer R. Abulateefeh, Mahmoud Y. Alkawareek, Alaaldin M. AlkilanyAbstractPoly(D,L-lactide-co-glycolide) (PLGA) and poly(D,L-lactide) (PLA) polymers were used successfully in the preparation of polymer shell microcapsules with mononuclear aqueous cores by the internal phase separation method. These microcapsules were prepared with varying amounts of polymer and water and loaded with fluorescein sodium as a model water soluble drug. Evaluation of drug loading and encapsulation efficiency reveals an optimum polymer to wa...
Source: International Journal of Pharmaceutics - January 12, 2019 Category: Drugs & Pharmacology Source Type: research

Dimensional analysis of in-situ crystal formation in droplet undergoing rapid dehydration
Publication date: Available online 12 January 2019Source: International Journal of PharmaceuticsAuthor(s): S. Shakiba, S. Mansouri, C. Selomulya, M.W. WooAbstractThe surface structure of the crystalline particles affects the functionality of the particles in drug delivery. Prediction of the final structure of particles that crystallize easily within the spray dryer is of interests of many applications. A theoretical framework was developed for the prediction of crystal structure precipitating on the surface of the particle. Mannitol was produced under different processing conditions in order to validate the theoretical mod...
Source: International Journal of Pharmaceutics - January 12, 2019 Category: Drugs & Pharmacology Source Type: research

Comparison of ice fog methods and monitoring of controlled nucleation success after freeze-drying
Publication date: 10 March 2019Source: International Journal of Pharmaceutics, Volume 558Author(s): Ilona Vollrath, Wolfgang Friess, Angelika Freitag, Andrea Hawe, Gerhard WinterAbstractImproving freeze-drying processes regarding drying time and batch homogeneity is subject of ongoing research work. In this context, controlled nucleation raised great expectations. However, practically we face some challenges, e.g. how to non-destructively monitor successfully performed controlled nucleation. The question if different controlled nucleation methods lead to comparable products, as not every method can easily be implemented in...
Source: International Journal of Pharmaceutics - January 12, 2019 Category: Drugs & Pharmacology Source Type: research

Albumin fusion improves the pharmacokinetics and in Vivo antitumor efficacy of canine interferon gamma
In this study, N- and C-terminal canine albumin fusions with canine IFN-γ were expressed in the baculovirus expression system. The fusion proteins stimulated Stat1 phosphorylation at levels similar to that of the recombinant IFN. The antiviral, anti-proliferative and promote apoptosis activity of CSA-IFN-γ was lower than IFN-γ-CSA and both were less than that of recombinant IFN-γ. In vivo pharmacokinetics demonstrated a significantly longer half-life for CSA-IFN-γ (21.73 h) than for IFN-γ-CSA (6.51 h) and canine reIFN-γ (2.22 h) in Wistar rats. CSA-IFN-γ was also more effecti...
Source: International Journal of Pharmaceutics - January 10, 2019 Category: Drugs & Pharmacology Source Type: research

Preparation of pH-responsive DOX-loaded chitosan nanoparticles using supercritical assisted atomization with an enhanced mixer
Publication date: Available online 9 January 2019Source: International Journal of PharmaceuticsAuthor(s): Hu-Hong Peng, Dong-Xiao Hong, Yi-Xin Guan, Shan-Jing YaoAbstractChemotherapeutics are used extensively in cancer and encapsulating the drug in nanoparticles is an effective method to enhance therapeutic efficacy and reduce side effect. In this work, DOX-loaded chitosan nanoparticles were prepared using supercritical fluid assisted atomization introduced by a hydrodynamic cavitation mixer (SAA-HCM) from aqueous solution. The influences of solution concentration, CO2/solution ratio, mixer pressure, chitosan/DOX ratio and...
Source: International Journal of Pharmaceutics - January 10, 2019 Category: Drugs & Pharmacology Source Type: research

Immobilization of antimicrobial and anti-quorum sensing enzymes onto GMA-grafted poly(vinyl chloride) catheters
Publication date: Available online 9 January 2019Source: International Journal of PharmaceuticsAuthor(s): Alejandro Costoya, Luis E. Velázquez Becerra, H. Iván Meléndez-Ortiz, Luis Díaz-Gómez, Celia Mayer, Ana Otero, Angel Concheiro, Emilio Bucio, Carmen Alvarez-LorenzoAbstractCatheter-associated infections still represent a challenging thread because of the likelihood of biofilm formation. The aim of this work was the surface modification of catheters to immobilize lysozyme and acylase under mild conditions while preserving antimicrobial and anti-quorum sensing performances. Glycidyl met...
Source: International Journal of Pharmaceutics - January 10, 2019 Category: Drugs & Pharmacology Source Type: research

A Novel Antimicrobial Peptide-Derived Vehicle for Oligodeoxynucleotide Delivery to Inhibit TNF-α Expression
This study provides a useful strategy of peptide vehicle design, which may facilitate the delivery of not only ODN but also other oligonucleotides, including siRNA and miRNA, to promote gene silence application.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 10, 2019 Category: Drugs & Pharmacology Source Type: research

Smartphone-based Ellman’s colourimetric methods for the analysis of D-penicillamine formulation and thiolated polymer
In conclusion, smartphone-based colourimetry has been proved to be a reliable, fast, simple and affordable alternative means for the analysis of d-penicillamine and cysteine-conjugated polymer and can be potentially applied to other thiol-containing drugs and excipients.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 10, 2019 Category: Drugs & Pharmacology Source Type: research

Evaluation of Dermal Tissue Regeneration Using Resveratrol Loaded Fibrous Matrix in a Preclinical Mouse Model of Full-Thickness Ischemic Wound
Publication date: Available online 9 January 2019Source: International Journal of PharmaceuticsAuthor(s): Rajesh Lakhsmanan, Jacob Campbell, Gopi Ukani, André O'Reilly Beringhs, Vaithinathan Selvaraju, Mahesh Thirunavukkarasu, Xiuling Lu, J. Alexander Palesty, Nilanjana MaulikAbstractThe complete loss of dermal tissue due to ischemia is a serious challenge facing clinicians. Frequently, the failure of wound healing is due to ischemic conditions prevailing at the site of damaged tissue. Restoration of lost vasculature at the ischemic site can be achieved by supplementing proangiogenic stimuli through an engineered sc...
Source: International Journal of Pharmaceutics - January 10, 2019 Category: Drugs & Pharmacology Source Type: research

Assessment of Doxorubicin Delivery Devices based on tailored bare Polycaprolactone against Glioblastoma
Publication date: Available online 9 January 2019Source: International Journal of PharmaceuticsAuthor(s): Enrique Niza, José A. Castro-Osma, Inmaculada Posadas, Carlos Alonso-Moreno, Iván Bravo, Andrés Garzón, Jesús Canales-Vázquez, Valentín Ceña, Agustín Lara-Sánchez, José Albaladejo, Antonio OteroAbstractBare polycaprolactones with controlled molar mass and dispersity were employed to manufacture biodegradable devices, which were applied for doxorubicin delivery in glioblastoma. Micro- and nanoscale devices were prepared by emulsion formation or...
Source: International Journal of Pharmaceutics - January 10, 2019 Category: Drugs & Pharmacology Source Type: research

Lipids and polymers in pharmaceutical technology: lifelong companions
Publication date: Available online 9 January 2019Source: International Journal of PharmaceuticsAuthor(s): Juergen Siepmann, Amina Faham, Sophie-Dorothée Clas, Ben J. Boyd, Vincent Jannin, Andreas Bernkop-Schnürch, Hang Zhao, Sébastien Lecommandoux, James C. Evans, Christine Allen, Olivia M. Merkel, Gabriella Costabile, Morgan R. Alexander, Ricky D. Wildman, Clive J. Roberts, Jean-Christophe LerouxAbstractIn pharmaceutical technology, lipids and polymers are considered pillar excipients for the fabrication of most dosage forms, irrespective of the administration route. They play various roles ranging from...
Source: International Journal of Pharmaceutics - January 10, 2019 Category: Drugs & Pharmacology Source Type: research

A Thermo-Responsive and Self-Healing Liposome-in-Hydrogel System as an Antitubercular Drug Carrier for Localized Bone Tuberculosis Therapy
Publication date: Available online 8 January 2019Source: International Journal of PharmaceuticsAuthor(s): Peng Liu, Binbin Guo, Shengfeng Wang, Jinsong Ding, Wenhu ZhouAbstractIsoniazid (INH) is a first-line therapy for bone tuberculosis (TB), but its clinic benefits are limited by severe side-effects after long-time administration. While nano-drug delivery systems present as promising strategies for INH delivery, the therapeutic efficacies are usually suboptimal due to ineffective drug accumulation at diseased sites. Local delivery system can achieve high drug concentration at focus sites with minimal systemic exposure, a...
Source: International Journal of Pharmaceutics - January 10, 2019 Category: Drugs & Pharmacology Source Type: research

Interpolymer complexes of Carbopol® 971 and poly(2-ethyl-2-oxazoline): physicochemical studies of complexation and formulations for oral drug delivery
Publication date: Available online 8 January 2019Source: International Journal of PharmaceuticsAuthor(s): Rouslan I. Moustafine, Anastasiya S. Viktorova, Vitaliy V. KhutoryanskiyAbstractCarbopol® 971 and poly(2-ethyl-2-oxazoline) form hydrogen-bonded interpolymer complexes in aqueous solutions and their complexation is strongly dependent on solution pH. This work investigated the complexation between these polymers in aqueous solutions. The compositions of interpolymer complexes as well as the critical pH values of complexation were determined. The structure of these complexes was studied in solutions using transmissio...
Source: International Journal of Pharmaceutics - January 10, 2019 Category: Drugs & Pharmacology Source Type: research

Mycobactericidal activity of some micro-encapsulated synthetic Host Defense peptides (HDP) by expediting the permeation of antibiotic: A new paradigm of drug delivery for tuberculosis
In this study, it was supposed that Host Defense peptides (HDP) which are known to permeabilize bacterial membranes may, therefore, help anti-TB antibiotics to target internal sites in bacteria. To test this hypothesis, we examined the effect of suboptimal concentration (10 µg/ml) of selected microencapsulated-HDP (Ub2-MS, K4-MS, and Aurein1.2-MS) with a standard anti-TB drug (Isoniazid, INH, 3 µg/ml). We also examined the combined effect of different concentrations of HDP-MS with a suboptimal concentration of anti-TB drug (INH, 1.5 µg/ml) which showed additive efficacy. A number of cationic HDP were enca...
Source: International Journal of Pharmaceutics - January 8, 2019 Category: Drugs & Pharmacology Source Type: research

Dual drug delivery from intraocular lens material for prophylaxis of endophthalmitis in cataract surgery
Publication date: Available online 7 January 2019Source: International Journal of PharmaceuticsAuthor(s): Ana Topete, A.P. Serro, B. SaramagoAbstractCataract is highly prevalent among old population worldwide and replacement of the opacified crystalline lens by an intraocular lens (IOL) is the safest and the most effective treatment. Although not very frequently (0.02-0.33% of the cases), the patients who undergo cataract surgery may develop endophthalmitis, which is a serious problem eventually leading to blindness. To avoid this complication, the postoperative instillation of antibiotics and anti-inflammatories is almost...
Source: International Journal of Pharmaceutics - January 7, 2019 Category: Drugs & Pharmacology Source Type: research

Advances in Orally-delivered pH-Sensitive Nanocarrier Systems; an Optimistic Approach for the Treatment of Inflammatory Bowel Disease
Publication date: Available online 4 January 2019Source: International Journal of PharmaceuticsAuthor(s): Mahira Zeeshan, Hussain Ali, Salman Khan, Saeed Ahmad Khan, Benno WeigmannAbstractInflammatory bowel disease (IBD) is the inflammation of the gastrointestinal tract (GIT) affecting the colon and ileum in particular. Increasing IBD prevalence worldwide is alarming, and needs to be resolved. Due to the limited therapeutic efficacy, accompanying adverse effects, dependence, and pharmacokinetics issues of the available therapy, IBD patients have compromised quality of life. Meanwhile, conventional drug delivery systems (DD...
Source: International Journal of Pharmaceutics - January 5, 2019 Category: Drugs & Pharmacology Source Type: research

Electrospun nanofibers for local anticancer therapy: Review of in vivo activity
Publication date: Available online 4 January 2019Source: International Journal of PharmaceuticsAuthor(s): Lenka Poláková, Jakub Širc, Radka Hobzová, Ana-Irina Cocarta, Eva HeřmánkováAbstractCurrently, chemotherapy is the most common treatment for oncological diseases. Systemic administration of chemotherapeutics provides an easy and effective distribution of the active agents throughout the patient's body, however organs may be severely impaired by serious life-threatening side effects. In many oncological diseases, particularly solid tumors, the local application of chemotherapeu...
Source: International Journal of Pharmaceutics - January 4, 2019 Category: Drugs & Pharmacology Source Type: research

Integrating the drug, disulfiram into the vitamin E-TPGS-modified PEGylated nanostructured lipid carriers to synergize its repurposing for anti-cancer therapy of solid tumors
Publication date: Available online 3 January 2019Source: International Journal of PharmaceuticsAuthor(s): Parikshit Banerjee, Tianjiao Geng, Arpan Mahanty, Tiantian Li, Li Zong, Bo WangAbstractThe ‘repurposed drug,’ disulfiram (DSF), is an inexpensive FDA-approved anti-alcoholism drug with multi-target anti-cancer effect. However, the use of DSF in clinical settings remains limited due to its high instability in blood. In the present study, we created nanostructured lipid carriers (NLC) encapsulated DSF modified with D-α-tocopheryl polyethylene glycol 1000 succinate (vitamin E-TPGS). A spherical shape, su...
Source: International Journal of Pharmaceutics - January 3, 2019 Category: Drugs & Pharmacology Source Type: research

Biotin Functionalized PEGylated Poly(Amidoamine) Dendrimer conjugate for Active Targeting of Paclitaxel in Cancer
Publication date: Available online 29 December 2018Source: International Journal of PharmaceuticsAuthor(s): Sri Vishnu Kiran Rompicharla, Preeti Kumari, Himanshu Bhatt, Balaram Ghosh, Swati BiswasAbstractIn the current study, we employed poly(amidoamine) (PAMAM) dendrimers of generation 4 (G4) to deliver paclitaxel (PTX), a poorly soluble anti-cancer agent precisely to cancer cells via its conjugation on dendrimer surface. Further, G4 PAMAM has been PEGylated (PEG) and tagged with Biotin, an essential micronutrient for cellular functions, receptors of which are overexpressed in certain cancers. The synthesized multifunctio...
Source: International Journal of Pharmaceutics - December 30, 2018 Category: Drugs & Pharmacology Source Type: research

Floating molecularly imprinted polymers based on liquid crystalline and polyhedral oligomeric silsesquioxanes for capecitabine sustained release
Publication date: Available online 29 December 2018Source: International Journal of PharmaceuticsAuthor(s): Chun-E Mo, Mei-Hong Chai, Li-Ping Zhang, Rui-Xue Ran, Yan-Ping Huang, Zhao-Sheng LiuAbstractMolecularly imprinted polymers (MIPs) have drawn extensive attention as carriers on drug delivery. However, most of MIPs suffer from insufficient drug loading capacity, burst release of drugs and/or low bioavailability. To solve the issues, this study designed an imprinted material with superior floating nature for oral drug delivery system of capecitabine (CAP) rationally. The MIPs was synthesized in the presence of 4-methylp...
Source: International Journal of Pharmaceutics - December 30, 2018 Category: Drugs & Pharmacology Source Type: research

Crack nucleation and propagation in microcrystalline-cellulose based granules subject to uniaxial and triaxial load
Publication date: Available online 29 December 2018Source: International Journal of PharmaceuticsAuthor(s): Henrik Jonsson, Caroline Öhman-Mägi, Göran Alderborn, Per Isaksson, Göran FrenningAbstractCracking patterns in four kinds of granules, based on the common pharmaceutical excipient microcrystalline cellulose (MCC) and subject to compressive load, were examined. The initial pore structure and the location of initial failure under uniaxial compression were assessed using X-ray micro-computed tomography, whereas contact force development and onset of cracking under more complex compressive load were e...
Source: International Journal of Pharmaceutics - December 30, 2018 Category: Drugs & Pharmacology Source Type: research

Emerging vistas in theranostic medicine
Publication date: Available online 29 December 2018Source: International Journal of PharmaceuticsAuthor(s): Yashna Shetty, Priyanka Prabhu, Bala PrabhakarAbstractRecent years have witnessed a paradigm shift in the focus of healthcare towards development of customized therapies which cater to the unmet needs in a myriad of disease areas such as cancer, infections, cardiovascular diseases, neurodegenerative disorders and inflammatory disorders. The term 'theranostic' refers to such multifunctional systems which combine the features of diagnosis and treatment in a single platform for superior control of the disease. Theranost...
Source: International Journal of Pharmaceutics - December 30, 2018 Category: Drugs & Pharmacology Source Type: research

Drug-delivering-drug approach-based codelivery of paclitaxel and disulfiram for treating multidrug-resistant cancer
Publication date: Available online 29 December 2018Source: International Journal of PharmaceuticsAuthor(s): Imran Shair Mohammad, Chao Teng, Birendra Chaurasiya, Lifang Yin, Chunyong Wu, Wei HeAbstractMultidrug resistance (MDR) is a common intractable barrier in success of clinical cancer chemotherapy. Codelivery of two drugs using nanocarriers is a commonly used approach to treat the MDR cancer. However, the drug payload in the conventional nanocarriers is low and thus compromises the treatment outcomes. Disulfiram (DSF) is promising to reverse MDR and increases the sensitivity of cancer cells to chemotherapy. While, pacl...
Source: International Journal of Pharmaceutics - December 30, 2018 Category: Drugs & Pharmacology Source Type: research

Effective co-encapsulation of doxorubicin and irinotecan for synergistic therapy using liposomes prepared with triethylammonium sucrose octasulfate as drug trapping agent
Publication date: Available online 29 December 2018Source: International Journal of PharmaceuticsAuthor(s): Jieru Liu, Dongxu Chi, Siyan Pan, Liwen Zhao, Xue Wang, Dun Wang, Yongjun WangAbstractThe combination regimen of irinotecan (IRI) and doxorubicin (DOX) for cancer treatment has been frequently exploited in clinical studies, but face challenges in design of efficacious combination drug delivery systems. Here we demonstrate a novel nanoliposome constructed by triethylammonium sucrose octasulfate gradient loading method for co-delivering the two therapeutic agents. In vitro cytotoxicity of IRI, DOX and their combination...
Source: International Journal of Pharmaceutics - December 30, 2018 Category: Drugs & Pharmacology Source Type: research

A multivariate approach to predict the volumetric and gravimetric feeding behavior of a low feed rate feeder based on raw material properties
In this study, the volumetric and gravimetric feeding behavior of 15 pharmaceutical powders on a low feed rate feeder was correlated with their material properties through a multivariate approach. The powders under investigation differ substantially in terms of material properties, making the selected powders representative for powders typically used in pharmaceutical manufacturing. The material properties were described by 25 material property descriptors, obtained from a rational selection of critical characterization techniques that provided maximal information with minimal characterization effort. From volumetric feedi...
Source: International Journal of Pharmaceutics - December 30, 2018 Category: Drugs & Pharmacology Source Type: research

Delivery of Liposome Encapsulated Temozolomide to Brain Tumour: understanding the drug transport for optimisation
In this study, mathematical modelling is applied to simulate the liposome-mediated delivery of temozolomide under different conditions in a 3-D realistic brain tumour model reconstructed from MR images. Delivery outcomes are evaluated by the bioavailability of free temozolomide across time. As compared to the oral and intravenous administration of free temozolomide, liposome-mediated delivery can successfully improve the drug accumulation in tumour while reducing the drug exposure in blood and normal tissue. Results show that the delivery is less sensitive to the duration of intravenous infusion but highly dependent on the...
Source: International Journal of Pharmaceutics - December 30, 2018 Category: Drugs & Pharmacology Source Type: research

Self-assembled organogelators as artificial stratum corneum models: key-role parameters for skin permeation prediction
Publication date: Available online 30 December 2018Source: International Journal of PharmaceuticsAuthor(s): Eleonora Maretti, Cecilia Rustichelli, Paola Miselli, Eliana Leo, Eleonora Truzzi, Valentina IannuccelliAbstractSelf-assembled organogelators were explored as artificial stratum corneum (SC) models for the in vitro skin permeation assessment. Four SC models consisting of binary (organogels) or ternary (microemulsion-based organogels) mixtures were developed using stearic acid, tristearin, or sorbitan tristearate, at two different concentrations, gelled in squalene. The permeation of lipophilic butyl-methoxydibenzoylm...
Source: International Journal of Pharmaceutics - December 30, 2018 Category: Drugs & Pharmacology Source Type: research

Type of pH sensitive linker reveals different time-dependent intracellular localization, in vitro and in vivo efficiency in alpha-fetoprotein receptor targeted doxorubicin conjugate
Publication date: Available online 30 December 2018Source: International Journal of PharmaceuticsAuthor(s): M. Mollaev, N. Gorokhovets, E. Nikolskaya, M. Faustova, A. Zabolotsky, O. Zhunina, M. Sokol, I. Zamulaeva, E. Severin, N. YabbarovAbstractDespite the presence of a variety of modern anticancer drugs at the market, doxorubicin (Dox) is still widely used in antineoplastic therapy, although its administration causes severe side effects. To enhance specific activity of such molecules, various approaches have been exploited: targeted moieties like monoclonal antibodies, onco-specific proteins and peptides are utilized as ...
Source: International Journal of Pharmaceutics - December 30, 2018 Category: Drugs & Pharmacology Source Type: research

The ocular pharmacokinetics and biodistribution of phospho-sulindac (OXT-328) formulated in nanoparticles: Enhanced and targeted tissue drug delivery
Publication date: Available online 28 December 2018Source: International Journal of PharmaceuticsAuthor(s): Ziyi Wen, Natsuko Muratomi, Wei Huang, Liqun Huang, Jinfeng Ren, Jennifer Yang, Yogeeta Persaud, Justin Loloi, Naveen Mallangada, Preston Kung, Robert Honkanen, Basil RigasAbstractWe studied the pharmacokinetics, biodistribution and metabolism of phospho-sulindac (PS), a novel agent efficacious in the treatment of dry eye, formulated in nanoparticles (PS-NPs) following its topical administration to the eye of New Zealand White rabbits. The nanoparticles were spherical with effective diameter = 108.9±41.7 nm, z...
Source: International Journal of Pharmaceutics - December 29, 2018 Category: Drugs & Pharmacology Source Type: research

Enzyme Nanovehicles: Histaminase and Catalase Delivered in Nanoparticulate Chitosan
Publication date: Available online 28 December 2018Source: International Journal of PharmaceuticsAuthor(s): Mihaela Leonida, Sabrina Belbekhouche, Faith Adams, Uday Kiran Bijja, Dinesh-Amraram Choudhary, Ish KumarAbstractWidespread skin allergies are of high societal concern. This pathology usually includes “histamine intolerance” and inflammatory processes affecting the skin. Oxidative stress, due to both intrinsic and environmental factors, leads to skin disorders, disease, and aging. Since the stratum corneum (SC) allows only small, lipophilic molecules to be absorbed through the skin, proteins, which are la...
Source: International Journal of Pharmaceutics - December 29, 2018 Category: Drugs & Pharmacology Source Type: research

Targeted inactivation of EPS8 using dendrimer-mediated delivery of RNA interference
Publication date: Available online 28 December 2018Source: International Journal of PharmaceuticsAuthor(s): Quan Yuan, W. Andrew Yeudall, Eunmee Lee, Hu YangAbstractWe developed polyamidoamine dendrimers conjugated with epidermal growth factor (EGF) for use in receptor-mediated delivery of therapeutics to cancer cells. Here, we demonstrate the utility of this approach to inhibit proliferation and migration of head and neck squamous carcinoma cells through targeting of EPS8. Use of EGF-dendrimers to deliver siRNA or shRNA against EPS8 resulted in inhibition of cell growth and reduction in cell motility. Moreover, more profo...
Source: International Journal of Pharmaceutics - December 29, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of processing conditions and excipients on dehydration kinetics of sodium naproxen hydrate in formulation
Publication date: Available online 28 December 2018Source: International Journal of PharmaceuticsAuthor(s): Seema Thakral, Javier Garcia-Barriocanal, Naveen K. ThakralAbstractThe manufacture of oral dosage form may induce changes in the physical form of an active pharmaceutical ingredient. Once such example includes formation of hydrate during granulation followed by the reverse transition to the anhydrous form during drying. We used naproxen sodium dihydrate (DH) as the model compound and studied its dehydration at elevated temperature under different processing conditions, (i) in ambient air, (ii) in flow of inert gas (i...
Source: International Journal of Pharmaceutics - December 29, 2018 Category: Drugs & Pharmacology Source Type: research

Development and Evaluation of Nanoemulsion and Microsuspension Formulations of Curcuminoids for Lung Delivery with a Novel Approach to Understanding the Aerosol Performance of Nanoparticles
Publication date: Available online 28 December 2018Source: International Journal of PharmaceuticsAuthor(s): Yuosef. Al ayoub, R.C. Gopalan, M. Najafzadeh, M. Amin, D. Anderson, A. Paradkar, K.H. AssiAbstractExtensive research has demonstrated the potential effectiveness of curcumin against various diseases, including asthma and cancers. However, few studies have used liquid-based vehicles in the preparation of curcumin formulations. Therefore, the current study proposed the use of nanoemulsion and microsuspension formulations to prepare nebulised curcuminoid for lung delivery. Furthermore, this work expressed a new approac...
Source: International Journal of Pharmaceutics - December 29, 2018 Category: Drugs & Pharmacology Source Type: research

Enhancement of oral bioavailability of salmon calcitonin through chitosan-modified, dual drug-loaded nanoparticles
In conclusion, the CS-based NPs and introduction of PR as a protease inhibitor improved the oral bioavailability of sCT and had potential to be developed as an oral delivery system of peptide drug.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - December 29, 2018 Category: Drugs & Pharmacology Source Type: research

Comparison of ice fog methods and monitoring of controlled nucleation success after freeze–drying
Publication date: Available online 28 December 2018Source: International Journal of PharmaceuticsAuthor(s): Ilona Vollrath, Wolfgang Friess, Angelika Freitag, Andrea Hawe, Gerhard WinterAbstractImproving freeze–drying processes regarding drying time and batch homogeneity is subject of ongoing research work. In this context, controlled nucleation raised great expectations. However, practically we face some challenges, e.g. how to non–destructively monitor successfully performed controlled nucleation. The question if different controlled nucleation methods lead to comparable products, as not every method can easi...
Source: International Journal of Pharmaceutics - December 29, 2018 Category: Drugs & Pharmacology Source Type: research

The impact of channel fill level on internal forces during continuous twin screw wet granulation
Publication date: Available online 28 December 2018Source: International Journal of PharmaceuticsAuthor(s): Carlota Mendez Torrecillas, Lee J. Gorringe, Nazer Rajoub, John Robertson, Richard G. Elkes, Dimitrios A. Lamprou, Gavin W. HalbertAbstractThe forces experienced by the particles inside a twin screw granulator (TSG) are one of the most difficult parameters to measure quantitatively. However, it is possible to perform accurately this measurement through the use of dye containing calibrated microencapsulated sensors (CAMES) whose rupture is directly dependant on their experienced shear stress. The current study measure...
Source: International Journal of Pharmaceutics - December 29, 2018 Category: Drugs & Pharmacology Source Type: research

Surface engineered excipients: III. Facilitating direct compaction tableting of binary blends containing fine cohesive poorly-compactable APIs
In this study, the feasibility of using fine, dry coated excipients is investigated instead of dry coating of the APIs, as was done previously. Avicel PH-105 (20.1µm) dry coated with 1wt% hydrophilic silica A200 as an engineered excipient was blended with fine (11.3µm) or semi-fine (30.2µm) Acetaminophen, or Ibuprofen 50 (55.4µm) in binary blends at low, medium and high drug loadings (10%, 30%, 60%). The blend uniformity, bulk density, flowability, as well as tablet properties such as friability, weight variation and strength demonstrate overall better performance compared to blends with Avicel PH-1...
Source: International Journal of Pharmaceutics - December 29, 2018 Category: Drugs & Pharmacology Source Type: research

Comparative analysis and properties evaluation of gelatin microspheres crosslinked with glutaraldehyde and 3-Glycidoxypropyltrimethoxysilane as drug delivery systems for the antibiotic vancomycin
Publication date: Available online 29 December 2018Source: International Journal of PharmaceuticsAuthor(s): Mohammad Nouri-Felekori, Mehrdad Khakbiz, Nader Nezafati, Javad Mohammadi, Mohamadreza Baghban EslaminejadAbstractIn the present comparative study, gelatin microspheres (GMs) were prepared by Emulsification-solvent-extraction method using well-known crosslinker: Glutaraldehyde (GA) and biocompatible silane-coupling agent: Glycidoxypropyltrimethoxysilane (GPTMS). Crosslinking with GA was done by a definite and common procedure, while GPTMS crosslinking potency was investigated after 5, 10, 24, and 48 h synthesis perio...
Source: International Journal of Pharmaceutics - December 29, 2018 Category: Drugs & Pharmacology Source Type: research

In vitro and in vivo studies of novel fabricated bioactive dressings based on collagen and zinc oxide 3D scaffolds
Publication date: Available online 29 December 2018Source: International Journal of PharmaceuticsAuthor(s): Paul Cătălin Balaure, Alina Maria Holban, Alexandru Mihai Grumezescu, George Dan Mogoşanu, Tudor Adrian Bălşeanu, Miruna S. Stan, Anca Dinischiotu, Adrian Volceanov, Laurenţiu MogoantăAbstractThe paper reports the synthesis and physico-chemical and biological characterization of novel wound dressings based on collagen and essential oil functionalized ZnO nanoparticles intended to improve the treatment of burns and to reduce the risk for developing wound sepsis in patients with burns or chronic wounds. The prep...
Source: International Journal of Pharmaceutics - December 29, 2018 Category: Drugs & Pharmacology Source Type: research

Hyaluronic acid enhances cell survival of encapsulated insulin-producing cells in alginate-based microcapsules
Publication date: Available online 29 December 2018Source: International Journal of PharmaceuticsAuthor(s): Alberto Cañibano-Hernández, Laura Saenz del Burgo, Albert Espona-Noguera, Gorka Orive, Rosa Mª Hernández, Jesús Ciriza, Jose Luis PedrazAbstractPancreatic islet transplantation has proved to be a promising therapy for T1DM, in spite of the chronic immunosuppression required. Although cell microencapsulation technology represents an alternative to circumvent the immune system rejection of transplanted pancreatic islets, the environment provided by classical alginate microcapsules does ...
Source: International Journal of Pharmaceutics - December 29, 2018 Category: Drugs & Pharmacology Source Type: research

Understanding the release performance of pellets with hydrophobic inclusions in sustained-release coating
Publication date: Available online 29 December 2018Source: International Journal of PharmaceuticsAuthor(s): Tze Ning Hiew, Desiree Li Hui Tan, Yi Long Tiang, Paul Wan Sia HengAbstractThe aim of this study was to evaluate how the addition of hydrophobic inclusions to sustained-release pellet film coat can affect drug release. Sustained-release formulations, in particular multiparticulate systems are gaining popularity because they are able to reduce the dosing frequency of drugs that require multiple dosing. In addition, the risk of dose dumping is low and local gastrointestinal irritation is minimised. Metformin-loaded pel...
Source: International Journal of Pharmaceutics - December 29, 2018 Category: Drugs & Pharmacology Source Type: research

PEGylated doxorubicin cloaked nano-graphene oxide for dual-responsive photochemical therapy
In this study, DOX-PEG polymers with different PEG molecular weights were synthesized to modify nano graphene oxide (NGO) to simultaneously realize the solubilization of NGO and the high loading capacity of DOX. The result showed that the drug release of NGO@DOX-PEG was pH sensitive. NIR irradiation could augment the drug release, cellular uptake, cytotoxicity and nuclear translocation of nanodrugs. Among the three kinds of nanodrugs, NGO@DOX-PEG5K was superior to others. It suggested that after conjugating with PEG, the bond between DOX-PEG and NGO was weakened, which resulted in a better drug release and treatment effect...
Source: International Journal of Pharmaceutics - December 29, 2018 Category: Drugs & Pharmacology Source Type: research

Heparin Appended ADH-Anionic Polysaccharide Nanoparticles for Site-Specific Delivery of Usnic Acid
Publication date: Available online 27 December 2018Source: International Journal of PharmaceuticsAuthor(s): Ashish Garg, Sweta Garg, Nitendra K. Sahu, Sarita Rani, Umesh Gupta, Awesh K. YadavAbstractThe intention of present research work is to formulate usnic acid (UA) loaded heparin modified gellan gum (HAG) nanoparticles (NPs). HAG copolymer based conjugation was synthesized and characterized by 1H-NMR and FT-IR spectroscopy. Plain and UA loaded HAG NPs were prepared via nanoprecipitation technique. NPs were typified and further characterized for particle size, polydispersity index, entrapment efficiency, zeta poten...
Source: International Journal of Pharmaceutics - December 28, 2018 Category: Drugs & Pharmacology Source Type: research

Highly mucus permeating and zeta potential changing self-emulsifying drug delivery systems: A potent gene delivery model for causal treatment of cystic fibrosis
Publication date: Available online 27 December 2018Source: International Journal of PharmaceuticsAuthor(s): Janine Griesser, Gergely Hetényi, Christoph Federer, Christian Steinbring, Helmut Ellemunter, Katharina Niedermayr, Andreas Bernkop-SchnürchAbstractAimIt was the aim of the study to develop self-emulsifying drug delivery systems (SEDDS) with the ability to change their zeta potential towards higher values at the adsorption membrane and in this way facilitate the release of the DNA-cetrimonium complex and enhance transfection.MethodsPlasmid DNA was complexed via hydrophobic ion pairing utilizing various su...
Source: International Journal of Pharmaceutics - December 28, 2018 Category: Drugs & Pharmacology Source Type: research

Oral administration of colitis tissue-accumulating porous nanoparticles for ulcerative colitis therapy
Publication date: Available online 27 December 2018Source: International Journal of PharmaceuticsAuthor(s): Qiubing Chen, Shuangquan Gou, Panpan Ma, Heliang Song, Xin Zhou, Yamei Huang, Moon Kwon Han, Ying Wan, Yuejun Kang, Bo XiaoAbstractTo improve the penetration and accumulation of anti-inflammatory drugs in colitis tissue, we functionalized the surface of porous poly(lactic-co-glycolic acid) nanoparticles (NPs) using pluronic F127 (PF127) and loaded curcumin (CUR) into the resulting NPs to obtain porous PF127-functionalized CUR-loaded NPs (porous PF127-NPs). These NPs had an average hydrodynamic diameter of about 270 n...
Source: International Journal of Pharmaceutics - December 28, 2018 Category: Drugs & Pharmacology Source Type: research

Impact on intestinal permeability of pediatric hyperosmolar formulations after dilution: studies with rat perfusion method
ConclusionsOsmolality parameter is of particular relevance in oral drug administration in neonate because the risk of damaging the gastrointestinal tract and because of the risk that modifying osmolality also modifies its permeability, resulting in a potential change in bioavailability.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - December 28, 2018 Category: Drugs & Pharmacology Source Type: research

Antimicrobial assessment of phage therapy using a porcine model of biofilm infection
Publication date: Available online 25 December 2018Source: International Journal of PharmaceuticsAuthor(s): C. Milho, M. Andrade, D. Vilas Boas, D. Alves, S. SillankorvaAbstractAntibiotic resistant bacterial communities persist in many types of wounds, chronic wounds in particular, in the form of biofilms. Biofilm formation is a major cause of severe infections and the main reason for a negative treatment outcome and slow healing progression. Chronic wounds are a silent epidemic essentially affecting people with co-morbid conditions such as diabetes and obesity and elderly persons particularly those with movement limitatio...
Source: International Journal of Pharmaceutics - December 25, 2018 Category: Drugs & Pharmacology Source Type: research

Production of dry-state ketoprofen-encapsulated PMMA NPs by coupling micromixer-assisted nanoprecipitation and spray drying
We present a two-step process to produce dry-state Ketoprofen-loaded poly(methyl methacrylate) nanoparticles (NPs) with controllable size and tunable drug release profile. A colloidal suspension of drug-loaded nanoparticles was first obtained from a nanoprecipitation process and then transferred into a commercial spray dryer. Three micromixers of different designs and mixing principles (molecular diffusion and impact mixing) were tested. After the first step, highly monomodal NPs in the size range 100 to 210 nm were obtained as seen by the low polydispersity index value (ca. PDI ∼ 0.2) returned by a dynamic light scatt...
Source: International Journal of Pharmaceutics - December 24, 2018 Category: Drugs & Pharmacology Source Type: research