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Experimental and computational study of the effect of breath-actuated mechanism built in the NEXThaler ® dry powder inhaler
In conclusion, the NEXThaler® BAM mechanism is a unique feature enabling high emitted fine particle fraction and enhanced drug delivery to the lungs. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Eyelid skin as a potential site for drug delivery to conjunctiva and ocular tissues
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): Gerard Lee See, Ayano Sagesaka, Satoko Sugasawa, Hiroaki Todo, Kenji Sugibayashi The feasibility of topical application onto the (lower) eyelid skin to deliver hydrophilic and lipophilic compounds into the conjunctiva and ocular tissues was evaluated by comparing with conventional eye drop application. Skin permeation and the concentration of several model compounds, and skin impedance were determined utilizing eyelid skin from hairless rats, as well as abdominal skin in the same animals for comparison. In vitr...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Development of fine solid-crystal suspension with enhanced solubility, stability, and aerosolization performance for dry powder inhalation
In this study, fine solid-crystal suspension (FSCS) was proposed as a solvent-free method to improve the solubility of a drug with poor solubility (itraconazole) and achieve high deposition efficiency simultaneously. The FSCS, in which the crystalline drug particle was highly dispersed in the crystalline excipient, was initially prepared as drug-excipient extrudate by hot melt extrusion, followed by jet milling into fine particles. Unlike the amorphous solid dispersion in the high-energy state, which is liable to recrystallize and aggregate, the FSCS was expected not only to improve the solubility of itraconazole, but also...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Co-delivery strategies to overcome multidrug resistance in ovarian cancer
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): Ikram Ullah Khan, Rizwan Ullah Khan, Hira Asif, Alamgeer, Syed Haroon Khalid, Sajid Asghar, Mohammad Saleem, Kifayat Ullah Shah, Shefat Ullah Shah, Syed A.A. Rizvi, Yasser Shahzad Cancer is one of the leading causes of death and equally strikes both genders. Among women, ovarian cancer is responsible for many deaths as it remains symptomless in the earlier stages and generally diagnosed in third stage. At this point it becomes difficult to carry out de-bulking surgery and treatment with different chemotherapeut...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Spontaneous nano-emulsification: Process optimization and modeling for the prediction of the nanoemulsion ’s size and polydispersity
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): G. Lefebvre, J. Riou, G. Bastiat, E. Roger, K. Frombach, J-C. Gimel, P. Saulnier, B. Calvignac The aim of the present study was to optimize the size and polydispersity of a lipid nanoemulsion as a function of the oil (Labrafac® WL1349), surfactant (Kolliphor® HS 15) and cosurfactant (Span® 80) phase composition and temperature. The nanoemulsions were prepared using a low-energy self-emulsification method. The Z-average diameter and the polydispersity index (PDI) were modeled with mixture ex...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Functionalized hBN as targeted photothermal chemotherapy for complete eradication of cancer cells
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Shazid Md. Sharker, Md. Ashraful Alam, Manik Chandra Shill, G.M.Sayedur Rahman, Hasan Mahmud Reza The development of combined anticancer therapeutic techniques has drawn increased attention for enhanced therapeutic efficacy. In this work, we synthesized Near Infrared (NIR) responsive ICG (I) functionalized hexagonal boron-nitride (hBN) as photothermal therapeutic agent (hBNI) and Doxorubicin (Dox)-conjugated Hyaluronic acid (HA) as tumor targeted chemotherapeutic agent (d-HA-Dox). Using adhesion proper...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Sapofectosid – Ensuring non-toxic and effective DNA and RNA delivery
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Simko Sama, Gerold Jerz, Peter Schmieder, Eric Woith, Matthias F. Melzig, Alexander Weng Different methods are being deployed for non-viral DNA/RNA delivery. However non-viral formulations for DNA/RNA-delivery are often accompanied by severe toxicity and thus low efficiency. Particular costly cell culture media are required as well. Here we introduce sapofection as a valuable enhancing method for non-viral DNA/RNA delivery. Sapofection is based on the application of DNA/RNA nanoplexes and sapofectosid,...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

ZnO-based nanocarriers for drug delivery application: From passive to smart strategies
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Xiao Huang, Xi Zheng, Zuojuan Xu, Caixia Yi Due to the excellent biocompatibility as well as the low cost, nanoscale ZnO shows a great potential in drug delivery application. The richness of the structures, easy modification and pleasant properties of nanoscale ZnO make these materials reasonable choices for drug delivery. In the recent decade, various ZnO nanostructures as well as nanohybrids have been carried out for optimizational drug loading and carrying. To control the drug release behavior, many...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

In situ hydrogels enhancing postoperative functional recovery by reducing iron overload after intracerebral haemorrhage
In this study, human hair keratose hydrogel (KG) loading with minocycline hydrochloride (MH) were prepared to reduce iron overload for the improvement of the postoperative functional recovery after ICH aspiration surgery. Hemoglobin-induced iron accumulation in rat primary neuronal culture was delayed by the adsorptive capacity of blank KG, while MH-loaded KG displayed a stronger and more thorough cytoprotective effect than blank KG due to the combined effect of absorptive action to iron and sustained release of the iron chelator. Moreover, high iron-chelating efficiency in the hematoma region supplied by MH-loaded KG sign...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Polymeric microspheres for the sustained release of a protein-based drug carrier targeting the PDGF β-receptor in the fibrotic kidney
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): N. Teekamp, F. Van Dijk, A. Broesder, M. Evers, J. Zuidema, R. Steendam, E. Post, J.L. Hillebrands, H.W. Frijlink, K. Poelstra, L. Beljaars, P. Olinga, W.L.J. Hinrichs Injectable sustained release drug delivery systems are an attractive alternative for the intravenous delivery of therapeutic proteins. In particular, for chronic diseases such as fibrosis, this approach could improve therapy by reducing the administration frequency while avoiding large variations in plasma levels. In fibrotic tissues the...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Doxorubicin-loaded micelles of amphiphilic diblock copolymer with pendant dendron improve antitumor efficacy: In vitro and in vivo studies
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Siew Hui Voon, Chin Siang Kue, Toyoko Imae, Wen Shang Saw, Hong Boon Lee, Lik Voon Kiew, Lip Yong Chung, Shin-ichi Yusa Previously reported amphiphilic diblock copolymer with pendant dendron moieties (P71D3) has been further evaluated in tumor-bearing mice as a potential drug carrier. This P71D3-based micelle of an average diameter of 100nm was found to be biocompatible, non-toxic and physically stable in colloidal system up to 15days. It enhanced the in vitro potency of doxorubicin (DOX) in 4T1 breast...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Development and implementation of an advanced model predictive control system into continuous pharmaceutical tablet compaction process
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Aparajith Bhaskar, Fernando N. Barros, Ravendra Singh In the context of continuous pharmaceutical oral dosage manufacturing, a control system is essential to ensure that the critical quality attributes (CQAs) are maintained within the regulatory constraints by mitigating variations generated in upstream operations. Such a system is essential to the Quality by Design (QbD) paradigm shift, which can ensure that predefined end quality attributes are achieved within an optimal economic and time bracket. In...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Quality by Design (QbD) approach to optimize the formulation of a bilayer combination tablet (Telmiduo ®) manufactured via high shear wet granulation
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Ah Ram Lee, Seok Young Kwon, Du Hyung Choi, Eun Seok Park A bilayer tablet, which consisted of telmisartan and amlodipine besylate, was formulated based on a Quality by Design (QbD) approach. The control and response factors were determined based on primary knowledge and the target values of the control tablet (Twynsta®). A D-optimal mixture design was used to obtain the optimal formulations in terms of D-mannitol, crospovidone, and MCC for the telmisartan layer, and CCM-Na, PVP K25, and Prosolv fo...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Cyanine derivative as a suitable marker for thermosensitive in situ gelling delivery systems: In vitro and in vivo validation of a sustained buccal drug delivery
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Ni Zeng, Johanne Seguin, Pierre-Louis Destruel, Gilles Dumortier, Marc Maury, Hélène Dhotel, Michel Bessodes, Daniel Scherman, Nathalie Mignet, Vincent Boudy Buccal administration route is a promising way for a large number of drugs exhibiting a low oral bioavailability. The present work describes the formulation and evaluation of a mucoadhesive and thermosensitive in situ gelling delivery system based on poloxamer 407, poloxamer 188 and xanthan gum for buccal drug delivery. First, the mu...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Thermal properties of compacted pharmaceutical excipients
In this study, various analytical methods were used to measure the thermal properties of widely used pharmaceutical excipients including microcrystalline cellulose (MCC) of three different grades (Avicel PH 101; Avicel PH 102 and Avicel DG), lactose and mannitol. The effect of relative density on the measured thermal properties was investigated by compressing the powders into specimen of different relative densities. Differential thermal analysis (DTA) was employed to explore endothermic or exothermic events in the temperature range endured during typical pharmaceutical manufacturing processes, such as tabletting and roll ...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Enhanced solubility and bioavailability of simvastatin by mechanochemically obtained complexes
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Ruiping Kong, Xingyi Zhu, Elizaveta S. Meteleva, Yulia S. Chistyachenko, Lyubov P. Suntsova, Nikolay E. Polyakov, Mikhail V. Khvostov, Dmitry S. Baev, Tatjana G. Tolstikova, Jianming Yu, Alexander V. Dushkin, Weike Su In the present work, complexes of simvastatin (SIM) with polysaccharide arabinogalactan (AG) or disodium salt of glycyrrhizin acid (Na2GA) have been prepared using mechanochemical technique to improve the solubility of SIM and enhance its oral bioavailability. The interactions of SIM with...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

HM10660A, a long-acting hIFN- α-2b, is a potent candidate for the treatment of hepatitis C through an enhanced biological half-life
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Sungmin Bae, Taehoon Sim, Chaemin Lim, Daejin Kim, Jongsoo Lee, Youngjin Park, Sungyoub Jung, Inyoung Choi, Sechang Kwon, Kyung Taek Oh Interferon-α (IFN-α) has been widely used for the treatment of infections due to the hepatitis C virus (HCV). Because of the short half-life of IFN-α in serum, it must be administered three times per week. To increase the half-life of IFN-α, the immunoglobulin G4 (IgG4) Fc fragment (HMC001) was conjugated with human IFN-α-2b to develop a l...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Clay minerals: Properties and applications to dermocosmetic products and perspectives of natural raw materials for therapeutic purposes —A review
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Jemima Daniela Dias Moraes, Silvana Raquel Alina Bertolino, Silvia Lucia Cuffini, Diego Fernando Ducart, Pedro Eriberto Bretzke, Gislaine Ricci Leonardi Clay minerals are layered materials with a number of peculiar properties, which find many relevant applications in various industries. Since they are easily found everywhere, they are particularly attractive due to their economic viability. In the cosmetic industry, clay minerals are often used as excipients to stabilize emulsions or suspensions and to...
Source: International Journal of Pharmaceutics - October 20, 2017 Category: Drugs & Pharmacology Source Type: research

Nanomanufacturing through microfluidic-assisted nanoprecipitation: Advanced analytics and structure-activity relationships
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Roberto Donno, Arianna Gennari, Enrique Lallana, Julio M. Rios De La Rosa, Richard d’Arcy, Kevin Treacher, Kathryn Hill, Marianne Ashford, Nicola Tirelli We have employed microfluidics (cross-shaped chip) for the preparation of drug-loaded poly(lactic acid-co-glycolic acid) (PLGA) nanoparticles. The polymer precipitates from an acetone solution upon its controlled laminar mixing (flow focusing) with an aqueous solution of a surfactant, allowing for an operator-independent, up-scalable and reprodu...
Source: International Journal of Pharmaceutics - October 13, 2017 Category: Drugs & Pharmacology Source Type: research

Heating treatments affect the thermal behaviour of doxorubicin loaded in PEGylated liposomes
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Diego R. Perinelli, Marco Cespi, Giulia Bonacucina, Filippo Rendina, Giovanni Filippo Palmieri Doxil® is a stealth marketed PEGylated liposomal formulation, containing the anticancer drug doxorubicin. After loading via a pH gradient, fibrillar supramolecular structures of doxorubicin sulfate originates inside the core of the liposomes. Recently, the crystallinity of doxorubicin sulfate has been confirmed by high-resolution calorimetry. However, no detailed information are available on the nature of...
Source: International Journal of Pharmaceutics - October 13, 2017 Category: Drugs & Pharmacology Source Type: research

Dual targeting mesoporous silica nanoparticles for inhibiting tumour cell invasion and metastasis
In this study, a CD44 and N-cadherin dual targeting drug delivery system based on mesoporous silica nanoparticles (MSNs) has been successfully constructed for inhibiting tumour cell invasion and metastasis. Amino modified MSN (MSN/NH2) was first synthesized and then functionalized with hyaluronic acid (HA) and ADH-1, constructing the carrier ADH-1-HA-MSN. Doxorubicin hydrochloride (DOX) was selected as a model anticancer drug. The prepared vector had a spherical shape with a narrow distribution of particle size. Flow cytometry and confocal microscopy studies showed that the modification with HA significantly enhanced CD44-...
Source: International Journal of Pharmaceutics - October 13, 2017 Category: Drugs & Pharmacology Source Type: research

Thermostability of the coating, antigen and immunostimulator in an adjuvanted oral capsule vaccine formulation
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Stephanie Longet, Vincenzo Aversa, Daire O’Donnell, Joshua Tobias, Monica Rosa, Jan Holmgren, Ivan S. Coulter, Ed C. Lavelle Oral vaccines present an attractive alternative to injectable vaccines for enteric diseases due to ease of delivery and the induction of intestinal immunity at the site of infection. However, susceptibility to gastrointestinal proteolysis, limited transepithelial uptake and a lack of clinically acceptable adjuvants present significant challenges. A further challenge to mass...
Source: International Journal of Pharmaceutics - October 13, 2017 Category: Drugs & Pharmacology Source Type: research

In vitro characterization and mouthfeel study of functionalized calcium carbonate in orally disintegrating tablets
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Leonie Wagner-Hattler, Katharina Wyss, Joachim Schoelkopf, Jörg Huwyler, Maxim Puchkov Orally disintegrating tablets (ODT) are comfortable and safe drug delivery methods beneficial for all age groups of patients. ODTs are characterized by fast disintegration, high physical stability, taste masking and acceptable mouthfeel. In this work, the applicability of Functionalized Calcium Carbonate (FCC) to formulate ODTs with enhanced mouthfeel was elaborated and tested for acceptability on twenty healthy...
Source: International Journal of Pharmaceutics - October 13, 2017 Category: Drugs & Pharmacology Source Type: research

Promises and limitations of nanoparticles in the era of cell therapy: Example with CD19-targeting chimeric antigen receptor (CAR)-modified T cells
Publication date: 5 November 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 2 Author(s): Hélène Jakobczyk, Flavien Sciortino, Soizic Chevance, Fabienne Gauffre, Marie-Bérengère Troadec A number of nanoparticles has been developed by chemists for biomedical applications to meet imaging and targeting needs. In parallel, adoptive T therapy with chimeric antigen receptor engineered T cells (CART cells) has recently held great promise in B-cell malignancy treatments thanks to the development of anti-CD19 CAR T cells. Indeed, CD19 is a reliable B cell marker and a validated tar...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Antibiotic incorporation in jet-sprayed nanofibrillar biodegradable scaffolds for wound healing
Publication date: 5 November 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 2 Author(s): Maxime Dzikowski, Naomi Castanié, Amélie Guedon, Bernard Verrier, Charlotte Primard, Jérôme Sohier In view of preparing antibiotic-loaded structures that can be used as dressing to prevent or contain wound infections, this study evaluates biodegradable nanofibrillar matrices obtained by jet-spraying and containing ciprofloxacin (CIF). The matrices were prepared from different blends of poly-(ε-caprolactone) (PCL) and poly-d,l-(lactic acid) (PDLLA) in view of controlling mechani...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Microgels of silylated HPMC as a multimodal system for drug co-encapsulation
Publication date: 5 November 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 2 Author(s): Mohamed Zayed, Corine Tourne-Peteilh, Michel Ramonda, Gildas Rethore, Pierre Weiss, Jean Martinez, Gilles Subra, Ahmad Mehdi, Jean-Marie Devoisselle, Philippe Legrand Combined therapy is a global strategy developed to prevent drug resistance in cancer and infectious diseases. In this field, there is a need of multifunctional drug delivery systems able to co-encapsulate small drug molecules, peptides, proteins, associated to targeting functions, nanoparticles. Silylated hydrogels are alkoxysilane hybrid polymers ...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Development and validation of an HPLC-fluorescence method for the quantification of IR780-oleyl dye in lipid nanoparticles
Publication date: 5 November 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 2 Author(s): Mathieu Varache, Marie Escudé, Corentin Laffont, Emilie Rustique, Anne-Claude Couffin A reversed-phase (RP) high-performance liquid chromatography (HPLC) method for the content determination of IR780-oleyl (IRO) dye in lipid nanoparticles was developed and validated. Chromatographic separation was performed on a RP C18 column with a gradient program of water and acetonitrile both with 0.1% (v/v) TFA, at a flow rate of 1.0mL/min and a total run of 21min. IRO dye detection was made by fluorescence at emissi...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Tuning complement activation and pathway through controlled molecular architecture of dextran chains in nanoparticle corona
Publication date: 5 November 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 2 Author(s): Jean-Baptiste Coty, Elquio Eleamen Oliveira, Christine Vauthier The understanding of complement activation by nanomaterials is a key to a rational design of safe and efficient nanomedicines. This work proposed a systematic study investigating how molecular design of nanoparticle coronas made of dextran impacts on mechanisms that trigger complement activation. The nanoparticles used for this work consisted of dextran-coated poly(isobutylcyanoacrylate) (PIBCA) nanoparticles have already been thoroughly characteriz...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Development and evaluation of injectable nanosized drug delivery systems for apigenin
Publication date: 5 November 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 2 Author(s): Reatul Karim, Claudio Palazzo, Julie Laloy, Anne-Sophie Delvigne, Stéphanie Vanslambrouck, Christine Jerome, Elise Lepeltier, Francois Orange, Jean-Michel Dogne, Brigitte Evrard, Catherine Passirani, Géraldine Piel The purpose of this study was to develop different injectable nanosized drug delivery systems (NDDSs) i.e. liposome, lipid nanocapsule (LNC) and polymeric nanocapsule (PNC) encapsulating apigenin (AG) and compare their characteristics to identify the nanovector(s) that can deliver the la...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Poly-isoprenylated ifosfamide analogs: Preactivated antitumor agents as free formulation or nanoassemblies
We present here, the in vitro activity of the nanoassembly formulations of preactivated IFO derivatives with a C-4 geranyloxy, farnesyloxy and squalenoxy substituent on a large panel of tumor cell lines. The chemical and colloidal stabilities of the geranyloxy-IFO (G-IFO), farnesyloxy-IFO (F-IFO) and squalenoxy-IFO (SQ-IFO) NAs were further evaluated in comparison to their free formulation. Finally, pharmacokinetic parameters and maximal tolerated dose of the most potent preactivated IFO analog (G-IFO) were determined and compared to IFO, paving the way to in vivo studies. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Thermo-responsive magnetic Fe3O4@P(MEO2MAX-OEGMA100-X) NPs and their applications as drug delivery systems
In this study, superparamagnetic Fe3O4 NPs were synthesized and functionalized with a biocompatible thermoresponsive copolymer to obtain temperature responsive core/shell NPs. The ultimate goal of this work is to build a drug delivery system able to release anticancer drugs in the physiological temperatures range. The core/shell NPs were first synthesized and their chemical, physical, magnetic and thermo-responsive properties where fully characterized in a second step. The lower critical solution temperature (LCST) of the core/shell NPs was tuned in physiological media in order to release the cancer drug at a controlled te...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Assessment of dually labelled PEGylated liposomes transplacental passage and placental penetration using a combination of two ex-vivo human models: the dually perfused placenta and the suspended villous explants
Publication date: 5 November 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 2 Author(s): Lucie Valero, Khair Alhareth, Sophie Gil, Christelle Simasotchi, Caroline Roques, Daniel Scherman, Nathalie Mignet, Thierry Fournier, Karine Andrieux Uptake and passage of nanocarriers through the placenta are critical information to develop new therapeutic approaches during pregnancy. In order to assess nanocarriers transplacental passage and penetration into the placenta, we studied and optimized two ex-vivo human models: the dually perfused placenta and the placenta explants. Doubly labelled PEGylated liposom...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Broad overview of engineering of functional nanosystems for skin delivery
Publication date: 5 November 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 2 Author(s): Ana Henriques Mota, Patrícia Rijo, Jesús Molpeceres, Catarina Pinto Reis Nanotechnology involves the engineering of functional systems at nanoscale and it can be described as a collection of methods and techniques for processing materials to create products with special physicochemical properties. The rapid developments in nanotechnology have allowed the incorporation of therapeutic agents, actives for cosmetic, sensing agents into nanoparticles, for detection, prevention, and treatment of skin dis...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Exploration of melanoma metastases in mice brains using endogenous contrast photoacoustic imaging
This study assessed the input of PAI for examination of melanoma brain metastases in an orthotopic mouse model and further focused on spatial analyses within the tumor tissue. Hemoglobin content appeared to be higher in tumors than in healthy brains. Spatial analyses further showed that angiogenesis was mainly at the tumor periphery. Concomitantly, while healthy brains were highly oxygenated, the tumors were hypoxic and subjected to a gradient of hypoxia from the periphery to the core. In tumor-bearing brains, spectroscopic PAI clearly revealed the presence of melanin, generating a signal 3 times higher than the background...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Photo-stimulation of persistent luminescence nanoparticles enhances cancer cells death
This study reveals the importance of considering light irradiation and surface coating of luminescent nanoparticles toxicity which open new perspectives for their use in photodynamic therapy. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Long-term toxicological effects of persistent luminescence nanoparticles after intravenous injection in mice
Publication date: 5 November 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 2 Author(s): Gonzalo Ramírez-García, Silvia Gutiérrez-Granados, Marco A. Gallegos-Corona, Lourdes Palma-Tirado, Fanny d’Orlyé, Anne Varenne, Nathalie Mignet, Cyrille Richard, Minerva Martínez-Alfaro The ZnGa1.995Cr0.005O4 persistent luminescence nanoparticles offer the promise of revolutionary tools for biological imaging with applications such as cell tracking or tumor detection. They can be re-excited through living tissues by visible photons, allowing observations without any time ...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Targeting tumors with cyclic RGD-conjugated lipid nanoparticles loaded with an IR780 NIR dye: In vitro and in vivo evaluation
In this study, we developed PEGylated LNPs loaded with IR780 iodide as a contrast agent for NIR fluorescence imaging and modified them with cyclic RGD peptides in order to target integrin avβ3. We demonstrate a specific targeting of the receptor with cRGD-LNPs but not with cRAD-LNP and standard LNP using HEK293(β3), HEK293(β3)-αvRFP, DU145 and PC3 cell lines. We also demonstrate that cRGD-LNPs bind to αvβ3, interfere with cell adhesion to vitronectin and co-internalize with αvβ3 within one hour. We then investigated their biodistribution and tumor targeting in mice bearing DU145 o...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Iron oxide core oil-in-water nanoemulsion as tracer for atherosclerosis MPI and MRI imaging
Conclusion Magnetic NE showed reasonable MRI/MPS signals and a significant labelling of the atheroma plaque. These preliminary results support that NE platform could selectively image atherosclerosis. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Stealth magnetic nanocarriers of siRNA as platform for breast cancer theranostics
Publication date: 5 November 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 2 Author(s): J. Bruniaux, S. Ben Djemaa, K. Hervé-Aubert, H. Marchais, I. Chourpa, S. David The endogenous mechanism of RNA interference is more and more used in research to obtain specific down-regulation of gene expression in diseases such as breast cancer. Currently, despite the new fields of study open up by RNA interference, the rapid degradation of siRNA by nucleases and their negative charges prevent them from crossing cell membranes. To overcome these limitations, superparamagnetic iron oxide nanoparticles (SP...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

How should we plan the future of nanomedicine for cancer diagnosis and therapy?
Publication date: 5 November 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 2 Author(s): Khair Alhareth, Lucie Sancey, Nicolas Tsapis, Nathalie Mignet (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Sustained intrathecal therapeutic protein delivery using genetically transduced tissue implants in a freely moving rat model
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): J.P. Aronson, H.A. Katnani, I. Pomerantseva, N. Shapir, H. Tse, R. Miari, H. Goltsman, O. Mwizerwa, C.M. Neville, G.A. Neil, E.N. Eskandar, C.A. Sundback Systemic delivery of therapeutic proteins to the central nervous system (CNS) is challenging because of the blood-brain barrier restrictions. Direct intrathecal delivery is possible but does not produce stable concentrations. We are proposing an alternative approach for localized delivery into the CNS based on the Transduced Autologous Restorative Gen...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Enhancing the viability of Lactobacillus rhamnosus GG after spray drying and during storage
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Géraldine Broeckx, Dieter Vandenheuvel, Tim Henkens, Shari Kiekens, Marianne F.L. van den Broek, Sarah Lebeer, Filip Kiekens Increasing knowledge about the human microbiome has led to a growing awareness of the potential of applying probiotics to improve our health. The pharmaceutical industry shows an emerging interest in pharmaceutical formulations containing these beneficial microbes, the so-called pharmabiotics. An important manufacturing step is the drying of the probiotics, as this can inc...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Formulation development of SYN-004 (ribaxamase) oral solid dosage form, a β-lactamase to prevent intravenous antibiotic-associated dysbiosis of the colon
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Andrew Bristol, Steven Hubert, Felix Hofmann, Hans Baer SYN-004 (ribaxamase) delayed release drug product is a multi-particulate, hard capsule for oral delivery of a recombinant β-lactamase enzyme designed to degrade β-lactam antibiotics administered intravenously, and thus prevent colon dysbiosis. Here we describe the development of the SYN-004 enteric coated pellet formulation, which has been tested in multiple clinical trials. Since the SYN-004 drug substance is a buffered liquid, several ...
Source: International Journal of Pharmaceutics - October 11, 2017 Category: Drugs & Pharmacology Source Type: research

Hyalugel-integrated liposomes as a novel ocular nanosized delivery system of fluconazole with promising prolonged effect
In conclusion, novel hyalugel-integrated liposomes significantly enhanced corneal permeability compared to conventional liposomes and FLZ suspension. They would be promising alternates for eye drops; decreasing frequency of administration and increasing patients’ compliance. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 10, 2017 Category: Drugs & Pharmacology Source Type: research

Improved oral bioavailability and therapeutic efficacy of erlotinib through molecular complexation with phospholipid
Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Chander Parkash Dora, Varun Kushwah, Sameer S. Katiyar, Pradeep Kumar, Viness Pillay, Sarasija Suresh, Sanyog Jain The current study was aimed to prepare a molecular complex of erlotinib (ERL) with phospholipid (PC) for enhancement of solubility and thus bioavailability, therapeutic efficacy and reducing the toxicity of erlotinib. Phospholipid complex of drug was prepared by solvent evaporation method and characterized by differential scanning calorimetry (DSC), Fourier transform infra-red spectroscopy...
Source: International Journal of Pharmaceutics - October 10, 2017 Category: Drugs & Pharmacology Source Type: research

An Electron Paramagnetic Resonance (EPR) spectroscopy study on the γ-irradiation sterilization of the pharmaceutical excipient l-histidine: Regeneration of the radicals in solution
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): C. Vallotto, H.E. Williams, D.M. Murphy, Z.J. Ayres, R. Edge, M.E. Newton, C.J. Wedge The effects of γ-radiation sterilization on the parenteral excipient l-histidine were analysed by means of EPR spectroscopy. The irradiation process was found to induce the formation of a deamination radical which was persistent in the solid state. The nature and reactivity of the radicals following dissolution in water was evaluated using spin-trapping EPR experiments. The deamination radical was found to regenerate in ...
Source: International Journal of Pharmaceutics - October 7, 2017 Category: Drugs & Pharmacology Source Type: research

A review of patient-specific gastrointestinal parameters as a platform for developing in vitro models for predicting the in vivo performance of oral dosage forms in patients with Parkinson ’s disease
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): Erik Wollmer, Sandra Klein Parkinson’s disease (PD) is a progressive neurodegenerative disease that presents with visible motor symptoms, but that is accompanied by several additional symptoms, including gastrointestinal symptoms that may affect pharmacokinetics of oral medications. A detailed understanding of the nature of PD-specific gastrointestinal parameters and of how they may affect drug release of orally administered dosage forms seems to be essential information for developing better oral PD medi...
Source: International Journal of Pharmaceutics - October 7, 2017 Category: Drugs & Pharmacology Source Type: research

Cellulose nanofibers as excipient for the delivery of poorly soluble drugs
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): Korbinian Löbmann, Anna J. Svagan Poor aqueous solubility of drugs is becoming an increasingly pronounced challenge in the formulation and development of drug delivery systems. To overcome the limitations associated with these problematic drugs, formulation scientists are required to use enabling strategies which often demands the use of new excipients. Cellulose nanofibers (CNFs) is such an excipient and it has only recently been described in the pharmaceutical field. In this review, the use of CNF in dru...
Source: International Journal of Pharmaceutics - October 6, 2017 Category: Drugs & Pharmacology Source Type: research

Preparation of mixed monoterpenes edge activated PEGylated transfersomes to improve the in vivo transdermal delivery efficiency of sinomenine hydrochloride
In this study, mixed monoterpenes edge activated PEGylated transfersomes (MMPTs) were prepared by ethanol injection process with sinomenine hydrochloride as a model drug. The formulation of MMPTs was optimized by an orthogonal design. We investigated skin permeation/deposition characteristics and pharmacokinetics of sinomenine hydrochloride loaded in MMPTs by comparing with liposomes using in vitro skin tests and in vivo cutaneous microdialysis. In in vitro study, the accumulative skin permeated quantity (ASPQ) and skin permeation rate (SPR) of simonenine (SIN) in the optimized MMPTs were prominently higher than that in th...
Source: International Journal of Pharmaceutics - October 6, 2017 Category: Drugs & Pharmacology Source Type: research

Technical aspects of preparing PEG-PLGA nanoparticles as carrier for chemotherapeutic ‎agents by nanoprecipitation method
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): Hassan A. Almoustafa, Mohammed A. Alshawsh, Zamri Chik Nanoprecipitation is a simple and increasingly trending method for nanoparticles preparation. The self-assembly feature of poly (ethylene glycol)-poly (lactide-co-glycolic acid) (PEG-PLGA) amphiphilic copolymer into a nanoparticle and its versatile structure makes nanoprecipitation one of the best methods for its preparation. The aim of this study is to review currently available literature for standard preparation of PEG-PLGA nanoparticles using nanoprecip...
Source: International Journal of Pharmaceutics - October 6, 2017 Category: Drugs & Pharmacology Source Type: research