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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

Novel freeze-dried DDA and TPGS liposomes are suitable for nasal delivery of vaccine
This study has shown that the novel liposomes have potential for development as a mucosal vaccine delivery system. Furthermore, the stability of the lyophilized liposomes offers potential additional benefits in terms of thermal stability over liquid formats. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 3, 2017 Category: Drugs & Pharmacology Source Type: research

Powder aerosol delivery through nasal high-flow system: In vitro feasibility and influence of process conditions
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): Tomoyuki Okuda, Patricia Tang, Jiaqi Yu, Warren H. Finlay, Hak-Kim Chan We aimed to obtain fundamental information for potential pulmonary delivery of powder aerosols using a clinically-approved nasal high-flow system (AIRVO), with spray-dried mannitol (SD-Man) being a model powder. Compressed air exiting the AIRVO at set ‘dispersion’ air flow rates dispersed SD-Man loaded in an Osmohaler® into a human nasal airway replica (NAR) coupled downstream to a Next Generation Impactor (NGI) running at s...
Source: International Journal of Pharmaceutics - October 3, 2017 Category: Drugs & Pharmacology Source Type: research

DNA nanostructure-based drug delivery nanosystems in cancer therapy
The objective of this review is to make a retrospect and summary about these different kinds of DNA nanostructure-based drug delivery nanosystems and their latest progresses: (1) active targeting; (2) mutidrug co-delivery; (3) construction of stimuli-responsive/intelligent nanosystems. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 2, 2017 Category: Drugs & Pharmacology Source Type: research

Applicability of low-melting-point microcrystalline wax to develop temperature-sensitive formulations
In this study, we focused on microcrystalline wax (MCW) as a low-melting-point substance. We evaluated the drug release behavior of wax matrix (WM) particles using various MCW under various temperature conditions. WM particles containing acetaminophen were prepared using a spray congealing technique. In the dissolution test at 37°C, WM particles containing low-melting-point MCWs whose melting was starting at approx. 40°C (Hi-Mic-1045 or 1070) released the drug initially followed by the release of only a small amount. On the other hand, in the dissolution test at 20 and 25°C for WM particles containing Hi-Mic-10...
Source: International Journal of Pharmaceutics - October 1, 2017 Category: Drugs & Pharmacology Source Type: research

In vitro dissolution testing of parenteral aqueous solutions and oily suspensions of paracetamol and prednisolone
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Mareike Probst, Martin Schmidt, Katharina Tietz, Sandra Klein, Werner Weitschies, Anne Seidlitz The number of intramuscularly applied dosage forms has been continuously increasing during the last decades. However, up to date no in vitro dissolution test method for parenteral dosage forms has been described in the Ph. Eur. or USP. It was the aim of this study to investigate dissolution test setups based on the compendial flow-through cell and the reciprocating holder for this purpose. Both apparatuses were equipp...
Source: International Journal of Pharmaceutics - October 1, 2017 Category: Drugs & Pharmacology Source Type: research

Shrinkage of spray-freeze-dried microparticles of pure protein for ballistic injection by manipulation of freeze-drying cycle
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Georg Straller, Geoffrey Lee Spray-freeze-drying was used to produce shrivelled, partially-collapsed microparticles of pure proteins that may be suitable for use in a ballistic injector. Various modifications of the freeze drying cycle were examined for their effects on collapse of the pure protein microparticles. The use of annealing at a shelf temperature of up to +10°C resulted in no visible particle shrinkage. This was because of the high Tg'of the pure protein. Inclusion of trehalose or sucrose l...
Source: International Journal of Pharmaceutics - October 1, 2017 Category: Drugs & Pharmacology Source Type: research

Expedited development of a high dose orally disintegrating metformin tablet enabled by sweet salt formation with acesulfame
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Chenguang Wang, Shenye Hu, Changquan Calvin Sun Salt formation has been extensively used to improve drug properties, including solubility, stability and mechanical properties. A sweet salt of metformin with acesulfame, prepared though an anion exchange reaction, showed superior properties over the commercial hydrochloride salt. These included both remarkable improvement of taste and significant enhancement in tabletability, which is explained by the different crystal structures and lower hardness as measured by ...
Source: International Journal of Pharmaceutics - October 1, 2017 Category: Drugs & Pharmacology Source Type: research

Shear strength of pharmaceutical tablets: Theoretical considerations, evaluation and relation with the capping tendency of biconvex tablets
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): V. Mazel, H. Diarra, V. Busignies, P. Tchoreloff Capping is a major industrial issue during pharmaceutical powder compression, especially in the case of biconvex tablets. Several articles proposed that capping was in fact a failure in shear. Shear strength should thus be interesting to study the capping tendency of a formulation. In this work, the ratio between the shear strength and the tensile strength obtained by diametral compression was first studied from a theoretical point of view considering different fa...
Source: International Journal of Pharmaceutics - October 1, 2017 Category: Drugs & Pharmacology Source Type: research

Ipratropium is ‘luminally recycled’ by an inter-play between apical uptake and efflux transporters in Calu-3 bronchial epithelial cell layers
This study suggests the absorption of ipratropium across the pulmonary barrier is primarily governed by paracellular passive diffusion but transporters might play a significant role in controlling the drug local concentrations in the lungs. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - October 1, 2017 Category: Drugs & Pharmacology Source Type: research

The discovery and investigation of a crystalline solid solution of an active pharmaceutical ingredient
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Mitulkumar A. Patel, Mohamed H.H. AbouGhaly, Keith Chadwick Understanding the phase behavior of crystal forms is essential in drug formulation development, as physical stability of the active pharmaceutical ingredient (API) is critical to achieving the desired bioavailability. Solvents greatly impact the physical stability of crystalline solids, resulting in a variety of well-known phase transitions, such as hydrate/solvate formation. However, solvent incorporation may also result in the formation of a less-know...
Source: International Journal of Pharmaceutics - October 1, 2017 Category: Drugs & Pharmacology Source Type: research

Novel lipidic and bienzymatic nanosomes for efficient delivery and enhanced bioactivity of catalase
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Yao Li, Yunli Zhou, Wenli Han, Mingxin Shi, Hua Zhao, Yuying Liu, Fengmei Zhang, Jingqing Zhang The purpose of this study was to evaluate the improved characteristics of catalase (CAE) when loaded in lipidic and bienzymatic nanosomes. Lipidic and bienzymatic nanosomes containing CAE and uricase (LSCU) were manufactured in two buffer solutions. Their micromorphologies, sizes, zeta potentials, enzymatic activities, kinetic characteristics, and hydrogen peroxide-lowering effects were compared with those of free CAE...
Source: International Journal of Pharmaceutics - October 1, 2017 Category: Drugs & Pharmacology Source Type: research

Targeting energy metabolism of cancer cells: Combined administration of NCL-240 and 2-DG
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Bhushan S. Pattni, Aditi Jhaveri, Ivy Dutta, James D. Baleja, Alexei Degterev, Vladimir Torchilin Cancer cells increase their metabolism to produce the energy and biomolecules necessary for growth and proliferation. Thus, energy metabolism pathways may serve as targets for anti-cancer therapy. NCL-240 is a second generation anti-cancer drug belonging to the PITenins class of PI3K-Akt inhibitors. Our analysis suggested that NCL-240 caused disruptions in mitochondrial oxidative phosphorylation and up-regulated gly...
Source: International Journal of Pharmaceutics - October 1, 2017 Category: Drugs & Pharmacology Source Type: research

Physicochemical properties of mucus and their impact on transmucosal drug delivery
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Jasmim Leal, Hugh D.C. Smyth, Debadyuti Ghosh Mucus is a selective barrier to particles and molecules, preventing penetration to the epithelial surface of mucosal tissues. Significant advances in transmucosal drug delivery have recently been made and have emphasized that an understanding of the basic structure, viscoelastic properties, and interactions of mucus is of great value in the design of efficient drug delivery systems. Mucins, the primary non-aqueous component of mucus, are polymers carrying a complex a...
Source: International Journal of Pharmaceutics - October 1, 2017 Category: Drugs & Pharmacology Source Type: research

The effect of particle shape on cellular interaction and drug delivery applications of micro- and nanoparticles
Publication date: 30 October 2017 Source:International Journal of Pharmaceutics, Volume 532, Issue 1 Author(s): Anil B. Jindal Encapsulation of therapeutic agents in nanoparticles offers several benefits including improved bioavailability, site specific delivery, reduced toxicity and in vivo stability of proteins and nucleotides over conventional delivery options. These benefits are consequence of distinct in vivo pharmacokinetic and biodistribution profile of nanoparticles, which is dictated by the complex interplay of size, surface charge and surface hydrophobicity. Recently, particle shape has been identified as a new ...
Source: International Journal of Pharmaceutics - October 1, 2017 Category: Drugs & Pharmacology Source Type: research

Performance comparison between crystalline and co-amorphous salts of indomethacin-lysine
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): Georgia Kasten, Khatera Nouri, Holger Grohganz, Thomas Rades, Korbinian Löbmann The introduction of a highly water soluble amino acid as co-amorphous co-former has previously been shown to significantly improve the dissolution rate of poorly water soluble drugs. In this work, dry ball milling (DBM) and liquid assisted grinding (LAG) were used to prepare different physical forms of salts of indomethacin (IND) with the amino acid lysine (LYS), allowing the direct comparison of their solid-state properties to...
Source: International Journal of Pharmaceutics - October 1, 2017 Category: Drugs & Pharmacology Source Type: research

Development and optimization of methotrexate-loaded lipid-polymer hybrid nanoparticles for controlled drug delivery applications
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): Nayab Tahir, Asadullah Madni, Vimalkumar Balasubramanian, Mubashar Rehman, Alexandra Correia, Prince Muhammad Kashif, Ermei Mäkilä, Jarno Salonen, Hélder A. Santos Lipid-polymer hybrid nanoparticles (LPHNPs) are emerging platforms for drug delivery applications. In the present study, methotrexate loaded LPHNPs consisted of PLGA and Lipoid S100 were fabricated by employing a single-step modified nanoprecipitation method combined with self-assembly. A three factor, three level Box Behnken design ...
Source: International Journal of Pharmaceutics - October 1, 2017 Category: Drugs & Pharmacology Source Type: research

Improving the wetting and dissolution of ibuprofen using solventless co-milling
Publication date: 25 November 2017 Source:International Journal of Pharmaceutics, Volume 533, Issue 1 Author(s): Sophia Varghese, Chinmay Ghoroi The wetting and dissolution of a BCS class II drug (Ibuprofen) is enhanced by solventless solid dispersion technique using co-milling. The co-milling is performed in a planetary ball mill using 1:1wt. ratio of Ibuprofen (drug) and Microcrystalline cellulose, MCC (excipient). The improvement in wettability and dissolution after co-milling are compared with the raw ibuprofen, ball-milled ibuprofen without any excipient and v-blend mixture of ibuprofen with an excipient. The changes...
Source: International Journal of Pharmaceutics - October 1, 2017 Category: Drugs & Pharmacology Source Type: research

Oligonucleotide-conjugated nanoparticles for targeted drug delivery via scavenger receptors class A: An in vitro assessment for proof-of-concept
In conclusions, OLN-NPs show considerable promise in targeted drug delivery and their potential applications should be further investigated. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - September 28, 2017 Category: Drugs & Pharmacology Source Type: research