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International Journal of Pharmaceutics

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https://read.qxmd.com/read/31100384/predicting-tablet-tensile-strength-with-a-model-derived-from-the-gravitation-based-high-velocity-compaction-analysis-data
#1
Tanner Timo, Antikainen Osmo, Pollet Arne, Räikkönen Heikki, Ehlers Henrik, Juppo Anne, Yliruusi Jouko
In the present study, a model was developed to estimate tablet tensile strength utilizing the gravitation-based high-velocity (G-HVC) method introduced earlier. Three different formulations consisting of microcrystalline cellulose (MCC), dicalcium phosphate dihydrate (DCP), hydroxypropyl methylcellulose (HPMC), theophylline and magnesium stearate were prepared. The formulations were granulated using fluid bed granulation and the granules were compacted with the G-HVC method and an eccentric tableting machine...
May 14, 2019: International Journal of Pharmaceutics
https://read.qxmd.com/read/31100383/correlation-between-the-solid-state-of-lipid-coating-and-release-profile-of-api-from-hot-melt-coated-microcapsules
#2
Sharareh Salar-Behzadi, Carolina Corzo, Lisa Schaden, Peter Laggner, Andreas Zimmer
Solvent-free hot melt coating (HMC) provides a safer and more economic process compared to the conventional solvent coating techniques. However, drug release instability and the lack of fundamental understanding on it are limiting factors for application of HMC for industrial productions. In this work, we investigated glyceryl dibehenate, glyceryl monostearate and behenoyl polyoxyl-8 glyceride as HMC materials. The microstructure and solid state alteration of lipids were studied via polarized light microscopy, DSC and powder x-ray diffraction...
May 14, 2019: International Journal of Pharmaceutics
https://read.qxmd.com/read/31100382/improved-oral-bioavailability-of-the-anticancer-drug-catechin-using-chitosomes-design-in-vitro-appraisal-and-in-vivo-studies
#3
Hadeer M Ezzat, Yosra S R Elnaggar, Ossama Y Abdallah
Improved oral bioavailability of the anticancer drug catechin using chitosomes: Design, in-vitro appraisal and in-vivo studiesAbstract: Catechin hydrate is a phytopharmaceutical with promising anticancer effects but poor bioavailability. This study aimed to elaborate catechin loaded chitosan-tethered liposomes (chitosomes) to enhance catechin oral bioavailability. Nanocarriers were optimized via ethanol injection method followed by physicochemical, ex vivo and biological appraisal in male Wistar albino rats...
May 14, 2019: International Journal of Pharmaceutics
https://read.qxmd.com/read/31100381/in-vitro-evaluation-of-solid-lipid-nanoparticles-ability-to-encapsulate-release-and-ensure-effective-protection-of-peptides-in-the-gastrointestinal-tract
#4
Camille Dumont, Sandrine Bourgeois, Hatem Fessi, Pierre-Yves Dugas, Vincent Jannin
Peptides are rarely orally administrated due to rapid degradation in the gastrointestinal tract and low absorption at the epithelial border. The objective of this study was to encapsulate a model water-soluble peptide in biodegradable and biocompatible solid lipid-based nanoparticles, i.e. Solid Lipid Nanoparticles (SLN) and Nanostructured Lipid Carriers (NLC) in order to protect it from metabolic degradation. Leuprolide (LEU) and a LEU-docusate Hydrophobic Ion Pair (HIP) were encapsulated in SLN and NLC by High Pressure Homogenization...
May 14, 2019: International Journal of Pharmaceutics
https://read.qxmd.com/read/31095984/tableting-performance-of-various-mannitol-and-lactose-grades-assessed-by-compaction-simulation-and-chemometrical-analysis
#5
Shubhajit Paul, Pirjo Tajarobi, Catherine Boissier, Changquan Calvin Sun
Mannitol and lactose are commonly used fillers in pharmaceutical tablets, available in several commercial grades that are produced using different manufacturing processes. These grades significantly differ in particulate and powder properties that impact tablet manufacturability. Choice of sub-optimum type or grade of excipient in tablet formulation can lead to manufacturing problems and difficulties, which are magnified during a continuous manufacturing process. Previous characterization of tableting performance of these materials was limited in scope and under conditions not always realistic to the commercial production of tablets...
May 13, 2019: International Journal of Pharmaceutics
https://read.qxmd.com/read/31095983/targeted-drug-delivery-to-the-brain-via-intranasal-nanoemulsion-available-proof-of-concept-and-existing-challenges
#6
REVIEW
Bappaditya Chatterjee, Bapi Gorain, Keithanchali Mohananaidu, Pinaki Sengupta, Uttam Kumar Mandal, Hira Choudhury
Intranasal delivery has shown to circumvent blood-brain-barrier (BBB) and deliver the drugs into the CNS at a higher rate and extent than other conventional routes. The mechanism of drug transport from nose-to-brain is not fully understood yet, but several neuronal pathways are considered to be involved. Intranasal nanoemulsion for brain targeting is investigated extensively. Higher brain distribution of drug after administering intranasal nanoemulsion was established by many researchers. Issues with nasomucosal clearance are solved by formulating modified nanoemulsion; for instance, mucoadhesive nanoemulsion or in situ nanoemulgel...
May 13, 2019: International Journal of Pharmaceutics
https://read.qxmd.com/read/31085260/optimization-of-mirna-delivery-by-using-a-polymeric-conjugate-based-on-deoxycholic-acid-modified-polyethylenimine
#7
Fatemeh Radmanesh, Hamid Sadeghi Abandansari, Sara Pahlavan, Mehdi Alikhani, Mahdi Karimi, Sarah Rajabi, Bahram Kazemi Demneh, Hossein Baharvand
Safe and efficient delivery of microRNA (miRNA) molecules is essential for their successful transition from research to the clinic setting. In the present study, we have used a bile acid, deoxycholic acid (DA), to modify 1.8 kDa branched polyethylenimine (bPEI1.8 ) and subsequently investigated gene delivery features of the resultant conjugates (PEI-DAn ). We found significant differences between the PEI-DAn conjugates and conventional bPEIs with respect to miRNA condensation ability, buffering capacity, cellular uptake, and intracellular gene release behavior in endothelial cells (ECs) isolated from human umbilical vein (HUVECs)...
May 11, 2019: International Journal of Pharmaceutics
https://read.qxmd.com/read/31085259/mrp2-mediated-transport-of-etoposide-in-mdckii-mrp2-cells-is-unaffected-by-commonly-used-non-ionic-surfactants
#8
Salli Nielsen, Anne Marijke Westerhoff, Lorraine Gaenaelle Gé, Krestine Lundgaard Carlsen, Maria Diana Læssøe Pedersen, Carsten Uhd Nielsen
The aim of the present study was to investigate the ability of non-ionic surfactants to inhibit MRP2-mediated transport in vitro in MDCKII MRP2 cells. Transport studies across MDCKII MRP2 cell monolayers were performed using 3 H-etoposide and 3 H-digoxin. 19 different non-ionic surfactants, including several polysorbates (PS), cremophor EL, vitamin E-TPGS, and n-nonyl β-D-glucopyranoside (NG), were investigated. Barrier function of the cells was investigated measuring TEER and transport of 14 C-glycine. The amount of isotope was quantified using liquid scintillation counting...
May 11, 2019: International Journal of Pharmaceutics
https://read.qxmd.com/read/31085258/prediction-of-dissolution-profiles-by-non-destructive-nir-spectroscopy-in-bilayer-tablets
#9
Yukteshwar Baranwal, Andrés D Román-Ospino, Golshid Keyvan, Jung Myung Ha, Eon Pyo Hong, Fernando J Muzzio, Rohit Ramachandran
This study describes how near infrared (NIR) spectroscopy can be used to predict the dissolution of bilayer tablets as a non-destructive approach. Tablets in this study consist of two APIs physically separated in layers and manufactured under three levels of hardness. NIR spectra were acquired for each layer in diffuse reflectance mode. Reference dissolution profile values were obtained using dissolution apparatus & HPLC. A multivariate PLS calibration model was developed for each API relating its dissolution profile with to spectral data...
May 11, 2019: International Journal of Pharmaceutics
https://read.qxmd.com/read/31085257/evaluating-the-potential-of-drug-eluting-contact-lenses-for-treatment-of-bacterial-keratitis-using-an-ex-vivo-corneal-model
#10
Uloma Ubani-Ukoma, Daniel Gibson, Gregory Schultz, Boladale Olanrewaju Silva, Anuj Chauhan
Corneal infections are treated by multiple instillations of eye drops each day. This study aims to investigate the effectiveness of ofloxacin-loaded contact lenses as prolonged release devices for the treatment of bacterial keratitis. Two silicone hydrogel contact lenses (SHCLs) Senofilcon A (ACUVUE OASYS® ) and Narafilcon A (ACUVUE TRUEYE® ) were modified by incorporation of ofloxacin alone or with vitamin E (VE). The drug uptake and in vitro release kinetics were investigated and the antibacterial efficacy was assessed against Staphylococcus aureus and Pseudomonas aeruginosa in an ex vivo rabbit corneal model...
May 11, 2019: International Journal of Pharmaceutics
https://read.qxmd.com/read/31085256/novel-polyurethane-based-nanoparticles-of-infliximab-to-reduce-inflammation-in-an-in-vitro-intestinal-epithelial-barrier-model
#11
Ritesh M Pabari, Clara Mattu, Sailesh Partheeban, Aqeel Almarhoon, Monica Boffito, Gianluca Ciardelli, Zebunnissa Ramtoola
In this study we examined the potential of novel biodegradable polymers of polyesterurethane (PU), and its PEGylated (PU-PEG) form as nanocarriers of Infliximab (INF), to treat inflammation in an in-vitro epithelial model. Nanoparticles (NPs) formulated were of average size of 200-287nm. INF loading of NPs (INF-NPs) resulted in an increase in size and zeta potential. No cytotoxicity was observed for any of the NPs. Cellular interaction and uptake of PU NPs were similar compared with polycaprolactone (PCL) NPs and significantly higher to Poly(lactic-co-glycolic) acid (PLGA) NPs...
May 11, 2019: International Journal of Pharmaceutics
https://read.qxmd.com/read/31085255/application-of-an-automated-small-scale-in-vitro-transfer-model-to-predict-in-vivo-precipitation-inhibition
#12
Christian Jede, Christian Wagner, Holger Kubas, Christian Weber, Markus Weigandt, Mirko Koziolek, Werner Weitschies
The majority of NCEs are weakly basic drugs. Consequently, their solubility is highly pH-dependent, with higher solubility in the acidic stomach and poor solubility in the neutral intestinal environment. The gastric emptying of dissolved drug can lead to the intestinal precipitation of the drug. One option of reducing this process is to formulate the drug together with a precipitation inhibitor (PI). The aim of this study was to investigate the effects of different PIs on the intestinal concentrations of ketoconazole and five orally administered kinase inhibitors (i...
May 11, 2019: International Journal of Pharmaceutics
https://read.qxmd.com/read/31085254/drug-stability-and-product-performance-characteristics-of-a-dapivirine-releasing-vaginal-ring-under-simulated-real-world-conditions
#13
Diarmaid J Murphy, Clare F McCoy, Peter Boyd, Tiffany Derrick, Patrick Spence, Brid Devlin, R Karl Malcolm
In two recent Phase III clinical trials, use of a 25 mg dapivirine vaginal ring significantly reduced HIV acquisition rates. Post hoc analysis from one of the trials indicated higher rates of protection among women over the age of 21 years when compared to younger women, most likely due to reduced adherence in the latter group. There is currently no information available on how release of dapivirine from the ring is affected by either its intermittent removal from the vagina or women's cleaning of the ring before re-insertion...
May 11, 2019: International Journal of Pharmaceutics
https://read.qxmd.com/read/31085253/the-development-of-an-inline-raman-spectroscopic-analysis-method-as-a-quality-control-tool-for-hot-melt-extruded-ramipril-fixed-dose-combination-products
#14
G P Andrews, D S Jones, Z Senta-Loys, A Almajaan, S Li, O Chevallier, C Elliot, A M Healy, J F Kelleher, A M Madi, G C Gilvary, Y Tian
Currently in the pharmaceutical industry, continuous manufacturing is an area of significant interest. In particular, hot-melt extrusion (HME) offers many advantages and has been shown to significantly reduce the number of processing steps relative to a conventional product manufacturing line. To control product quality during HME without process interruption, integration of inline analytical technology is critical. Vibrational spectroscopy (Raman, NIR and FT-IR) is often employed and used for real-time measurements because of the non-destructive and rapid nature of these analytical techniques...
May 11, 2019: International Journal of Pharmaceutics
https://read.qxmd.com/read/31082468/diversity-of-%C3%AE-cyclodextrin-based-nanosponges-for-transformation-of-actives
#15
REVIEW
Sandip Pawar, Pravin Shende, Francesco Trotta
β-Cyclodextrin-based nanosponges (β-CDNSs) play an important role in new arrays of agriculture, floriculture, cosmetics, medicine, high molecular weight proteins, novel flame retardants, gas carriers and water filters. In recent years, the field of advance nanostructured systems witnesses a rapid development due to miniaturization, dose-reduction, sustained and controlled release of actives and long-term stability of material. β-CDNSs are colloidal and cross-linked nanocarrier comprising of solid mesh-like structure with nano-cavities for encapsulation of complex lipophilic and hydrophilic chemical substances...
May 10, 2019: International Journal of Pharmaceutics
https://read.qxmd.com/read/31078647/biodistribution-biostability-assessment-of-sirna-after-intravenous-and-intratracheal-administration-to-mice-based-on-comprehensive-analysis-of-in-vivo-ex-vivo-polyacrylamide-gel-electrophoresis-fluorescence-imaging
#16
Tomoyuki Okuda, Yoko Toyoda, Takashi Murakami, Hirokazu Okamoto
We performed in vivo/ex vivo/polyacrylamide gel electrophoresis (PAGE) fluorescence imaging of near-infrared fluorescence (NIRF)-labeled siRNA (Cy5.5-siGL3) in mice to investigate the validity of each fluorescence imaging result as the biodistribution/biostability assessment of siRNA. Statistically significant correlations could be obtained between the in vivo and ex vivo fluorescence intensities of Cy5.5 in the relevant regions/tissues, except the lung region/tissue after intravenous administration. On PAGE fluorescence images with the naked formulation, there was no band corresponding to intact Cy5...
May 9, 2019: International Journal of Pharmaceutics
https://read.qxmd.com/read/31078646/phase-transition-and-release-kinetics-of-polyphenols-encapsulated-lyotropic-liquid-crystals
#17
Heng Zhang, Zhongni Wang
In this paper, the lyotropic liquid crystals formed in SL/IP/H2 O system were prepared as a drug carrier system to encapsulate polyphenols. The components and introduction of drug had influences in the structure and rheological properties of lyotropic liquid crystals. The structure underwent a phase transition from lamellar phase (Lα) to Lα+HII (reverse hexagonal phase) mixed phases and micelle by increasing its IP/H2 O mass ratio from 5/35 to 20/20 and 35/5, consistent with the transition from solid-like properties to viscous fluid properties...
May 9, 2019: International Journal of Pharmaceutics
https://read.qxmd.com/read/31077764/evaluation-of-the-solid-state-form-of-tadalafil-in-sub-micron-thin-films-using-nanomechanical-infrared-spectroscopy
#18
Fatemeh Samaeifar, Andrea Casci Ceccacci, Sanjukta Bose Goswami, Line Hagner Nielsen, Ahmad Afifi, Kinga Zór, Anja Boisen
Assessing physical stability of drugs is important both in the development as well as in the production phase in the pharmaceutical industry. We used nanomechanical infrared (NAM-IR) spectroscopy based on photothermal response of a nanomechanical resonator, to investigate the solid state forms of tadalafil (TAD), under various storage conditions in sub-micron thin films. The amorphous TAD was stable, when kept at normal storage conditions of 24°C, 45% relative humidity (RH) and shielded from light, however, it crystallized after four days when it was at stress storage conditions (40°C, 70% RH, and direct sunlight)...
May 8, 2019: International Journal of Pharmaceutics
https://read.qxmd.com/read/31077763/effect-of-thermal-and-shear-stresses-in-the-spray-drying-process-on-the-stability-of-sirna-dry-powders
#19
Jingya Wu, Lan Wu, Feng Wan, Jukka Rantanen, Dongmei Cun, Mingshi Yang
Pulmonary delivery of small interfering RNAs (siRNAs) has shown promising results for the treatment of lung diseases with gene disorders. The aim of this work was to evaluate the effect of processing-induced thermal and shear stresses during the spray drying process on the solid-state properties, the chemical integrity and the bioactivity of spray-dried siRNA powder intended for inhalation. To this end, inhalable siRNA dry powders composed of EGFP-siRNA and mannitol were prepared by using a lab-scale spray drier...
May 8, 2019: International Journal of Pharmaceutics
https://read.qxmd.com/read/31077762/surface-conjugation-of-ep67-to-biodegradable-nanoparticles-increases-the-generation-of-long-lived-mucosal-and-systemic-memory-t-cells-by-encapsulated-protein-vaccine-after-respiratory-immunization-and-subsequent-t-cell-mediated-protection-against-respiratory
#20
Shailendra B Tallapaka, Bala V K Karuturi, Pravin Yeapuri, Stephen M Curran, Yogesh A Sonawane, Joy A Phillips, D David Smith, Sam D Sanderson, Joseph A Vetro
Encapsulation of protein vaccines in biodegradable nanoparticles (NP) increases T-cell expansion after mucosal immunization but requires incorporating a suitable immunostimulant to increase long-lived memory T-cells. EP67 is a clinically viable, host-derived peptide agonist of the C5a receptor that selectively activates antigen presenting cells over neutrophils. We previously found that encapsulating EP67-conjugated CTL peptide vaccines in NP increases long-lived memory subsets of CTL after respiratory immunization...
May 8, 2019: International Journal of Pharmaceutics
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