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International Journal of Pharmaceutics

Sahar Awwad, Richard M Day, Peng T Khaw, Steve Brocchini, Hala Fadda
Corticosteroids have long been used to treat intraocular inflammation by intravitreal injection. We describe dexamethasone loaded poly-DL-lactide-co-glycolide (PLGA) microparticles that were fabricated by thermally induced phase separation (TIPS). The dexamethasone loaded microparticles were evaluated using a two-compartment, in vitro aqueous outflow model of the eye (PK-Eye) that estimates drug clearance time from the back of the eye via aqueous outflow by the anterior route. A dexamethasone dose of 0.20±0...
February 20, 2017: International Journal of Pharmaceutics
Pegah Varamini, Friederike M Mansfeld, Ashwini Kumar Giddam, Frederik Steyn, Istvan Toth
No abstract text is available yet for this article.
February 20, 2017: International Journal of Pharmaceutics
Bryn D Monnery, Michael Wright, Rachel Cavill, Richard Hoogenboom, Sunil Shaunak, Joachim H G Steinke, Maya Thanou
The mechanism of polycation cytotoxicity and the relationship to polymer molecular weight is poorly understood. To gain an insight into this important phenomenon a range of newly synthesized uniform (near monodisperse) linear polyethylenimines, commercially available poly(L-lysine)s and two commonly used PEI-based transfectants (broad 22kDa linear and 25kDa branched) were tested for their cytotoxicity against the A549 human lung carcinoma cell line. Cell membrane damage assays (LDH release) and cell viability assays (MTT) showed a strong relationship to dose and polymer molecular weight, and increasing incubation times revealed that even supposedly "non-toxic" low molecular weight polymers still damage cell membranes...
February 20, 2017: International Journal of Pharmaceutics
Lasse Ingerslev Blaabjerg, Eleanor Lindenberg, Thomas Rades, Holger Grohganz, Korbinian Löbmann
The glass forming ability (GFA), i.e. the ease of amorphization of drugs, is mostly investigated using the critical cooling rate upon melt quenching to generate an amorphous product via the thermodynamic pathway. However, amorphous materials can also be prepared via the kinetic pathway by milling. In this case, the time required to generate an amorphous product is called the minimal milling time. This study investigates the correlation of the GFA between these two pathways. Eighteen compounds were chosen and their GFA was investigated by determining the critical cooling rate and the minimal milling time...
February 20, 2017: International Journal of Pharmaceutics
Amirali Ebrahimi, Morteza Saffari, Timothy Langrish
The dissolution rates of indomethacin (IMC) and nifedipine (NIF) as poorly water-soluble model drugs have been significantly improved by encapsulating their molecules in the porous structure of engineered-particles of lactose as a new biocompatible porous carrier. The formulation method used in this study utilized a template-based spray-drying technique for in-situ production of porous lactose followed by two solvent-based drug-loading methods: (i) adsorption from organic solution, and (ii) incipient wetness impregnation to incorporate the drugs inside the porous lactose...
February 20, 2017: International Journal of Pharmaceutics
Tomonobu Uchino, Ichiro Hatta, Yasunori Miyazaki, Tomoya Onai, Takuto Yamazaki, Fuyoko Sugiura, Yoshiyuki Kagawa
We evaluated the interaction between human stratum corneum (SC) and surfactant-based rigid or elastic vesicles during permeation using synchrotron X-ray diffraction to obtain the mechanism action of surfactant-based vesicles for enhanced skin permeation. The effects of vesicle elasticity on the interaction with SC were also investigated. Changes in the small-angle X-ray diffraction peaks of the human SC after buffer control and vesicle application were monitored. In the small-angle region, the control as the citrate buffer induced no significant changes of diffraction peaks for the lamellar structure of short periodicity phase (SPP), which is observed as a main peak in the human SC...
February 20, 2017: International Journal of Pharmaceutics
Shubhajit Paul, Lisa J Taylor, Brendan Murphy, Joseph F Krzyzaniak, Neil Dawson, Matthew P Mullarney, Paul Meenan, Changquan Calvin Sun
Punch sticking is a frequently occurring problem that challenges successful tablet manufacturing. A mechanistic understanding of the punch sticking phenomenon facilitates the design of effective strategies to solve punch sticking problems of a drug. The first step in this effort is to identify process parameters and particle properties that can profoundly affect sticking performance. This work was aimed at elucidating the key material properties and compaction parameters that influence punch sticking by statistically analyzing punch sticking data of 24 chemically diverse compounds obtained using a set of tooling with removable upper punch tip...
February 20, 2017: International Journal of Pharmaceutics
Maria Aurora Grimaudo, Elena Tratta, Silvia Pescina, Cristina Padula, Patrizia Santi, Sara Nicoli
Apart from molecular weight and net surface charge, there are other macromolecule-related factors that could, in principle, influence their diffusion across biological tissues, such as shape, conformability, water solubility and surface charge distribution. Lysozyme and cytochrome, proteins with comparable molecular weight, isoelectric point and net surface charge in physiological conditions (approx. +7.8), are suitable model compounds for comparative studies, in particular to find out if other properties can have a role in the permeation across the sclera...
February 19, 2017: International Journal of Pharmaceutics
Marianne Parent, Igor Clarot, Sébastien Gibot, Marc Derive, Philippe Maincent, Pierre Leroy, Ariane Boudier
The LR12 peptide has been reported to reduce the size of infarct and improve both cardiac function and survival in myocardial infarction in murine models, after daily repeated intraperitoneal injections. In order to protect peptide from degrading and to prolong its release, in situ implants based on biocompatible biodegradable polymers were prepared and both in vitro and in vivo releases were evaluated after subcutaneous administration to Wistar rats. A progressive and complete release was obtained in vitro in 3 weeks...
February 19, 2017: International Journal of Pharmaceutics
Miriam Colombo, Sven Staufenbiel, Eckart Rühl, Roland Bodmeier
The aim of this study was to determine, in situ, the saturation solubility and dissolution rate of nanocrystals of three poorly water-soluble drugs for dermal application. The nanocrystals were prepared by wet bead milling. Their size could be controlled by various process parameters. The saturation solubility was measured in water or in the presence of surfactant at 32°C with a Sirius(®) inForm based on in situ UV/VIS spectroscopy. The saturation solubility of nanocrystals with sizes of ∼300nm increased for each drug in comparison to non-milled drug powders, with factors of increase in the range 1...
February 18, 2017: International Journal of Pharmaceutics
K Agossa, M Lizambard, T Rongthong, E Delcourt-Debruyne, J Siepmann, F Siepmann
In-situ forming implants (ISFI) offer an interesting potential for the treatment of periodontitis, allowing for time-controlled drug release directly at the site of action (which is difficult to reach). For this purpose, ISFI loaded with antibiotics have been reported in the literature. But the use of antibiotic drugs at low doses over prolonged periods of time can lead to the development of bacterial resistances. This risk should be avoided. The aim of this study was to develop a novel type of in-situ forming implants, loaded with the antiseptic drug chlorhexidine...
February 18, 2017: International Journal of Pharmaceutics
Noriyasu Kamei, El-Sayed Khafagy, Jun Hirose, Mariko Takeda-Morishita
We have reported that cell-penetrating peptides, such as oligoarginine, act as powerful absorption enhancers for the development of oral insulin delivery systems. However, the minimal essential sequence of oligoarginine that stimulates intestinal insulin absorption remains unclear. Therefore, the present study was conducted to clarify this minimum sequence of oligoarginine and to examine the effect of single cationic amino acid arginine on the intestinal and oral absorption of insulin. The results demonstrated that a remarkable enhancement of intestinal insulin absorption was observed after coadministration of insulin with l-arginine...
February 18, 2017: International Journal of Pharmaceutics
María J Blanco-Prieto, Elisa Garbayo
No abstract text is available yet for this article.
February 17, 2017: International Journal of Pharmaceutics
Chun Gwon Park, Young Kook Kim, Se-Na Kim, Seung Ho Lee, Beom Kang Huh, Min-A Park, Hyein Won, Ki Ho Park, Young Bin Choy
Dorzolamide eye drops are widely prescribed to reduce intraocular pressure (IOP) in the treatment of ocular hypertension and glaucoma. However, in an eye drop formulation, dorzolamide is rapidly cleared from the preocular space, hence requiring multiple daily administrations. Here, we sought to increase the preocular retention of dorzolamide using nanostructured, mucoadhesive microparticles (MUCO_NM) as carriers for topical delivery to the eye. MUCO_NM were prepared by freeze-milling dorzolamide-loaded, electrospun nanofibers composed of poly(lactic-co-glycolic acid) and polyethylene glycol...
February 16, 2017: International Journal of Pharmaceutics
J C Debouzy, L Mehenni, D Crouzier, M Lahiani-Skiba, G Nugue, M Skiba
Several biologically relevant phospholipids are considered as potential excipients for IV administration liposome's formulation of AMB (Biopharmaceututics Classification System Class IV). On the basis of in vivo bioavaibility studies, DMPC and DMPG were ranked as the first potent encapsulation enhancers for this model drug, especially if one expects to target DMPG rich systems as pulmonary surfactant. Subsequently, dispersions (multilayers) of DMPC, DMPG or in binary systems with various molar ratios were prepared with or without AMB (molar ratios AMB/lipid) and further investigated using the (1)H-,(31)P-NMR methods...
February 16, 2017: International Journal of Pharmaceutics
Qinqin Chen, Umair Zafar, Mojtaba Ghadiri, Jinfeng Bi
Powder caking is a ubiquitous problem, which could significantly decrease product quality and lead to economic losses. Hence it is important to know the conditions under which it occurs. The caking behaviour of three powder materials (PVP, HPC and CaHPO4) has been investigated by the ball indentation method (BIM) as affected by relative humidity (RH), temperature and time. The resistance to powder flow, as indicated by the hardness is measured by a ball indenting the powder bed surface. The surface hardness increases with increasing RH and temperature, indicating caking of the powder bed...
February 16, 2017: International Journal of Pharmaceutics
G Mamadou, C Charrueau, J Dairou, N Limas Nzouzi, B Eto, G Ponchel
Despite various beneficial biological properties, resveratrol lacks therapeutic applications because of poor bioavailability due to variable absorption and extensive metabolism. The present study aims at evaluating the capability of self-emulsifying drug delivery systems (SEDDS) to enhance resveratrol permeation across rat intestine and to modulate its presystemic metabolism. For that purpose, semi-solid (SS) and liquid (L) SEDDS were prepared and dispersed in an aqueous buffer to produce nanoemulsions (NE)...
February 16, 2017: International Journal of Pharmaceutics
Xin-Chi Jiang, Jian-Qing Gao
Clinical treatments have stalled in certain diseases due to a lack of proper therapeutic delivery systems. Recent studies have identified exosomes for their potential use as cell-free therapies, which may provide a novel mechanism for solving this problem. Exosomes are nanoscale extracellular vesicles that can transport rich cargos of proteins, lipids, DNA, and RNA. It is increasingly recognized that exosomes play a complex role in not only the physiological conditions but also pathological ones. Accumulating evidence suggests that exosomes are of paramount importance in distant cell-cell communication because they can enter the circulation when secreted and pass through additional biological barriers...
February 16, 2017: International Journal of Pharmaceutics
Anastasia Ripolin, James Quinn, Eneko Larrañeta, Eva Maria Vicente-Perez, Johanne Barry, Ryan F Donnelly
We describe, for the first time, the design, production and evaluation of large microneedle patches. Such systems, based on 16 individual microneedle arrays (needle height 600μm), were prepared from aqueous blends of 15% w/w Gantrez(®) S97 and 7.5% w/w poly(ethyleneglycol) 10,000Da. Ester-based crosslinking was confirmed by FTIR and mechanical strength was good. Insertion depths in a validated skin model were approximately 500μm. Ten human volunteers successfully self-inserted the microneedles of these larger patches in their skin, following appropriate instruction, as confirmed by transepidermal water loss measurements...
February 16, 2017: International Journal of Pharmaceutics
Thao Do Thi, Rob Van Hooghten, Guy Van den Mooter
The aggregation of three different cyclodextrins (CDs): 2-hydroxypropyl-β-cyclodextrin (HP-β-CD), 2-hydroxypropyl-γ-cyclodextrin (HP-γ-CD) and sulfobutylether-β-cyclodextrin (SBE-β-CD) was studied. The critical aggregation concentration (cac) of these three CDs is quite similar and is situated at ca. 2% (m/v). There was only a small difference in the cac values determined by DLS and (1)H NMR. DLS measurements revealed that CDs in solution have three size populations wherein one of them is that of a single CD molecule...
February 16, 2017: International Journal of Pharmaceutics
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