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International Journal of Pharmaceutics

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https://www.readbyqxmd.com/read/28733244/response-surface-optimization-ex-vivo-and-in-vivo-investigation-of-nasal-spanlastics-for-bioavailability-enhancement-and-brain-targeting-of-risperidone
#1
Fatma Elzahraa Abdelrahman, Ibrahim Elsayed, Mary Kamal Gad, Ahmed Hassen Elshafeey, Magdi Ibrahim Mohamed
Transnasal brain drug targeting could ensure better drug delivery to the brain through the olfactory pathway. Risperidone bioavailability is 66% in extensive metabolizers and 82% in slow metabolizers. The aim of this study is to investigate the ability of the nanovesicular spanlastics to effectively deliver risperidone through the nasal route to the brain and increase its bioavailability. Spanlastics formulae, composed of span and polyvinyl alcohol, were designed based on central composite statistical design...
July 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28733243/application-of-machine-learning-in-prediction-of-hydrotrope-enhanced-solubilisation-of-indomethacin
#2
Safa A Damiati, Luigi G Martini, Norman W Smith, Jayne M Lawrence, David J Barlow
Systematic in-vitro studies have been conducted to determine the ability of a range of 10 potential hydrotropes to improve the apparent aqueous solubility of the poorly water soluble drug, indomethacin. Solubilisation of the drug in the presence of the hydrotropes was determined experimentally using high-performance liquid chromatography (HPLC) with ultraviolet (UV) detection. These experimental data, together with various known and computed physicochemical properties of the hydrotropes were thereafter used in silico to train an artificial neural network (ANN) to allow for predictions of indomethacin solubilisation...
July 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28733242/dual-centrifugation-a-new-technique-for-nanomilling-of-poorly-soluble-drugs-and-formulation-screening-by-an-doe-approach
#3
Martin Hagedorn, Ansgar Bögershausen, Matthias Rischer, Rolf Schubert, Ulrich Massing
The development of nanosuspensions of poorly soluble APIs takes a lot of time and high amount of active material is needed. In this publication the use of dual centrifugation (DC) for an effective and rapid API-nanomilling is described for the first time. DC differs from normal centrifugation by an additional rotation of the samples during centrifugation, resulting in a very fast and powerful movement of the samples inside the vials, which - in combination with milling beads - result in effective milling. DC-nanomilling was compared to conventional wet ball milling and results in same or even smaller particle sizes...
July 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28729175/brain-targeting-efficiency-of-antimigrain-drug-loaded-mucoadhesive-intranasal-nanoemulsion
#4
Ebtsam M Abdou, Soha M Kandil, Hala M F El Miniawy
Zolmitriptan (ZT) is a well-tolerated drug in migraine treatment suffering from low bioavailability due to low amount of the drug that reaches the brain after oral and nasal delivery. Development of new nasal mucoadhesive nanoemulsion formulation for zolmitriptan may success in delivering the drug directly from the nose to the brain to achieve rapid onset of action and high drug concentration in the brain which is required for treatment of acute migraine. ZT mucoadhesive nanoemulsion were prepared and characterized for drug content, zeta potential, particle size, morphology, residence time and permeation through the nasal mucosa...
July 17, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28729174/challenges-and-strategies-to-facilitate-formulation-development-of-pediatric-drug-products-safety-qualification-of-excipients
#5
Lorrene A Buckley, Smita Salunke, Karen Thompson, Gerri Baer, Darren Fegley, Mark A Turner
A public workshop entitled "Challenges and strategies to facilitate formulation development of pediatric drug products" focused on current status and gaps as well as recommendations for risk-based strategies to support the development of pediatric age-appropriate drug products. Representatives from industry, academia, and regulatory agencies discussed the issues within plenary, panel, and case-study breakout sessions. By enabling practical and meaningful discussion between scientists representing the diversity of involved disciplines (formulators, nonclinical scientists, clinicians, and regulators) and geographies (eg, US, EU), the Excipients Safety workshop session was successful in providing specific and key recommendations for defining paths forward...
July 17, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28723410/innovative-pmdi-formulations-of-spray-dried-nanoparticles-for-efficient-pulmonary-drug-delivery
#6
Hao-Ying Li, En-Yu Xu
For drug delivery to the lungs, the aerodynamic size of drug particles plays a predominant role in determining the sites of deposition in the airway, and the particles with the size less than 2 microns are highly expected as they will be preferably delivered to the ideal site of alveolar regions. In this paper, a novel platform technology has been developed, where the water (containing pharmaceutically active agents)-in-oil (w/o) microemulsions were spray-dried to generate nanosized drug particles that were able to be homogeneously dispersed in the propellant to form an exceptionally stable suspensions with no precipitates or flocculates during a long time storage...
July 16, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28723409/layering-of-different-materials-to-achieve-optimal-conditions-for-treatment-of-painful-wounds
#7
T Maver, L Gradišnik, M Kurečič, S Hribernik, D M Smrke, U Maver, K Stana Kleinschek
Despite a range of advanced wound dressings that can facilitate wound healing, there are still no clinically used dressings for effective local pain management. The latter was the main motivation of the present study. We designed a novel wound dressing with three layers. A macro-porous polyethylene terephthalate (PET) mesh with incorporated lidocaine, a fast-acting local anesthetic, was chosen as the layer in direct contact with the skin. Fast release from this layer enables an immediate pain relieving effect, caused by dressing changes...
July 16, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28723408/in-line-raman-spectroscopic-monitoring-and-feedback-control-of-a-continuous-twin-screw-pharmaceutical-powder-blending-and-tableting-process
#8
Brigitta Nagy, Attila Farkas, Martin Gyürkés, Szofia Komaromy-Hiller, Balázs Démuth, Bence Szabó, Dávid Nusser, Enikő Borbás, György Marosi, Zsombor Kristóf Nagy
The integration of Process Analytical Technology (PAT) initiative into the continuous production of pharmaceuticals is indispensable for reliable production. The present paper reports the implementation of in-line Raman spectroscopy in a continuous blending and tableting process of a three-component model pharmaceutical system, containing caffeine as model active pharmaceutical ingredient (API), glucose as model excipient and magnesium stearate as lubricant. The real-time analysis of API content, blend homogeneity, and tablet content uniformity was performed using a Partial Least Squares (PLS) quantitative method...
July 16, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28723407/nano-lipid-drug-conjugate-an-integrated-review
#9
REVIEW
Piya Adhikari, Paulami Pal, Anup Kr Das, Subhabrata Ray, Arpita Bhattacharjee, Bhaskar Mazumder
Lipid-drug conjugates (LDC), which may also be addressed as lipoidal prodrug, have the therapeutic actives chemically bound to a lipid moiety like fatty acids or phospholipids. Fabricated in nano-size, lipid-drug conjugate forms another breed of lipid nanoparticles. LDCs are prepared in order to increase the drug loading and hence prevent leakage of a highly polar drug from a lipophilic matrix. In turn, it assists to achieve active targeting of therapeutics with reduced side effect by altering the pharmacokinetic profile of the drug...
July 16, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28720538/direct-compaction-an-update-of-materials-trouble-shooting-and-application
#10
REVIEW
Zhe Li, LiJie Zhao, Xiao Lin, Lan Shen, Yi Feng
Direct compaction (DC) is the preferred choice for tablet manufacturing; however, only less than 20% of active pharmaceutical ingredients could be compacted via DC as its high requirement for functional properties of materials. Materials with improper functionalities could lead to serious troubles during DC manufacturing, such as content non-uniformity, sticking, and capping, all of which profoundly affect the properties of final products and, thus, severely restrict the practical application of DC. With undoubted importance, these seem to be unexpectedly ignored by reviewers but not researchers in terms of many original research articles published recently...
July 16, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28720540/formulations-and-toxicologic-in-vivo-studies-of-aqueous-cyclosporin-a-eye-drops-with-cyclodextrin-nanoparticles
#11
Sunna Jóhannsdóttir, Johannes K Kristinsson, Zoltán Fülöp, Gudrún Ásgrímsdóttir, Einar Stefánsson, Thorsteinn Loftsson
Cyclosporin A (CyA) is an immunosuppressive drug used topically to treat ocular inflammatory disorder such as dry eye disease (DES). It is a lipophilic cyclic peptide with molecular weight of 1202.6Da. The aim of this study was to develop surfactant free aqueous 0.2% (w/v) CyA eye drops where the drug is present in an aqueous vehicle containing CyA/cyclodextrin (CyA/CD) nanoparticles and then do three-month toxicological testing in rabbits. Five formulations of different CD concentrations were studied, all of them contained 12...
July 15, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28720539/in-depth-experimental-analysis-of-pharmaceutical-twin-screw-wet-granulation-in-view-of-detailed-process-understanding
#12
Maxim Verstraeten, Daan Van Hauwermeiren, Kai Lee, Neil Turnbull, David Wilsdon, Mary Am Ende, Pankaj Doshi, Chris Vervaet, Davinia Brouckaert, Séverine T F C Mortier, Ingmar Nopens, Thomas De Beer
Twin-screw wet granulation is gaining increasing interest within the pharmaceutical industry for the continuous manufacturing of solid oral dosage forms. However, limited prior fundamental physical understanding has been generated relating to the granule formation mechanisms and kinetics along the internal compartmental length of a twin-screw granulator barrel, and about how process settings, barrel screw configuration and formulation properties such as particle size, density and surface properties influence these mechanisms...
July 15, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28720537/inhaled-powder-formulation-of-naked-sirna-using-spray-drying-technology-with-l-leucine-as-dispersion-enhancer
#13
Michael Y T Chow, Yingshan Qiu, Fiona F K Lo, Hinson H S Lin, Hak-Kim Chan, Philip C L Kwok, Jenny K W Lam
Pulmonary delivery of short interfering RNA (siRNA) has been widely studied in both animal and clinical studies to treat various respiratory diseases by gene silencing through RNA interference. Some of these studies showed that the administration of naked siRNA (without the use of any delivery vectors) could achieve satisfactory gene silencing effect, a unique feature to pulmonary delivery. Liquid aerosols were mostly used with very limited studies on the use of powder aerosols for siRNA. In this study, siRNA was co-spray dried with mannitol and L-leucine, the latter being a dispersion enhancer...
July 15, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28720536/a-diffusing-wave-spectroscopy-study-of-pharmaceutical-emulsions-for-physical-stability-assessment
#14
Andreas Niederquell, Alexandra H E Machado, Martin Kuentz
Emulsions are broadly used in pharmaceutics either as intermediate products or as final dosage forms. Such disperse systems are only kinetically stabilized and therefore early detection of physical instability is highly desirable. This work employed diffusing wave spectroscopy (DWS) to study a series of model emulsions that were categorized, based on their composition, as either "simple" or "complex". DWS data were compared with results of droplet size imaging, apparent viscosity obtained by microfluidics, and near-infrared (NIR) analytical centrifugation...
July 15, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28720535/effect-of-polymer-type-on-the-surface-energy-of-acetaminophen-solid-dispersions-prepared-by-melt-method
#15
Tereza Školáková, Jan Patera, Petr Zámostný
Many newly developed active pharmaceutical ingredients (APIs) have very low solubility in aqueous media. The preparation of solid dispersions (SDs) is one way of avoiding this problem. However, compound wettability and thus solubility are influenced by surface energy. In this study, we used inverse gas chromatography (IGC) to evaluate the surface energies of prepared SDs, and compared them with those obtained for physical mixtures (PMs). SDs containing different weight ratios of crystalline acetaminophen and one of three polymers (Kollidon(®) 12 PF, Kollidon(®) VA 64 or Soluplus(®)) were prepared by the melt-quenching of corresponding PMs...
July 15, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28713002/photo-stimulation-of-persistent-luminescence-nanoparticles-enhances-cancer-cells-death
#16
Gonzalo Ramírez-García, Minerva Martínez-Alfaro, Fanny d'Orlyé, Fethi Bedioui, Nathalie Mignet, Anne Varenne, Silvia Gutiérrez-Granados, Cyrille Richard
Persistent luminescence nanoparticles made of ZnGa1.995Cr0.005O4 (ZGO-NPs) are innovative nanomaterials that emit photons during long periods of time after the end of the excitation, allowing their use as diagnosis probes for in vivo optical imaging. During the excitation process, a part of the energy is stored in traps to further emit photons over long time. However, we observed in this study that some of the energy reduces molecular oxygen to produce reactive oxygen species (ROS). Following this observation, theoxidative stress induction and cytotoxic effects of these NPs were investigated on human breast cancer cells...
July 13, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28713001/comparison-of-the-properties-of-implantable-matrices-prepared-from-degradable-and-non-degradable-polymers-for-bisphosphonate-delivery
#17
Tamás Sovány, Anna Csüllög, Ernő Benkő, Géza Regdon, Klára Pintye-Hódi
The aim of the present study was the development of directly compressed tablets for implantable delivery of risedronate sodium for osteoporosis treatment and the comparison of the mechanism and kinetics of drug release from biogradable (chitosan) and non-degradable (PVC) polymer matrices. The compositions and process parameters were optimized in accordance to a mixed 2 and 3 level full factorial design. Critical Quality Attributes (CQA), such as diametral breaking hardness, porosity and speed of drug dissolution were investigated...
July 13, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28713000/discrete-particle-modeling-and-micromechanical-characterization-of-bilayer-tablet-compaction
#18
B Yohannes, M Gonzalez, A Abebe, O Sprockel, F Nikfar, S Kiang, A M Cuitiño
A mechanistic particle scale model is proposed for bilayer tablet compaction. Making bilayer tablets involves the application of first layer compaction pressure on the first layer powder and a second layer compaction pressure on entire powder bed. The bonding formed between the first layer and the second layer particles is crucial for the mechanical strength of the bilayer tablet. The bonding and the contact forces between particles of the first layer and second layer are affected by the deformation and rearrangement of particles due to the compaction pressures...
July 13, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28711641/tacrolimus-loaded-biocompatible-lecithin-based-microemulsions-with-improved-skin-penetration-structure-characterization-and-in-vitro-in-vivo-performances
#19
Vedrana Savić, Marija Todosijević, Tanja Ilić, Milica Lukić, Evgenia Mitsou, Vassiliki Papadimitriou, Spyridon Avramiotis, Bojan Marković, Nebojša Cekić, Snežana Savić
In order to improve skin penetration of tacrolimus we aimed to develop potentially non-irritant, lecithin-based microemulsions containing ethanol, isopropanol and/or propylene glycol as cosurfactants, varying caprylic/capric triglycerides and propylene glycol monocaprylate as oil phase. The influence of excipients on the size of microemulsion region in pseudo-ternary phase diagrams and their ability to form different types of microemulsions was evaluated. The comprehensive physicochemical characterization of microemulsions and the evaluation of their structure was performed, while the localization of tacrolimus in microemulsions was further investigated using electron paramagnetic resonance spectroscopy...
July 12, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28711640/recent-advances-in-tpgs-based-nanoparticles-of-docetaxel-for-improved-chemotherapy
#20
REVIEW
Hira Choudhury, Bapi Gorain, Manisha Pandey, Santosh Ashok Kumbhar, Rakesh Kumar Tekade, Arun K Iyer, Prashant Kesharwani
Docetaxel (DTX) is one of the important antitumor drugs, being used in several common chemotherapies to control leading cancer types. Severe toxicities of the DTX are prominent due to sudden parenteral exposure of desired loading dose to maintain the therapeutic concentration. Field of nanotechnology is leading to resist sudden systemic exposure of DTX with more specific delivery to the site of cancer. Further nanometric size range of the formulation aid for prolonged circulation, thereby extensive exposure results better efficacy...
July 12, 2017: International Journal of Pharmaceutics
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