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Pharmaceutics

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https://www.readbyqxmd.com/read/28509850/accessing-mefenamic-acid-form-ii-through-high-pressure-recrystallisation
#1
Nasir Abbas, Iain D H Oswald, Colin R Pulham
High-pressure crystallisation has been successfully used as an alternative technique to prepare Form II of a non-steroidal anti-inflammatory drug, mefenamic acid (MA). A single crystal of Form II, denoted as high-pressure Form II, was grown at 0.3 GPa from an ethanolic solution by using a diamond anvil cell. A comparison of the crystal structures shows that the efficient packing of molecules in Form II was enabled by the structural flexibility of MA molecules. Compression studies performed on a single crystal of Form I resulted in a 14% decrease of unit cell volume up to 2...
May 16, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28420213/folate-decorated-nanomicelles-loaded-with-a-potent-curcumin-analogue-for-targeting-retinoblastoma
#2
Hashem Alsaab, Rami M Alzhrani, Prashant Kesharwani, Samaresh Sau, Sai Hs Boddu, Arun K Iyer
The aim of this study was to develop a novel folate receptor-targeted drug delivery system for retinoblastoma cells using a promising anticancer agent, curcumin-difluorinated (CDF), loaded in polymeric micelles. Folic acid was used as a targeting moiety to enhance the targeting and bioavailability of CDF. For this purpose, amphiphilic poly(styrene-co-maleic acid)-conjugated-folic acid (SMA-FA) was synthesized and utilized to improve the aqueous solubility of a highly hydrophobic, but very potent anticancer compound, CDF, and its targeted delivery to folate overexpressing cancers...
April 18, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28406450/what-does-it-mean-a-review-of-interpreting-and-calculating-different-types-of-means-and-standard-deviations
#3
REVIEW
Marilyn N Martinez, Mary J Bartholomew
Typically, investigations are conducted with the goal of generating inferences about a population (humans or animal). Since it is not feasible to evaluate the entire population, the study is conducted using a randomly selected subset of that population. With the goal of using the results generated from that sample to provide inferences about the true population, it is important to consider the properties of the population distribution and how well they are represented by the sample (the subset of values). Consistent with that study objective, it is necessary to identify and use the most appropriate set of summary statistics to describe the study results...
April 13, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28346376/blend-hydrogel-microspheres-of-carboxymethyl-chitosan-and-gelatin-for-the-controlled-release-of-5-fluorouracil
#4
Vanarchi Rajini Kanth, Praveen B Kajjari, Priya M Madalageri, Sakey Ravindra, Lata S Manjeshwar, Tejraj M Aminabhavi
Carboxymethyl chitosan (CMCS) was synthesized and blended with gelatin (GE) to prepare hydrogel microspheres by w/o emulsion cross-linking in the presence of glutaraldehyde (GA), which acted as a cross-linker. 5-Fluorouracil (5-FU) was encapsulated to investigate its controlled release (CR) characteristics in acidic (pH 1.2) and alkaline (pH 7.4) buffer media. The microspheres which formed were spherical in nature, with smooth surfaces, as judged by the scanning electron microscopy (SEM). Fourier transform infrared spectroscopy (FTIR) confirmed the carboxymethylation of CS and the chemical stability of 5-FU in the formulations...
March 27, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28346375/liposomal-formulations-in-clinical-use-an-updated-review
#5
REVIEW
Upendra Bulbake, Sindhu Doppalapudi, Nagavendra Kommineni, Wahid Khan
Liposomes are the first nano drug delivery systems that have been successfully translated into real-time clinical applications. These closed bilayer phospholipid vesicles have witnessed many technical advances in recent years since their first development in 1965. Delivery of therapeutics by liposomes alters their biodistribution profile, which further enhances the therapeutic index of various drugs. Extensive research is being carried out using these nano drug delivery systems in diverse areas including the delivery of anti-cancer, anti-fungal, anti-inflammatory drugs and therapeutic genes...
March 27, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28245574/a-robust-liquid-chromatographic-method-for-confirmation-of-drug-stability-of-azithromycin-in-bulk-samples-tablets-and-suspensions
#6
Alex O Okaru, Kennedy O Abuga, Franco N Kamau, Stanley N Ndwigah, Dirk W Lachenmeier
A simple, isocratic and robust RP-HPLC method for the analysis of azithromycin was developed, validated and applied for the analysis of bulk samples, tablets and suspensions. The optimum chromatographic conditions for separation were established as a mobile phase comprised of acetonitrile-0.1 M KH₂PO₄ pH 6.5-0.1 M tetrabutyl ammonium hydroxide pH 6.5-water (25:15:1:59 v/v/v/v) delivered at a flow rate of 1.0 mL/min. The stationary phase consisted of reverse-phase XTerra(®) (250 mm × 4.6 mm i.d., 5 µm particle size) maintained at a temperature of 43 °C with a UV detection at 215 nm...
February 24, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28241435/polypharmacy-in-zoological-medicine
#7
REVIEW
Robert P Hunter, Ramiro Isaza
Polypharmacy is a term that describes the inappropriate, concurrent use of multiple drugs in an individual patient. Zoological medicine practitioners must take approved agents (veterinary or human) and extrapolate their use to non-approved species often with little species-specific pharmacological evidence to support their decisions. When considering polypharmacy, even less information exists concerning multi-drug pharmacokinetics, pharmacodynamics, or potential drug-drug interactions in non-domestic species...
February 22, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28230738/clinical-implications-of-20-hydroxyeicosatetraenoic-acid-in-the-kidney-liver-lung-and-brain-an-emerging-therapeutic-target
#8
REVIEW
Osama H Elshenawy, Sherif M Shoieb, Anwar Mohamed, Ayman O S El-Kadi
Cytochrome P450-mediated metabolism of arachidonic acid (AA) is an important pathway for the formation of eicosanoids. The ω-hydroxylation of AA generates significant levels of 20-hydroxyeicosatetraenoic acid (20-HETE) in various tissues. In the current review, we discussed the role of 20-HETE in the kidney, liver, lung, and brain during physiological and pathophysiological states. Moreover, we discussed the role of 20-HETE in tumor formation, metabolic syndrome and diabetes. In the kidney, 20-HETE is involved in modulation of preglomerular vascular tone and tubular ion transport...
February 20, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28218636/lobular-distribution-and-variability-in-hepatic-atp-binding-cassette-protein-b1-abcb1-p-gp-ontogenetic-differences-and-potential-for-toxicity
#9
Ngu Njei Abanda, Zoe Riches, Abby C Collier
The ATP Binding Cassette B1 (ABCB1) transporter has critical roles in endo- and xenobiotic efficacy and toxicity. To understand population variability in hepatic transport we determined ABCB1 mRNA and protein levels in total liver lysates sampled from 8 pre-defined sites (n = 24, 18-69 years), and in S9 from randomly acquired samples (n = 87, 7 days-87 years). ABCB1 levels did not differ significantly throughout individual livers and showed 4.4-fold protein variation between subjects. Neither mRNA nor protein levels varied with sex, ethnicity, obesity or triglycerides in lysates or S9 (that showed the same relationships), but protein levels were lower in pediatric S9 (p < 0...
February 17, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28275214/investigation-of-drug-polymer-compatibility-using-chemometric-assisted-uv-spectrophotometry
#10
Amir Ibrahim Mohamed, Amr Mohamed Elsayed Abd-Motagaly, Osama A A Ahmed, Suzan Amin, Alaa Ibrahim Mohamed Ali
A simple chemometric-assisted UV-spectrophotometric method was used to study the compatibility of clindamycin hydrochloride (HC1) with two commonly used natural controlled-release polymers, alginate (Ag) and chitosan (Ch). Standard mixtures containing 1:1, 1:2, and 1:0.5 w/w drug-polymer ratios were prepared and UV scanned. A calibration model was developed with partial least square (PLS) regression analysis for each polymer separately. Then, test mixtures containing 1:1 w/w drug-polymer ratios with different sets of drug concentrations were prepared...
January 16, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28075379/veterinary-compounding-regulation-challenges-and-resources
#11
REVIEW
Gigi Davidson
The spectrum of therapeutic need in veterinary medicine is large, and the availability of approved drug products for all veterinary species and indications is relatively small. For this reason, extemporaneous preparation, or compounding, of drugs is commonly employed to provide veterinary medical therapies. The scope of veterinary compounding is broad and focused primarily on meeting the therapeutic needs of companion animals and not food-producing animals in order to avoid human exposure to drug residues. As beneficial as compounded medical therapies may be to animal patients, these therapies are not without risks, and serious adverse events may occur from poor quality compounds or excipients that are uniquely toxic when administered to a given species...
January 10, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/28042818/doxorubicin-delivery-using-ph-and-redox-dual-responsive-hollow-nanocapsules-with-a-cationic-electrostatic-barrier
#12
Ryoma Teranishi, Ryota Matsuki, Eiji Yuba, Atsushi Harada, Kenji Kono
For the delivery of doxorubicin (DOX), pH and redox dual responsive hollow nanocapsules were prepared through the stabilization of polymer vesicles, which spontaneously formed from polyamidoamine dendron-poly(l-lysine) (PAMAM dendron-PLL), by the introduction of disulfide (SS) bonds between PLLs. The SS-bonded nanocapsules exhibited a very slow release of DOX under an extracellular environment because the cationic PLL membrane acted as an electrostatic barrier against the protonated DOX molecules. However, increasing the glutathione concentration to the intracellular level facilitated the immediate release of DOX through the collapse of nanocapsules by the spontaneous cleavage of SS bonds...
December 30, 2016: Pharmaceutics
https://www.readbyqxmd.com/read/28036031/drug-transporter-expression-and-activity-in-human-hepatoma-huh-7-cells
#13
Elodie Jouan, Marc Le Vée, Claire Denizot, Yannick Parmentier, Olivier Fardel
Human hepatoma cells may represent a valuable alternative to the use of human hepatocytes for studying hepatic drug transporters, which is now a regulatory issue during drug development. In the present work, we have characterized hepatic drug transporter expression, activity and regulation in human hepatoma HuH-7 cells, in order to determine the potential relevance of these cells for drug transport assays. HuH-7 cells displayed notable multidrug resistance-associated protein (MRP) activity, presumed to reflect expression of various hepatic MRPs, including MRP2...
December 28, 2016: Pharmaceutics
https://www.readbyqxmd.com/read/28035945/design-and-biological-evaluation-of-delivery-systems-containing-bisphosphonates
#14
REVIEW
Blessing Aderibigbe, Isiaka Aderibigbe, Patricia Popoola
Bisphosphonates have found application in the treatment of reoccurrence of bone diseases, breast cancer, etc. They have also been found to exhibit antimicrobial, anticancer and antimalarial activities. However, they suffer from pharmacological deficiencies such as toxicity, poor bioavailability and low intestinal adsorption. These shortcomings have resulted in several researchers developing delivery systems that can enhance their overall therapeutic effectiveness. This review provides a detailed overview of the published studies on delivery systems designed for the delivery of bisphosphonates and the corresponding in vitro/in vivo results...
December 26, 2016: Pharmaceutics
https://www.readbyqxmd.com/read/28025505/chitosan-based-nano-embedded-microparticles-impact-of-nanogel-composition-on-physicochemical-properties
#15
Paromita Islam, Jorrit J Water, Adam Bohr, Jukka Rantanen
Chitosan-based nanogels have been widely applied as drug delivery vehicles. Spray-drying of said nanogels allows for the preparation of dry powder nano-embedded microparticles. In this work, chitosan-based nanogels composed of chitosan, alginate, and/or sodium tri-penta phosphate were investigated, particularly with respect to the impact of composition on the resulting physicochemical properties. Different compositions were obtained as nanogels with sizes ranging from 203 to 561 nm. The addition of alginate and exclusion of sodium tri-penta phosphate led to an increase in nanogel size...
December 22, 2016: Pharmaceutics
https://www.readbyqxmd.com/read/28009829/evaluation-of-extrusion-technique-for-nanosizing-liposomes
#16
Sandy Gim Ming Ong, Mallikarjun Chitneni, Kah Seng Lee, Long Chiau Ming, Kah Hay Yuen
The aim of the present study was to study the efficiency of different techniques used for nanosizing liposomes. Further, the aim was also to evaluate the effect of process parameters of extrusion techniques used for nanosizing liposomes on the size and size distribution of the resultant liposomes. To compare the efficiency of different nanosizing techniques, the following techniques were used to nanosize the liposomes: extrusion, ultrasonication, freeze-thaw sonication (FTS), sonication and homogenization. The extrusion technique was found to be the most efficient, followed by FTS, ultrasonication, sonication and homogenization...
December 21, 2016: Pharmaceutics
https://www.readbyqxmd.com/read/27854292/the-influence-of-solid-microneedles-on-the-transdermal-delivery-of-selected-antiepileptic-drugs
#17
Julia Nguyen, Kevin B Ita, Matthew J Morra, Inna E Popova
The aim of this project was to examine the effect of microneedle rollers on the percutaneous penetration of tiagabine hydrochloride and carbamazepine across porcine skin in vitro. Liquid chromatography-mass spectrometric analysis was carried out using an Agilent 1200 Series HPLC system coupled to an Agilent G1969A TOF-MS system. Transdermal flux values of the drugs were determined from the steady-state portion of the cumulative amount versus time curves. Following twelve hours of microneedle roller application, there was a 6...
November 15, 2016: Pharmaceutics
https://www.readbyqxmd.com/read/27854289/contribution-of-the-hair-follicular-pathway-to-total-skin-permeation-of-topically-applied-and-exposed-chemicals
#18
Fadli Mohd, Hiroaki Todo, Masato Yoshimoto, Eddy Yusuf, Kenji Sugibayashi
Generally, the blood and skin concentration profiles and steady-state skin concentration of topically applied or exposed chemicals can be calculated from the in vitro skin permeation profile. However, these calculation methods are particularly applicable to chemicals for which the main pathway is via the stratum corneum. If the contribution of hair follicles to the total skin permeation of chemicals can be obtained in detail, their blood and skin concentrations can be more precisely predicted. In the present study, the contribution of the hair follicle pathway to the skin permeation of topically applied or exposed chemicals was calculated from the difference between their permeability coefficients through skin with and without hair follicle plugging, using an in vitro skin permeation experiment...
November 15, 2016: Pharmaceutics
https://www.readbyqxmd.com/read/27827989/activated-carbon-based-system-for-the-disposal-of-psychoactive-medications
#19
Yang Song, Mahima Manian, William Fowler, Andrew Korey, Ajay Kumar Banga
The misuse and improper disposal of psychoactive medications is a major safety and environmental concern. Hence, the proper disposal of these medications is critically important. A drug deactivation system which contains activated carbon offers a unique disposal method. In the present study, deactivation efficiency of this system was tested by using three model psychoactive drugs. HPLC validation was performed for each drug to ensure that the analytical method employed was suitable for its intended use. The method was found to be specific, accurate and precise for analyzing the drugs...
November 7, 2016: Pharmaceutics
https://www.readbyqxmd.com/read/27740594/cross-linked-dependency-of-boronic-acid-conjugated-chitosan-nanoparticles-by-diols-for-sustained-insulin-release
#20
Nabil A Siddiqui, Nashiru Billa, Clive J Roberts, Yaa Asantewaa Osei
Boronic acids have been widely investigated for their potential use as glucose sensors in glucose responsive polymeric insulin delivery systems. Interactions between cyclic diols and boronic acids, anchored to polymeric delivery systems, may result in swelling of the delivery system, releasing the drug. In this study, 4-formylphenylboronic acid conjugated chitosan was formulated into insulin containing nanoparticles via polyelectrolyte complexation. The nanoparticles had an average diameter of 140 ± 12.8 nm, polydispersity index of 0...
October 8, 2016: Pharmaceutics
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