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AAPS PharmSciTech

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https://www.readbyqxmd.com/read/28432615/fabrication-physicochemical-characterization-and-performance-evaluation-of-biodegradable-polymeric-microneedle-patch-system-for-enhanced-transcutaneous-flux-of-high-molecular-weight-therapeutics
#1
Viral Shah, Bijaya Krushna Choudhury
A revolutionary paradigm shift is being observed currently, towards the use of therapeutic biologics for disease management. The present research was focused on designing an efficient dosage form for transdermal delivery of α-choriogonadotropin (high molecular weight biologic), through biodegradable polymeric microneedles. Polyvinylpyrrolidone-based biodegradable microneedle arrays loaded with high molecular weight polypeptide, α-choriogonadotropin, were fabricated for its systemic delivery via transdermal route...
April 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28432614/dual-activity-of-hydroxypropyl-%C3%AE-cyclodextrin-and-water-soluble-carriers-on-the-solubility-of-carvedilol
#2
Abdelmoumin Zoghbi, Tianjiao Geng, Bo Wang
Carvedilol (CAR) is a non-selective α and β blocker categorized as class II drug with low water solubility. Several recent studies have investigated ways to overcome this problem. The aim of the present study was to combine two of these methods: the inclusion complex using hydroxypropyl-β-cyclodextrin (HPβCD) with solid dispersion using two carriers: Poloxamer 188 (PLX) and Polyvinylpyrrolidone K-30 (PVP) to enhance the solubility, bioavailability, and the stability of CAR. Kneading method was used to prepare CAR-HPβCD inclusion complex (KD)...
April 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28429294/ocular-cubosome-drug-delivery-system-for-timolol-maleate-preparation-characterization-cytotoxicity-ex-vivo-and-in-vivo-evaluation
#3
Jiayuan Huang, Tingting Peng, Yanrong Li, Zhengwen Zhan, Youmei Zeng, Ying Huang, Xin Pan, Chuan-Yu Wu, Chuanbin Wu
Glaucoma is an ocular disease featuring increased intraocular pressure (IOP) and its primary treatment strategy is to lower IOP by medication. Current ocular drug delivery in treating glaucoma is confronting a variety of challenges, such as low corneal permeability and bioavailability due to the unique anatomical structure of the human eye. To tackle these challenges, a cubosome drug delivery system for glaucoma treatment was constructed for timolol maleate (TM) in this study. The TM cubosomes (liquid crystalline nanoparticles) were prepared using glycerol monooleate and poloxamer 407 via high-pressure homogenization...
April 20, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28429293/topical-delivery-of-fenoprofen-calcium-via-elastic-nano-vesicular-spanlastics-optimization-using-experimental-design-and-in-vivo-evaluation
#4
Dalia Ali Farghaly, Ahmed A Aboelwafa, Manal Y Hamza, Magdy I Mohamed
The aim of this study was to investigate the potential of surfactant-based nanovesicular system (spanlastics) for topical delivery of fenoprofen calcium (FPCa) to eliminate its oral gastrointestinal adverse effects. FPCa-loaded spanlastics were prepared by thin film hydration (TFH) technique according to a full factorial design to investigate the influence of formulation variables on the drug entrapment efficiency (%EE), particle size (PS), deformability index (DI), and the % drug released after 24 h through the cellulose membrane (Q24h) using Design-Expert® software...
April 20, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28429292/preparation-of-chloramphenicol-amino-acid-combinations-exhibiting-enhanced-dissolution-rates-and-reduced-drug-induced-oxidative-stress
#5
Vanesa B Sterren, Virginia Aiassa, Claudia Garnero, Yamila Garro Linck, Ana K Chattah, Gustavo A Monti, Marcela R Longhi, Ariana Zoppi
Chloramphenicol is an old antibiotic agent that is re-emerging as a valuable alternative for the treatment of multidrug-resistant pathogens. However, it exhibits suboptimal biopharmaceutical properties and toxicity profiles. In this work, chloramphenicol was combined with essential amino acids (arginine, cysteine, glycine, and leucine) with the aim of improving its dissolution rate and reduce its toxicity towards leukocytes. The chloramphenicol/amino acid solid samples were prepared by freeze-drying method and characterized in the solid state by using Fourier transform infrared spectroscopy, powder X-ray diffraction, differential scanning calorimetry, scanning electron microscopy, and solid-state nuclear magnetic resonance...
April 20, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28424979/studies-on-core-shell-nanocapsules-of-felodipine-in-vitro-in-vivo-evaluations
#6
Jerome K Geroge, Priya Ranjan Prasad Verma, Jayachandran Venkatesan, Jin-Young Lee, Dong-Han Yoon, Se-Kwon Kim, Sandeep Kumar Singh
The present study aimed for in vitro-in vivo-in silico simulation studies of experimentally designed (3(2)-factorial) Capmul PG-8-cored, Eudragit RSPO-Lutrol F 127 nanocapsules to ferry felodipine using GastroPlus™. The in silico parameter sensitivity analysis for pharmacokinetic parameters was initially assessed to justify the preparation of felodipine-loaded nanocapsules (FLNs) with enhanced solubility to overcome the bioavailability issues of felodipine. The overall integrated desirability ranged between 0...
April 19, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28424978/the-physicochemical-investigation-of-17%C3%AE-estradiol-crystalline-prepared-by-in-situ-ph-dependent-solubility-technique-with-polyvinylpyrrolidone
#7
Hui Xiong, Jinping Fu, Hanjing Sun, Enfu Wang, Yunhui Ding, Guobin Ren, Qiufang Jing, Fuzheng Ren
Micro-particles of 17β-estradiol (ED) were prepared with polyvinylpyrrolidone (PVP) by in situ pH-dependent solubility technique. Products were characterized using multiple instruments, and molecular interactions between ED and PVP were explored. Powder X-ray diffraction and thermal analysis revealed crystalline ED in the micro-particles is hemihydrated. PVP was also present in the micro-particles. Laser particle size analysis and scanning electron microscopy revealed thin slice morphology, which might have resulted from the influence of PVP...
April 19, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28421352/a-new-role-of-fine-excipient-materials-in-carrier-based-dry-powder-inhalation-mixtures-effect-on-deagglomeration-of-drug-particles-during-mixing-revealed
#8
Ahmed O Shalash, Mustafa M A Elsayed
The potential of fine excipient materials to improve the performance of carrier-based dry powder inhalation mixtures is well acknowledged. The mechanisms underlying this potential are, however, open to question till date. Elaborate understanding of these mechanisms is a requisite for rational rather than empirical development of ternary dry powder inhalation mixtures. While effects of fine excipient materials on drug adhesion to and detachment from surfaces of carrier particle have been extensively investigated, effects on other processes, such as carrier-drug mixing, capsule/blister/device filling, or aerosolization in inhaler devices, have received little attention...
April 18, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28411333/technological-device-for-manufacturing-transdermal-films-possible-applications-to-the-individualized-treatment-for-erectile-dysfunction
#9
Francisco José Raposo, Hudson Caetano Polonini, Anderson Ferreira, Nádia Rezende Barbosa Raposo, Marcos Antônio Fernandes Brandão
Pharmacological advances in erectile dysfunction (ED) treatment have aroused growing interest among health professionals towards sexual dysfunction, generating an increasing demand for dosage forms and drug delivery systems, including tadalafil. This study aimed to develop a device to generate patches that would enable drug dosage individualization and transdermal administration. To create such a mechanical device, technical drawings were made using the CAD software. A functional prototype was built, and a pharmaceutical formulation containing tadalafil (10 mg cm(-2)) was prepared...
April 14, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28411332/evaluation-of-rosin-gum-and-eudragit%C3%A2-rs-po-as-a-functional-film-coating-material
#10
Suélen Plaza Pomin, Isabela Angeli de Lima, Rogério Ribeiro Pezarini, Osvaldo Albuquerque Cavalcanti
Polymers are essential tools in the research and development of new therapeutic devices. The diversity and flexibility of these materials have generated high expectations in the composition of new materials with extraordinary abilities, especially in the design of new systems for the modified release of pharmaceutically active ingredients. The natural polymer rosin features moisture protection and pH-dependent behavior (i.e., it is sensitive to pH > 7.0), suggesting its possible use in pharmaceutical systems...
April 14, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28397161/alginate-nanoparticles-containing-curcumin-and-resveratrol-preparation-characterization-and-in-vitro-evaluation-against-du145-prostate-cancer-cell-line
#11
Pushkar Saralkar, Alekha K Dash
Curcumin and resveratrol are naturally occurring polyphenolic compounds having anti-cancer potential. However, their poor aqueous solubility and bioavailability limit their clinical use. Entrapment of hydrophobic drugs into hydrophilic nanoparticles such as calcium alginate presents a means to deliver these drugs to their target site. Curcumin and resveratrol-loaded calcium alginate nanoparticles were prepared by emulsification and cross-linking process. The nanoparticles were characterized for particle size, zeta potential, moisture content, physical state of the drugs, physical stability, and entrapment efficiency...
April 10, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28382603/evaluation-of-the-potential-use-of-laminar-extrudates-on-stabilizing-micronized-coumarin-particles-by-supercritical-fluids-ress-study-of-different-ress-processing-variables-and-mode-of-operation
#12
Gonçalo E Oliveira, João F Pinto
The study evaluates the ability of extrudates to deliver coumarin particles micronized by the rapid expansion of supercritical solutions (RESS). The RESS parameters were drug load (2-50 g), pressure (15-42 MPa) and temperature (40-60°C) in the extraction and pressure in the expansion (0.1-5 MPa) chambers in batch or continuous and CO2 flow rate in the continuous mode of operation. Particles were characterized for size (laser diffractometry, optical and electronic microscopies-19-61 μm), surface area (BET-0...
April 5, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28382602/effects-of-chamber-pressure-and-partial-pressure-of-water-vapor-on-secondary-drying-in-lyophilization
#13
James A Searles, Sridhar Aravapalli, Cody Hodge
Secondary drying is the final step of lyophilization before stoppering, during which water is desorbed from the product to yield the final moisture content. We studied how chamber pressure and partial pressure of water vapor during this step affected the time course of water content of aqueous solutions of polyvinylpyrrolidone (PVP) in glass vials. The total chamber pressure had no effect when the partial pressure of water vapor was very low. However, when the vapor phase contained a substantial fraction of water vapor, the PVP moisture content was much higher...
April 5, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28374340/ketoprofen-microemulsion-for-improved-skin-delivery-and-in-vivo-anti-inflammatory-effect
#14
Ana Luisa Murbach Aliberti, Alemer Cortat de Queiroz, Fabíola Silva Garcia Praça, Josimar O Eloy, Maria Vitória Lopes Badra Bentley, Wanessa Silva Garcia Medina
We have designed a microemulsion (ME) containing Ketoprofen (KET) for anti-inflammatory effect evaluated using the rat paw edema model. The ME was prepared by adding propylene glycol (PG) loaded with 1% KET/water (3:1, w/w), to a mixture of sorbitan monooleate and polysorbate 80 (47.0%) at 3:1 (w/w) and canola oil (38.0%). The physicochemical characterization of KET-loaded ME involved particle size and zeta potential determination, entrapment efficiency, calorimetric analysis, and in vitro drug release. The in vivo anti-inflammatory study employed male Wistar rats...
April 3, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28361455/development-of-albumin-coupled-cholesterol-stabilized-lipid-nanoemulsion-of-methotrexate-and-tnf-%C3%AE-inhibitor-for-improved-in-vivo-efficacy-against-rheumatoid-arthritis
#15
Xiao-Yan Li, Hui Li, Yan Zhang, Shan Gao, Chun-Ping Dong, Gui-Fu Wu
Methotrexate (MTX; an anti-folate) and etanercept (ET; a TNF-α inhibitor) are used against arthritis; however, limitations like short biological half-life, low cutaneous absorption, and acidic instability limit their clinical relevance. Therefore, the aim of the investigation was to develop albumin coupled lipid nanoemulsion of MTX and ET for improved efficacy by virtue of their controlled release and specificity at the arthritic site. This emulsion was prepared by high-speed homogenization and stabilized using cholesterol...
March 30, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28357684/setting-ideal-lubricant-mixing-time-for-manufacturing-tablets-by-evaluating-powder-flowability
#16
Shohei Nakamura, Saori Yamaguchi, Rikiha Hiraide, Kumi Iga, Takatoshi Sakamoto, Hiroshi Yuasa
We investigated the effectiveness of using Carr's flowability index (FI) and practical angle of internal friction (Φ) as indexes for setting the target Mg-St mixing time needed for preparing tablets with the target physical properties. We used FI as a measure of flowability under non-loaded conditions, and Φ as a measure of flowability under loaded conditions for pharmaceutical powders undergoing direct compression with varying concentrations of Mg-St and mixing times. We evaluated the relationship between Mg-St mixing conditions and pharmaceutical powder flowability, analyzed the correlation between the physical properties of the tablets (i...
March 29, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28353174/application-of-quality-by-design-development-to-manufacturing-of-diclofenac-sodium-topical-gel
#17
Aruna Khanolkar, Viraj Thorat, Preeti Raut, Gautam Samanta
The objective of the present study was to develop and optimize generic topical gel formulation of diclofenac sodium through quality by design approaches. The quality target product profile was set for the critical quality attributes of the gel. The key material variables like hydrophilic gelling agent carbopol and penetration enhancer kolliphor were optimized using design of experiments. A central composite design was used considering viscosity and cumulative percent diffusion of the drug after 0.5, 1, 2, 4 and 6 h as responses...
March 28, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28353173/recent-trends-in-the-development-of-chitosan-based-drug-delivery-systems
#18
EDITORIAL
Claudio Salomon, Francisco M Goycoolea, Bruno Moerschbacher
No abstract text is available yet for this article.
March 28, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28353172/dodecylamine-template-based-hexagonal-mesoporous-silica-hms-as-a-carrier-for-improved-oral-delivery-of-fenofibrate
#19
Nitin V Jadhav, Pradeep R Vavia
The aim of present investigation was the preparation of dodecylamine template-based hexagonal mesoporous silica (HMS) as a carrier for poorly water-soluble drug (fenofibrate). HMS material has distinctive characteristics such as easy synthesis, high surface area and wormhole pores. These characteristics are highly admirable to make use of it as a carrier in drug delivery system. HMS was prepared by pH and temperature-independent process. Fenofibrate was loaded into the HMS by solvent immersion method using organic solvent...
March 28, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28353171/lidocaine-loaded-fish-scale-nanocellulose-biopolymer-composite-microneedles
#20
Pangkhi Medhi, Ololade Olatunji, Atul Nayak, Chandra Teja Uppuluri, Richard T Olsson, Buchi N Nalluri, Diganta B Das
Microneedle (MN) technology has emerged as an effective drug delivery system, and it has tremendous potential as a patient friendly substitute for conventional methods for transdermal drug delivery (TDD). In this paper, we report on the preparation of lidocaine-loaded biodegradable microneedles, which are manufactured from fish scale-derived collagen. Lidocaine, a common tissue numbing anaesthetic, is loaded in these microneedles with an aim of delivering the drug with controlled skin permeation. Evaluation of lidocaine permeation in porcine skin has been successfully performed using Franz diffusion cell (FDC) which has shown that the drug permeation rate increases from 2...
March 28, 2017: AAPS PharmSciTech
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