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AAPS PharmSciTech

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https://www.readbyqxmd.com/read/27909943/simulating-different-dosing-scenarios-for-a-child-appropriate-valproate-er-formulation-in-a-new-pediatric-two-stage-dissolution-model
#1
Frank Karkossa, Antonia Krueger, Jana Urbaniak, Sandra Klein
Predictive in vitro test methods addressing the parameters relevant to drug release in the pediatric gastrointestinal tract could be an appropriate means for reducing the number of in vivo studies in children. However, dissolution models addressing the particular features of pediatric gastrointestinal physiology and typical pediatric dosing scenarios have not yet been described. The objective of the present study was to combine the knowledge on common vehicle types and properties and current information on pediatric gastrointestinal physiology to design a dissolution model that enables a biorelevant simulation of the gastrointestinal conditions in young children...
December 1, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27905004/ocular-disposition-of-%C3%A2-8-tetrahydrocannabinol-from-various-topical-ophthalmic-formulations
#2
Nagendra S Punyamurthula, Goutham R Adelli, Waseem Gul, Michael A Repka, Mahmoud A ElSohly, Soumyajit Majumdar
The purposes of this project are to enhance the trans-membrane penetration of Δ(8)-Tetrahydrocannabinol (Δ(8)-THC) and to study the effect of various lipid based systems in delivering the compound, non-invasively, to anterior and posterior ocular chambers. Solid lipid nanoparticles (SLNs), fast gelling films were manufactured using high pressure homogenization and melt cast techniques, respectively. The formulations were characterized for drug content, entrapment efficiency, particle size and subsequently evaluated in vitro for trans-corneal permeation...
November 30, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27882479/albendazole-microcrystal-formulations-based-on-chitosan-and-cellulose-derivatives-physicochemical-characterization-and-in-vitro-parasiticidal-activity-in-trichinella-spiralis-adult-worms
#3
Josefina Priotti, Ana V Codina, Darío Leonardi, María D Vasconi, Lucila I Hinrichsen, María C Lamas
The oral route has notable advantages to administering dosage forms. One of the most important questions to solve is the poor solubility of most drugs which produces low bioavailability and delivery problems, a major challenge for the pharmaceutical industry. Albendazole is a benzimidazole carbamate extensively used in oral chemotherapy against intestinal parasites, due to its extended spectrum activity and low cost. Nevertheless, the main disadvantage is the poor bioavailability due to its very low solubility in water...
November 23, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27873181/inhalable-ipratropium-bromide-particle-engineering-with-multicriteria-optimization
#4
Bhavani Prasad Vinjamuri, Rahul V Haware, William C Stagner
Spray-dried ipratropium bromide (IPB) microspheres for oral inhalation were engineered using Quality by Design. The interrogation of material properties, process parameters, and critical product quality attributes interplay enabled rational product design. A 2(7-3) screening design exhibited the Maillard reaction between L-leucine (LL) and lactose at studied outlet temperatures (OT) >130°C. A response surface custom design was used in conjunction with multicriteria optimization to determine the operating design space to achieve inhalable microparticles...
November 21, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27858253/microemulsion-transdermal-formulation-for-simultaneous-delivery-of-valsartan-and-nifedipine-formulation-by-design
#5
Jatin Sood, Bharti Sapra, Ashok K Tiwary
The objective of the study was to optimize the proportion of different components for formulating oil in water microemulsion formulation meant for simultaneous transdermal delivery of two poorly soluble antihypertensive drugs. Surface response methodology of Box-Behnken design was utilized to evaluate the effect of two oils (Captex 500 - x1 and Capmul MCM - x2) and surfactant (Acrysol EL135 - x3) on response y1 (particle size), y2 (solubility of valsartan), and y3 (solubility of nifedipine). The important factors which significantly affected the responses were identified and validated using ANOVA...
November 17, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27858252/polymeric-nanofiber-antifungal-formulations-using-a-novel-co-extrusion-approach
#6
Mohammad Mofidfar, Jia Wang, Lisa Long, Christopher L Hager, Chairut Vareechon, Eric Pearlman, Eric Baer, Mahmoud Ghannoum, Gary E Wnek
We report the successful implementation of a novel melt co-extrusion process to fabricate ca. 1 μm diameter fibers of poly(caprolactone) (PCL) containing the antifungal compound clotrimazole in concentrations between 4 and 8 wt%. The process involves co-extrusion of a clotrimazole-loaded PCL along with poly(ethylene oxide) (PEO) as a co-feed, with subsequent removal of PEO to isolate PCL-clotrimazole fibers. In vitro tests of the clotrimazole-containing fibers against the fungus Aspergillus fumigatus, Candida albicans, and Trichophyton mentagrophytes strains demonstrated good antifungal activity which was maintained for more than 3 weeks...
November 17, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27853995/determination-of-relative-response-factors-of-cefazolin-impurities-by-quantitative-nmr
#7
Shuyu Liu, Shangchen Yao, Hailing Zhang, Changqin Hu
The relative response factors (RRFs) of ten cefazolin impurities were determined by quantitative nuclear magnetic resonance (qNMR) and high-performance liquid chromatography (HPLC) equipped with an ultraviolet (UV) detector. The purities of these ten cefazolin impurities were successfully measured by qNMR for the purpose of RRFs determination by HPLC. The RRF values and their uncertainties determined by the two approaches are comparable. While the qNMR approach is effective and makes it easier to determine the RRFs for impurities, it also has the advantage of allowing the universal detection of protons without the limitations of common mass detectors...
November 16, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27853994/development-of-interleukin-2-loaded-chitosan-based-nanogels-using-artificial-neural-networks-and-investigating-the-effects-on-wound-healing-in-rats
#8
Canan Aslan, Nevin Çelebi, I Tuncer Değim, Ayşegül Atak, Çiğdem Özer
The aim of this study was to develop and characterize rh- IL-2 loaded chitosan-based nanogels for the healing of wound incision in rats. Nanogels were prepared using chitosan and bovine serum albumin (BSA) by ionic gelation method and high temperature application, respectively. Particle size, zeta potential, and polydispersity index were measured for characterization of nanogels. The morphology of nanogels was examined by using SEM and AFM. The IL-2 loading capacity of nanogels was determined using ELISA method...
November 16, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27844417/systematically-optimized-ketoprofen-loaded-novel-proniosomal-formulation-for-periodontitis-in-vitro-characterization-and-in-vivo-pharmacodynamic-evaluation
#9
N K Yadav, Sanju Nanda, Gajanand Sharma, O P Katare
Various preclinical/clinical studies support the effectiveness of ketoprofen in periodontitis; however, the literature reveals that novel delivery systems have been less explored for the drug in periodontitis. The current investigation aims to explore the potential of a pro-vesicular approach-based proniosomal drug delivery of ketoprofen for its effectiveness and validation in experimental periodontal disease (EPD). Formulations were developed using I-optimal mixture design. Developed formulations were characterized for entrapment efficiency, vesicle size, and in vitro drug release...
November 14, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27844416/two-synthetic-methods-for-preparation-of-chiral-stationary-phases-using-crystalline-degradation-products-of-vancomycin-column-performance-for-enantioseparation-of-acidic-and-basic-drugs
#10
Assem Abdollahpour, Rouhollah Heydari, Mojtaba Shamsipur
Two chiral stationary phases (CSPs) based on crystalline degradation products (CDPs) of vancomycin by using different synthetic methods were prepared and compared. Crystalline degradation products of vancomycin were produced by hydrolytic loss of ammonia from vancomycin molecules. Performances of two chiral columns prepared with these degradation products were investigated using several acidic and basic drugs as model analytes. Retention and resolution of these analytes on the prepared columns, as two main parameters, in enantioseparation were studied...
November 14, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27844415/powder-flow-testing-judicious-choice-of-test-methods
#11
Justin Yong Soon Tay, Celine Valeria Liew, Paul Wan Sia Heng
Flow property of pharmaceutical powders can be assessed by various flow testers and test methods. In this study, eight commercially available lactose grades were sourced and tested for angles of repose, tapping studies, shear cell measurements, stirred powder rheometry, and avalanching powder measurements. The relationships between various flow parameters and particle size were analyzed. Deviations from the general trend could be attributed to either the insensitivity of the test or differences in particle shape...
November 14, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27834056/ultradeformable-liposomes-a-novel-vesicular-carrier-for-enhanced-transdermal-delivery-of-procyanidins-effect-of-surfactants-on-the-formation-stability-and-transdermal-delivery
#12
Rencai Chen, Rongli Li, Qian Liu, Chao Bai, Benlin Qin, Yue Ma, Jing Han
The aims of this work were to develop a novel vesicular carrier, procyanidins, ultradeformable liposomes (PUDLs), to expand the applications for procyanidins, and increase their stability and transdermal delivery. In this study, we prepared procyanidins ultradeformable liposomes using thin film hydration method and evaluated their encapsulation efficiency, vesicle deformability, storage stability, and skin permeation in vitro. The influence of different surfactants on the properties of PUDLs was also investigated...
November 10, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27834055/biopharmaceutical-assessment-and-irritation-potential-of-microemulsions-and-conventional-systems-containing-oil-from-syagrus-cearensis-for-topical-delivery-of-amphotericin-b-using-alternative-methods
#13
Giovana D Sousa, Juliana Kishishita, Kátia A S Aquino, Octávio A F Presgrave, Leila B Leal, Davi P Santana
The aim of this study was to compare the biopharmaceutical characteristics and irritation potentials of microemulsions (MEs) and conventional systems (CSs) containing oil from Syagrus cearensis for topical delivery of Amphotericin B (AmB). Pseudo-ternary phase diagrams were constructed using a water titration method to develop the MEs, and the CSs were prepared according to the classical technique of phase inversion. In the skin permeation and retention study, dermatomed pig skin without stratum corneum was used as an alternative disturbed skin model...
November 10, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27834054/development-and-optimisation-of-spironolactone-nanoparticles-for-enhanced-dissolution-rates-and-stability
#14
H R Kelidari, M Saeedi, J Akbari, K Morteza-Semnani, H Valizadeh, Mohammed Maniruzzaman, Ali Farmoudeh, Ali Nokhodchi
Stable solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) formulations to enhance the dissolution rates of poorly soluble drug spironolactone (SP) were being developed. Probe ultra-sonication method was used to prepare SLNs and NLCs. All NLCs contained stearic acid (solid lipid carrier) and oleic acid (liquid lipid content), whereas, SLNs were prepared and optimised by using the solid lipid only. The particles were characterised in terms of particle size analysis, thermal behaviour, morphology, stability and in vitro release...
November 10, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27830515/improvement-of-the-ocular-bioavailability-of-econazole-nitrate-upon-complexation-with-cyclodextrins
#15
Abd El-Gawad Helmy Abd El-Gawad, Osama A Soliman, Marwa S El-Dahan, Saeed A S Al-Zuhairy
Econazole nitrate (EC) is an active, imidazole antifungal agent. However, low aqueous solubility and dissolution rate of EC has discouraged its usage for the treatment of ophthalmic fungal infection. In this study, inclusion complexes of EC with cyclodextrins were prepared to enhance its solubility, dissolution, and ocular bioavailability. To achieve this goal, EC was complexed with β-CyD/HP-β-CyD using kneading, co-precipitation, and freeze-drying techniques. Phase-solubility studies were performed to investigate the complexes in the liquid form...
November 9, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27830514/development-of-eudragit-rs-100-microparticles-loaded-with-ropinirole-optimization-and-in-vitro-evaluation-studies
#16
Prince Muhammad Kashif, Asadullah Madni, Muhammad Ashfaq, Mubashar Rehman, Muhammad Ahmad Mahmood, Muhammad Imran Khan, Nayab Tahir
The current study aimed to develop novel pH independent microparticles loaded with ropinirole (ROP) for sustained drug release. Eudragit RS 100 was used as release retardant and microparticles were fabricated by oil-in-oil emulsion solvent evaporation method. A three-factor three-level Box-Behnken design using Design-Expert software was employed to optimize formulation variables. Ropinirole loaded microparticles were evaluated with respect to morphology, particle size, encapsulation efficiency, and in vitro release profile...
November 9, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27826799/colon-targeted-delivery-of-igy-against-clostridium-difficile-toxin-a-and-b-by-encapsulation-in-chitosan-ca-pectinate-microbeads
#17
Pingping Xing, Yanan Shi, Chuangchuang Dong, Hong Liu, Yan Cheng, Junbo Sun, Dalei Li, Min Li, Kaoxiang Sun, Dongxiao Feng
This study investigated the use of a newly developed chitosan-Ca pectinate microbead formulation for the colon-targeted delivery of anti-A/B toxin immunoglobulin of egg yolk (IgY) to inhibit toxin binding to colon mucosa cells. The effect of the three components (pectinate, calcium chloride, and chitosan) used for the microbead production was examined with the aim of identifying the optimal levels to improve drug encapsulation efficiency, swelling ratio, and cumulative IgY release rate. The optimized IgY-loaded bead component was pectin 5% (w/v), CaCl2 3% (w/v), and chitosan 0...
November 8, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27800567/investigation-of-the-dissolution-profile-of-gliclazide-modified-release-tablets-using-different-apparatuses-and-dissolution-conditions
#18
K K S Skripnik, M K Riekes, B R Pezzini, S G Cardoso, H K Stulzer
In the absence of an official dissolution method for modified-release tablets of gliclazide, dissolution parameters, such as apparatuses (1, 2, and 3), rotation speeds, pH, and composition of the dissolution medium were investigated. The results show that although the drug presents a pH-mediated solubility (pH 7.0 > 6.8 > 6.4 > 6.0 > 5.5 > 4.5), the in vitro release of the studied tablets was not dependent on this parameter, despite of the apparatus tested. On the other hand, the rotation speed demonstrated a greater influence (100 rpm >50 rpm)...
October 31, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27796909/in-vitro-model-simulating-gastro-intestinal-digestion-in-the-pediatric-population-neonates-and-young-infants
#19
Danna Kamstrup, Ragna Berthelsen, Philip Jonas Sassene, Arzu Selen, Anette Müllertz
The focus on drug delivery for the pediatric population has been steadily increasing in the last decades. In terms of developing in vitro models simulating characteristics of the targeted pediatric population, with the purpose of predicting drug product performance after oral administration, it is important to simulate the gastro-intestinal conditions and processes the drug will encounter upon oral administration. When a drug is administered in the fed state, which is commonly the case for neonates, as they are typically fed every 3 h, the digestion of the milk will affect the composition of the fluid available for drug dissolution/solubilization...
October 28, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27796908/nanogold-gallate-chitosan-targeted-pulmonary-delivery-for-treatment-of-lung-cancer
#20
Seamkwan Komenek, Urarika Luesakul, Sanong Ekgasit, Tirayut Vilaivan, Narong Praphairaksit, Songchan Puthong, Nongnuj Muangsin
Lung cancer is one of the most of cancer type founds and a leading cause of death worldwide. Through the development of new candidate compound (3,4,5-tribenzyloxybenzoic acid (GAOBn)) and a drug delivery system of our design of quaternized chitosan-gallic acid-folic acid stabilized gold nanoparticles (Au@QCS-GA-FA) as the targeted nanocarrier for treatment of lung cancer, we have found that GAOBn not only showed high cytotoxicity against lung cancer cells (CHAGO) with more than tenfold than cisplatin, but also showed low toxicity against normal cells (CRL-1947)...
October 27, 2016: AAPS PharmSciTech
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