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AAPS PharmSciTech

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https://www.readbyqxmd.com/read/29218583/promising-antibacterial-effects-of-silver-nanoparticle-loaded-tea-tree-oil-nanoemulsion-a-synergistic-combination-against-resistance-threat
#1
Roqya Najafi-Taher, Behnaz Ghaemi, Sharmin Kharazi, Samira Rasoulikoohi, Amir Amani
Highly resistant pathogens may be developed in patients with immune disorders after prolonged exposure to antibiotics, a growing threat worldwide. In order to overcome these problems, this study introduces a new class of engineered nanosystems comprising of tea tree oil nanoemulsion (TTO NE) loaded with Ag nanoparticles (NPs). Silver shows a strong toxicity towards a wide range of microorganisms. Also, TTO NE could be employed as a promising and safe antimicrobial agent for local therapies of bacterial infections...
December 7, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29218582/application-of-fluorescence-emission-for-characterization-of-albendazole-and-ricobendazole-micellar-systems-elucidation-of-the-molecular-mechanism-of-drug-solubilization-process
#2
Josefina Priotti, Darío Leonardi, Guillermo Pico, María C Lamas
Albendazole (ABZ) and ricobendazole (RBZ) are referred to as class II compounds in the Biopharmaceutical Classification System. These drugs exhibit poor solubility, which profoundly affects their oral bioavailability. Micellar systems are excellent pharmaceutical tools to enhance solubilization and absorption of poorly soluble compounds. Polysorbate 80 (P80), poloxamer 407 (P407), sodium cholate (Na-C), and sodium deoxycholate (Na-DC) have been selected as surfactants to study the solubilization process of these drugs...
December 7, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29218581/fabrication-of-tip-dissolving-microneedles-for-transdermal-drug-delivery-of-meloxicam
#3
Jianmin Chen, Weiyue Huang, Ziyao Huang, Shiqi Liu, Yaling Ye, Qinglian Li, Meiping Huang
Dissolving microneedles (MNs) offered a simple, minimally invasive method for meloxicam (MX) delivery to the skin. However, the fabrication of dissolving MNs still faced some challenges, such as significant time consumption, loss of drug activity, and difficulty in regulating MN drug loading. To address these issues, we developed the tip-dissolving (TD) MNs. Several kinds of drugs were encapsulated successfully, and the quantity of MX ranged from 37.23 ± 8.40 to 332.53 ± 13.37 μg was precisely controlled...
December 7, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29214609/soy-protein-microparticles-for-enhanced-oral-ibuprofen-delivery-preparation-characterization-and-in-vitro-release-evaluation
#4
Maria Antonieta Anaya Castro, Isabelle Alric, Fabien Brouillet, Jérôme Peydecastaing, Sophie Girod Fullana, Vanessa Durrieu
The objective of this work was to evaluate soy protein isolate (SPI) and acylated soy protein (SPA) as spray-drying encapsulation carriers for oral pharmaceutical applications. SPI acylation was performed by the Schotten-Baumann reaction. SPA, with an acylation rate of 41%, displayed a decrease in solubility in acidic conditions, whereas its solubility was unaffected by basic conditions. The drug encapsulation capacities of both SPI and SPA were tested with ibuprofen (IBU) as a model poorly soluble drug. IBU-SPI and IBU-SPA particles were obtained by spray-drying under eco-friendly conditions...
December 6, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29214608/a-science-and-risk-based-pragmatic-methodology-for-blend-and-content-uniformity-assessment
#5
Naheed Sayeed-Desta, Ajay Babu Pazhayattil, Jordan Collins, Chetan Doshi
This paper describes a pragmatic approach that can be applied in assessing powder blend and unit dosage uniformity of solid dose products at Process Design, Process Performance Qualification, and Continued/Ongoing Process Verification stages of the Process Validation lifecycle. The statistically based sampling, testing, and assessment plan was developed due to the withdrawal of the FDA draft guidance for industry "Powder Blends and Finished Dosage Units-Stratified In-Process Dosage Unit Sampling and Assessment...
December 6, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29192405/development-of-itraconazole-tablets-containing-viscous-kinetisol%C3%A2-solid-dispersions-in-vitro-and-in-vivo-analysis-in-dogs
#6
Justin M Keen, Justin S LaFountaine, Justin R Hughey, Dave A Miller, James W McGinity
The formulation factors relevant to developing immediate and controlled release dosage forms containing poorly soluble drugs dispersed in amorphous systems are poorly understood. While the utility of amorphous solid dispersions is becoming apparent in the pharmaceutical marketplace, literature reports tend to concentrate on the development of solid dispersion particulates, which then must be formulated into a tablet. Amorphous solid dispersions of itraconazole in high molecular weight hydroxypropyl methylcellulose were prepared by KinetiSol® Dispersing and tablets were formulated to immediately disintegrate or control the release of itraconazole...
November 30, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29181706/self-assembling-raloxifene-loaded-mixed-micelles-formulation-optimization-in-vitro-cytotoxicity-and-in-vivo-pharmacokinetics
#7
Radhika Kanade, Mithila Boche, Varsha Pokharkar
Raloxifene (RLX) has been strongly recommended for postmenopausal women at high risk of invasive breast cancer and for prevention of osteoporosis. However, low aqueous solubility and reduced bioavailability hinder its clinical application. The objective of this study was to explore the potential of RLX loaded mixed micelles (RLX-MM) using Pluronic F68 and Gelucire 44/14 for enhanced bioavailability and improved anticancer activity on human breast cancer cell line (MCF-7). RLX-MM were prepared by solvent evaporation method and optimized using 32 factorial design...
November 27, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29181705/coenzyme-q10-loaded-fish-oil-based-bigel-system-probing-the-delivery-across-porcine-skin-and-possible-interaction-with-fish-oil-fatty-acids
#8
Mohd Hanif Zulfakar, Lee Mei Chan, Khurram Rehman, Lam Kok Wai, Charles M Heard
Coenzyme Q10 (CoQ10) is a vitamin-like oil-soluble molecule that has anti-oxidant and anti-ageing effects. To determine the most optimal CoQ10 delivery vehicle, CoQ10 was solubilised in both water and fish oil, and formulated into hydrogel, oleogel and bigel. Permeability of CoQ10 from each formulation across porcine ear skin was then evaluated. Furthermore, the effects of the omega-3 fatty eicosapentaenoic (EPA) and docosahexaenoic (DHA) acids from fish oil on skin permeation were investigated by means of nuclear magnetic resonance (NMR) and computerised molecular modelling docking experiments...
November 27, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29168128/enhancement-of-galantamine-hbr-skin-permeation-using-sonophoresis-and-limonene-containing-pegylated-liposomes
#9
Worranan Rangsimawong, Yasuko Obata, Praneet Opanasopit, Tanasait Ngawhirunpat, Kozo Takayama
This study aimed to investigate the effect of low-frequency sonophoresis (SN) and limonene-containing PEGylated liposomes (PL) on the transdermal delivery of galantamine HBr (GLT). To evaluate the skin penetration mechanism, confocal laser scanning microscopy (CLSM), Fourier transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC) were employed. The application of SN led to more GLT penetration into and through the skin than GLT solution alone. The liposomes also improved GLT permeation, and 2% limonene-containing PL (PL-LI2%) exhibited the highest GLT permeation, followed by PL-LI1%, PL-LI0...
November 22, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29164481/excipient-stability-a-critical-aspect-in-stability-of-pharmaceuticals
#10
EDITORIAL
S Narasimha Murthy, Michael A Repka
No abstract text is available yet for this article.
November 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29159749/fullerenol-based-intracellular-delivery-of-methotrexate-a-water-soluble-nanoconjugate-for-enhanced-cytotoxicity-and-improved-pharmacokinetics
#11
Shradha Bahuguna, Manish Kumar, Gajanand Sharma, Rajendra Kumar, Bhupinder Singh, Kaisar Raza
Derivatization of fullerenes to polyhydroxylated fullerenes, i.e., fullerenols (FLU), dramatically decreases their toxicity and has been reported to enhance the solubility as well as cellular permeability. In this paper, we report synthesis of FLU as nanocarrier and subsequent chemical conjugation of Methotrexate (MTX) to FLU with a serum-stable and intracellularly hydrolysable ester bond between FLU and MTX. The conjugate was characterized for physiochemical attributes, micromeritics, drug-loading, and drug-release and evaluated for cancer cell-toxicity, cellular-uptake, hemocompatibility, protein binding, and pharmacokinetics...
November 20, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29147872/fluidized-bed-hot-melt-granulation-as-a-tool-to-improve-curcuminoid-solubility
#12
Cristiane C C Teixeira, Elias de Paiva Junior, Luis Alexandre Pedro de Freitas
Curcumin is the main bioactive component of Curcuma longa L. and has recently aroused growing interest from the scientific community. Unfortunately, the medicinal properties attributed to curcuminoids are impaired by their low oral bioavailability or low solubility in aqueous solutions. Many strategies have been studied to improve curcumin solubility; however, the preparation of granules using hydrophilic materials has never been attempted. The aim of this work was to develop curcumin granules by fluidized bed hot-melt granulation using the hydrophilic carrier Gelucire® 50:13...
November 16, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29147871/an-optimized-and-feasible-preparation-technique-for-the-industrial-production-of-hydrogel-patches
#13
Wei-Ze Li, Wen-Xia Han, Xu-Liang Hao, Ning Zhao, Xi-Feng Zhai, Li-Bin Yang, Shu-Miao He, Yu-Chuan Cheng, Han Zhang, Li-Na Fu, Yan Zhang, Ze Liang
For hydrogel patches, the laboratory tests could not fully reveal the existing problems of full scale of industrial production, and there are few studies about the preparation technique for the industrial manufacturing process of hydrogel patches. So, the purpose of this work was to elucidate the effects of mainly technological operation and its parameters on the performance of hydrogel patches at the industrial-scale production. The results revealed the following: (1) the aqueous phase was obtained by polyvinylpyrrolidone (PVP) along with tartaric acid dissolved in purified water, then feeding this into a vacuum mixer as a whole in one batch, thus extended the crosslinking reaction time of hydrogel paste (matrix) and allowed the operation of coating/cutting-off to be carried out easily, and there was no permeation of backing layer; (2) the gel strength of the hydrogel patches increased with the increase of working temperature, however, once the temperature exceeded 35 ± 2 °C, the hydrogel paste would lose water severely and the resultant physical crosslinking structure which has lower gel/cohesive strength would easily bring gelatinization/residues during application; (3) the relative humidity (RH) of the standing-workshop was dynamically controlled (namely at 35 ± 2 °C, keeping the RH at 55 ± 5% for 4 days, then 65 ± 5% for 2 days), which would make patches with satisfactory characteristics such as better flexibility, higher adhesive force, smooth flat matrix surface, and without gelatinization/residues and warped edge during the using process; (4) the aging of the packaged hydrogel patches was very sensitive to storage temperature, higher temperature, higher gel strength and lower adhesiveness...
November 16, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29138987/optimized-ciclopirox-based-eudragit-rlpo-nail-lacquer-effect-of-endopeptidase-enzyme-as-permeation-enhancer-on-transungual-drug-delivery-and-efficiency-against-onychomycosis
#14
Abeer Khattab, Samia Shalaby
The aims of our investigation were to develop and optimize ciclopirox (CPX) nail lacquer using nonbiodegradable Eudragit RLPO (E-RLPO) as a film former and to assess its penetration efficiency across the human nail plate. Preliminary trials such as hydration enhancement factor (HEF), a retained drug in the nail plate, and SEM were studied to select the optimized permeation enhancer to be incorporated in the optimized lacquer formulation. A 3(3) full factorial design was built up to study the effect of three different factors, concentration of E-RLPO (10, 20, and 30%), Tween 80 (0...
November 14, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29134578/experimental-and-computational-comparative-study-of-the-supercritical-fluid-technology-sft-and-kneading-method-in-preparing-%C3%AE-cyclodextrin-complexes-with-two-essential-oils-linalool-and-carvacrol
#15
Nizar A Al-Shar'i, Rana M Obaidat
Supercritical fluid technology (SFT) offers many advantages as a potential complexation method compared to the conventional kneading technique. Its applicability to processess in which solvents are not required is a significant benefit. The main aim of this study was to evaluate, experimentally and computationally, the applicability of SFT in the preparation of β-cyclodextrin complexes with two selected essential oils, namely, carvacrol and linalool. Preparation of the complexes was performed using kneading and SFT method...
November 13, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29124477/correction-to-drug-delivery-from-an-innovative-lama-laba-co-suspension-delivery-technology-fixed-dose-combination-mdi-evidence-of-consistency-robustness-and-reliability
#16
Amber Doty, Jon Schroeder, Kou Vang, Mark Sommerville, Mervin Taylor, Brad Flynn, David Lechuga-Ballesteros, Peter Mack
This article was originally published Online First without open access. After publication it was discovered that the author had ordered open access during the production process. The incorrect license was assigned to this paper due to a technical error.
November 9, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29116619/evaluation-of-efficiency-of-modified-polypropylenimine-ppi-with-alkyl-chains-as-non-viral-vectors-used-in-co-delivery-of-doxorubicin-and-trail-plasmid
#17
Mahboubeh Ebrahimian, Sahar Taghavi, Maryam Ghoreishi, Shahrzad Sedghi, Sara Amel Farzad, Mohammad Ramezani, Maryam Hashemi
In this study, co-delivery system was achieved via plasmid encoding TNF related apoptosis inducing ligand (pTRAIL) and doxorubicin (DOX) using carrier based on polypropylenimine (PPI) modified with 10-bromodecanoic acid. Incorporation of alkylcarboxylate chain to PPIs (G4 and G5) could improve transfection efficiency via overcoming the plasma membrane barrier of the cells and decrease cytotoxicity of PPI. Characterization of fabricated NPs revealed that PPI G5 in which 30% of primary amines were substituted by alkyl carboxylate chain (PPI G5-Alkyl 30%) has higher drug loading as compared to the other formulations...
November 7, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29110294/chemometric-methods-to-quantify-1d-and-2d-nmr-spectral-differences-among-similar-protein-therapeutics
#18
Kang Chen, Junyong Park, Feng Li, Sharadrao M Patil, David A Keire
NMR spectroscopy is an emerging analytical tool for measuring complex drug product qualities, e.g., protein higher order structure (HOS) or heparin chemical composition. Most drug NMR spectra have been visually analyzed; however, NMR spectra are inherently quantitative and multivariate and thus suitable for chemometric analysis. Therefore, quantitative measurements derived from chemometric comparisons between spectra could be a key step in establishing acceptance criteria for a new generic drug or a new batch after manufacture change...
November 6, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29110293/evaluation-of-streptococcus-thermophilus-iffi-6038-microcapsules-prepared-using-an-ultra-fine-particle-processing-system
#19
Huanbin Zhou, Shunyi Li, Yao Chen, Qian Zhang, Xuequn Bai, Chune Zhu, Hu Liu, Lili Wang, Chuanyu Wu, Xin Pan, Chuanbin Wu
Microencapsulation technology has the potential to protect probiotics and to deliver them to the gut, and extrusion is one of the most commonly used methods. However, the rather large diameters of 1~5 mm produced tend to cause oral grittiness and result in low compliance. In this article, Streptococcus thermophilus IFFI 6038 (IFFI 6038) microcapsules were prepared using an ultra-fine particle processing system (UPPS) previously developed by this research group. IFFI 6038 suspension was pumped by a peristaltic pump to the feeding inlet nozzle and then dispersed into micro-droplets by a rotating disk, followed by solidification...
November 6, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29110292/development-of-chitosan-based-ph-sensitive-polymeric-micelles-containing-curcumin-for-colon-targeted-drug-delivery
#20
Thisirak Woraphatphadung, Warayuth Sajomsang, Theerasak Rojanarata, Tanasait Ngawhirunpat, Prasopchai Tonglairoum, Praneet Opanasopit
pH-sensitive N-naphthyl-N,O-succinyl chitosan (NSCS) and N-octyl-N,O-succinyl chitosan (OSCS) polymeric micelles carriers have been developed to incorporate curcumin (CUR) for colon-targeted drug delivery. The physical entrapment methods (dialysis, co-solvent evaporation, dropping, and O/W emulsion) were applied. The CUR-loaded micelles prepared by the dialysis method presented the highest loading capacity. Increasing initial amount of CUR from 5 to 40 wt% to polymer resulted in the increase in loading capacity of the polymeric micelles...
November 6, 2017: AAPS PharmSciTech
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