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https://www.readbyqxmd.com/read/29148228/evaluation-of-markers-out-of-the-steroid-profile-for-the-screening-of-testosterone-misuse-part-i-transdermal-administration
#1
Aristotelis Kotronoulas, Àlex Gomez-Gómez, Andreu Fabregat, Jordi Segura, Sheng Yang, Yanyi Xing, Wu Moutian, Josep Marcos, Jesús Joglar, Rosa Ventura, Oscar J Pozo
Although the introduction by WADA of the steroid module of the athlete biological passport (ABP) marked an important step forward in the screening of testosterone (T) misuse, it still remains one of the most difficult challenges in doping control analysis. The urinary determination of alternative markers has been recently reported as a promising tool for improving the screening of T oral administration. However, their evaluation for other, commonly used, administration routes is still required. The main goal of this study is the evaluation of the potential of two groups of metabolites (cysteinyl conjugated and glucuronoconjugated) after transdermal and intramuscular administration of T...
November 17, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29147871/an-optimized-and-feasible-preparation-technique-for-the-industrial-production-of-hydrogel-patches
#2
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/29144055/confocal-raman-spectroscopic-imaging-for-in-vitro-monitoring-of-active-ingredient-penetration-and-distribution-in-reconstructed-human-epidermis-model
#3
Lynda Miloudi, Franck Bonnier, Ali Tfayli, Florent Yvergnaux, Hugh J Byrne, Igor Chourpa, Emilie Munnier
Topically applied Active Cosmetic Ingredients (ACI) or Active Pharmaceutical Ingredients (API) efficacy is directly related to their efficiency of penetration in the skin. In vitro Reconstructed Human Epidermis (RHE) surrogate models offer in vivo like skin samples for transdermal studies. Using Delipidol®, an ACI currently used in the cosmetics industry, the capabilities to deliver accurate distribution maps and penetration profiles of this molecule by means of Confocal Raman spectroscopic Imaging have been demonstrated...
November 16, 2017: Journal of Biophotonics
https://www.readbyqxmd.com/read/29141479/development-of-a-carboxymethyl-chitosan-functionalized-nanoemulsion-formulation-for-increasing-aqueous-solubility-stability-and-skin-permeability-of-astaxanthin-using-low-energy-method
#4
Liang Hong, Chuan-Li Zhou, Feng-Ping Chen, Dan Han, Chun-Yuan Wang, Jia-Xin Li, Zhe Chi, Chen-Guang Liu
In this research, firstly astaxanthin (ASX)-loaded nanoemulsions (NEs) were produced using a convenient low-energy emulsion phase inversion method. The optimised ASX-NEs were prepared in the presence of Cremophor(®) EL and Labrafil(®) M 1944 CS, with a surfactant-to-oil ratio of 4:6. The ASX-NE droplets were spherical with a mean droplet diameter below 100 nm and a small negative surface charge. The system was stable without alteration of mean droplet diameter for three months. Then, the ASX-NE was functionalised with carboxymethyl chitosan (CMCS) through direct CMCS (0...
November 15, 2017: Journal of Microencapsulation
https://www.readbyqxmd.com/read/29133235/can-the-cellular-internalization-of-cargo-proteins-be-enhanced-by-fusing-a-tat-peptide-in-the-center-of-proteins-a-fluorescence-study
#5
Xiaochao Chen, Jing Chen, Rong Fu, Pingfan Rao, Richard Weller, Jeremy Brasdshaw, Shutao Liu
Aim to investigate whether the cellular uptake of cargo proteins can be enhanced by fusing a Tat peptide in the center of proteins, GST-Tat-GFP and GST-GFP-Tat proteins were firstly constructed and expressed. The cellular internalization of both proteins was then evaluated and compared in HeLa cells by using fluorescent microscopy and flow cytometry, as well as the transdermal delivery in human skin by using confocal microscopy. Results from in-vitro cell experiments showed that GST-Tat-GFP protein efficiently internalized into HeLa cells when a Tat peptide was fused in the center of proteins, whereas its efficiency is lower than that of GST-GFP-Tat protein with a Tat peptide terminal fused...
November 10, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29132090/the-potential-use-of-transdermal-drug-delivery-for-the-prophylaxis-and-management-of-stroke-and-coronary-artery-disease
#6
REVIEW
Kevin Ita
In 2013, cardiovascular disease was responsible for 30.8% (800,937) of all 2,596,993 deaths, or approximately 1 of every 3 deaths while stroke caused about 1 of every 20 deaths in the United States [1]. To put it in context, about 795,000 people continue to have a new or recurrent stroke (ischemic or hemorrhagic) [1] in the USA. Mechanical vascular recanalization and thrombolysis with tissue plasminogen activator are the only clinically useful approaches available now for the management of ischemic stroke [2]...
June 4, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29132043/the-effect-of-diethylene-glycol-monoethyl-ether-on-skin-penetration-ability-of-diclofenac-acid-nanosuspensions
#7
Rosa Pireddu, Chiara Sinico, Guido Ennas, Michele Schlich, Donatella Valenti, Sergio Murgia, Francesca Marongiu, Anna Maria Fadda, Francesco Lai
The poor ability of many drugs to cross skin layers is the main limiting factor for the exploitation of the transdermal route for drug delivery. As a consequence, several approaches have been proposed to overcome the skin barrier, such as the inclusion of penetration enhancers in the topically applied drug solutions and emulsions. In this work, the penetration enhancer diethylene glycol monoethyl ether was included in novel diclofenac acid nanocrystal formulations, developed using the wet media milling technique and Poloxamer 188 as stabilizer...
November 6, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29131564/light-emitting-photon-upconversion-nanoparticles-in-the-generation-of-transdermal-reactive-oxygen-species
#8
Martin Prieto, Alina Rwei, Teresa Alejo, Wei Tuo, Maria Teresa Lopez-Franco, Gracia Mendoza, Victor Sebastian, Daniel S Kohane, Manuel Arruebo
Common photosensitizers used in photodynamic therapy do not penetrate the skin effectively. In addition, the visible blue and red lights used to excite such photosensitizers have shallow penetration depths through tissue. To overcome these limitations, we have synthesized ultraviolet and visible light emitting, energy-transfer based upconversion nanoparticles, and co-encapsulated them inside PLGA-PEG nanoparticles with photosensitizer protoporphyrin IX. Nd3+ has been introduced as sensitizer in the upconversion nanostructures to allow their excitation at 808 nm...
November 13, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/29131306/comparative-effectiveness-and-safety-of-cognitive-enhancers-for-treating-alzheimer-s-disease-systematic-review-and-network-metaanalysis
#9
Andrea C Tricco, Huda M Ashoor, Charlene Soobiah, Patricia Rios, Areti Angeliki Veroniki, Jemila S Hamid, John D Ivory, Paul A Khan, Fatemeh Yazdi, Marco Ghassemi, Erik Blondal, Joanne M Ho, Carmen H Ng, Brenda Hemmelgarn, Sumit R Majumdar, Laure Perrier, Sharon E Straus
BACKGROUND/OBJECTIVES: To examine the comparative effectiveness and safety of cognitive enhancers for Alzheimer's disease (AD). DESIGN: Systematic review and Bayesian network metaanalysis (NMA). SETTING: MEDLINE, EMBASE, Cochrane Library, CINAHL, Ageline (inception-March 2016). PARTICIPANTS: Individuals with AD in randomized controlled trials (RCTs), quasi-RCTs, and nonrandomized studies. INTERVENTION: Any combination of donepezil, rivastigmine, galantamine, or memantine...
September 29, 2017: Journal of the American Geriatrics Society
https://www.readbyqxmd.com/read/29130758/proniosomes-derived-niosomes-recent-advancements-in-drug-delivery-and-targeting
#10
Maryam Khatoon, Kifayat Ullah Shah, Fakhar Ud Din, Shefaat Ullah Shah, Asim Ur Rehman, Naz Dilawar, Ahmad Nawaz Khan
Vesicular drug delivery systems have gained wide attention in the field of nanotechnology. Among them proniosomes become the superior over other vesicular carriers. Proniosomes are dry formulations of water soluble nonionic surfactant coated carrier system which immediately forms niosomes upon hydration. They have the capability to overcome the instability problems associated with niosomes and liposomes and have the potential to improve solubility, bioavailability, and absorption of various drugs. Furthermore, they offer versatile drug delivery concept for enormous number of hydrophilic and hydrophobic drugs...
2017: Drug Delivery
https://www.readbyqxmd.com/read/29128593/nanochitosan-enriched-poly-%C3%AE%C2%B5-caprolactone-electrospun-wound-dressing-membranes-a-fine-tuning-of-physicochemical-properties-hemocompatibility-and-curcumin-release-profile
#11
Reshmi Cr, Suja Ps, Manaf O, Sanu Pp, Sujith A
Nanochitosan (NC) enriched Poly (ε-caprolactone) (PCL) nanofibrous membranes were fabricated for controlled curcumin delivery and wound dressing. A significant increase in hydrophilicity, PBS sorption, and vapour transmission were observed by incorporation of NC in PCL. Hemolysis assay, blood clot kinetics and platelet adhesion studies on PCL/NC membrane confirmed the hemocompatibility of the scaffold. NC also imparts appropriate antibacterial activity and biocompatibility promising for a wound dressing material...
November 8, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29127106/a-melanin-mediated-cancer-immunotherapy-patch
#12
Yanqi Ye, Chao Wang, Xudong Zhang, Quanyin Hu, Yuqi Zhang, Qi Liu, Di Wen, Joshua Milligan, Adriano Bellotti, Leaf Huang, Gianpietro Dotti, Zhen Gu
Melanin is capable of transforming 99.9% of the absorbed sunlight energy into heat, reducing the risk of skin cancer. We here develop a melanin-mediated cancer immunotherapy strategy through a transdermal microneedle patch. B16F10 whole tumor lysate containing melanin is loaded into polymeric microneedles that allow sustained release of the lysate upon insertion into the skin. In combination with the near-infrared light irradiation, melanin in the patch mediates the generation of heat, which further promotes tumor-antigen uptake by dendritic cells, and leads to enhanced antitumor vaccination...
November 10, 2017: Science Immunology
https://www.readbyqxmd.com/read/29125423/management-of-chronic-neuropathic-pain-with-single-and-compounded-topical-analgesics
#13
Nebojsa Nick Knezevic, Tatiana Tverdohleb, Farid Nikibin, Ivana Knezevic, Kenneth D Candido
The goal of our review was to emphasize important aspects that physicians should take into consideration when prescribing topical analgesics as part of chronic neuropathic pain treatment. We discuss the dermatopharmacokinetics and microstructural components of the skin, differences between topical and transdermal drug delivery, and topical medication effects on peripheral neuropathy and central sensitization. Even though the US FDA approved topical analgesics are 8%-capsaicin and 5%-lidocaine patches for treating postherpetic neuralgia, there are many other studies conducted on the efficacy of topical ketamine cream, clonidine gel, topical gabapentin, topical baclofen and topical phenytoin for peripheral neuropathic pain, either alone or in combination with other formulations...
November 10, 2017: Pain Management
https://www.readbyqxmd.com/read/29125060/dendritic-polymers-for-dermal-drug-delivery
#14
Kaushalkumar Dave, Venkata Vamsi Krishna Venuganti
Skin-mediated therapeutic delivery is a potential alternative to traditional drug delivery approaches. However, dermal drug delivery is limited to the molecules with optimal physico-chemical properties. To overcome this barrier for delivering 'nonideal' drug molecules across the skin, different drug carriers and penetration enhancement methods have been investigated. Conventional chemical and physical approaches for dermal drug delivery are limited by their skin irritation potential, complexity of application and poor patient compliance...
December 2017: Therapeutic Delivery
https://www.readbyqxmd.com/read/29120894/advances-in-pharmacotherapies-for-movement-disorders-in-children-current-limitations-and-future-progress
#15
Jean-Pierre Lin
PURPOSE OF REVIEW: In childhood, movement disorders are generated by a very large number of disorders of the nervous system, and the very different developmental ages at which these occur make studies of pharmacotherapy efficacy extremely difficult. In most clinical practices, medication used in management is by trial and error, and limited by lack of efficacy and/or adverse drug reactions leading to drug intolerance. Nevertheless, symptom reduction using polypharmacy must be balanced against any accompanying comorbidities such as poor attention and concentration, constipation, ileus, urinary retention, blurred vision sedation and respiratory depression...
December 2017: Current Opinion in Pediatrics
https://www.readbyqxmd.com/read/29116267/permeation-pathways-through-lateral-domains-in-model-membranes-of-skin-lipids
#16
Annalaura Del Regno, Rebecca Notman
An understanding of how molecules permeate the complex lipid matrix of the stratum corneum (SC) skin barrier is important for transdermal drug delivery, preventing the adsorption of toxic chemicals and tackling skin diseases. In this paper we present atomistic molecular dynamics simulations of skin-lipid bilayers composed of ceramides, cholesterol (CHOL) and free fatty acids at different lipid compositions and levels of hydration and investigate both perpendicular and lateral permeation pathways through the systems...
November 8, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/29116244/delivery-of-neostigmine-and-glycopyrrolate-by-iontophoresis-a-nonrandomized-study-in-individuals-with-spinal-cord-injury
#17
Mark A Korsten, Brian L Lyons, Miroslav Radulovic, Tradd M Cummings, Gautam Sikka, Kamaldeep Singh, Anton Sabiev, Ann M Spungen, William A Bauman
STUDY DESIGN: Phase I Clinical Trial. OBJECTIVES: In this proof-of-principle study, the effectiveness and safety of transdermal administration of neostigmine/glycopyrrolate to elicit a bowel movement was compared to intravenous administration in patients with spinal cord injury. SETTING: James J. Peters Veterans Affairs Medical Center (Bronx, NY). METHODS: Individuals were screened for responsiveness (Physical Response) to intravenous neostigmine (0...
November 8, 2017: Spinal Cord
https://www.readbyqxmd.com/read/29115187/hyaluronate-parathyroid-hormone-peptide-conjugate-for-transdermal-treatment-of-osteoporosis
#18
Minsoo Cho, Seulgi Han, Hyemin Kim, Ki Su Kim, Sei Kwang Hahn
Human parathyroid hormone 1-34 fragment (PTH1-34) has been used as a FDA-approved therapeutics to treat osteoporosis by daily subcutaneous injection. In this work, we successfully developed PTH1-34 conjugated hyaluronic acid (HA) for the transdermal treatment of osteoporosis with improved patient compliance. HA-PTH1-34 conjugate was synthesized by the coupling reaction between aldehyde group introduced to HA and amine group of PTH1-34. After characterization by gel permeation chromatography (GPC) and ELISA, the biological effect of HA-PTH1-34 conjugate on the proliferation of human osteoblast cells was confirmed by in vitro calcium colorimetric assay and cAMP assay...
November 8, 2017: Journal of Biomaterials Science. Polymer Edition
https://www.readbyqxmd.com/read/29113805/octenylsuccinate-hydroxypropyl-phytoglycogen-enhances-the-solubility-and-in-vitro-antitumor-efficacy-of-niclosamide
#19
Ying Xie, Yuan Yao
Niclosamide is a promising antitumor agent, but its low aqueous solubility places limit on its antitumor efficacy. The aim of this study was to improve the solubility and dissolution of niclosamide through using octenylsuccinate hydroxypropyl phytoglycogen (OHPP), an amphiphilic dendrimer-like biopolymer. The niclosamide-OHPP solid dispersion (niclo-OHPP SD) was prepared and characterized in terms of crystallinity, molecular interactions, solubility and dissolution profile, in-vitro antitumor efficacy, and in-vitro transdermal amount...
November 4, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29111097/lipid-nanocarriers-as-skin-drug-delivery-systems-properties-mechanisms-of-skin-interactions-and-medical-applications
#20
REVIEW
M Sala, R Diab, A Elaissari, H Fessi
During the past decades, lipid nanocarriers are gaining momentum with their multiple advantages for the management of skin diseases. Lipid nanocarriers enable to target the therapeutic payload to deep skin layers or even to reach the blood circulation making them a promising cutting-edge technology. Lipid nanocarriers refer to a large panel of drug delivery systems. Lipid vesicles are the most conventional, known to be able to carry lipophilic and hydrophilic active agents. A variety of lipid vesicles with high flexibility and deformability could be obtained by adjusting their composition; namely ethosomes, transfersomes and penetration enhancer lipid vesicles which achieve the best results in term of skin permeation...
October 27, 2017: International Journal of Pharmaceutics
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