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Melanie D Palm, Lisa M Misell
OBJECTIVE: The efficacy of various pre-medication strategies for comfort management during microfocused ultrasound with visualization (MFU-V) treatment has not been studied. The present objective was to compare 2 topical analgesics (lidocaine 4% and benzocaine 20%) formulated with a novel transdermal delivery system with compounded lidocaine 23%/tetracaine 7% (23/7) to mitigate discomfort during MFU-V treatment. METHODS: This was a randomized, double-blinded, split-face study...
July 1, 2018: Journal of Drugs in Dermatology: JDD
William Buhles, Jessica M Quimby, Daizie Labelle, Valentine S Williams
Single and multiple dose pharmacokinetics (PK) of mirtazapine transdermal ointment applied to the inner ear pinna of cats were assessed. Study 1 was a randomized, cross-over single dose study (n = 8). Cats were treated once with 0.5 mg/kg of mirtazapine transdermal ointment applied topically to the inner ear pinna (treatment) or administered orally (control) and then crossed over after washout. Plasma was collected predose and at specified intervals over 96 hr following dosing. Study 2 was a multiple dose study (n = 8)...
July 13, 2018: Journal of Veterinary Pharmacology and Therapeutics
Cecilia P Chung, William D Dupont, Katherine T Murray, Kathi Hall, C Michael Stein, Wayne A Ray
PURPOSE: Despite significant growth of opioid prescriptions, only limited data are available regarding the comparative safety of long-acting opioids for chronic non-cancer pain. Recent data suggest that transdermal fentanyl and oxycodone CR may have greater toxicity than morphine SR in patients with non-cancer pain. Thus, we compared the risk of out-of-hospital deaths in patients with non-cancer pain filling prescriptions for transdermal fentanyl or oxycodone CR with that for morphine SR...
July 12, 2018: Pharmacoepidemiology and Drug Safety
Jiangang Liu, Hong Luo, Paul Pu Zheng, Si Jia Wu, Kang Lee
Human cardiovascular activities are important indicators of a variety of physiological and psychological activities in human neuroscience research. The present proof-of-concept study aimed to reveal the spatiotemporal patterns of cardiovascular activities from the dynamic changes in hemoglobin concentrations in the face. We first recorded the dynamics of facial transdermal blood flow using a digital video camera and the Electrocardiography (ECG) signals using an ECG system simultaneously. Then we decomposed the video imaging data extracted from different sub-regions of a face into independent components using group independent component analysis (group ICA)...
July 12, 2018: Scientific Reports
Young Seok Ji, In Sook Kim, Tae Kon Kim, Hye Hyun Yoo
In this study, the plasma concentration profiles of tolterodine and its active metabolite, 5-hydroxymethyl tolterodine (5-HM tolterodine) were investigated in rats with tolterodine transdermal patches using liquid chromatography-tandem mass spectrometry. The plasma samples were extracted by a liquid-liquid extraction method, with an n-hexane/isopropyl alcohol mixture (9:1, v/v). Tiropramide was used as an internal standard (IS). Chromatographic separation was achieved using a C18 column (2.0 mm × 150 mm, 5 μm), with a mobile phase consisting of 5 mM ammonium acetate in distilled water/acetonitrile (50:50, v/v)...
July 1, 2018: Die Pharmazie
Cemile Kilic Bektas, Ilgin Kimiz, Aylin Sendemir Urkmez, Vasif Hasirci, Nesrin Hasirci
Treatment of chronic skin wound such as diabetic ulcers, burns, pressure wounds are challenging problems in the medical area. The aim of this study was to design a bilayer skin equivalent mimicking the natural one to be used as a tissue engineered skin graft for use in the treatments of problematic wounds, and also as a model to be used in research related to skin, such as determination of the efficacy of transdermal bioactive agents on skin cells and treatment of acute skin damages that require immediate response...
July 12, 2018: Journal of Biomaterials Science. Polymer Edition
Aaron J Courtenay, Maelíosa T C McCrudden, Kathryn J McAvoy, Helen O McCarthy, Ryan F Donnelly
Bevacizumab is a recombinant humanised monoclonal antibody used clinically as a combination chemotherapeutic. Antibody therapeutics are usually formulated as parenteral injections, owing to their low oral bioavailability. Microneedle technology provides a transdermal alternative for drug-delivery using micron-scale needle structures to penetrate directly through the stratum corneum into the dermal interstitium. This study describes the design, formulation and in vitro characterisation of both dissolving and hydrogel-forming microneedle array platforms for transdermal delivery of bevacizumab...
July 11, 2018: Molecular Pharmaceutics
Eman M Migdadi, Aaron J Courtenay, Ismaiel A Tekko, Maelíosa T C McCrudden, Mary-Carmel Kearney, Emma McAlister, Helen O McCarthy, Ryan F Donnelly
We investigated, for the first time, the potential for a hydrogel-forming microneedle (MN) patch to deliver the high-dose drug metformin HCl transdermally in a sustained manner. This may minimize some gastrointestinal side effects and small intestine absorption variations associated with oral delivery. Patches (two layers) were assembled from a lyophilised drug reservoir layer, with the MN layer made from aqueous blend of 20% w/w poly (methylvinylether-co-maleic acid) crosslinked by esterification with 7.5% w/w poly (ethylene glycol) 10,000 Da...
July 7, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
Gaurav Kumar Gulati, Lily Rachel Berger, Bruce Jackson Hinds
Nicotine replacement therapy in the form of transdermal nicotine patches and nicotine gums combined with behavioral counseling still has a low smoking cessation rate of 25%. A promising approach to smoking cessation is to remotely program variable transdermal nicotine delivery rates, with inputs from counselor and patient through a smartphone counseling application. A switchable carbon nanotube (CNT) membrane device has been developed for transdermal nicotine delivery that can be programmed to deliver variable doses matching those of nicotine patches (7, 14 and 21 mg/24 h) and nicotine gums (2 mg /4 mg)...
July 7, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
Mithila Boche, Varsha Pokharkar
Alendronate (ALD) is clinically indicated for the treatment of osteoporosis, but its therapeutic use has been marred by severe GIT adverse effects affecting quality of life in patients. In this study, we selected novel transdermal microemulsion (TDME) as a suitable carrier for ALD as the way of avoiding intestinal toxicity and highlighted its anti-osteoporotic efficacy with extensive pharmacokinetic and pharmacodynamic analysis. TDME achieved two fold increase in bioavailability as compared to oral administration in pharmacokinetic studies...
July 9, 2018: Drug Delivery and Translational Research
Eun Kyung Park, Hyo-Jung Lee, Hyemin Lee, Ju-Ha Kim, Jisung Hwang, Ja Il Koo, Sung-Hoon Kim
Though melatonin is known to improve ultraviolet B (UVB)-induced oxidative damage and inflammatory conditions via the blockade of the nuclear factor (NF)-κB, interleukin (IL)-6, there is no report on the anti-wrinkle effect of melatonin to date. Hence in the present study, the anti-wrinkle mechanism of melatonin was elucidated in UVB treated HaCaT keratinocytes and hairless mice. Herein melatonin protected against a radical initiator tert-Butyl hydroperoxide (t-BOOH) induced reactive oxygen species (ROS) production, matrix metalloprotease 1 (MMP-1), pro-collagen and cytotoxicity in HaCaT keratinocytes...
July 8, 2018: International Journal of Molecular Sciences
Karolina Anna Kosakowska, Brittany Kaylee Casey, Julie N L Albert, Yang Wang, Henry S Ashbaugh, Scott Michael Grayson
A series of branched polymers, consisting of a poly(ethylene glycol) (PEG) core and lipophilic peripheral dendrons, were synthesized and their self-assembly into reverse micelles studied towards the ultimate goal of carrier-mediated transdermal drug delivery. More specifically, this investigation systematically explored the structure-property contributions arising from location and extent of branching by varying the number of branch points at the core and the generation of dendrons at the hydrophilic-hydrophobic interface...
July 9, 2018: Biomacromolecules
Karolina Anna Kosakowska, Brittany Kaylee Casey, Samantha Leigh Kurtz, Louise B Lawson, Scott Michael Grayson
The reverse micelle self-assembly of lipophile-functionalized poly(ethylene glycol) (PEG) dendrimer hybrids is probed for applications in carrier-mediated transdermal drug delivery. Under investigation are topologically diverse amphiphiles featuring controlled branching motifs at either the polymer core (one-, two- and four-arm PEG) and/or the hydrophilic-hydrophobic interface (peripheral dendritic generations 0 to 2). Thus, a systematic investigation of the effect of branching location (core versus peripheral) on carrier properties is described...
July 9, 2018: Biomacromolecules
N V Alekseeva, I P Osnovina, E L Vladimirtseva, A V Ivanov
The present study was designed to elucidate the influence of the magnetic field on the spectroscopic characteristics of nimesulide and glucosamine sulfate preparations. The secondary objective of the study was to evaluate the clinical effectiveness of the combined application of magnetotherapy and transdermal forms containing a non-steroidal anti-inflammatory preparation and a chondroprotector with the use of magnetophoresis. For this purpose, we analyzed the samples exposed to the running magnetic field in an infrared spectrometer to elucidate the changes in the optical characteristics of the preparations of interest...
2018: Voprosy Kurortologii, Fizioterapii, i Lechebnoĭ Fizicheskoĭ Kultury
Panagiotis Anagnostis, Stavroula A Paschou, Niki Katsiki, Dimitrios Krikidis, Irene Lambrinoudaki, Dimitrios G Goulis
Transition to menopause is associated with an increase in cardiovascular disease (CVD) risk, mainly attributed to lipid and glucose metabolism dysregulation, as well as to body fat redistribution, leading to abdominal obesity. Indeed, epidemiological evidence suggests that both early menopause (EM, defined as age at menopause <45 years) and premature ovarian insufficiency (POI, defined as age at menopause <40 years) are associated with 1.5-2-fold increase in CVD risk. Menopausal hormone therapy (MHT) exerts a favorable effect on CVD risk factors (with subtle differences regarding estrogen dose, route of administration, monotherapy or combination with progestogen and type of progestogen)...
July 8, 2018: Current Vascular Pharmacology
Petra Hartmann, Edina Butt, Ágnes Fehér, Ágnes Lilla Szilágyi, Kurszán Dávid Jász, Boglárka Balázs, Mónika Bakonyi, Szilvia Berkó, Gábor Erős, Mihály Boros, Gyöngyi Horváth, Endre Varga, Erzsébet Csányi
Purpose: Since electroporation (EP) can increase the permeability of biological membranes, we hypothesized that it offers an opportunity to enhance the transdermal delivery of drugs for intra-articular indications. Our aim was to compare the anti-inflammatory and analgesic efficacy of EP-combined topical administration of diclofenac sodium hydrogel (50 mg mL-1 in 230 µL volume) with that of an equivalent dose of oral (75 mg kg-1 ) and simple topical administration. Methods: Arthritis was induced with the injection of 2% λ-carrageenan and 4% kaolin into the right knee joints of male Sprague Dawley rats...
2018: Drug Design, Development and Therapy
Xiang Yu, Yiguang Jin, Lina Du, Mengchi Sun, Jian Wang, Qiu Li, Xiangyu Zhang, Zisen Gao, Pingtian Ding
Transdermal delivery is one of important controlled drug release strategies for drug development. Cubic phases are the assemblies of amphiphilic molecules in water with the hydrophilic-hydrophobic interpenetrating network for transdermal delivery of both hydrophilic and hydrophobic drugs. However, many details about the transdermal delivery of cubic phases remain unclear. Here, metformin hydrochloride (Met) cubic phases were prepared with glyceryl monooleate (GMO), ethanol and water. The cubic structure was identified with the polarizing light microscopy and small-angle X-ray scattering method...
July 6, 2018: Molecular Pharmaceutics
Elise B Nguyen, Jeremy Wishner, Katarzyna Slowinska
Electrical stimulation of tissues has many uses in pain management, antibacterial treatment, and wound healing. The electric field stimulates epidermal migration and increases fibroblast cell proliferation. Here we show the effects of electrical field (EF) stimulation of human dermal fibroblasts (HDF) on the expression of collagen, elastin, and collagenase (MMP1; matrix metalloproteinase 1). The effects of EF stimulation are evaluated in terms of changes in cell morphology and extracellular matrix (ECM) protein expression, defined as intracellular concentration of collagen, elastin, and MMP1...
March 1, 2018: Journal of Electroanalytical Chemistry
Madhulika Pradhan, Shikha Srivastava, Deependra Singh, Shailendra Saraf, Swarnlata Saraf, Manju Rawat Singh
Transdermal delivery serves as non-invasive and effortless terminable means for systemic as well as topical drug delivery and finds itself as an option to conventional delivery route. Significant impervious nature of skin is the greatest hurdle for successful delivery of drug molecules to the deeper layers of skin for systemic absorption. Many approaches have been carried out for delivery of a medicament across skin barrier to enhance the efficacy. Among them lipid-based colloidal carriers have gained a unique position for transdermal delivery of drugs and bioactives owing to the presence of epidermal lipids as the chief component within the penetration barrier in high amount...
2018: Critical Reviews in Therapeutic Drug Carrier Systems
Noriyuko Uchida, Noriko Nishizawa Horimoto, Kuniyo Yamada, Takaaki Hikima, Yasuhiro Ishida
Mixtures of a phospholipid (1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine: DPPC) and a sodium cholate-derived surfactant (SC-C5) at room temperature formed phospholipid bilayer fragments that were edge-stabilized by SC-C5 so-called bicelles. Because the bilayer melting point of DPPC (41 °C) is above room temperature and because SC-C5 has an exceptionally low critical micelle concentration (<0.5 mM), the bicelles are kinetically frozen at room temperature. Consequently, they exist even when the mixture is diluted to a concentration of 0...
July 3, 2018: Chembiochem: a European Journal of Chemical Biology
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