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https://www.readbyqxmd.com/read/28534130/tissue-distribution-and-dermal-drug-determination-of-indomethacin-transdermal-absorption-patches
#1
Jingjing Ma, Ying Gao, Yinghua Sun, Dawei Ding, Qi Zhang, Bingjun Sun, Menglin Wang, Jin Sun, Zhonggui He
The tissue distribution and percutaneous drug absorption of indomethacin (IND) patches were studied using commercial IND as a comparison. The concentration of IND in skin, plasma, and muscle in mice was measured by LC-MS/MS, and the IND concentration in the dermis of rats was also monitored by microdialysis. After percutaneous administration, the "double-peak" phenomenon occurred in different tissues, and the IND concentration was ranked as skin first, followed by plasma and then muscle. In particular, skin acted as a reservoir for drug release, and the "secondary hump" in tissue distribution was attributed to the subsequent release of lipophilic IND in skin...
May 22, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28530093/iron-oxide-nanoparticles-powered-micro-optical-coherence-tomography-for-in-situ-imaging-the-penetration-and-swelling-of-polymeric-microneedles-in-skin
#2
Razina Z Seeni, Xiaojun Yu, Hao Chang, Peng Chen, Linbo Liu, Chenjie Xu
In recent years, polymeric microneedles (MNs) have attracted keen interests among researchers for their applicability in transdermal drug delivery and interstitial skin fluid (ISF) extraction. When design and characterize such devices, it is critical to monitor their real-time in vitro and in vivo performances to optimize the desired effects, yet most of the existing methods are incapable of such functions. To address this unmet need, we develop a real-time non-invasive imaging methodology by integrating iron oxide (Fe3O4) nanoparticles into polymeric MNs to enhance image contrast for micro-optical coherence tomography (µOCT) imaging...
May 22, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28526486/plasma-concentrations-of-transdermal-fentanyl-and-buprenorphine-in-pigs-sus-scrofa-domesticus
#3
Suzanne Osorio Lujan, Walid Habre, Youssef Daali, Zhaoxin Pan, Peter W Kronen
OBJECTIVE: To determine the absorption characteristics of fentanyl and buprenorphine administered transdermally in swine. STUDY DESIGN: A randomized comparative experimental trial. ANIMALS: Twenty-four Yorkshire gilts weighing 27.8±2.2 kg (mean±standard deviation). METHODS: Animals were randomly assigned to different doses of transdermal patches (TPs) of fentanyl (50 μg hour(-1), 75 μg hour(-1) and 100 μg hour(-1)) or buprenorphine (35 μg hour(-1) and 70 μg hour(-1)), once or twice...
January 11, 2017: Veterinary Anaesthesia and Analgesia
https://www.readbyqxmd.com/read/28525889/eugenol-alleviated-breast-precancerous-lesions-through-her2-pi3k-akt-pathway-induced-cell-apoptosis-and-s-phase-arrest
#4
Min Ma, Yi Ma, Gui-Juan Zhang, Rui Liao, Xue-Feng Jiang, Xian-Xin Yan, Feng-Jie Bie, Xiao-Bo Li, Yan-Hong Lv
Eugenol can be separated from the oil extract of clove bud, and has many pharmacological functions such as anticancer and transdermal absorption. HER2/PI3K-AKT is a key signaling pathway in the development of breast cancer. In this study, 80 μM eugenol could significantly inhibit the proliferation of HER-2 positive MCF-10AT cells and the inhibition rate was up to 32.8%, but had no obvious inhibitory effect on MCF-7 and MCF-10A cells with HER2 weak expression. Eugenol also significantly induced human breast precancerous lesion MCF-10AT cell apoptosis and cell cycle S-phase arrest, but the biological effects nearly disappeared after HER2 over-expression through transfecting pcDNA3...
May 5, 2017: Oncotarget
https://www.readbyqxmd.com/read/28524111/synthesis-and-pharmacological-properties-of-novel-esters-based-on-monoterpenoids-and-glycine
#5
Mariia Nesterkina, Iryna Kravchenko
Esters based on mono- and bicyclic terpenoids with glycine have been synthesized via Steglich esterification and characterized by ¹H-NMR, IR, and mass spectral studies. Their analgesic and anti-inflammatory activities were investigated after transdermal delivery on models of formalin, capsaicin, and AITC-induced pain, respectively. Glycine esters of menthol and borneol exhibited higher antinociceptive action, whereas eugenol derivative significantly suppressed the development of the inflammatory process. The mechanism of competitive binding between terpenoid esters and TRPA1/TRPV1 agonists was proposed explaining significant analgesic effect of synthesized derivatives...
May 18, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28523100/transdermal-bioavailability-in-rats-of-lidocaine-in-the-forms-of-ionic-liquids-salts-and-deep-eutectic
#6
Paula Berton, Kristin R Di Bona, Denise Yancey, Syed A A Rizvi, Marquita Gray, Gabriela Gurau, Julia L Shamshina, Jane F Rasco, Robin D Rogers
Tuning the bioavailability of lidocaine was explored by its incorporation into the ionic liquid lidocainium docusate ([Lid][Doc]) and the deep eutectic Lidocaine·Ibuprofen (Lid·Ibu) and comparing the transdermal absorption of these with the crystalline salt lidocainium chloride ([Lid]Cl). Each form of lidocaine was dissolved in a vehicle cream and topically applied to Sprague-Dawley rats. The concentrations of the active pharmaceutical ingredients (APIs) in blood plasma were monitored over time as an indication of systemic absorption...
May 11, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28514299/application-of-a-buprenorphine-transdermal-patch-for-the-perioperative-analgesia-in-patients-who-underwent-simple-lumbar-discectomy
#7
Jian Tang, Jin Fan, Yilun Yao, Weihua Cai, Guoyong Yin, Wei Zhou
This study aimed to investigate the perioperative analgesic effect of a buprenorphine transdermal patch in patients who underwent simple lumbar discectomy.In total, 96 patients were randomly divided into parecoxib intravenous injection (Group A), oral celecoxib (Group B), and buprenorphine transdermal patch groups (Group C). The pain status, degree of satisfaction, adverse effects, and condition in which the patient received tramadol hydrochloride for uncontrolled pain were recorded on the night before surgery, postoperative day 1, postoperative day 3, and postoperative day 5...
May 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28509626/custom-compounded-bioidentical-hormone-therapy-why-so-popular-despite-potential-harm-the-case-against-routine-use
#8
M L'Hermite
Wide rejection of conventional hormone therapy (HT) after the initial publication of the Women's Health Initiative (WHI) led to unjustified use of custom-compounded bioidentical hormones. In the USA, it became an unregulated drug manufacturer industry in disguise, without proper control and making false claims and misleading advertisements. Manufacturing quality is not ensured. Unspecific harm from compounding has occurred on a large scale, such as deaths from infected products and end-stage renal failure plus carcinoma due to confusion between different Chinese herbs...
June 2017: Climacteric: the Journal of the International Menopause Society
https://www.readbyqxmd.com/read/28508376/in-vivo-and-qualitative-studies-investigating-the-translational-potential-of-microneedles-for-use-in-the-older-population
#9
Helen L Quinn, Carmel M Hughes, Ryan F Donnelly
Microneedles (MNs) are a novel transdermal drug delivery platform, rapidly progressing from a substantive evidence base, towards commercialisation. As part of this transition, it is important to consider the future use of MNs by older people in order to ensure optimal therapeutic outcomes for this unique and increasing population group. This paper, therefore, considers the use of MNs by those aged over 65 years, investigating insertion parameters in ageing skin, alongside the feasibility and acceptability of the technology...
May 15, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28506203/optimization-of-microemulsion-based-transdermal-gel-of-triamcinolone
#10
Bhagyashree Chaudhari, Swati Jagdale
BACKGROUND: Triamcinolone is a long acting corticosteroid used in the treatment of arthritis, eczema, psoriasis and similar conditions which causes inflammation. Triamcinolone has half-life of 88 minutes. Prolonged oral use is associated with gastrointestinal adverse effects as peptic ulcer, abdominal distention and ulcerative esophagitis. Microemulgel offers advantage of better stability, better loading capacity and controlled release especially for drug with short half life. OBJECTIVE: Objective of the present study was to optimize microemulgel based transdermal delivery of triamcinolone...
April 25, 2017: Recent Patents on Anti-infective Drug Discovery
https://www.readbyqxmd.com/read/28504046/formulation-and-characterization-of-phospholipon%C3%A2-90%C3%A2-g-and-tween-%C3%A2-80-based-transfersomes-for-transdermal-delivery-of-eprosartan-mesylate
#11
Abdul Ahad, Abdulmohsen A Al-Saleh, Abdullah M Al-Mohizea, Fahad I Al-Jenoobi, Mohammad Raish, Alaa Eldeen B Yassin, Mohd Aftab Alam
The objective of the current study was to formulate the eprosartan mesylate loaded transfersomes using different proportions of Phospholipon(®) 90 G and Tween(®) 80 (95-75: 5-25% w/w). The prepared transfersomes were characterized for their vesicles size, shape, polydispersity index, zeta potential, entrapment efficiency, in vitro skin permeation, confocal laser scanning microscopy and in vivo skin irritation. Results revealed that the formulated transfersomes were negatively charged, spherical unilamellar structure of 71...
May 15, 2017: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/28503066/essential-oil-mediated-glycerosomes-increase-transdermal-paeoniflorin-delivery-optimization-characterization-and-evaluation-in-vitro-and-in-vivo
#12
Kai Zhang, Yongtai Zhang, Zhe Li, Nana Li, Nianping Feng
In this study, a novel glycerosome carrier containing essential oils was prepared for topical administration of paeoniflorin (PF) to enhance its transdermal drug delivery and improve drug absorption in the synovium. The formulation of glycerosomes was optimized by a uniform design, and the final vehicle was composed of 5% (w/v) phospholipid, 0.6% (w/v) cholesterol, and 10% (v/v) glycerol, with 2% (v/v) Speranskia tuberculata essential oil (STO) as the transdermal enhancer. The in vitro transdermal flux of PF loaded in the STO-glycerosomes was 1...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28502717/preferential-accumulation-of-gold-nanorods-into-human-skin-hair-follicles-effect-of-nanoparticle-surface-chemistry
#13
Nouf N Mahmoud, Alaaldin M Alkilany, Dörthe Dietrich, Uwe Karst, Amal G Al-Bakri, Enam A Khalil
HYPOTHESIS: Gold nanoparticles (GNP) are considered an ideal model to help understanding the nano-skin interface. The surface functionality of gold nanorods (GNR) is expected to influence the uptake of nanoparticles into specific targets of skin such as hair follicles or dermis. Hence, it should be possible to modify the surface chemistry of GNP to achieve more targeted and safe skin therapy. EXPERIMENTS: GNR functionalized with various surface ligands (neutral, anionic, cationic, and hydrophobic) were evaluated for their accumulation into hair follicles of human skin sheets using ex-vivo setup...
May 6, 2017: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28501290/use-of-transdermal-selegiline-in-pregnancy-and-lactation-a-case-report
#14
Rebecca L Bauer, Joanne Orfei, Christina L Wichman
No abstract text is available yet for this article.
March 15, 2017: Psychosomatics
https://www.readbyqxmd.com/read/28500373/effects-of-varenicline-versus-transdermal-nicotine-replacement-therapy-on-cigarette-demand-on-quit-day-in-individuals-with-substance-use-disorders
#15
Cara M Murphy, James MacKillop, Rosemarie A Martin, Jennifer W Tidey, Suzanne M Colby, Damaris J Rohsenow
RATIONALE: Cigarette demand is a behavioral economic measure of the relative value of cigarettes. Decreasing the value of cigarette reinforcement may help with quitting smoking. OBJECTIVES: This study aimed to evaluate the effects of initial use of varenicline (VAR) versus nicotine replacement therapy (NRT) on demand for cigarettes on quit day among smokers with substance use disorders (SUD) and to determine whether reduced demand was associated with subsequent abstinence from smoking at 1 and 3 months...
May 13, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28498504/varenicline-versus-nicotine-patch-with-brief-advice-for-smokers-with-substance-use-disorders-with-or-without-depression-effects-on-smoking-substance-use-and-depressive-symptoms
#16
Damaris J Rohsenow, Jennifer W Tidey, Rosemarie A Martin, Suzanne M Colby, Robert M Swift, Lorenzo Leggio, Peter M Monti
AIMS: Varenicline was compared with transdermal nicotine (NRT) for smokers with current substance use disorders (SUD) for effects on 3-month smoking abstinence (primary outcome) and, secondarily, on 3 and 6 month abstinence while adjusting for medication adherence, and on additional smoking and substance use outcomes. Moderation by major depressive disorder history (MDD) and adherence were investigated. DESIGN: Double-blind double-placebo controlled randomized design, stratifying by MDD, gender and nicotine dependence, with 3 and 6 months follow up...
May 12, 2017: Addiction
https://www.readbyqxmd.com/read/28496491/the-effects-of-transdermal-estrogen-delivery-on-bone-mineral-density-in-postmenopausal-women-a-meta-analysis
#17
Fatemeh Abdi, Hamid Mobedi, Farhad Bayat, Nariman Mosaffa, Mahrokh Dolatian, Fahimeh Ramezani Tehrani
Due to its minimal systematic adverse effects, transdermal estrogen is widely used for the prevention of osteoporosis in postmenopausal women. The present meta-analysis aimed to clarify the effects of transdermal estrogen on bone mineral density (BMD) of postmenopausal women. Studies were identified by searching electronic databases including Cochrane Library, MEDLINE, Embase , and CINAHL databases, and also the Sciences Citation Index. Systematic review of articles was published between January 1989 to February 2016...
2017: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/28495196/pharmacokinetics-of-a-novel-spot-on-formulation-of-praziquantel-for-dogs
#18
María Laura Gutiérrez, Guillermo Di Federico, Jorge A Dale, Juan M Minoia, Carlos D Corrales, Paula Schaiquevich, Silvia Wikinski
Praziquantel (PZQ) is an anthelmintic drug used both in humans and animals that can be administered through various routes. There are transdermal formulations for cats, but only oral or subcutaneous dosage forms for dogs. Given the fact that the cat's skin and the dog's skin have different characteristics, which in turn affect bioavailability, we developed a PZQ spot-on formulation for dogs. This study was aimed at determining the plasmatic behavior of topically administered PZQ (Labyes(®)) in adult dogs. Dogs were administered PZQ (14...
May 30, 2017: Veterinary Parasitology
https://www.readbyqxmd.com/read/28494734/recent-advances-in-skin-penetration-enhancers-for-transdermal-gene-and-drug-delivery
#19
Morteza Amjadi, Babak Mostaghaci, Metin Sitti
There is a growing interest in transdermal delivery systems because of their noninvasive, targeted, and on-demand delivery of gene and drugs. However, efficient penetration of therapeutic compounds into the skin is still challenging largely due to the impermeability of the outermost layer of the skin, known as stratum corneum. Recently, there have been major research activities to enhance the skin penetration depth of pharmacological agents. This article reviews recent advances in the development of various strategies for skin penetration enhancement...
May 10, 2017: Current Gene Therapy
https://www.readbyqxmd.com/read/28493744/does-menthol-cigarette-use-moderate-the-effect-of-nicotine-metabolism-on-short-term-smoking-cessation
#20
Nancy C Jao, Anna K Veluz-Wilkins, Matthew J Smith, Allison J Carroll, Sonja Blazekovic, Frank T Leone, Rachel F Tyndale, Robert A Schnoll, Brian Hitsman
The nicotine metabolite ratio (NMR) has been shown to predict response to the transdermal nicotine patch, such that faster nicotine metabolism is associated with a lower abstinence rate. Menthol cigarette use, versus nonmenthol cigarette use, slows nicotine metabolism and therefore may attenuate the effect of NMR on smoking abstinence. In this study, we evaluated whether cigarette type (menthol vs. nonmenthol) modified the association between NMR and short-term abstinence. This was a secondary analysis examining treatment in the first 8 weeks of 21 mg/day nicotine patch therapy in a completed clinical trial (n = 474)...
June 2017: Experimental and Clinical Psychopharmacology
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