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Yaozhen Wang, Xiaofeng Yu, Ping Zhang, Yinglin Ma, Lei Wang, Huali Xu, Dayun Sui
Parkinson's disease (PD) is characterized by the selective death of dopaminergic neurons. To avoid inconvenience of frequent administration caused by short half life and recurrence of symptoms such as tremor and bradykinesia incurred by drug elimination, a novel long-acting pramipexole transdermal patch has been made. In the present study, we evaluated the neuroprotective effects and underlying mechanisms of pramipexole patch (PPX patch) in a subacute PD mouse model induced by 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)...
August 26, 2018: Journal of Pharmacological Sciences
Karen E Burke
Skin is an efficient protective barrier armed with an intricate network of antioxidants. External environmental stress diminishes and sometimes overwhelms these innate protective mechanisms; aging slows their efficacy. Topical antioxidants enhance natural endogenous defenses to create an indwelling reservoir for sustained protection with far higher concentrations than possible with oral intake. The challenge is creating formulations of these labile molecules that are stable, active, and can be effectively absorbed transdermally to deliver high concentrations...
September 21, 2018: Clinical Pharmacology and Therapeutics
Tatsuro Amano, Anna Igarashi, Naoto Fujii, Daichi Hiramatsu, Yoshimitsu Inoue, Narihiko Kondo
PURPOSE: This study investigated the influence of β-adrenergic receptor blockade on sweating during bilateral static knee extension (KE) and lateral isometric handgrip (IH) exercises followed by post-exercise muscle ischemia (PEMI) in habitually trained individuals. METHOD: Ten habitually trained men (maximum oxygen uptake, 57.1 ± 3.4 ml kg-1  min-1 ) were mildly heated by increasing their skin temperature, and bilateral KE or lateral IH exercises at an intensity of 60% maximum voluntary contraction were subsequently performed for 1 min, followed by PEMI to stimulate muscle metaboreceptors for 2 min...
September 20, 2018: European Journal of Applied Physiology
Francesco Cilurzo, Umberto M Musazzi, Silvia Franzé, Guido Fedele, Paola Minghetti
Transdermal patches and medicated plasters are designed to sustain efficacious systemic or loco-regional drug concentrations, respectively. In both cases, drug skin permeation is a critical attribute from the early stage of the pharmaceutical development. In 2014, the EMA introduced the guideline "on the quality of transdermal patches", in which the importance of equivalence of drug fluxes in vitro skin permeation study was particularly emphasized to generic or abridged applications for the marketing authorization or manage dossier variations during the product cycle life...
September 17, 2018: European Journal of Pharmaceutical Sciences
Irina Khripun, Sergey Vorobyev, Igor Belousov, Michel Kogan, Michael Zitzmann
Effects of testosterone (T) on the cardiovascular system of men remain controversial. The impact of T-replacement therapy (TRT) in men with functional hypogonadism and type 2 diabetes mellitus (T2DM) has to be elucidated. This study included 80 men (mean age 51.5 ± 6.3 years) with newly diagnosed T2DM (according to ADA criteria) and functional hypogonadism (according to EAU criteria). Randomization: Group1 (n = 40): TRT using 1%-transdermal T-gel (50 mg/day), Group2 (n = 40) no TRT (controls)...
September 20, 2018: Aging Male: the Official Journal of the International Society for the Study of the Aging Male
Noriaki Nagai, Fumihiko Ogata, Hiroko Otake, Yosuke Nakazawa, Naohito Kawasaki
Purpose: In the clinical setting, raloxifene, a second-generation selective estrogen receptor modulator, is administered orally; however, the bioavailability (BA) is only 2% because of its poor solubility in aqueous fluids and its extensive first-pass metabolism. Therefore, it is expected that the development of a transdermally delivered formulation may reduce the necessary dose without compromising its therapeutic efficacy. In this study, we designed transdermal formulations containing raloxifene nanoparticles and evaluated their usefulness for osteoporosis therapy...
2018: International Journal of Nanomedicine
Benjamin E Maimon, Maurizio Diaz, Emilie C M Revol, Alexis M Schneider, Ben Leaker, Claudia E Varela, Shriya Srinivasan, Matthew B Weber, Hugh M Herr
Optogenetic technologies have been the subject of great excitement within the scientific community for their ability to demystify complex neurophysiological pathways in the central (CNS) and peripheral nervous systems (PNS). The excitement surrounding optogenetics has also extended to the clinic with a trial for ChR2 in the treatment of retinitis pigmentosa currently underway and additional trials anticipated for the near future. In this work, we identify the cause of loss-of-expression in response to transdermal illumination of an optogenetically active peroneal nerve following an anterior compartment (AC) injection of AAV6-hSyn-ChR2(H134R) with and without a fluorescent reporter...
September 19, 2018: Scientific Reports
Patrick Poulin, Severine H Collet, Nicolas Atrux-Tallau, Jean-Michel Linget, Laurent Hennequin, Claire E Wilson
The minipig continues to build a reputation as a viable alternative large animal model to predict human in dermatology and toxicology studies. Therefore, it is essential to describe and predict the pharmacokinetics (PK) in that species to speed-up the clinical candidate selection. A key parameter in whole-body physiologically-based pharmacokinetic (PBPK) models is the tissue-to-plasma partition coefficients (Kp-tissue ) and the resulting volume of distribution at steady-state (Vss ). Mechanistic in vitro- and/or in silico-based models used for predicting these parameters of tissue distribution of drugs refer to the tissue composition-based model (TCM)...
September 14, 2018: Journal of Pharmaceutical Sciences
Rawia M Khalil, Ahmed Abdelbary, Silvia Kocova El Arini, Mona Basha, Hadeer A El-Hashemy
Bilosomes were developed in order to investigate their efficacy as nanocarriers for transdermal delivery of Tizanidine HCl (TZN), a skeletal muscle relaxant with low oral bioavailability. Full factorial experimental design consisting of 27 combinations was generated to study the effects of surfactant type, surfactant to cholesterol ratio and the amount of bile salt on the entrapment efficiency, the vesicle size and in-vitro dissolution of the TZN-loaded bilosomes. The permeation through the stratum cornea (SC) was optimized with the vertical diffusion assembly using excised rat skin...
September 16, 2018: Journal of Liposome Research
Muhammad Suleman Khan, Michael S Roberts
Both drug delivery performance and various age-related physical, mental and physiological changes can affect their effectiveness and safety in elderly patients. The many drug delivery systems developed over the years include recent novel transdermal, nasal, pulmonary and orally disintegrating tablet delivery systems that provide consistent, precise, timely and more targeted absorption. Certain drug delivery systems may be associated with suboptimal outcomes in the elderly because of the nature of drug present, a lack of appreciation of the impact of age-related changes in drug absorption, distribution and clearance on their pharmacokinetics, the limited availability of pharmacokinetic, safety and clinical data...
September 11, 2018: Advanced Drug Delivery Reviews
Yongwei Gu, Meng Yang, Xiaomeng Tang, Ting Wang, Dishun Yang, Guangxi Zhai, Jiyong Liu
BACKGROUND: In recent years, nanoparticles (NPs) including nanostructured lipid carries (NLC) and solid lipid nanoparticles (SLN) captured an increasing amount of attention in the field of transdermal drug delivery system. However, the mechanisms of penetration enhancement and transdermal transport properties of NPs are not fully understood. Therefore, this work applied different platforms to evaluate the interactions between skin and NPs loading triptolide (TPL, TPL-NLC and TPL-SLN)...
September 15, 2018: Journal of Nanobiotechnology
Chutima Jantarat, Pornpak Sirathanarun, Somruedee Boonmee, Wanida Meechoosin, Husna Wangpittaya
Curcumin is a naturally occurring substance with various pharmacological activities. It has not been developed as a drug because of its low bioavailability due to its low solubility and absorption. Piperine is a natural enhancer that is popularly used to increase the absorption of curcumin in oral applications; however, it has not been applied for transdermal curcumin delivery. This study aims to develop a transdermal curcumin delivery system using piperine as a skin permeation enhancer in the form of composite double-layer membrane; the upper layer consisted of curcumin and the lower layer consisted of piperine...
September 13, 2018: Scientia Pharmaceutica
Elwira Lasoń, Elżbieta Sikora, Małgorzata Miastkowska, Elvira Escribano, Maria Jose Garcia-Celma, Conxita Solans, Meritxell Llinas, Jan Ogonowski
Nanostructured lipid carriers (NLC) composed of the substances generally recognized as safe (GRAS) were obtained by using a hot high-pressure homogenization technique (HPH). The influence of the number of homogenization cycles and concentration of a decyl glucoside surfactant on the NLC properties were studied. The system's stability was assessed by macroscopic observation, light backscattering and zeta potential measurements. NLC particle size was measured using dynamic light scattering (DLS). The kinetically stable formulations were loaded with forskolin and selected for in vitro drug permeation study using the Franz cell method...
2018: Acta Biochimica Polonica
Maryam Rameshk, Fariba Sharififar, Mitra Mehrabani, Abbas Pardakhty, Alireza Farsinejad, Mehrnaz Mehrabani
PURPOSE: In Traditional Persian Medicine (TPM), different natural treatments have been suggested for skin damages such as Narcissus tazetta L. bulb application. New drug delivery systems such as niosomes have shown considerable increase transdermal drug delivery through stratum corneum, the main barrier against substances transport into skin. The aim of this study is preparation of niosomal formulations from N. tazetta bulb extract and evaluation of its in vitro wound healing effect. MATERIALS AND METHODS: Non-ionic surfactant vesicles (NSVs or niosomes) were prepared by film hydration method from percolated extract of N...
September 12, 2018: Daru: Journal of Faculty of Pharmacy, Tehran University of Medical Sciences
Mona G Arafa, Reham F El-Kased, M M Elmazar
Thermoresponsive gels containing gold nanoparticles (AuNPs) were prepared using Pluronic®127 alone (F1) and with hydroxypropyl methylcellulose (F2) at ratios of 15% w/w and 15:1% w/w, respectively. AuNPs were evaluated for particle size, zeta-potential, polydispersity index (PDI), morphology and XRD pattern. AuNP-containing thermoresponsive gels were investigated for their gelation temperature, gel strength, bio-adhesive force, viscosity, drug content, in vitro release and ex-vivo permeation, in addition to in vitro antibacterial activity against bacteria found in burn infections, Staphylococcus aureus...
September 12, 2018: Scientific Reports
Xiao-Qin Chu, Jie Huang, Zheng-Guang Li, Qian Li, Jiao-Jiao Cao, Jian-Qin Jiang, Shuang-Ying Gui
There has been a growing concern in transdermal drug technology over the past several decades. As a novel transdermal delivery system, Lyotropic liquid crystals (LLC) still face challenges such as drug loading, limited drug permeation and instability of systems. LLC system is so sensitive that a very subtle change in composition may induce a phase transformation or conversion of spatial configuration, and result in a diverse percutaneous delivery subsequently. To find out the effects of hydrophilic and lipophilic components on the structure and transdermal properties of LLCs, hydrophilic sinomenine hydrochloride (SH) and lipophilic cinnamaldehyde (CA) was chosen as a model drug and a skin permeation enhancer, respectively, several formulations were prepared and compared...
September 10, 2018: Current Drug Delivery
Carla Bonetti Madelaire, Bruna de Oliveira Cassettari, Fernando Ribeiro Gomes
Androgens and glucocorticoids play important roles in vertebrate's reproduction and display complex immunomodulatory functions that may affect survival. In anurans, testosterone and corticosterone are correlated to sexual behavior, reproduction, and immune function. Male toads (Rhinella jimi) were treated with acute doses of testosterone (T) and corticosterone (CORT) and immune variables (plasma bacterial killing ability [BKA], swelling after phytohemagglutinin [PHA] injection and the time point of maximum PHA swelling response) were measured...
September 5, 2018: General and Comparative Endocrinology
Jason A Gandelman, Hakmook Kang, Ashleigh Antal, Kimberly Albert, Brian D Boyd, Alexander C Conley, Paul Newhouse, Warren D Taylor
OBJECTIVE: Late-life depression (LLD) is characterized by poor antidepressant response and cognitive dysfunction. This study examined whether transdermal nicotine benefits mood symptoms and cognitive performance in LLD. METHODS: In a 12-week open-label outpatient study conducted between November 2016 and August 2017, transdermal nicotine was given to 15 nonsmoking older adults (≥ 60 years of age). Eligible participants met DSM-IV-TR criteria for major depressive disorder with ≥ 15 on the Montgomery-Asberg Depression Rating scale (MADRS) and endorsed subjective cognitive impairment...
August 28, 2018: Journal of Clinical Psychiatry
Chih-Hao Chen, Victor Bong-Hang Shyu, Chien-Tzung Chen
In this study, dissolving polymeric microneedle (MN) patches composed of gelatin and sodium carboxymethyl cellulose (CMC) were used to localize insulin. Their in vitro skin insertion capabilities were determined using tissue-marking dye to stain the skin after patches removal. Scanning electron microscopy (SEM) was used to determine changes in the MNs over time, and optical coherence tomography (OCT) was used to monitor their real-time penetration depth. Confocal microscopy images revealed that rhodamine 6G gradually diffuses from the puncture sites to deeper dermal tissue...
September 5, 2018: Materials
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