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https://www.readbyqxmd.com/read/28647443/dermal-and-transdermal-delivery-of-pharmaceutically-relevant-macromolecules
#1
REVIEW
S Münch, J Wohlrab, R H H Neubert
The skin offers an attractive way for dermal and transdermal drug delivery that is why the drug still needs certain qualities to transcend the outermost layer of the skin, the stratum corneum. The requirements are: drugs with a maximum molecular weight of 1kDa, high lipophilicity and a certain polarity. This would restrict the use of a transdermal delivery of macromolecules, which would make the drug more effective in therapeutic administration. Various studies have shown that macromolecules without support do not penetrate the human skin...
June 21, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28644090/transdermal-administration-of-melatonin-coupled-to-cryopass-laser-treatment-as-noninvasive-therapy-for-prostate-cancer
#2
Laura Terraneo, Paola Bianciardi, Eleonora Virgili, Elena Finati, Michele Samaja, Rita Paroni
Melatonin, a pineal gland hormone, exerts oncostatic activity in several types of human cancer, including prostate, the most common neoplasia and the third most frequent cause of male cancer death in the developed world. The growth of androgen-sensitive LNCaP prostate cancer cells in mice is inhibited by 3 mg/kg/week melatonin (0.09 mg/mouse/week) delivered by i.p. injections, which is equivalent to a dose of 210 mg/week in humans. The aim of this study is to test an alternative noninvasive delivery route based on transdermal administration of melatonin onto the tumor area followed by cryopass-laser treatment...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28633107/effects-of-chemical-and-physical-enhancement-techniques-on-transdermal-delivery-of-3-fluoroamphetamine-hydrochloride
#3
Ashana Puri, Kevin S Murnane, Bruce E Blough, Ajay K Banga
The present study investigated the passive transdermal delivery of 3-fluoroamphetamine hydrochloride (PAL-353) and evaluated the effects of chemical and physical enhancement techniques on its permeation through human skin. In vitro drug permeation studies through dermatomed human skin were performed using Franz diffusion cells. Passive permeation of PAL-353 from propylene glycol and phosphate buffered saline as vehicles was studied. Effect of oleic acid, maltose microneedles, ablative laser, and anodal iontophoresis on its transdermal permeation was investigated...
June 17, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28610893/an-insight-into-the-molecular-mechanism-of-the-temporary-enhancement-effect-of-isopulegol-decanoate-on-the-skin
#4
Xiaochang Liu, Meiying Liu, Chao Liu, Peng Quan, Yongshan Zhao, Liang Fang
Chemical enhancers are widely used to facilitate drug permeation in transdermal drug delivery system (TDDS) and the effect of chemical enhancers is desired to be temporary. Though temporary enhancement effect of chemical enhancers has been widely discussed, there is still a lack of knowledge about the molecular mechanism of temporary enhancement effect. Using the skin permeation of flurbiprofen as a probe, the temporary enhancement effect of isopulegol decanoate (ISO-10) was evaluated with in vitro permeation experiment and confocal laser scanning microscopy (CLSM)...
June 10, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28600224/enhancement-of-transdermal-protein-delivery-by-photothermal-effect-of-gold-nanorods-coated-on-polysaccharide-based-hydrogel
#5
Aung Thu Haine, Yuki Koga, Yuta Hashimoto, Taishi Higashi, Keiichi Motoyama, Hidetoshi Arima, Takuro Niidome
Transdermal protein delivery is a useful and attractive method for protein therapy and dermal vaccination. However, this delivery method is restricted by the low permeability of the stratum corneum. The purpose of this study was to develop a transdermal delivery system for enhancement of protein permeability into the skin. First, we prepared a transparent gel patch made of polysaccharides with gold nanorods on the gel surface and fluorescein isothiocyanate-modified ovalbumin (FITC-OVA) inside. Next, the gel patch was placed on mouse skin to allow contact with the coated gold nanorods, and irradiated by a continuous-wave laser...
June 6, 2017: European Journal of Pharmaceutics and Biopharmaceutics
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
#6
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/28502717/preferential-accumulation-of-gold-nanorods-into-human-skin-hair-follicles-effect-of-nanoparticle-surface-chemistry
#7
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...
October 1, 2017: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28494734/recent-advances-in-skin-penetration-enhancers-for-transdermal-gene-and-drug-delivery
#8
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/28490875/mechanism-of-transdermal-permeation-promotion-of-lipophilic-drugs-by-ethosomes
#9
Li Yang, Lifang Wu, Dongze Wu, Deshun Shi, Tai Wang, Xiaoliang Zhu
Ethosomes can promote the penetration of lipophilic drugs into the skin, but the underlying mechanism is still unknown. The purpose of this study was to investigate the mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes. The formulation of ethosomes was optimized using the Box-Behnken experimental design, in which Rhodamine B and 1-palmitoyl-2-{12-[(7-nitro-2-1,3-benzoxadiazol-4-yl)amino]dodecanoyl}-sn-glycero-3-phosphocholine were used to simulate a model lipophilic drug and act as a fluorescent tracer of ethosomal phospholipids, respectively...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28418076/ultrasonic-modulation-of-tissue-optical-properties-in-ex-vivo-porcine-skin-to-improve-transmitted-transdermal-laser-intensity
#10
Paul J D Whiteside, Chenxi Qian, Nicholas Golda, Heather K Hunt
BACKGROUND AND OBJECTIVE: Applications of light-based energy devices involving optical targets within the dermis frequently experience negative side-effects resultant from surface scattering and excess optical absorption by epidermal melanin. As a broadband optical absorber, melanin decreases the efficacy of light-based treatments throughout the ultraviolet, visible, and near-infrared spectra while also generating additional heat within the surface tissue that can lead to inflammation or tissue damage...
April 18, 2017: Lasers in Surgery and Medicine
https://www.readbyqxmd.com/read/28361607/fabrication-characterization-and-application-of-sugar-microneedles-for-transdermal-drug-delivery
#11
Hiep X Nguyen, Ajay K Banga
AIM: This study aimed to fabricate, characterize and use maltose microneedles for transdermal delivery of doxorubicin. MATERIALS & METHODS: Microneedles were fabricated by micromolding technique and evaluated for dimensions, mechanical properties and in situ dissolution. Microporation of human cadaver skin was confirmed by dye binding, histology, pore uniformity, confocal laser microscopy and skin integrity measurement. In vitro permeation studies were performed on vertical Franz diffusion cells...
March 2017: Therapeutic Delivery
https://www.readbyqxmd.com/read/28321676/transdermal-delivery-of-human-growth-hormone-via-laser-generated-micropores
#12
Yang Song, Karishma Hemmady, Ashana Puri, Ajay K Banga
The epidermal skin barrier plays an important role in protecting underlying structures. It allows the passage of low molecular weight lipophilic molecules, but restricts the passage of hydrophilic molecules and macromolecules. The objective of this study was to investigate the feasibility of transdermal delivery of human growth hormone (hGH) through laser-microporated dermatomed porcine ear skin. The permeation of hGH was evaluated at different laser fluences and micropore densities. In vitro permeation studies were performed on vertical Franz diffusion cells using dermatomed porcine ear skin treated with ablative laser (2940 nm; P...
March 20, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28277004/fractional-laser-assisted-percutaneous-drug-delivery-via-temperature-responsive-liposomes
#13
Takahiro Fujimoto, Masayuki Ito, Shinobu Ito, Hideko Kanazawa
Liposomes are used for transdermal delivery of drugs and vaccines. Our objective was to develop temperature-responsive (TR) liposomes to achieve temperature-dependent, controlled release of an encapsulated drug, and use fractional laser irradiation to enhance transdermal permeability of these liposomes. TR-liposomes prepared using a thermosensitive polymer derived from poly-N-isopropylacrylamide, N,N-dimethylacrylamide, egg phosphatidylcholine, and dioleoylphosphatidylethanolamine, delivered fluorescein isothiocyanate-conjugated ovalbumin (OVA-FITC) as a model drug...
May 2017: Journal of Biomaterials Science. Polymer Edition
https://www.readbyqxmd.com/read/28167201/efficacy-of-iontophoresis-assisted-ablative-fractional-laser-photodynamic-therapy-with-short-incubation-time-for-the-treatment-of-actinic-keratosis-12-month-follow-up-results-of-a-prospective-randomised-comparative-trial
#14
Seung-Hwan Choi, Tae-Hoon Kim, Ki-Hoon Song
BACKGROUND: Iontophoresis is a transdermal drug-delivery technique that enhances the transport of ionic species across membranes and may have significant benefit for the treatment of actinic keratosis (AK) by ablative fractional laser-primed photodynamic therapy (AFL-PDT). The aim of this study were to compare the efficacy, recurrence rate, cosmetic outcome and safety of iontophoresis-assisted AFL-PDT with 2hours of incubation vs. those of conventional AFL-PDT with 2- and 3-hour incubation in patients with facial and scalp AK...
February 3, 2017: Photodiagnosis and Photodynamic Therapy
https://www.readbyqxmd.com/read/28157088/transdermal-optogenetic-peripheral-nerve-stimulation
#15
Benjamin E Maimon, Anthony N Zorzos, Rhys Bendell, Alexander Harding, Mina Fahmi, Shriya Srinivasan, Peter Calvaresi, Hugh M Herr
OBJECTIVE: A fundamental limitation in both the scientific utility and clinical translation of peripheral nerve optogenetic technologies is the optical inaccessibility of the target nerve due to the significant scattering and absorption of light in biological tissues. To date, illuminating deep nerve targets has required implantable optical sources, including fiber-optic and LED-based systems, both of which have significant drawbacks. APPROACH: Here we report an alternative approach involving transdermal illumination...
June 2017: Journal of Neural Engineering
https://www.readbyqxmd.com/read/28132934/sustained-epidermal-powder-drug-delivery-via-skin-microchannels
#16
Yan Cao, Prateek Kakar, Md Nazir Hossen, Mei X Wu, Xinyuan Chen
Transdermal delivery of hydrophilic drugs is challenging. This study presents a novel sustained epidermal powder delivery technology (sEPD) for safe, efficient, and sustained delivery of hydrophilic drugs across the skin. sEPD is based on coating powder drugs into high-aspect-ratio, micro-coating channels (MCCs) followed by topical application of powder drug-coated array patches onto ablative fractional laser-generated skin MCs to deliver drugs into the skin. We found sEPD could efficiently deliver chemical drugs without excipients and biologics drugs in the presence of sugar excipients into the skin with a duration of ~12h...
March 10, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28088574/time-dependence-of-the-enhancement-effect-of-chemical-enhancers-molecular-mechanisms-of-enhancing-kinetics
#17
Xiaochang Liu, Peng Quan, Shanshan Li, Chao Liu, Yuan Zhao, Yongshan Zhao, Liang Fang
Chemical enhancers are widely used for facilitating drug penetration in transdermal drug delivery system (TDDS). However, there is a lack of knowledge about how the enhancement effect changes over time. In this study, on the basis of kinetic parameters of enhancement effect, molecular details of the dynamic enhancement process was described and a new hypothesis of the recovery mechanism of the skin barrier function was proposed. Using pretreated skin and flurbiprofen patch, the effects of Azone (AZ) and menthyl decanoate (MT-10) were evaluated with in vitro permeation experiment and further confirmed by confocal laser scanning microscopy (CLSM) and TEWL...
January 11, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28031354/intra-arterial-nitroglycerin-as-directed-acute-treatment-in-experimental-ischemic-stroke
#18
Michael E Maniskas, Jill M Roberts, Rebecca Trueman, Annastazia E Learoyd, Amanda Gorman, Justin F Fraser, Gregory J Bix
BACKGROUND: Nitroglycerin (also known as glyceryl trinitrate (GTN)), a vasodilator best known for treatment of ischemic heart disease, has also been investigated for its potential therapeutic benefit in ischemic stroke. The completed Efficacy of Nitric Oxide in Stroke trial suggested that GTN has therapeutic benefit with acute (within 6 hours) transdermal systemic sustained release therapy. OBJECTIVE: To examine an alternative use of GTN as an acute therapy for ischemic stroke following successful recanalization...
December 28, 2016: Journal of Neurointerventional Surgery
https://www.readbyqxmd.com/read/27990655/transcutaneous-drug-delivery-by-liposomes-using-fractional-laser-technology
#19
Takahiro Fujimoto, Jian Wang, Kazuki Baba, Yuka Oki, Yuki Hiruta, Masayuki Ito, Shinobu Ito, Hideko Kanazawa
OBJECTIVE: Transdermal delivery of hydrophilic peptides remains a challenge due to their poor cellular uptake and transdermal penetration. We hypothesize that combination of a CO2 fractional laser to enhance percutaneous absorption and liposomes as transdermal carriers would improve skin penetration of hydrophilic drugs. STUDY DESIGN: NA. METHODS: Liposomes were prepared using membrane fusion lipid dioleoylphosphatidylethanolamine, and used to deliver 5-carboxyfluorescein (CF) and fluorescein isothiocyanate-conjugated ovalbumin (OVA-FITC) as model hydrophilic peptide drugs...
December 19, 2016: Lasers in Surgery and Medicine
https://www.readbyqxmd.com/read/27917779/low-pressure-sequential-compression-of-lower-limbs-enhances-forearm-skin-blood-flow
#20
Guy Amah, Sebastian Voicu, Philippe Bonnin, Nathalie Kubis
PURPOSE: We investigated whether forearm skin blood flow could be improved when a multilayer pulsatile inflatable suit was applied at a low pressure to the lower limbs and abdomen. We hypothesized that a non-invasive purely mechanical stimulation of the lower limbs could induce remote forearm blood flow modifications. METHODS: The pulsatile suit induced a sequential compartmentalized low compression (65 mmHg), which was synchronized with each diastole of the cardiac cycle with each phase evolving centripetally (lower limbs to abdomen)...
December 1, 2016: Clinical and Investigative Medicine. Médecine Clinique et Experimentale
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