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https://www.readbyqxmd.com/read/28228077/antioxidant-nanoplatforms-for-dermal-delivery-melatonin
#1
Aroha Belen Sánchez Milán, Ana C Calpena Campmany, Beatriz Clares Naveros
Melatonin (MLT) is emerging as a promising therapeutic agent, mainly due to its role as antioxidant. Substantial evidences show that melatonin is potentially effective on a variety of diseases as cancer, inflammation and neurodegenerative diseases. The excellent antioxidant capacity with pharmacokinetics characteristics and the emerging search for new pharmaceutical nanotechnology based systems, make it particularly attractive to elaborate nanoplatforms based on MLT for biomedical or cosmetic dermal applications...
February 22, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28228076/transdermal-drug-delivery-opportunities-and-challenges-for-controlled-delivery-of-therapeutic-agents-using-nanocarriers
#2
Balak Das Kurmi, Pawan Tekchandani, Rishi Paliwal, Shivani Rai Paliwal
BACKGROUND: Transdermal drug delivery represents an extremely attractive and innovative route across the skin owing to the possibility for achieving systemic effect of drugs. Present scenario demands a special focus on developing safe medicine with minimize toxic adverse effects related to most of the pharmacologically active agents. Transdermal drug delivery would be a focal paradigm which provides patient convenience, first-pass hepatic metabolism avoidance, local targeting and reduction in toxic effect related to various categories of drugs like, analgesics, anti-inflammatory, antibiotics, antiviral, anaesthetic, anticancer etc...
February 22, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28222612/in-vitro-ex-vivo-correlations-between-a-cell-laden-hydrogel-and-mucosal-tissue-for-screening-composite-delivery-systems
#3
Anna K Blakney, Adam B Little, Yonghou Jiang, Kim A Woodrow
Composite delivery systems where drugs are electrospun in different layers and vary the drug stacking-order are posited to affect bioavailability. We evaluated how the formulation characteristics of both burst- and sustained-release electrospun fibers containing three physicochemically diverse drugs: dapivirine (DPV), maraviroc (MVC) and tenofovir (TFV) affect in vitro and ex vivo release. We developed a poly(hydroxyethyl methacrylate) (pHEMA) hydrogel release platform for the rapid, inexpensive in vitro evaluation of burst- and sustained-release topical or dermal drug delivery systems with varying microarchitecture...
November 2016: Drug Delivery
https://www.readbyqxmd.com/read/28216463/successful-application-of-large-microneedle-patches-by-human-volunteers
#4
Anastasia Ripolin, James Quinn, Eneko Larrañeta, Eva Maria Vicente-Perez, Johanne Barry, Ryan F Donnelly
We describe, for the first time, the design, production and evaluation of large microneedle patches. Such systems, based on 16 individual microneedle arrays (needle height 600μm), were prepared from aqueous blends of 15% w/w Gantrez(®) S97 and 7.5% w/w poly(ethyleneglycol) 10,000Da. Ester-based crosslinking was confirmed by FTIR and mechanical strength was good. Insertion depths in a validated skin model were approximately 500μm. Ten human volunteers successfully self-inserted the microneedles of these larger patches in their skin, following appropriate instruction, as confirmed by transepidermal water loss measurements...
February 16, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28194704/challenges-and-future-prospects-for-the-delivery-of-biologics-oral-mucosal-pulmonary-and-transdermal-routes
#5
Javier O Morales, Kristin R Fathe, Ashlee Brunaugh, Silvia Ferrati, Song Li, Miguel Montenegro-Nicolini, Zeynab Mousavikhamene, Jason T McConville, Mark R Prausnitz, Hugh D C Smyth
Biologic products are large molecules such as proteins, peptides, nucleic acids, etc., which have already produced many new drugs for clinical use in the last decades. Due to the inherent challenges faced by biologics after oral administration (e.g., acidic stomach pH, digestive enzymes, and limited permeation through the gastrointestinal tract), several alternative routes of administration have been investigated to enable sufficient drug absorption into systemic circulation. This review describes the buccal, sublingual, pulmonary, and transdermal routes of administration for biologics with relevant details of the respective barriers...
February 13, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28181840/transdermal-delivery-of-isoniazid-and-rifampin-in-guinea-pigs-by-electro-phonophoresis
#6
Suting Chen, Yi Han, Daping Yu, Fengmin Huo, Fen Wang, Yunxu Li, Lingling Dong, Zhidong Liu, Hairong Huang
Electro-phonophoresis (EP) has been used as a drug delivery approach in clinical fields. The objective of the present study is to evaluate the skin permeability of isoniazid and rifampin in guinea pigs by EP to provide reference basis for clinical applications of such transdermal delivery system in the treatment of patients with superficial tuberculosis. Isoniazid and rifampin solutions were delivered transdermally with or without EP in health guinea pigs for 0.5 h. Local skin and blood samples were collected serially at 0, 1/2, 1, 2, 4, 6 and 24 h after dosing...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28168430/poly-lactic-co-glycolic-acid-drug-delivery-systems-through-transdermal-pathway-an-overview
#7
REVIEW
Lucas Naves, Chetna Dhand, Luis Almeida, Lakshminarayanan Rajamani, Seeram Ramakrishna, Graça Soares
In past few decades, scientists have made tremendous advancement in the field of drug delivery systems (DDS), through transdermal pathway, as the skin represents a ready and large surface area for delivering drugs. Efforts are in progress to design efficient transdermal DDS that support sustained drug release at the targeted area for longer duration in the recommended therapeutic window without producing side-effects. Poly(lactic-co-glycolic acid) (PLGA) is one of the most promising Food and Drug Administration approved synthetic polymers in designing versatile drug delivery carriers for different drug administration routes, including transdermal drug delivery...
February 6, 2017: Progress in biomaterials
https://www.readbyqxmd.com/read/28163134/development-of-a-predictive-model-for-the-stabilizer-concentration-estimation-in-microreservoir-transdermal-drug-delivery-systems-mtdds-using-lipophilic-pressure-sensitive-adhesives-as-matrix-carrier
#8
Clémence Chenevas-Paule, Hans-Michael Wolff, Mark Ashton, Martin Schubert, Kalliopi Dodou
Microreservoir-type transdermal drug delivery systems (MTDDS) can prevent drug crystallization; however no current predictive model considers the impact of drug load and hydration on their physical stability. We investigated MTDDS films containing polyvinylpyrrolidone (PVP) as polymeric drug stabilizer in lipophilic pressure sensitive adhesive (silicone). Medicated and unmedicated silicone films with different molar N-vinylpyrrolidone (VP):drug ratios were prepared and characterized by FTIR, differential scanning calorimetry (DSC), scanning electron microscopy (SEM), microscopy, Dynamic Vapour Sorption (DVS) and stability testing for four months at different storage conditions...
February 2, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28160257/exploring-unsaturated-fatty-acid-cholesteryl-esters-as-transdermal-permeation-enhancers
#9
Sanjeev Rambharose, Rahul S Kalhapure, Mahantesh Jadhav, Thirumala Govender
The intrinsic protective barrier property of skin, one of the major challenges in the design of transdermal drug delivery systems, can be overcome through the use of chemical permeation enhancers (CPEs). Herein, we explore the potential of unsaturated fatty acid (UFA) esters of cholesterol (Chol) viz., oleate, linoleate and linolenate, as transdermal CPEs using tenofovir (TNF) as a model drug. All Chol UFA esters at 1% w/w were found to be more effective enhancers when compared to their respective parent fatty acids (FAs) and saturated FA counterparts...
February 3, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28159724/rationalising-polymer-selection-for-supersaturated-film-forming-systems-produced-by-an-aerosol-spray-for-the-transdermal-delivery-of-methylphenidate
#10
A Edwards, S Qi, F Liu, M B Brown, W J McAuley
Film forming systems offer a number of advantages for topical and transdermal drug delivery, in particular enabling production of a supersaturated state which can greatly improve drug absorption and bioavailability. However the suitability of individual film forming polymers to stabilise the supersaturated state and optimise delivery of drugs is not well understood. This study reports the use of differential scanning calorimetry (DSC) to measure the solubility of methylphenidate both as the free base and as the hydrochloride salt in two polymethacrylate copolymers, Eudragit RS (EuRS) and Eudragit E (EuE) and relates this to the ability of films formed using these polymers to deliver methylphenidate across a model membrane...
January 31, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28134262/doe-optimization-of-nano-based-carrier-of-pregabalin-as-hydrogel-new-therapeutic-chemometric-approaches-for-controlled-drug-delivery-systems
#11
Mona G Arafa, Bassam M Ayoub
Niosomes entrapping pregabalin (PG) were prepared using span 60 and cholesterol in different molar ratios by hydration method, the remaining PG from the hydrating solution was separated from vesicles by freeze centrifugation. Optimization of nano-based carrier of pregabalin (PG) was achieved. Quality by Design strategy was successfully employed to obtain PG-loaded niosomes with the desired properties. The optimal particle size, drug release and entrapment efficiency were attained by Minitab(®) program using design of experiment (DOE) that predicted the best parameters by investigating the combined effect of different factors simultaneously...
January 30, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28126641/the-application-of-skin-metabolomics-in-the-context-of-transdermal-drug-delivery
#12
REVIEW
Jinling Li, Weitong Xu, Yibiao Liang, Hui Wang
Metabolomics is a powerful emerging tool for the identification of biomarkers and the exploration of metabolic pathways in a high-throughput manner. As an administration site for percutaneous absorption, the skin has a variety of metabolic enzymes, except other than hepar. However, technologies to fully detect dermal metabolites remain lacking. Skin metabolomics studies have mainly focused on the regulation of dermal metabolites by drugs or on the metabolism of drugs themselves. Skin metabolomics techniques include collection and preparation of skin samples, data collection, data processing and analysis...
October 13, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28121196/nanoethosomes-for-transdermal-delivery-of-tropisetron-hcl-multi-factorial-predictive-modeling-characterization-and-ex-vivo-skin-permeation
#13
Hanaa A Abdel Messih, Rania A H Ishak, Ahmed S Geneidi, Samar Mansour
OBJECTIVE: The aim of the present work is to exclusively optimize and model the effect of phospholipid type either egg phosphatidylcholine (EPC) or soybean phosphatidylcholine (SPC), together with other formulation variables, on the development of nano-ethosomal systems for transdermal delivery of a water-soluble antiemetic drug. Tropisetron HCl (TRO) is available as hard gelatin capsules and IV injections. The transdermal delivery of TRO is considered as a novel alternative route supposing to improve BAV as well as patient convenience...
January 25, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28119111/cellular-interactions-of-a-lipid-based-nanocarrier-model-with-human-keratinocytes-unravelling-transport-mechanisms
#14
Elisabete Silva, Luísa Barreiros, Marcela A Segundo, Sofia A Costa Lima, Salette Reis
: Knowledge of delivery system transport through epidermal cell monolayer is vital to improve skin permeation and bioavailability. Recently, nanostructured lipid carriers (NLCs) have gained great attention for transdermal delivery due to their biocompatibility, high drug payload, occlusive properties and skin hydration effect. However, the nanocarriers transport related mechanisms in epidermal epithelial cells are not yet understood. In this research, the internalization and transport pathways of the NLCs across the epidermal epithelial cell monolayer (HaCaT cells) were investigated...
January 22, 2017: Acta Biomaterialia
https://www.readbyqxmd.com/read/28102556/structurally-stable-attractive-nanoscale-emulsions-with-dipole-dipole-interaction-driven-interdrop-percolation
#15
Kyounghee Shin, Gyeonghyeon Gong, Jonas Cuadrado, Serim Jeon, Mintae Seo, Hong Sung Choi, Jae Sung Hwang, Youngbok Lee, Alberto Fernandez-Nieves, Jin Woong Kim
This study introduces an extremely stable attractive nanoscale emulsion fluid, in which the amphiphilic block copolymer, poly(ethylene oxide)-block-poly(ε-caprolactone) (PEO-b-PCL), is tightly packed with lecithin, thereby forming a mechanically robust thin-film at the oil-water interface. The molecular association of PEO-b-PCL with lecithin is critical for formation of a tighter and denser molecular assembly at the interface, which is systematically confirmed by T2 relaxation and DSC analyses. Moreover, our suspension rheology studies also reflect the interdroplet attractions over a wide volume fraction range of the dispersed oil phase; this results in a percolated network of stable drops that exhibit no signs of coalescence or phase separation...
January 19, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28088574/time-dependence-of-the-enhancement-effect-of-chemical-enhancers-molecular-mechanisms-of-enhancing-kinetics
#16
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/28088456/development-of-a-predictive-model-for-the-long-term-stability-assessment-of-drug-in-adhesive-transdermal-films-using-polar-pressure-sensitive-adhesives-as-carrier-matrix
#17
Clémence Chenevas-Paule, Hans-Michael Wolff, Mark Ashton, Martin Schubert, Kalliopi Dodou
Drug crystallization in transdermal drug delivery systems (TDDS) is a critical quality defect. The impact of drug load and hydration on the physical stability of polar (acrylic) drug-in-adhesive (DIA) films was investigated with the objective to identify predictive formulation parameters with respect to drug solubility and long-term stability. Medicated acrylic films were prepared over a range of drug concentrations below and above saturation solubility; and were characterized by FTIR, differential scanning calorimetry (DSC), polarized microscopy and Dynamic Vapor Sorption (DVS) analysis...
January 11, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28071597/three-dimensional-printing-of-a-microneedle-array-on-personalized-curved-surfaces-for-dual-pronged-treatment-of-trigger-finger
#18
Seng Han Lim, Jian Yao Ng, Lifeng Kang
The hand function of patients who suffer from trigger finger can be impaired by the use of traditional splints. There is also a risk of systemic side effects with oral non-steroidal anti-inflammatory drugs (NSAIDs) used for pain relief. Microneedle-assisted transdermal drug delivery offers an attractive alternative for local delivery of NSAIDs. However, traditional microneedle arrays fabricated on flat surfaces are unable to deliver drugs effectively across the undulating skin surface of affected finger(s)...
January 10, 2017: Biofabrication
https://www.readbyqxmd.com/read/28068767/microneedle-assisted-skin-permeation-by-non-toxic-bioengineerable-gas-vesicle-nanoparticles
#19
Abhay U Andar, Ram Karan, Wolf T Pecher, Priya DasSarma, William D Hedrich, Audra L Stinchcomb, Shiladitya DasSarma
Gas vesicle nanoparticles (GVNPs) are hollow, buoyant protein organelles produced by the extremophilic microbe Halobacterium sp. NRC-1 and are being developed as bioengineerable and biocompatible antigen and drug-delivery systems (DDS). Dynamic light scattering measurements of purified GVNP suspensions showed a mean diameter of 245 nm. In vitro diffusion studies using Yucatan miniature pig skin showed GVNP permeation to be enhanced after MN-treatment compared to untreated skin. GVNPs were found to be non-toxic to mammalian cells (human kidney and rat mycocardial myoblasts)...
January 9, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28063969/hii-mesophase-as-a-drug-delivery-system-for-topical-application-of-methyl-salicylate
#20
Xin Liang, Yu-Lin Chen, Xiao-Jing Jiang, Sheng-Mei Wang, Ji-Wen Zhang, Shuang-Ying Gui
The main objective of this study was to develop reversed hexagonal (HII) mesophase for transdermal delivery of methyl salicylate. The formulation was prepared, characterized and evaluated for its skin penetration in vitro and skin retention in vivo. Preliminary pharmacodynamics and skin irritation were also investigated. The formulation was identified as hexagonal structure. In vitro study exhibited that HII mesophase enhanced the skin permeation by delivering 2.61 times more methyl salicylate than the commercially available cream...
January 4, 2017: European Journal of Pharmaceutical Sciences
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