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transdermal delivery system

Mona M A Abdel-Mottaleb, Alf Lamprecht
Recently, a selective preferential accumulation of polymeric nanoparticles (in the size range around 100nm) has been observed in the follicular system of dermatitis skin. The present investigation aimed at clearly investigating the effect of irritant contact dermatitis on the barrier permeability for colloidal systems below this size range, namely quantum dots and hydrophilic macromolecules. Irritant dermatitis was induced in mice and the penetrability of quantum dots (5nm) and hydrophilic dextran molecules has been tracked in both healthy and inflamed skin using confocal laser scanning microscopy...
October 19, 2016: International Journal of Pharmaceutics
Giuseppe Pontrelli, Marco Lauricella, José A Ferreira, Gonçalo Pena
We present a multi-layer mathematical model to describe the transdermal drug release from an iontophoretic system. The Nernst-Planck equation describes the basic convection-diffusion process, with the electric potential obtained by solving the Laplace's equation. These equations are complemented with suitable interface and boundary conditions in a multi-domain. The stability of the mathematical problem is discussed in different scenarios and a finite-difference method is used to solve the coupled system. Numerical experiments are included to illustrate the drug dynamics under different conditions...
October 13, 2016: Mathematical Medicine and Biology: a Journal of the IMA
Kevin Ita
With the increasing proportion of the global geriatric population, it becomes obvious that neurodegenerative diseases will become more widespread. From an epidemiological standpoint, it is necessary to develop new therapeutic agents for the management of Alzheimer's disease, Parkinson's disease, multiple sclerosis and other neurodegenerative disorders. An important approach in this regard involves the use of the transdermal route. With transdermal drug delivery systems, it is possible to modulate the pharmacokinetic profiles of these medications and improve patient compliance...
October 5, 2016: Journal of Drug Targeting
Haruyoshi Seino, Yukari Arai, Norio Nagao, Noriyasu Ozawa, Kazuhiko Hamada
Partially myristoylated chitosan pyrrolidone carboxylate (PMCP) is a cationic amphiphilic chitosan derivative. Glabridin (Glab) from licorice root extracts is a hydrophobic antimelanogenic agent. Here we assessed the effects of cationic Glab-containing polymeric micelles derived from PMCP (Glab/PMCP-PM) on the ability of Glab to penetrate the skin and inhibit melanogenesis using a human skin model. The amount of Glab absorbed 24 h after the application of Glab/PMCP-PM was approximately four times higher than that of conventional oil-in-water micelles (control) prepared using Tween 60...
2016: PloS One
Venkata Ramana Malipeddi, Rajendra Awasthi, Daniela Dal Molim Ghisleni, Marina de Souza Braga, Irene Satiko Kikuchi, Terezinha de Jesus Andreoli Pinto, Kamal Dua
The present study aimed to develop matrix-type transdermal drug delivery system (TDDS) of metoprolol tartrate using polyvinyl pyrrolidone (PVP) and polyvinyl alcohol (PVA). The transdermal films were evaluated for physical parameters, Fourier transform infrared spectroscopy analysis (FTIR), differential scanning calorimetry (DSC), in vitro drug release, in vitro skin permeability, skin irritation test and stability studies. The films were found to be tough, non-sticky, easily moldable and possess good tensile strength...
September 27, 2016: Drug Delivery and Translational Research
Nadia M Morsi, Ahmed A Aboelwafa, Marwa H S Dawoud
Timolol maleate (TiM), a nonselective β-adrenergic blocker, is a potent highly effective agent for management of hypertension. The drug suffers from extensive first pass effect, resulting in a reduction of oral bioavailability (F%) to 50% and a short elimination half-life of 4 h; parameters necessitating its frequent administration. The current study was therefore, designed to formulate and optimize the transfersomal TiM gel for transdermal delivery. TiM loaded transfersomal gel was optimized using two 2(3) full factorial designs; where the effects of egg phosphatidyl choline (PC): surfactant (SAA) molar ratio, solvent volumetric ratio, and the drug amount were evaluated...
September 2016: Journal of Advanced Research
Preeti Verma, Sunil Kumar Prajapati, Rajbharan Yadav, Danielle Senyschyn, Peter R Shea, Natalie L Trevaskis
Vesicular and colloidal delivery systems can be designed to control drug release spatially and temporally to improve drug efficacy and side effect profiles. Niosomes (vesicles prepared from nonionic surfactants in aqueous media) are gaining interest as an alternative vesicular delivery system as they offer advantages such as biocompatibility, chemical stability, low cost, high purity and versatility. However, the physical stability of niosomes, like other vesicular systems, is limited by vesicle fusion, aggregation and leakage...
September 15, 2016: Molecular Pharmaceutics
Mukul Ashtikar, Kalpa Nagarsekar, Alfred Fahr
Strong barrier properties of stratum corneum often limits the efficiency of drug delivery through skin. Several strategies were tried to improve permeation of drug through skin for local as well as systemic drug delivery. Incorporation of the drug within flexible liposomal vesicles has been one of the popular and well-studied approaches for delivering drug to deeper layers of the skin or even systemic circulation. Flexible/deformable/elastic liposomal systems such as invasomes, Transfersomes®, ethosomes, niosomes, etc...
September 10, 2016: Journal of Controlled Release: Official Journal of the Controlled Release Society
Wenping Wang, Yaqin Cai, Yanhua Liu, Yunsheng Zhao, Jun Feng, Chen Liu
In this work, microemulsion-based gels were prepared for transdermal delivery of paeonol. Microemulsions containing eutectic mixtures of paeonol and menthol were developed. The obtained microemulsions were evaluated for particle size, viscosity and physical stability. The selected microemulsions were incorporated into Carbopol gels. Drug crystallization behavior during a short-term storage was compared and in vitro permeation and deposition study were conducted on mouse skin. Results showed that the eutectic liquids of paeonol and menthol at all ratio (6:4, 5:5 and 4:6) could form microemulsions but with significantly different physical characteristics...
September 7, 2016: Artificial Cells, Nanomedicine, and Biotechnology
J P Borges, G O Lopes, V Verri, M P Coelho, P M C Nascimento, D A Kopiler, E Tibirica
Evaluation of microvascular endothelial function is essential for investigating the pathophysiology and treatment of cardiovascular and metabolic diseases. Although laser speckle contrast imaging technology is well accepted as a noninvasive methodology for assessing microvascular endothelial function, it has never been used to compare male patients with coronary artery disease with male age-matched healthy controls. Thus, the aim of this study was to determine whether laser speckle contrast imaging could be used to detect differences in the systemic microvascular functions of patients with established cardiovascular disease (n=61) and healthy age-matched subjects (n=24)...
September 1, 2016: Brazilian Journal of Medical and Biological Research, Revista Brasileira de Pesquisas Médicas e Biológicas
Panoraia I Siafaka, Neslihan Üstündağ Okur, Evangelos Karavas, Dimitrios N Bikiaris
Nanocarriers, due to their unique features, are of increased interest among researchers working with pharmaceutical formulations. Polymeric nanoparticles and nanocapsules, involving non-toxic biodegradable polymers, liposomes, solid lipid nanoparticles, and inorganic-organic nanomaterials, are among the most used carriers for drugs for a broad spectrum of targeted diseases. In fact, oral, injectable, transdermal-dermal and ocular formulations mainly consist of the aforementioned nanomaterials demonstrating promising characteristics such as long circulation, specific targeting, high drug loading capacity, enhanced intracellular penetration, and so on...
2016: International Journal of Molecular Sciences
Chao Liu, Peng Quan, Liang Fang
The aim of this study was to investigate the influence of drug physicochemical properties on drug release behaviors and their relationship with skin permeation behaviors, which provided transdermal enhancement strategies for the design of transdermal drug delivery system. Six model drugs with different physicochemical properties were selected and hydroxyl pressure sensitive adhesive (PSA) was synthesized. Horizontal diffusion cell was used to evaluate drug release and skin permeation behaviors. The relationship between physicochemical properties and release behaviors was conducted with regression analysis...
October 10, 2016: European Journal of Pharmaceutical Sciences
Shinying Lau, Jie Fei, Haoran Liu, Weixing Chen, Ran Liu
Dissolving microneedles have been employed as a safe and convenient transdermal delivery system for drugs and vaccines. To improve effective drug delivery, a multilayered pyramidal dissolving microneedle patch, composed of silk fibroin tips with the ability of robust mechanical strength, rapid dissolution and drug release supported on a flexible polyvinyl alcohol (PVA) pedestal is reported. To show the utility of this approach the ability of the fabricated microneedles to deliver insulin is demonstrated. The dissolving microneedles have sufficient mechanical strength to be inserted into abdomen skin of mice to a depth of approximately 150μm, and release their encapsulated insulin into the skin to cause a hypoglycemic effect...
August 26, 2016: Journal of Controlled Release: Official Journal of the Controlled Release Society
Alice Simon, Maria Inês Amaro, Anne Marie Healy, Lucio Mendes Cabral, Valeria Pereira de Sousa
In the present study, in vitro permeation experiments in a Franz diffusion cell were performed using different synthetic polymeric membranes and pig ear skin to evaluate a rivastigmine (RV) transdermal drug delivery system. In vitro-in vivo correlations (IVIVC) were examined to determine the best model membrane. In vitro permeation studies across different synthetic membranes and skin were performed for the Exelon(®) Patch (which contains RV), and the results were compared. Deconvolution of bioavailability data using the Wagner-Nelson method enabled the fraction of RV absorbed to be determined and a point-to-point IVIVC to be established...
October 15, 2016: International Journal of Pharmaceutics
Yen-Heng Lin, I-Chi Lee, Wei-Chieh Hsu, Ching-Hong Hsu, Kai-Ping Chang, Shao-Syuan Gao
The main issue of transdermal drug delivery is that macromolecular drugs cannot diffuse through the stratum corneum of skin. Many studies have pursued micro-sized needles encapsulated with drugs to overcome this problem, as these needles can pierce the stratum corneum and allow drugs to enter the circulatory system of the human body. However, most microneedle fabrication processes are time-consuming and require expensive equipment. In this study, we demonstrate a rapid method for fabricating a microneedle mold using drawing lithography and a UV-cured resin...
October 2016: Biomedical Microdevices
Raida Al-Kassas, Jingyuan Wen, Angel En-Miao Cheng, Amy Moon-Jung Kim, Stephanie Sze Mei Liu, Joohee Yu
This study aimed at improving the systemic bioavailability of propranolol-HCl by the design of transdermal drug delivery system based on chitosan nanoparticles dispersed into gels. Chitosan nanoparticles were prepared by ionic gelation technique using tripolyphosphate (TPP) as a cross-linking agent. Characterization of the nanoparticles was focused on particle size, zeta potential, surface texture and morphology, and drug encapsulation efficiency. The prepared freeze dried chitosan nanoparticles were dispersed into gels made of poloxamer and carbopol and the rheological behaviour and the adhesiveness of the gels were investigated...
November 20, 2016: Carbohydrate Polymers
Shery Jacob, Anroop B Nair, Bandar E Al-Dhubiab
Niosomes suggest a versatile vesicle delivery system with possible transport of drugs via topical route for skin delivery. The aim of the present research was to optimize niosome gel formulation of acyclovir and evaluate in both in vitro and in vivo rabbit model. Niosome formulations were formulated by coacervation phase separation technique with different ratios of non-ionic surfactants, phospholipids and cholesterol using 3(2) factorial design. Altering the surfactant concentration has influenced the drug entrapment, but not vesicle size...
August 25, 2016: Journal of Liposome Research
Cornel Burger, Yasser Shahzad, Alicia Brümmer, Jeanetta Du Plessis, Minja Gerber
In recent years, colloidal delivery systems based on nano-emulsion are gaining popularity; being used for encapsulation and delivery of many drugs. Nano-emulsions are thermokinetically stable dispersion systems, which have been used in topical and transdermal delivery of a number of pharmaceutically active compounds. Nano-emulsions have a narrow droplet size range with tuneable surface properties, which make them an ideal delivery vehicle. Nano-emulsions have a number of advantages over conventional emulsions, i...
August 24, 2016: Current Drug Delivery
Bingwu Liao, Hao Ying, Chenhuan Yu, Zhaoyang Fan, Weihua Zhang, John Shi, Huazhong Ying, Nagaiya Ravichandran, Yongquan Xu, Junfeng Yin, Yongwen Jiang, Qizhen Du
(-)-Epigallocatechin-3-O-gallate (EGCG), a versatile natural product in fresh tea leaves and green tea, has been investigated as a preventative treatment for cancers and cardiovascular disease. The objective of this study was to develop EGCG-nanoethosomes for transdermal delivery and to evaluate them for treating subcutaneously implanted human melanoma cell tumors. EGCG-nanoethosomes, composed of 0.2% EGCG, 2% soybean phosphatidylcholine, 30% ethanol, 1% Tween-80 and 0.1% sugar esters, were prepared and characterized using laser transmission electron microscopy...
October 15, 2016: International Journal of Pharmaceutics
Alam Zeb, Omer Salman Qureshi, Hyung-Seo Kim, Ji-Hye Cha, Hoo-Seong Kim, Jin-Ki Kim
The aim of this study is to investigate methotrexate-entrapped ultradeformable liposomes (MTX-UDLs) for potential transdermal application. MTX-UDLs were prepared by extrusion method with phosphatidylcholine as a bilayer matrix and sodium cholate or Tween 80 as an edge activator. The physicochemical properties of MTX-UDLs were determined in terms of particle size, polydispersity index, zeta potential, and entrapment efficiency. The deformability of MTX-UDLs was compared with that of methotrexate-entrapped conventional liposomes (MTX-CLs) using a steel pressure filter device...
2016: International Journal of Nanomedicine
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