Search results for "permeability"
showing 10 items of 596 documents
A UHPLC-UV Method to Quantify Skin Deposition and Transdermal Permeation of Tizanidine Hydrochloride
2015
Tizanidine hydrochloride is an α2-adrenergic agonist used for the symptomatic relief of spasticity associated with multiple sclerosis or with spinal cord injury or disease. The objective of this study was to develop an isocratic, robust and sensitive ultra-high performance liquid chromatography method using UV detection for use in a project to develop a transdermal therapeutic system to deliver tizanidine across the skin. Isocratic separation was achieved using a C18 column and a mobile phase comprising a 80:20 mixture of 0.004% trifluoroacetic acid in water and MeCN (pH* 3.2) at a flow rate of 0.2 mL min(-1) Tizanidine eluted at 1.499 min and the total run time was 2 min. The method was sp…
Hidden complexity in membrane permeabilization behavior of antimicrobial polycations.
2021
A promising alternative to classical antibiotics are antimicrobial peptides and their synthetic mimics (smAMPs) that supposedly act directly on membranes. For a more successful design of smAMPs, we need to know how the type of interaction with the membrane determines the type of membrane perturbation. How this, in turn, transfers into selectivity and microbial killing activity is largely unknown. Here, we characterize the action of two smAMPs: MM:CO (a copolymer of hydrophobic cyclooctyl subunits and charged β-monomethyl-α-aminomethyl subunits) and the highly charged poly-NM (a homopolymer of α-aminomethyl subunits). By thorough characterization of vesicle leakage experiments, we elucidate …
Modeling mass transfer in fracture flows with the time domain-random walk method
2019
The time domain-random walk method was developed further for simulating mass transfer in fracture flows together with matrix diffusion in surrounding porous media. Specifically, a time domain-random walk scheme was developed for numerically approximating solutions of the advection-diffusion equation when the diffusion coefficient exhibits significant spatial variation or even discontinuities. The proposed scheme relies on second-order accurate, central-difference approximations of the advective and diffusive fluxes. The scheme was verified by comparing simulated results against analytical solutions in flow configurations involving a rectangular channel connected on one side with a porous ma…
One-dimensional compression and consolidation of shales
2016
This paper presents a comprehensive methodology for analysing the compression and consolidation behaviour of shales. An apparatus was designed to perform oedometric high-pressure tests by applying a maximum vertical total stress of 100 MPa and simultaneously controlling the pore water pressure of the specimen. An analytical method was formulated to analyse the shale consolidation behaviour, which allows information to be gathered on the coefficient of consolidation, stiffness, poroelastic properties, secondary compression and permeability of the tested material as a function of the applied stress conditions. Results obtained on Opalinus Clay shale using the developed methodology are present…
Nanoparticles of a polyaspartamide-based brush copolymer for modified release of sorafenib: In vitro and in vivo evaluation.
2017
Abstract In this paper, we describe the preparation of polymeric nanoparticles (NPs) loaded with sorafenib for the treatment of hepatocellular carcinoma (HCC). A synthetic brush copolymer, named PHEA-BIB-ButMA (PBB), was synthesized by Atom Trasnfer Radical Polymerization (ATRP) starting from the α-poly( N -2-hydroxyethyl)- d , l -aspartamide (PHEA) and poly butyl methacrylate (ButMA). Empty and sorafenib loaded PBB NPs were, then, produced by using a dialysis method and showed spherical morphology, colloidal size, negative ζ potential and the ability to allow a sustained sorafenib release in physiological environment. Sorafenib loaded PBB NPs were tested in vitro on HCC cells in order to e…
Reversible Hydrogels with Switchable Diffusive Permeability
2021
Hydrogels are polymer networks swollen in water that are characterized by soft mechanics and high permeability. This makes them good candidates for separation and membrane technologies. The diffusion is controlled by the mesh size of the network, and this can be made tunable through the introduction of thermoresponsive polymers. However, this is still a developing field. To contribute to this development, a dual dynamic network is formed composed of four-arm polyethylene glycol precursors in which each arm is functionalized with both a terpyridine moiety capable of forming reversible metal–ligand complexes along with branches of poly(N-isopropylacrylamide) (pNIPAAm), which can be swit…
Innovative in vitro method and permeability estimation procedure to predict drug transport across the blood-brain barrier
2014
La Barrera Hematoencefálica (BHE) es una entidad caracterizada por su naturaleza restrictiva al paso de sustancias. Las propiedades de la barrera están determinadas por la confluencia de tres componentes principales: 1) uniones celulares endoteliales con presencia de proteínas especificas intramembrana y citoplasmáticas unidas estrechamente al citoesqueleto. Esta circunstancia restringe la difusión paracelular de compuestos. Adicionalmente a las células endoteliales, la barrera presenta una membrana basal, en la cual se localizan pericitos y astrocitos, que conforman una capa que refuerza las propiedades de la barrera; 2) la presencia de transportadores de absorción y la sobreexpresión de t…
Permeability of three-dimensional random fiber webs
1998
We report the results of essentially ab initio simulations of creeping flow through large threedimensional random fiber webs that closely resemble fibrous sheets such as paper and nonwoven fabrics. The computational scheme used in this Letter is that of the lattice-Boltzmann method and contains no free parameters concerning the properties of the porous medium or the dynamics of the flow. The computed permeability of the web is found to be in good agreement with experimental data, and confirms that permeability depends exponentially on porosity over a large range of porosity. [S0031-9007(97)05087-4]
Polyoxypregnanes as safe, potent, and specific ABCB1-inhibitory pro-drugs to overcome multidrug resistance in cancer chemotherapy in vitro and in vivo
2021
Multidrug resistance (MDR) mediated by ATP binding cassette subfamily B member 1 (ABCB1) is significantly hindering effective cancer chemotherapy. However, currently, no ABCB1-inhibitory drugs have been approved to treat MDR cancer clinically, mainly due to the inhibitor specificity, toxicity, and drug interactions. Here, we reported that three polyoxypregnanes (POPs) as the most abundant constituents of Marsdenia tenacissima (M. tenacissima) were novel ABCB1-modulatory pro-drugs, which underwent intestinal microbiota-mediated biotransformation in vivo to generate active metabolites. The metabolites at non-toxic concentrations restored chemosensitivity in ABCB1-overexpressing cancer cells v…
Selective downregulation of the MDR1 gene product in Caco-2 cells by stable transfection to prove its relevance in secretory drug transport.
2005
Considerable interest is focused on overcoming multidrug resistance (MDR) in cancer chemotherapy. The in vitro experiments to characterize P-glycoprotein's (P-gp) function and to decrease its effects have led to a variety of strategies such as addition of competitors or supplementation of the medium with oligonucleotides complementary to the 5'-end of the MDR1-mRNA. For the Caco-2 cell line, an in vitro model for absorption screening, expressing multiple transporters including P-gp, which pumps substances back into the apical solution, P-gp activity might mask other relevant transport proteins' activity. The objective of the present study was to construct a Caco-2 subline with reduced P-gp …