Search results for "permeation"
showing 10 items of 274 documents
Physical Methods for Enhancing Oral Mucosal Delivery: Sonophoresis, Iontophoresis and Electroporation
2015
The need for more rapid onset of action and improved absorption of medications has resulted in great development of drug delivery technologies. Transmucosal drug delivery offers a convenient route of administration for a variety of clinical indications. Unfortunately, the wide variability in structure of the oral mucosal tissues could constitute a key factor in drug penetration and absorption. To circumvent this obstacle and to increase the drug flux through the mucosal membranes, different approaches to permeation enhancement are used. This chapter describes the most significant aspects of the physical techniques widely used such as sonophoresis, iontophoresis, and electroporation. These p…
Quantitative Prediction of Concentration Effects in Steric Exclusion Chromatography
1986
Abstract A semiempirical model, based on a previous one quantitatively describing the dependence of the elution volume, V(cA), on the concentration of injected polymer, cA, in exclusion chromatography (SEC) at dilute solutions, has been developed. In the derived equation, concentration effects are mainly governed by the Huggins' coefficient, kA, and by the quadratic coefficient in the polynomial expansion of the reduced specific viscosity, kA. Because of the incertitudes on reliable kA and kA' values, these are respectively removed from the model through she Imai's equation and the empirical correlation kA' + 0.122=kA, here obtained. Thus, A predicted elution volumes besides polymer concent…
Polymer-enhanced ultrafiltration for heavy metal removal: Influence of chitosan and carboxymethyl cellulose on filtration performances
2018
Abstract Reclaiming of wastewaters contaminated by heavy metals has become a major challenge over the last decades. For this reason, nanoporous membrane processes have awaken the interest of industry and local community, and the possible ways to improve their performances has become a priority goal for researchers. Metal removal enhancement by polymer addition is a potential way that is deeply investigated herein on nickel ion rejection with chitosan and carboxymethyl cellulose addition. Due to the vanishing of electrostatic interactions induced by the large amount of salt usually contained in effluents, ion rejection consequently drastically drops. However, it is highlighted that a suffici…
Continuous spin fractionation and characterization by size-exclusion chromatography for styrene-butadiene block copolymers.
2005
Abstract Linear and star-shaped styrene–butadiene block copolymers synthesized by anionic polymerization of butadiene and styrene were fractionated by applying a newly developed large-scale fractionation technique, named continuous spin fractionation (CSF). Their molecular weight and polydispersity index ( d = M w / M n ) were measured with size-exclusion chromatography and static light scattering. For the linear triblock copolymer a fractionation via temperature variation turned out to be better suited than the usual isothermal procedure. The star-shaped polymer with the d value of 1.33 was fractionated in two CSF steps to get the targeted sample, which has a considerably more uniform st…
Improvement of Resveratrol Permeation through Sublingual Mucosa: Chemical Permeation Enhancers versus Spray Drying Technique to Obtain Fast-Disintegr…
2021
Resveratrol (RSV) is a natural polyphenol with several interesting broad-spectrum pharmacological properties. However, it is characterized by poor oral bioavailability, extensive first-pass effect metabolism and low stability. Indeed, RSV could benefit from the advantage of the sublingual route of administration. In this view, RSV attitudes to crossing the porcine sublingual mucosa were evaluated and promoted both by six different chemical permeation enhancers (CPEs) as well as by preparing four innovative fast-disintegrating sublingual mini-tablets by spray drying followed by direct compression. Since RSV by itself exhibits a low permeation aptitude, this could be significantly enhanced by…
Permeability properties of a three-cell type in vitro model of blood-brain barrier.
2005
We previously found that RBE4.B brain capillary endothelial cells (BCECs) form a layer with blood‐brain barrier (BBB) properties if co‐cultured with neurons for at least one week. As astrocytes are known to modulate BBB functions, we further set a culture system that included RBE4.B BCECs, neurons and astrocytes. In order to test formation of BBB, we measured the amount of (3)H‐sucrose able to cross the BCEC layer in this three‐cell type model of BBB. Herein we report that both neurons and astrocytes induce a decrease in the permeability of the BCEC layer to sucrose. These effects are synergic as if BCECs are cultured with both neurons and astrocytes for 5 days, permeability to sucrose decr…
Polymeric drug delivery micelle-like nanocarriers for pulmonary administration of beclomethasone dipropionate
2017
In this paper, the potential of novel polymeric micelles as drug delivery systems for Beclomethasone Dipropionate (BDP) administration into the lung is investigated. These nanostructures are obtained starting from α,β-poly(N-2-hydroxyethyl)-D,L-aspartamide (PHEA), which was subsequently functionalized with O-(2-aminoethyl)-Oâ-methylpolyethylenglycole (PEG2000), ethylenediamine (EDA) and lipoic acid (LA), obtaining PHEA-PEG2000-EDA-LA graft copolymer. Empty and drug-loaded micelles possess adequate chemical-physical characteristics for pulmonary administration such as spherical shape, slightly positive surface charge and mean size of about 200 nm. Besides, BDP-loaded micelles, obtained …
The mechanism of aquaporin inhibition by gold compounds elucidated by biophysical and computational methods
2017
The inhibition of water and glycerol permeation via human aquaglyceroporin-3 (AQP3) by gold(iii) complexes has been studied by stopped-flow spectroscopy and, for the first time, its mechanism has been described using molecular dynamics (MD), combined with density functional theory (DFT) and electrochemical studies. The obtained MD results showed that the most effective gold-based inhibitor, anchored to Cys40 in AQP3, is able to induce shrinkage of pores preventing glycerol and water permeation. Moreover, the good correlation between the affinity of the Au(iii) complex to Cys binding and AQP3 inhibition effects was highlighted, while no influence of the different oxidative character of the c…
The effect of chitosan on the bioaccessibility and intestinal permeability of acyclovir
2019
Chitosan is object of pharmaceutical research as a candidate permeability enhancer. However, chitosan was recently shown to reduce the oral bioavailability of acyclovir in humans. The effect of chitosan on two processes determining the oral bioavailability of acyclovir, bioaccessibility and intestinal absorption, was now investigated. Acyclovir's bioaccessibility was studied using the dynamic TNO gastro-Intestinal Model (TIM-1). Four epithelial models were used for permeability experiments: a Caco-2 cell model in absence and presence of mucus and both rat and porcine excised intestinal segments. Study concentrations of acyclovir (0.8 g/l) and chitosan (1.6 g/l and 4 g/l) were in line with t…
How Does the Benzamide Antipsychotic Amisulpride get into the Brain?—An In Vitro Approach Comparing Amisulpride with Clozapine
2003
This study evaluated the disposition of the two atypical antipsychotics, amisulpride (AMS) and clozapine (CLZ), and its main metabolite N-desmethylclozapine (DCLZ), to their target structures in the central nervous system by applying an in vitro blood-brain barrier and blood-cerebrospinal fluid (CSF) barrier based on monolayers of porcine brain microvessel endothelial cells (PMEC) or porcine choroid plexus epithelial cells (PCEC). Permeation studies through PMEC- and PCEC-monolayers were conducted for 60 min at drug concentrations of 1, 5, 10, and 30 muM applied to the donor compartment. PMEC were almost impermeable for AMS (permeation coefficient, P1 x 10(-7) cm/s) in the resorptive direct…