polidocanol and dodecyltetraethylene-glycol-monoether

In this contribution, we attempt to correlate the change in water dynamics in a reverse micellar (RM) core caused by the modification of the interface by mixing an anionic surfactant, sodium bis(2-ethylhexyl) sulfosuccinate (AOT), and a nonionic surfactant, tetraethylene glycol monododecyl ether (Brij-30), at different proportions, and its consequent effect on the reactivity of water, measured by monitoring the solvolysis reaction of benzoyl chloride (BzCl). The dimension of the RM droplets at different mixing ratios of AOT and Brij-30 (X(Brij-30)) has been measured using dynamic light scattering (DLS) technique. The physical properties of the RM water have been determined using Fourier transform infrared spectroscopy (FTIR) and compressibility studies, which show that with increasing X(Brij-30), the water properties tend toward that of bulk-like water. The solvation dynamics, probed by coumarin 500 dye, gets faster with X(Brij-30). The rotational anisotropy studies along with a wobbling-in-cone analysis show that the probe experiences less restriction at higher X(Brij-30). The kinetics of the water-mediated solvolysis also gets faster with X(Brij-30). The increased rate of solvolysis has been correlated with the accelerated solvation dynamics, which is another consequence of surfactant headgroup-water interaction.

Topics: Micelles; Polidocanol; Polyethylene Glycols; Spectroscopy, Fourier Transform Infrared; Surface-Active Agents; Thermodynamics; Time Factors; Water

A new water-based topical formulation is presented that aims at providing good penetration properties for both lipophilic and hydrophilic drugs with as small a disturbance of the skin barrier function as possible. The formulation contains dispersed lipids in a ratio resembling that of human skin. The capacity to deliver is addressed in this first study while the mild effect on skin will be presented later. Three variations of the lipid formulation were investigated by use of pigskin in vitro diffusion cell. The hydrophilic 5(6)-carboxyfluorescein (CF) and the lipophilic acridine orange 10-nonyl bromide (AO) were used as model drug substances. The results showed that the delivery properties of the new formulation exceeded that of the references (vaseline and xanthan gum gel). The effect was largest for lipophilic AO where all lipid matrix formulations were superior in amount detected in the skin. The results for the hydrophilic CF were also promising. Especially efficient was the lipid formulation containing the non-ionic adjuvants tetra ethylene glycol monododecyl ether and polyoxyethylene 23 dodecyl ether. The additional in vivo study suggests that the used in vitro model has qualitative bearing on relevant in vivo situations.

Topics: Acridine Orange; Administration, Topical; Animals; Chemistry, Pharmaceutical; Diffusion; Drug Carriers; Fluoresceins; In Vitro Techniques; Lipids; Permeability; Polidocanol; Polyethylene Glycols; Skin; Skin Physiological Phenomena; Swine; Water

The uptake, distribution, and clearance of three labeled nonionic surfactants, 14C-labeled dodecyl tetra(oxyethylene) ether [14C-C12-AE(4)], 14C-labeled dodecyl octa(oxyethylene) ether [14C-C12-AE(8)], and 14C-labeled dodecyl hexadeca(oxyethylene) ether [14C-C12-AE(16)] were investigated in carp (Cyprinus carpio) exposed to concentrations of 0.2-0.6 mg X liter-1, using whole-body autoradiography and the liquid scintillation counting method. 14C radioactivity was rapidly absorbed into the fish body and distributed in skin, nasal and oral cavities, gills, brain, hepatopancreas, kidney, gall bladder, and intestinal content at comparatively high concentrations. The calculated wet weight whole-body bioconcentration factor at steady state in the fish exposed to 14C-C12-AE(4), 14C-C12-AE(8), or 14C-C12-AE(16) for 72 hr was 310, 220, or 4.3, respectively. Clearance of 14C radioactivity from the fish body was rapid, with half-lives of 30-80 hr. The metabolites of 14C-C12-AE(4) were also examined in gills, blood, kidney, hepatopancreas, or gall bladder by thin-layer chromatography.

Topics: Animals; Autoradiography; Carps; Chromatography, Thin Layer; Cyprinidae; Polidocanol; Polyethylene Glycols; Software; Surface-Active Agents; Tissue Distribution