0000000000174358
AUTHOR
Marina Herráez
Partition Behavior of Anilines in Bulk‐Phase and High‐Performance Liquid Chromatographic Systems: Influence on Correlation with Biological Constants
Abstract The partition behavior of a mixed series of ring‐substituted anilines in reversed‐phase high‐performance liquid chromatographic systems is substantially different from that observed in a classical bulk‐phase partition system with n ‐heptane as the aprotic reference solvent. On the basis of the equivalence of each ring substituent in the p ‐straight‐chain methylene groups (ν value) as a function of the fraction of organic solvent (acetonitrile or methanol) in the mobile phase, the biased partition behavior for imperfect homologues and heterologues is verified relative to that of perfect homologues. This behavior was tentatively attributed, mainly, to differences in the hydrogen bond…
Enhancement of nortriptyline penetration through human epidermis: influence of chemical enhancers and iontophoresis.
Abstract Different known percutaneous chemical enhancers and iontophoresis have been tested in-vitro to study their ability to increase transdermal absorption of nortriptyline hydrochloride (20 mg mL−1). The chemicals 1-dodecanol, Span 20, Azone, (R)-(+)-limonene or isopropyl myristate were used as an overnight pretreatment at 5% (w/w) in ethanol. Furthermore, isopropyl myristate (20%, w/w) and propylene glycol (15%, w/w) were tested in the same vehicle. Iontophoresis was applied directly to the nortriptyline hydrochloride donor solution for three different concentrations (20, 2 and 0.5 mgmL−1). The chemical enhancers slightly increased the nortriptyline transdermal flux but iontophoresis w…
In Vitro Percutaneous Penetration of Acyclovir from Solvent Systems and Carbopol 971-P Hydrogels: Influence of Propylene Glycol
The mechanism underlying propylene glycol (PG) effects on acyclovir (ACV) penetration through human epidermis were studied. Solvent systems and Carbopol gels containing increasing percentage of PG (from 0% to 70%, w/w) were used. Viscosity studies of both vehicles were carried out to characterise the influence of rheological behaviour. In solvent systems skin permeation values of ACV increase as the concentration of PG increase yielding a maximum enhancement ratio (ER = 10) for 70% PG. The release rate of ACV from gels was determined. Higuchi's model was used to estimate the apparent diffusion coefficient of the drug. These values show a decrease as the content of PG in the vehicle increase…
Acyclovir Delivery Matrices Based on Poly(Ethylene Glycol)/Chitosan Semi-Interpenetrating Networks
Abstract Chitosan matrix systems have been studied as potential vehicles for the prolonged release of acyclovir (ACV). The influence of chitosan concentration (from 0.83% to 1.67%) on viscoelastic properties of formulations with and without glyoxal was analyzed. For chitosan‐poly(ethylene glycol) 400 formulations loss modulus ( G ″) are greater than storage modulus ( G ′). This corresponds to the characteristic behavior of nonstructured systems. When glyoxal was added to the chitosan‐poly(ethylene glycol) 400 formulations, gelled matrix was obtained (i.e., G ′ is higher than G ″), except for the lowest chitosan concentration. ACV release rates for the both types of systems, with and without…
Transdermal nortriptyline hydrocloride patch formulated within a chitosan matrix intended to be used for smoking cessation.
The aim of this study was to prepare and characterize both physically and biopharmaceutically, a nortriptyline hydrochloride (NTP-HCl) patch formulated in chitosan.16 g of each chitosan patch formulation (I, II and III, see Table 1 ) was poured onto rectangular glass plates (64 cm²) at a height of 1 mm and dried for 24 h at room temperature. In order to characterize the chitosan patches, polarized microscopy, in vitro skin permeation studies by passive diffusion and iontophoresis and rheological and bioadhesion studies were performed.Polarized microscopy revealed the absence of aggregates and crystal forms of NTP-HCl in all transdermal patches after 30 days of storage. The rheological behav…