Effects of Various Penetration Enhancers on Penetration of Aminophylline Through Shed Snake Skin

Abstract

Background:Cellulite is the accumulation of subcutaneous fat and connective tissue in tights and buttocks. Xanthines, such as aminophylline, are used as phosphodiesterase inhibitors, and are also adenosine receptor antagonists. Objectives: The aim of the present study was to characterize in vitro aminophylline transdermal absorption through shed snake skin, and to investigate the absorption enhancing effect of various enhancers. Materials and Methods: Aminophylline gels were prepared using theophylline and ethylenediamine as raw materials of aminophylline, hydroxypropyl methyl cellulose (HPMC) F4M as gelling agent, and propylene glycol as a co-solvent. Sodium tauroglycocholate (STGC) (100, 200, and 500 μg/mL), lauric acid (1.7 and 15%), and ethanol (60%) were added as enhancers. In vitro percutaneous absorption experiments were performed on snake skin using Franz diffusion cells. Flux (J), permeability coefficient (P), and enhancement factor (EF) for each formulation were calculated. Results:The results indicated that all of enhancers significantly enhanced drug permeability. This effect was decreased by increasing the concentration of STGC; in contrast, by increasing the concentration of lauric acid from 1.7 to 15%, EF was enhanced Although ethanol (60%) and STGC (100 μg/mL) showed the highest EFs, the effect of ethanol on drug permeability appeared with a lag time. Conclusions: According to the findings, type and concentration of penetration enhancers can effect on transdermal permeation of drug.

Permeability of frog skin to chemicals: effect of penetration enhancers

“…In mammals, the first mechanism (membrane fluidisation, decreased lag time and increased permeability) is dominant for ethanol concentrations up to ∼60% [21, 24], with lag times increasing higher ethanol concentrations. In reptiles, no lag phase was reported in shed snake skin when an aminophylline gel was formulated with the penetration enhancers lauric acid, sodium tauroglycocholate (a surfactant), or PG, however a lag time was reported when formulated in 60% ethanol [25]. It is therefore not surprising that a lag time was observed with the higher ethanol concentration in the current study, but not with the lower concentrations.…”

Nanoemulsion: A Review on Mechanisms for the Transdermal Delivery of Hydrophobic and Hydrophilic Drugs

“…Researchers compared the effectiveness of ethanol as a PE with lauric acid and sodium tauroglycocholate to help facilitate the passage of aminophylline through skin. Lauric acid showed the best enhancing ability in the first hour, while after four hours ethanol leaped ahead, resulting in a 60% permeation enhancement, which is explained by ethanol's ability to temporarily modify the SC to increase permeation [45].…”

“…Their rate of enhanced penetration is influenced by two possible mechanisms. At the beginning, the surfactant enters the intercellular regions of the SC, fluidizing, solubilizing, and extracting the lipid components [45]. Following this process, the surfactant penetrates the intercellular matrix, interacting and binding with keratin filaments, hypothetically resulting in the disruption of corneocytes [46,47].…”

Absorption-Enhancing Effects of Bile Salts

“…Kouchak et al . in 2014 found that NaTGC (100 μg/mL) improved the flux of aminophylline through snake skin compared to simple gel ( p < 0.05) [62]. Moreover, in previous studies, it was reported that NaTGC could increase absorption of theophylline through shed snake skin [63].…”