2018
DOI: 10.1208/s12249-018-1160-7
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Third-Generation Transdermal Delivery Systems Containing Zidovudine: Effect of the Combination of Different Chemical Enhancers and a Microemulsion System

Abstract: This study aimed to examine the influence of the combination of chemical enhancers and a microemulsion on the transdermal permeation of zidovudine (AZT). Ethanol, 1,8-cineole, and geraniol were incorporated in a microemulsion. The droplet size, zeta potential, rheology, and SAXS analysis were performed. The permeation enhancer effect was evaluated using pig ear skin. Snake skin (Boa constrictor) treated with the formulations was also used as a stratum corneum model and studied by attenuated total reflectance-i… Show more

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Cited by 15 publications
(4 citation statements)
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“…Nanocarriers and the chemical permeation enhancers can effectively promote penetration with convenient application. In recent years, microemulsion has been widely used in transdermal drug administration due to its prominent penetration-promoting effect (5)(6)(7)(8)(9)(10).…”
Section: Introductionmentioning
confidence: 99%
“…Nanocarriers and the chemical permeation enhancers can effectively promote penetration with convenient application. In recent years, microemulsion has been widely used in transdermal drug administration due to its prominent penetration-promoting effect (5)(6)(7)(8)(9)(10).…”
Section: Introductionmentioning
confidence: 99%
“…Where synergistic effects can be obtained, the combinatorial approach has the potential for effective permeation enhancement at lower active concentrations than separate approaches (du Toit et al 2016). For example, the study by Carvalho et al (2018) about the combination of chemical enhancers incorporated a microemulsion of ethanol, 1,8-cineole, and geraniol and showed that the ethanol and cineole causes an increase in the diffusion and partition coefficients. Karande et al (2004) proposed an experimental tool, in vitro skin impedance guided by highthroughput screening, to investigate particular mixtures of penetration enhancers for increased skin permeability to macromolecules (~10 kDa), which yielded up to~100fold enhancement without inducing skin irritation.…”
Section: Combining Permeation Enhancersmentioning
confidence: 99%
“…Also, the microemulsions that contained a high eugenol concentration and Polyethylene Glycol (PEG) were able to increase the loading capacity of indomethacin as evidenced by a significant improvement in the solubility of the drug in these formulations compared to its water solubility (logP of indomethacin=4.46). In another study, ME was prepared with cineole as a chemical enhancer, a combination that promoted a higher skin permeation of zidovudine [67]. Zidovudine, a poorly bioavailable drug with a short half-life of 0.53h, significantly permeated through pig ear skin and snake skin from the cineole containing ME (by threefold) compared with the control.…”
Section: Microemulsionmentioning
confidence: 99%