Effect of Azone upon the in vivo antiviral efficacy of cidofovir or acyclovir topical formulations in treatment/prevention of cutaneous HSV-1 infections and its correlation with skin target site free drug concentration in hairless mice

Afouna, Mohsen I.; Fincher, Timothy K.; Zaghloul, Abdel-Azim; Reddy, Indra K.

doi:10.1016/s0378-5173(02)00705-6

Cited by 22 publications

(12 citation statements)

References 18 publications

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“…However, due to the impervious nature of the SC towards macromolecules, a suitable penetration enhancer should substantially improve transport of macromolecules through the skin. A variety of technologies have been developed to enhance penetration for macromolecules through the skin, including the use of microneedles,23–25 electroporation,26, 27 laser generated pressure waves,28–31 hyperthermia,32 low‐frequency sonophoresis,33–39 iontophoresis,40–43 penetration enhancers,44–51 or a combination of these methods 52–54. Many penetration enhancement techniques face inherent challenges, such as scale‐up and safety concerns 7…”

Section: Introductionmentioning

confidence: 99%

Hydration Effects on Skin Microstructure as Probed by High-Resolution Cryo-Scanning Electron Microscopy and Mechanistic Implications to Enhanced Transcutaneous Delivery of Biomacromolecules

Tan

Lawson

et al. 2010

Journal of Pharmaceutical Sciences

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Although hydration is long known to improve the permeability of skin, penetration of macromolecules such as proteins is limited and the understanding of enhanced transport is based on empirical observations. This study uses high-resolution cryo-scanning electron microscopy to visualize microstructural changes in the stratum corneum (SC) and enable a mechanistic interpretation of biomacromolecule penetration through highly hydrated porcine skin. Swollen corneocytes, separation of lipid bilayers in the SC intercellular space to form cisternae, and networks of spherical particulates are observed in porcine skin tissue hydrated for a period of 4–10 h. This is explained through compaction of skin lipids when hydrated, a reversal in the conformational transition from unilamellar liposomes in lamellar granules to lamellae between keratinocytes when the SC skin barrier is initially established. Confocal microscopy studies show distinct enhancement in penetration of fluorescein isothiocyanate-bovine serum albumin (FITC-BSA) through skin hydrated for 4–10 h, and limited penetration of FITC-BSA once skin is restored to its natively hydrated structure when exposed to the environment for 2–3 h. These results demonstrate the effectiveness of a 4–10 h hydration period to enhance transcutaneous penetration of large biomacromolecules without permanently damaging the skin.

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Section: Introductionmentioning

confidence: 99%

Hydration Effects on Skin Microstructure as Probed by High-Resolution Cryo-Scanning Electron Microscopy and Mechanistic Implications to Enhanced Transcutaneous Delivery of Biomacromolecules

Tan

Lawson

et al. 2010

Journal of Pharmaceutical Sciences

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“…1. Azone 1 is a well-documented penetration enhancer (Afouna et al, 2003;Hadgraft et al, 1996;Ló pez et al, 2000;Williams & Barry, 2004). It appears to act by reducing the SC diffusional barrier, because it inserts itself into the lipid domain located in the intercellular channels.…”

Section: Introductionmentioning

confidence: 99%

In Vivo Skin Permeation of Sodium Naproxen Formulated in Pluronic F-127 Gels: Effect of Azone® and Transcutol®

Escobar-Chávez

Quintanar‐Guerrero

Ganem-Rondero

2005

Drug Development and Industrial Pharmacy

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The objective of this study was to determine the penetration of sodium naproxen, formulated in Pluronic F-127 (PF-127) gels containing Azone and Transcutol as penetration enhancers, through human skin in vivo. It was found that the combination of Azone and Transcutol in PF-127 gels enhanced sodium naproxen penetration, with enhancement ratios of up to two fold compared with the formulation containing only Transcutol. These results were confirmed by TEWL and ATR-FTIR spectroscopy, suggesting a synergic action for Azone and Transcutol. Because of the thermo-reversible behavior of Pluronic gels, the influence of the components added to the gel formulations on viscosity, as a function of temperature, was also studied.

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“…One of the reasons is the fact that Azone shows a slight antiviral effect. On the other hand, it is included in the Chinese Pharmacopoeia and is used in this country …”

Section: Azone‐like Enhancersmentioning

confidence: 99%

Azone analogues: classification, design, and transdermal penetration principles

Jampílek

Brychtova

2010

Medicinal Research Reviews

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The development in the field of pharmaceutical dosage forms results in the discovery of additional highly sophisticated drug delivery systems that allow maintaining a constant level of the active substance in an organism. Transdermal therapeutic systems are an excellent alternative to conventional pharmaceutical dosage forms. However, the application of transdermal drug delivery faces the problem of insufficient or no penetration of active pharmaceutical substances through the skin. This review article describes the possible fundamental mechanisms of penetration through the skin barrier and refers to the classification of skin penetration enhancers. Azone-like enhancers are considered in detail and classified according to their structure on the basis of medicinal chemistry approaches. The article also provides a review of original transdermal penetration enhancers prepared in our laboratory and discusses the relationship between the chemical structure of the described Azone analogues and their penetration activity (SAR/QSAR).

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Effect of Azone upon the in vivo antiviral efficacy of cidofovir or acyclovir topical formulations in treatment/prevention of cutaneous HSV-1 infections and its correlation with skin target site free drug concentration in hairless mice

Cited by 22 publications

References 18 publications

Hydration Effects on Skin Microstructure as Probed by High-Resolution Cryo-Scanning Electron Microscopy and Mechanistic Implications to Enhanced Transcutaneous Delivery of Biomacromolecules

Hydration Effects on Skin Microstructure as Probed by High-Resolution Cryo-Scanning Electron Microscopy and Mechanistic Implications to Enhanced Transcutaneous Delivery of Biomacromolecules

In Vivo Skin Permeation of Sodium Naproxen Formulated in Pluronic F-127 Gels: Effect of Azone® and Transcutol®

Azone analogues: classification, design, and transdermal penetration principles

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