Chemical Penetration Enhancers for Transdermal Drug Delivery Systems

Abstract

Skin as an important site of drug application for both local and systemic effects. However in skin, the stratum corneum is the main barrier for drug penetration. Penetration enhancement technology is a challenging development that would increase the number of drugs available for transdermal administration. The permeation of drug through skin can be enhanced by both chemical penetration enhancement and physical methods. In this review, we have discussed the chemical penetration enhancement technology for transdermal drug delivery as well as the probable mechanisms of action.

Transdermal Protein Delivery Using Choline and Geranate (CAGE) Deep Eutectic Solvent

“…To improve skin penetrability, physical/chemical enhancers such as electricity, ultrasound, microneedles, dimethyl sulfoxide (DMSO), urea, azone, pyrrolidones, alcohols, oils, and fatty acids are often used. [18,21,40,41] Although effective, concomitant irritation at the site of application and toxicity has impeded clinical utility of chemical penetration enhancers. [40] In this study, we present CAGE as a novel transdermal delivery material that can significantly improve penetration of proteins through the skin.…”

“…[11][12][13][14][15][16][17][18][19] Notwithstanding these developments, toxicities arising due to chemical penetration enhancers, infections resulting from chronic disruption of the SC or occurrence of burns and scars have curtailed their clinical application. [20,21] For example, Zecuity (sumatriptan iontophoretic transdermal system) marketed by Teva Pharmaceuticals for the treatment of migraine has been recently discontinued due to development of adverse events such as burns and scars. [22] In addition, device based systems can only be used over a limited skin area.…”

Assessment of solid microneedle rollers to enhance transmembrane delivery of doxycycline and inhibition of MMP activity

“…This can be achieved by using penetration enhancers which chemically or physically alter the skin to transiently increase its permeability (Pathan & Setty, 2009). These include skin pretreatments such as hyaluronidase administration, sonophoresis and iontophoresis (Williams & Barry, 2004;Benson, 2005).…”

Development and evaluation of occlusive systems employing polyvinyl alcohol for transdermal delivery of sumatriptan succinate

“…Is a highly lipophilic agent, with a logP octanol/water of ∼ 6.2, is soluble and compatible with most organic solvents, including alcohol and propylene glycol (Pathan & Setty, 2009), and it can be employed with lipophilic and hydrophilic molecules. Its mechanism of action is based on its capacity to alter the organization of the lipid structure of the stratum corneum and augment the diffusion of a drug across the skin (Smith & Maibach, 1995;López-Cervantes et al, 2006).…”