Potential of Stratum Corneum Lipid Liposomes for Screening of Chemical Skin Penetration Enhancers

Abstract

The evaluation of effective skin chemical penetration enhancers (CPEs) is a crucial process in the development of transdermal and dermal formulations with the capacity to overcome the stratum corneum barrier. In the present study, we aimed to investigate the potential of stratum corneum lipid liposomes (SCLLs) as an alternative tool for the screening of various types and concentrations of CPEs. SCLLs were prepared using a thin-film hydration technique, and two types of fluorescent probes ( Key words stratum corneum lipid liposome; chemical skin penetration enhancer; liposome; high-throughput screening Skin has been recognized as an application site of therapeutic drugs for several decades. However, only small numbers of drugs are available nowadays intended for systemic absorption through the skin. The stratum corneum (SC), the outermost layer of the skin, provides a strong barrier to protect against extraneous molecules from entering the body, and thus limits the skin penetration of drugs. The structure of the SC consists of keratin-rich corneocytes embedded in an intercellular lipid matrix.

Improved skin penetration using active and passive enhancement methods

“…Transcutol is needed to increase the efflux to a great extent ( Figure 8B). This finding is in agreement with a previous study [24]. Transcutol is reported to interact with the aqueous domain of the lipid bilayer which increase the solubility of drugs in the skin.…”

“…Transcutol, a monoethyl ether of diethylene glycol, is classified into the group of alcohols and glycols, which are reported to interact with the aqueous domain of the lipid bilayers, which increase the solubility of drugs in the skin [24]. Harrison et al reported that the penetration enhancement property of Transcutol is the result of changes in solubility rather than diffusion in the membrane [25].…”

Stratum corneum lipid liposomes for investigating skin penetration enhancer effects

“…This finding is in agreement with a previous study. 1 Transcutol is reported to interact in the aqueous domain of the lipid bilayers which increase the solubility of drugs in the skin. According to Moghadam et al , Transcutol caused only a slight disordering effect within the SC membrane.…”

“…The skin has been recognized as a highly attractive application site of therapeutic agents with both local and systemic effects. 1 However, the outermost layer of the skin, the stratum corneum (SC) forms a barrier, which makes it hard for active pharmaceutical ingredients (API) to pass through this layer and exert their pharmacological effects. 2 It has been shown that the transdermal flux of API and SC lipid conformation is strongly correlated.…”

“…Transcutol, a monoethyl ether of diethylene glycol, is classified into the group of alcohols and glycols, which are reported to interact with the aqueous domain of the lipid bilayers, which increase the solubility of drugs in the skin. 1 Harrison et al reported that the penetration enhancement property of Transcutol is the result of changes in solubility rather than diffusion in the membrane. Another study stated that the enhancing ability of Transcutol is attributed to its ability to pass through the skin and get incorporated into the multiple lipid bilayers, thereby swelling the intercellular lipids.…”