Transdermal penetrants surfactants

Chemical PEs have recently been studied for increasing transdermal delivery of ASOs or other polar macromolecules [35]. Chemically induced transdermal penetration results from a transient reduction in the barrier properties of the stratum corneum. The reduction may be attributed to a variety of factors such as the opening of intercellular junctions due to hydration [36], solubilization of the stratum corneum [37, 38], or increased lipid bilayer fluidization [39, 40]. Combining various surfactants and co-solvents can be used to achieve skin penetration, purportedly resulting in therapeutically relevant concentrations of ASO in the viable epidermis and dermis [41]. In summary, it appears feasible to deliver ASO to the skin using a number of different delivery techniques and formulations. 

A wide variety of long-chain fatty acids increase transdermal delivery the most popular is oleic acid. It is relevant that many penetration enhancers contain saturated or unsaturated hydrocarbon chains and some structure-activity relationships have been drawn from the extensive studies of Aungst et al. [22,23] who employed a range of fatty acids and alcohols, sulfoxides, surfactants, and amides as enhancers for naloxone. From these experiments, it appears that saturated alkyl chain lengths of around Cio to C12 attached to a polar head... 

Surfactants—traditionally common constituents and stabilizers of topical vehicles, ranging from hydro-phobic agents such as oleic acid to hydrophilic sodium lauryl sulphate— have been tested as penetration enhancers to improve transdermal drug delivery. 

Ionic surfactants are thought to enhance transdermal absorption by disordering the lipid layer of the stratum corneum and by denaturation of keratin. The use of penetration enhancers in general, and surfactants in particular, in transdermal therapeutic systems has been reviewed by Walters. 

The cosmetics and transdermal drug delivery fields are also expected to further benefit from the formulation of microemulsions from mild sugarbased surfactants. Lehmann et al. have studied the effect of such a microemulsion on dermal and corneal irritation, and hydrocortisone incorporation [105]. A microemulsion containing commercially available sucrose esters, isopropyl myristate, and propylene glycol and water was prepared as a water continuous system, and 16.5% hydrocortisone was loaded into the anhydrous base mixture. The formulation spread well on the skin due to the low surface tension of the system at 26 mN/m. While the microemulsion provided greater drug penetration, it also resulted in irritation and barrier compromise. The authors make the point that the formulation may be better suited to drugs that do not induce an irritation themselves. 

Som I, Bhatia K, Yasir M. Status of surfactants as penetration enhancers in transdermal drug delivery. /Pharm Bioallied Sci. 4 (1) 2-9,2012. 

---