Surfactants transdermal drug delivery

Nevertheless, there are reports on enhancement of ocular drug absorption by bile salts [33], surfactants [200], and chelators [149], Newton et al. [35] demonstrated that Azone, an enhancer widely tested in transdermal drug delivery [201], increased the ocular absorption of cyclosporine, an immunosuppressant, by a factor of 3, thereby prolonging the survival of a corneal allograft. In 1986, Lee et al. [34] reported that 10 pg/mL cytochalasin B, an agent capable of condensing the actin microfilaments, increased the aqueous humor and iris-ciliary body concentrations of topically applied inulin (5 kDa) by about 70% and 700%, respectively, in the albino rabbit. 

Tiemessen, H.L.G.M., Nonionie Surfactant Systems for Transdermal Drug Delivery, Ph.D. Thesis Leiden University, The Netherlands, 1989. 

Clinical Drug Trials and Tribulations Second Edition, Revised and Expanded, edited by Allen Cato, Lynda Sutton, and Allen Cato III Modern Pharmaceutics Fourth Edition, Revised and Expanded, edited by Gilbert S. Banker and Christopher T. Rhodes Surfactants and Polymers in Drug Delivery, Martin Malmsten Transdermal Drug Delivery Second Edition, Revised and Expanded, edited by Richard H. Guy and Jonathan Hadgraft... 

D. A. van Hal, Nonionic surfactant vesicles for dermal and transdermal drug delivery, thesis, Leiden University, 1994, pp. 149-176. 

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. 

Cappel, M.J. and Kreuter, J. (1991) Effect of nonionic surfactants on transdermal drug delivery II poloxaraer and poloxamine surfactants. International Journal of Pharmaceutics, 69, 155-167. 

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. 

Azone (laurocapram) is used extensively as a transdermal permeation enhancer, and has also found use in buccal drug delivery. It is a lipophilic surfactant in nature (Figure 10.4). Permeation of salicylic acid was enhanced by the pre-application of an Azone emulsion in vivo in a keratinized hamster cheek pouch model [35]. Octreotide and some hydrophobic compounds absorption have also been improved by the use of Azone [36], Azone was shown to interact with the lipid domains and alter the molecular moment on the surface of the bilayers [37], In skin it has been proposed that Azone was able to form ion pairs with anionic drugs to promote their permeation [38],... 

Badran, M.M., Taha, E.I., Tayel, M.M., Al-Suwayeh, S.A., 2014. Ultra-fine self nanoemulsifying drug delivery system for transdermal delivery of meloxicam dependency on the t)fpe of surfactants. J. Mol. Liq. 190, 16—22. 

Recently, for the transdermal delivery of drugs using carrier systems, attention has been focused on the development of transformable [284,285] or elastic vesicles [12], These vesicles are liposomes that contain surfactants or in general edge activators in addition to phospholipids in their lipid membranes (Figure 10), a fact that... 

Localized tissue irritation can be seen from the intramuscular (IM) route. This is especially an issue when the formulation pH differs from the pH of the surrounding tissue or when precipitation of poorly soluble drugs occurs. Incorrect administration of IM injections is probably the most important factor that causes local adverse effects. Local skin irritation can also be seen with transdermal delivery systems due to the alcohols, nonionic surfactants, and adhesives. 

---