Transdermal enhancer patent literature

Santus, Giancarlo; Baker, R.W.

doi:10.1016/0168-3659(93)90090-r

Cited by 48 publications

(27 citation statements)

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“…Permeation enhancers, supersaturated solutions, and in vitro methods including diffusion cell studies, IR-spectroscopy and tape stripping have been reported by Moser [50]. Classification of enhancers according to their structure has been reviewed in several reports [51][52][53][54][55][56]. Magnusson has focused on the potential of enhancers in veterinary drug delivery [57].…”

Section: Skin Permeation Enhancersmentioning

confidence: 99%

Amphiphilic Transdermal Permeation Enhancers: Structure-Activity Relationships

Vávrová

Zbytovská²,

Hrabálek³

2005

CMC

113

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Transdermal drug delivery offers numerous advantages over conventional routes of administration; however, poor permeation of most drugs across the skin barrier constitutes a serious limitation of this methodology. One of the approaches used to enlarge the number of transdermally-applicable drugs uses permeation enhancers. These compounds promote drug permeation through the skin by a reversible decrease of the barrier resistance. Enhancers can act on the stratum corneum intracellular keratin, influence desmosomes, modify the intercellular lipid domains or alter the solvent nature of the stratum corneum. Even though, hundreds of substances have been identified as permeation enhancers to date, yet our understanding of the structure-activity relationships is limited. In general, enhancers can be divided into two large groups: small polar solvents, e.g. ethanol, propylene glycol, dimethylsulfoxide and amphiphilic compounds containing a polar head and a hydrophobic chain, e.g. fatty acids and alcohols, 1-dodecylazepan-2-one (Azone), 2-nonyl-1,3-dioxolane (SEPA 009), and dodecyl-2-dimethylaminopropanoate (DDAIP). In this review we have focused on structure-activity relationships of amphiphilic permeation enhancers, including the properties of the hydrophobic chains, e.g. length, unsaturation, and branching, as well as the polar heads characteristics, e.g. hydrogen bonding ability, lipophilicity, and size. We present over 180 examples of enhancers with different polar head to illustrate the structural requirements and the possible role of the polar head. We have given an overview of the methods used for investigation of the mechanisms of permeation enhancement, namely differential scanning calorimetry (DSC), infrared (IR) and Raman spectroscopy, X-ray diffraction and future perspectives in this field. Furthermore, biodegradability and chirality of the enhancers are discussed.

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Section: Skin Permeation Enhancersmentioning

confidence: 99%

Amphiphilic Transdermal Permeation Enhancers: Structure-Activity Relationships

Vávrová

Zbytovská²,

Hrabálek³

2005

CMC

113

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“…10 Much research has been performed to identify penetration enhancers with the aid of in vitro screens, 11,12 and literally hundreds of different chemicals with a wide divergence of chemical structure that are able to modify the penetration characteristics of different drugs and marker compounds into the skin have been identified. 13,14 However, only a small number of these agents have been shown to produce useful enhancement in vivo, only a few have actually been incorporated into products and successfully tested in humans, and, other than previously used ingredients of topical preparations, none has yet been successful in the market place. This review is intended to examine why, despite all this work, we seem to have had very little success to date.…”

Section: Introductionmentioning

confidence: 99%

Transdermal penetration enhancers: Applications, limitations, and potential

Finnin

Morgan

1999

Journal of Pharmaceutical Sciences

232

137

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“…Reports in the literature have shown that penetration enhancers may alter the composition and/or the organization of SC intercellular lipids, thus decreasing the barrier function and allowing an appropriate diffusion of drugs through the skin (25,26).…”

Section: Introductionmentioning

confidence: 99%