Transdermal Delivery of Drugs with Differing Lipophilicities Using Azone Analogs as Dermal Penetration Enhancers

Phillips, Christine A.; Michniak, B. B.

doi:10.1002/jps.2600841208

Cited by 66 publications

(33 citation statements)

References 41 publications

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“…limonene) provided higher permeation for lipophilic drugs (41,42). It was revealed that the lipophilicity of the permeant, as well as the enhancer molecule played an important role in determining the penetration promoting activity (13,41,(43)(44)(45)(46)(47)(48)(49)(50).…”

Section: D-limonenementioning

confidence: 99%

Percutaneous Permeation Enhancement by Terpenes: Mechanistic View

Sapra

Jain

Tiwary

2008

AAPS J

141

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Abstract. A popular approach for improving transdermal drug delivery involves the use of penetration enhancers (sorption promoters or accelerants) which penetrate into skin to reversibly reduce the barrier resistance. The potential mechanisms of action of penetration enhancers include disruption of intercellular lipid and/or keratin domains and tight junctions. This results in enhanced drug partitioning into tissue, altered thermodynamic activity/solubility of drug etc. Synthetic chemicals (solvents, azones, pyrrolidones, surfactants etc.) generally used for this purpose are rapidly losing their value in transdermal patches due to reports of their absorption into the systemic circulation and subsequent possible toxic effect upon long term application. Terpenes are included in the list of Generally Recognized As Safe (GRAS) substances and have low irritancy potential. Their mechanism of percutaneous permeation enhancement involves increasing the solubility of drugs in skin lipids, disruption of lipid/protein organization and/or extraction of skin micro constituents that are responsible for maintenance of barrier status. Hence, they appear to offer great promise for use in transdermal formulations. This article is aimed at reviewing the mechanisms responsible for percutaneous permeation enhancement activity of terpenes, which shall foster their rational use in transdermal formulations.

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Section: D-limonenementioning

confidence: 99%

Percutaneous Permeation Enhancement by Terpenes: Mechanistic View

Sapra

Jain

Tiwary

2008

AAPS J

141

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“…These include the use of permeation enhancers, employing vesicular drug delivery systems, delivering hydrophilic drugs using microneedles, or augmenting transdermal flux using laser systems. [15][16][17][18][19][20][21][22][23][24] Microdermabrasion, which involves blowing of aluminum oxide crystals or other abrasive substances onto the face and then vacuuming them off, 24peels the stratum corneum, leading to better penetration of topical preparations.…”

Section: Discussionmentioning

confidence: 99%

Assessment of response of microdermabrasion with 2% kojic acid in melasma

Agarwal

2016

Int J Res Med Sci

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“…PG promotes intracellular transport. Azone and PG act as great permeation enhancers across the stratum corneum through both hydrophilic and lipophilic routes 9 . Azone is known to facilitate the flow through the lipid bilayer.…”

Section: Fatty Acids (Fasmentioning

confidence: 99%

Untitled

2017

IJPSR

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ABSTRACT:The human skin serves as an impediment, a thermo regulator and prevents excessive loss of water from the internal organs. Various ways of transferring the drugs have been developed by modifying the barrier properties of the skin. Enhancement in skin penetration by hydration of the stratum corneum, or by use of chemical enhancers acting on the lipids and keratinized structures in the stratum corneum, partitioning and solubility effects is a promising tool in potential clinical applications. Penetration enhancement is a new emerging technology which has the potential to increase the number of drugs taken trans-dermally. Also the drugs with short biological half-life could be easily administered. Among many advantages over other routes the three crucial ones are avoiding metabolism in liver, minimal negative effects and increased bioavailability. Also, the stratum corneum prevents the loss of physiologically essential substances and as a result provides penetration resistance by acting as a protective barrier. This is the rate limiting step in the absorption of the drug percutaneously. In this review article, we present a summary of various advances made in the field of permeation enhancers based on literature survey of various research articles.

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Transdermal Delivery of Drugs with Differing Lipophilicities Using Azone Analogs as Dermal Penetration Enhancers

Cited by 66 publications

References 41 publications

Percutaneous Permeation Enhancement by Terpenes: Mechanistic View

Percutaneous Permeation Enhancement by Terpenes: Mechanistic View

Assessment of response of microdermabrasion with 2% kojic acid in melasma

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