Status of Fatty Acids as Skin Penetration Enhancers-A Review

2009 ◽  
Vol 6 (3) ◽  
pp. 274-279 ◽  
Author(s):  
Ashu Mittal ◽  
U. Sara ◽  
Asgar Ali ◽  
Mohd. Aqil
Keyword(s):  
Fatty Acids ◽  
Skin Penetration ◽  
Penetration Enhancers

scholarly journals New Insights on the Mechanism of Fatty Acids as Buccal Permeation Enhancers

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 201 ◽  
Author(s):  
Cristina Padula ◽  
Silvia Pescina ◽  
Sara Nicoli ◽  
Patrizia Santi
Keyword(s):  
Fatty Acids ◽  
Fatty Acid ◽  
Fluorescein Isothiocyanate ◽  
Penetration Enhancers ◽  
Systemic Delivery ◽  
Permeation Enhancers ◽  
Maximum Value ◽  
The Relationship ◽  
Insight Into ◽  
The Ideal

Buccal mucosa has recently received much attention as a potential route for systemic delivery of drugs, including biologics and vaccines. The aim of this work was to gain insight into the mechanism of fatty acids as buccal permeation enhancers, by studying the effect of a series of medium and long chain fatty acids on the permeation of a model high molecular weight and hydrophilic molecule, fluorescein isothiocyanate labelled dextran (FD-4, m.w. 4 kDa) across porcine esophageal epithelium. A parabolic relationship between fatty acid lipophilicity and enhancement was obtained, regardless of the presence and number of double bonds. The relationship, which resembles the well-known relationship between permeability and lipophilicity of transdermal delivery, presents a maximum value in correspondence of C10 (logP approx. 4). This is probably the ideal lipophilicity for the fatty acid to interact with the lipid domains of the mucosa. When the same analysis was performed on skin data, the same trend was observed, although the maximum value was reached for C12 (logP approx. 5), in agreement with the higher lipophilicity of the skin. The results obtained in the present work represent a significant advancement in the understanding of the mechanisms of action of fatty acids as buccal penetration enhancers.

scholarly journals QSAR Analyses of Skin Penetration Enhancers.

ChemInform ◽  
2007 ◽  
Vol 38 (34) ◽  
Author(s):  
Manisha Iyer ◽  
Tao Zheng ◽  
A. J Hopfinger ◽  
Yufeng J. Tseng
Keyword(s):  
Skin Penetration ◽  
Penetration Enhancers

A Review on Terpenes as Skin Penetration Enhancers in Transdermal Drug Delivery

2009 ◽  
Vol 21 (5) ◽  
pp. 423-428 ◽  
Author(s):  
Perry Fung Chye Lim ◽  
Xiang Yang Liu ◽  
Sui Yung Chan
Keyword(s):  
Drug Delivery ◽  
Transdermal Drug Delivery ◽  
Skin Penetration ◽  
Penetration Enhancers

Status of terpenes as skin penetration enhancers

2007 ◽  
Vol 12 (23-24) ◽  
pp. 1061-1067 ◽  
Author(s):  
Mohammed Aqil ◽  
Abdul Ahad ◽  
Yasmin Sultana ◽  
Asgar Ali
Keyword(s):  
Skin Penetration ◽  
Penetration Enhancers

scholarly journals Esters of terpene alcohols as highly potent, reversible, and low toxic skin penetration enhancers

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Monika Kopečná ◽  
Miloslav Macháček ◽  
Anna Nováčková ◽  
Georgios Paraskevopoulos ◽  
Jaroslav Roh ◽  
...  
Keyword(s):  
Electrical Impedance ◽  
Ex Vivo ◽  
Skin Penetration ◽  
Transepidermal Water Loss ◽  
Penetration Enhancers ◽  
Cinnamyl Alcohol ◽  
Permeation Enhancers ◽  
Terpene Alcohols ◽  
Dermal Drug Delivery ◽  
Toxic Skin

Abstract Skin penetration/permeation enhancers are compounds that improve (trans)dermal drug delivery. We designed hybrid terpene-amino acid enhancers by conjugating natural terpenes (citronellol, geraniol, nerol, farnesol, linalool, perillyl alcohol, menthol, borneol, carveol) or cinnamyl alcohol with 6-(dimethylamino)hexanoic acid through a biodegradable ester linker. The compounds were screened for their ability to increase the delivery of theophylline and hydrocortisone through and into human skin ex vivo. The citronellyl, bornyl and cinnamyl esters showed exceptional permeation-enhancing properties (enhancement ratios up to 82) while having low cellular toxicities. The barrier function of enhancer-treated skin (assessed by transepidermal water loss and electrical impedance) recovered within 24 h. Infrared spectroscopy suggested that these esters fluidized the stratum corneum lipids. Furthermore, the citronellyl ester increased the epidermal concentration of topically applied cidofovir, which is a potent antiviral and anticancer drug, by 15-fold. In conclusion, citronellyl 6-(dimethylamino)hexanoate is an outstanding enhancer with an advantageous combination of properties, which may improve the delivery of drugs that have a limited ability to cross biological barriers.

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