Testosterone skin permeation enhancement by menthol through formation of eutectic with drug and interaction with skin lipids

Journal of Pharmaceutical Sciences
Y Kaplun-Frischoff, E Touitou

Abstract

The aim of this investigation was to elucidate the mechanism of skin permeation enhancement of the lipophilic drug, testosterone, by menthol. Menthol was found to form eutectic mixtures with testosterone, cholesteryl oleate, and ceramides. DSC measurements showed that menthol drastically lowers the Tm of testosterone, from 153.7 to 39.9 degrees C. The decrease in Tm resulted in an increase in the solubility of testosterone in an aqueous ethanol vehicle by 2.8-fold, which caused a corresponding 2.8-fold increase in the flux of testosterone. A further increase in skin flux, to eight times the base line, could be attributed to the effect of menthol on the skin barrier properties. This assumption is supported by DSC results showing that menthol decreases the Tm of cholesteryl oleate and ceramides and modifies the thermogram profile of isolated stratum corneum. The results of this investigation indicate that menthol affects skin permeation by a dual mechanism: by forming a eutectic with the penetrating compound, thereby increasing its solubility, and by altering the barrier properties of the stratum corneum. Moreover, this study indicates that both types of interactions must be taken into consideration when using chemical enhancers ...Continue Reading

References

Oct 1, 1975·The Journal of Investigative Dermatology·B F Van Duzee
Sep 1, 1971·Journal of Pharmaceutical Sciences·W L Chiou, S Riegelman
Sep 1, 1994·Journal of Pharmaceutical Sciences·E TouitouM Mezei
Dec 1, 1963·Archives of Dermatology·A M KLIGMAN, E CHRISTOPHERS

❮ Previous
Next ❯

Citations

May 21, 2011·Graefe's Archive for Clinical and Experimental Ophthalmology = Albrecht Von Graefes Archiv Für Klinische Und Experimentelle Ophthalmologie·Xiaolin XuHao Cui
Jun 7, 2006·Pharmaceutical Research·Marie-Laure LeichtnamRichard H Guy
Dec 6, 2012·Archives of Pharmacal Research·Chun-Woong ParkEun-Seok Park
Dec 4, 2003·Journal of Controlled Release : Official Journal of the Controlled Release Society·M LodzkiE Touitou
Mar 17, 2004·Journal of Controlled Release : Official Journal of the Controlled Release Society·Sunil Thomas Kumar Narishetty, Ramesh Panchagnula
May 29, 2000·Journal of Controlled Release : Official Journal of the Controlled Release Society·A D WoolfsonJ A Russell
Mar 20, 2003·Journal of Controlled Release : Official Journal of the Controlled Release Society·Ming-Thau SheuHsiu-O Ho
Mar 16, 2001·International Journal of Pharmaceutics·A F El-KattanB B Michniak
Sep 5, 2001·International Journal of Pharmaceutics·K KatayamaT Koizumi
Sep 29, 2001·International Journal of Pharmaceutics·K M MackayB W Barry
Jan 16, 2002·International Journal of Pharmaceutics·J A H van LaarhovenH Vromans
Nov 24, 1999·International Journal of Pharmaceutics·A H ShojaeiR Khosravan
May 1, 2008·The AAPS Journal·Bharti SapraA K Tiwary
Aug 31, 2013·International Journal of Nanomedicine·Shu MengJianxin Li
Aug 6, 1999·Drug Development and Industrial Pharmacy·D A Godwin, B B Michniak
Nov 9, 2000·Drug Development and Industrial Pharmacy·V R Sinha, M P Kaur
Oct 22, 2002·Expert Opinion on Biological Therapy·Elka Touitou
Jun 3, 2010·Drug Development and Industrial Pharmacy·Wenjuan CongGuoan Luo
Jan 5, 2011·Cutaneous and Ocular Toxicology·Jakob Torp MadsenKlaus Ejner Andersen
Oct 6, 1998·Journal of Pharmaceutical Sciences·T M MorganB C Finnin
Dec 28, 2011·European Journal of Pharmacology·Jingjing LiuHao Cui
Nov 7, 2015·International Journal of Pharmaceutics·Jadwiga RembiesaTautgirdas Ruzgas
Oct 13, 2011·The Journal of Pharmacy and Pharmacology·Sarah FialaStuart A Jones
Aug 25, 2010·Contact Dermatitis·Jakob Torp MadsenKlaus E Andersen
Jan 18, 2005·International Journal of Pharmaceutics·Chomchan AmnuaikitToshikiro Kimura
Jan 18, 2005·Journal of Controlled Release : Official Journal of the Controlled Release Society·Sunil T K Narishetty, Ramesh Panchagnula
May 9, 2006·Journal of Controlled Release : Official Journal of the Controlled Release Society·Marie-Laure LeichtnamRichard H Guy
Dec 6, 2005·The Veterinary Journal·P C Mills, S E Cross
Apr 16, 2016·International Journal of Pharmaceutics·Zheng Li, Ping I Lee
Aug 5, 2014·Bioresource Technology·Zhangran ChenTianling Zheng
May 7, 2014·Pharmaceutical Development and Technology·Shu MengJianxin Li
Nov 5, 2010·International Journal of Pharmaceutics·Taner SenyiğitOzgen Ozer
Sep 8, 2009·Biochimica Et Biophysica Acta·Pankaj Karande, Samir Mitragotri
Jun 1, 2010·Nicotine & Tobacco Research : Official Journal of the Society for Research on Nicotine and Tobacco·Christopher A SquierPhilip W Wertz
Mar 28, 2017·Journal of Pharmaceutical Sciences·Ahmed S ZidanMuhammad Ashraf
Aug 9, 2019·Chemical Communications : Chem Comm·Dinis O AbranchesJoão A P Coutinho
Feb 26, 2020·Pharmaceutical Development and Technology·Shahram Emami, Ali Shayanfar
Jul 28, 2019·International Journal of Molecular Sciences·Noriaki NagaiNaohito Kawasaki
May 27, 2009·Drug Development and Industrial Pharmacy·Ligang ZhaoZhonggui He
Feb 9, 2021·AAPS PharmSciTech·Jamshed HaneefRenu Chadha
Nov 23, 2020·AAPS PharmSciTech·Faisal Al-AkaylehMayyas Al-Remawi

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.

Related Papers

Journal of Controlled Release : Official Journal of the Controlled Release Society
P W StottB W Barry
Journal of Controlled Release : Official Journal of the Controlled Release Society
Amit Kumar JainRamesh Panchagnula
Journal of Controlled Release : Official Journal of the Controlled Release Society
Sunil Thomas Kumar Narishetty, Ramesh Panchagnula
© 2021 Meta ULC. All rights reserved