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Molecules. 2016 Dec 11;21(12). pii: E1709.

Natural Terpenes as Penetration Enhancers for Transdermal Drug Delivery.

Author information

1
Hubei Collaborative Innovation Center of Targeted Antitumor Drug, Jingchu University of Technology, Jingmen 448000, China. chenjun75@163.com.
2
Pharmaceutical Research Laboratory of Chinese Medicine, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China. chenjun75@163.com.
3
Pharmaceutical Research Laboratory of Chinese Medicine, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China. qiudong_J@126.com.
4
Pharmaceutical Research Laboratory of Chinese Medicine, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China. 15951837195@163.com.
5
Pharmaceutical Research Laboratory of Chinese Medicine, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210023, China. zh20150908@sina.com.
6
Hubei Collaborative Innovation Center of Targeted Antitumor Drug, Jingchu University of Technology, Jingmen 448000, China. pengpei2011@126.com.
7
Hubei Collaborative Innovation Center of Targeted Antitumor Drug, Jingchu University of Technology, Jingmen 448000, China. yxixiong163@163.com.

Abstract

The greatest hindrance for transdermal drug delivery (TDD) is the barrier property of skin, especially the stratum corneum (SC). Various methodologies have been investigated and developed to enhance the penetration of drugs through the skin. Among them, the most popular approach is the application of penetration enhancers (PEs), including natural terpenes, a very safe and effective class of PEs. In the present paper, we focused on terpenes as skin PEs for TDD. The mechanism of their action, the factors affecting their penetration enhancement effect, as well as their possible skin toxicity were discussed. Terpenes abundant in nature have great potential in the development of PEs. Compared to synthetic PEs, natural terpenes have been proved to possess higher enhancement activity. Interaction with SC intercellular lipids is the main mechanism of action for terpenes. The key factor affecting the enhancement effect is the lipophilicity of both terpenes and drug molecules. In addition, a lot of terpenes have also been proved to be much less toxic compared to azone, the classic synthetic PE. In summary, terpenes may be preferred over the chemically synthesized compounds as safe and effective PEs to promote the percutaneous absorption of drugs.

KEYWORDS:

penetration enhancer; stratum corneum; terpenes; transdermal drug delivery

PMID:
27973428
PMCID:
PMC6273457
DOI:
10.3390/molecules21121709
[Indexed for MEDLINE]
Free PMC Article

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