Effect of Terpenes on the enhancement of skin permeation of lipophilic drugs: A systematic review
https://doi.org/10.47895/amp.vi0.6505
- Author:
Llani D. Longgos
1
;
Erikka B. Pequiro
1
;
Lord Sam B. Liston
1
;
Kathrine Anne M. Flores
1
;
Gea Abigail U. Ecoy
1
;
Pajaree Sakdiset
2
;
Gerard Lee L. See
1
,
3
,
4
;
Florencio V. Arce, Jr.
1
,
3
,
4
Author Information
1. Department of Pharmacy, School of Health Care Professions, University of San Carlos, Cebu City, Philippines
2. Center for Drug and Cosmetics Excellence, School of Pharmacy, Walailak University, Thasala, Nakhon Si Thammarat, Thailand
3. Pharmaceutical Research and Drug Development Laboratories, Department of Pharmacy, School of Health Care Professions, University of San Carlos, Cebu City, Philippines
4. Pharmaceutical Sciences Division, National Research Council of the Philippines, Taguig City, Philippines
- Publication Type:Journal Article
- Keywords:
Lipophilic drugs;
Permeation enhancer;
Enhancement ratio
- MeSH:
Terpenes;
Skin
- From:
Acta Medica Philippina
2024;58(4):59-71
- CountryPhilippines
- Language:English
-
Abstract:
Objectives:The stratum corneum (SC) remains an obstacle to the passage of drugs applied topically. Several
investigations have focused on enhancing the penetration of drugs through the SC by integrating permeation
enhancers (PE) into the drug formulation. Terpenes are among the PE utilized in formulations and are categorized by the regulatory bodies as generally recognized as safe (GRAS). This study aimed to comparatively analyze the skin permeation enhancing effect of terpenes on lipophilic drugs.
Methods:The present study reviewed the effects of terpenes on the permeation of lipophilic small-molecule drugs through the skin using original research published between 2000 - 2022 retrieved from PubMed®. The search phrase used was (lipophilic drug) AND (terpene) AND (permeation enhancer).
Results:Terpenes increase the percutaneous permeation of lipophilic small molecule drugs by 1.06 – 256.80-fold. Linear correlation analysis of terpenes’ cLog P with enhancement ratio (ER) revealed moderate and strong positive correlations in pig skin (r = 0.21) and mouse skin (r = 0.27), and rat skin (r = 0.41) and human skin (r = 0.67), respectively. Drug cLog P is a poor (r = -0.06) predictor of permeation enhancement. Terpenes with cLog P higher than 2.40 had ER greater than 10. Higher ERs (>30) were recorded for nerolidol, carvacrol, borneol, terpineol, limonene, menthone, pulegone, and menthol among the terpene-chemical penetration enhancers.
Conclusion:cLog P of terpene-based chemical permeation enhancers (CPE) is strongly correlated with ER of lipophilic drugs across human skin. Non-polar groups in terpenes and hydrogen bond interactions by terpenes with SC lipid enhance cutaneous drug penetration of lipophilic drugs.
- Full text:6505-Article Text-104530-2-10-20240313.pdf
