Effect of Terpenes on the Enhancement of Skin Permeation of Lipophilic Drugs: A Systematic Review.

Autor:	Longgos LD; Department of Pharmacy, School of Health Care Professions, University of San Carlos, Cebu City, Philippines., Pequiro EB; Department of Pharmacy, School of Health Care Professions, University of San Carlos, Cebu City, Philippines., Liston LSB; Department of Pharmacy, School of Health Care Professions, University of San Carlos, Cebu City, Philippines., Flores KAM; Department of Pharmacy, School of Health Care Professions, University of San Carlos, Cebu City, Philippines., Ecoy GAU; Department of Pharmacy, School of Health Care Professions, University of San Carlos, Cebu City, Philippines., Sakdiset P; Center for Drug and Cosmetics Excellence, School of Pharmacy, Walailak University, Thasala, Nakhon Si Thammarat, Thailand., See GLL; Department of Pharmacy, School of Health Care Professions, University of San Carlos, Cebu City, Philippines.; Pharmaceutical Research and Drug Development Laboratories, Department of Pharmacy, School of Health Care Professions, University of San Carlos, Cebu City, Philippines.; Pharmaceutical Sciences Division, National Research Council of the Philippines, Taguig City, Philippines., Arce FV Jr; Department of Pharmacy, School of Health Care Professions, University of San Carlos, Cebu City, Philippines.; Pharmaceutical Research and Drug Development Laboratories, Department of Pharmacy, School of Health Care Professions, University of San Carlos, Cebu City, Philippines.; Pharmaceutical Sciences Division, National Research Council of the Philippines, Taguig City, Philippines.
Jazyk:	angličtina
Zdroj:	Acta medica Philippina [Acta Med Philipp] 2024 Mar 15; Vol. 58 (4), pp. 59-71. Date of Electronic Publication: 2024 Mar 15 (Print Publication: 2024).
DOI:	10.47895/amp.vi0.6505
Abstrakt:	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. Competing Interests: All authors declared no conflicts of interest. (© 2024 Acta Medica Philippina.)
Databáze:	MEDLINE
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