Abstract

Natural oils are commonly used in topical pharmaceutical formulations as emulsifiers, stabilizers or solubility enhancers. They are presented as safe and inert components, mainly used for formulation purposes. It is confirmed that natural oils can affect the skin penetration of various substances. Fatty acids are mainly responsible for this effect. Current understanding lacks reliable scientific data on penetration of natural oils into the skin and their skin penetration enhancement potential. In the current study, fatty acid content analysis was used to determine the principal fatty acids in soybean, olive, avocado, sea-buckthorn pulp, raspberry seed and coconut oils. Time of flight secondary ion mass spectrometry bioimaging was used to determine the distribution of these fatty acids in human skin ex vivo after application of the oils. Skin penetration enhancement ratios were determined for a perspective antioxidant compound dihydroquercetin. The results demonstrated skin penetration of fatty acids from all oils tested. Only soybean and olive oils significantly increased the skin distribution of dihydroquercetin and can be used as skin penetration enhancers. However, no correlation can be determined between the fatty acids’ composition and skin penetration enhancement using currently available methodological approaches. This indicates that potential chemical penetration enhancement should be evaluated during formulation of topically applied products containing natural oils.

Highlights

  • Natural oils are common ingredients in topical pharmaceutical formulations

  • Coconut oil was mainly composed of saturated short chain C8:0, C10:0, C12:0, C14:0 and lower amounts of C16–C18 fatty acids

  • We found that the application of olive, avocado, soybean, sea-buckthorn pulp, coconut and soybean oils increases the content of fatty acids (FAs) in the ex vivo skin layers

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Summary

Introduction

Natural oils are common ingredients in topical pharmaceutical formulations. They can be categorized into essential and fixed oils [1]. The current study was performed using fixed natural oils. They are presented as “safe agents” and used as emulsifiers, stabilizers or solubility enhancers. Due to favorable technological properties, they can be found in novel nano-scaled dosage forms [2]. Scientific data demonstrate that natural oils can change the skin’s permeability and be utilized as skin permeability enhancers in topical drug formulations [3]

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