Phospholipid Vesicles for Dermal/Transdermal and Nasal Administration of Active Molecules: The Effect of Surfactants and Alcohols on the Fluidity of Their Lipid Bilayers and Penetration Enhancement Properties.

Hiba Natsheh,Elka Touitou

doi:10.3390/molecules25132959

Hiba Natsheh, Elka Touitou

Open Access

https://doi.org/10.3390/molecules25132959

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Journal: Molecules (Basel, Switzerland)	Publication Date: Jun 27, 2020
Citations: 66	License type: CC BY 4.0

Affiliation: Hebrew University of Jerusalem

Abstract

This is a comprehensive review on the use of phospholipid nanovesicles for dermal/transdermal and nasal drug administration. Phospholipid-based vesicular carriers have been widely investigated for enhanced drug delivery via dermal/transdermal routes. Classic phospholipid vesicles, liposomes, do not penetrate the deep layers of the skin, but remain confined to the upper stratum corneum. The literature describes several approaches with the aim of altering the properties of these vesicles to improve their penetration properties. Transfersomes and ethosomes are the most investigated penetration-enhancing phospholipid nanovesicles, obtained by the incorporation of surfactant edge activators and high concentrations of ethanol, respectively. These two types of vesicles differ in terms of their structure, characteristics, mechanism of action and mode of application on the skin. Edge activators contribute to the deformability and elasticity of transfersomes, enabling them to penetrate through pores much smaller than their own size. The ethanol high concentration in ethosomes generates a soft vesicle by fluidizing the phospholipid bilayers, allowing the vesicle to penetrate deeper into the skin. Glycerosomes and transethosomes, phospholipid vesicles containing glycerol or a mixture of ethanol and edge activators, respectively, are also covered. This review discusses the effects of edge activators, ethanol and glycerol on the phospholipid vesicle, emphasizing the differences between a soft and an elastic nanovesicle, and presents their different preparation methods. To date, these differences have not been comparatively discussed. The review presents a large number of active molecules incorporated in these carriers and investigated in vitro, in vivo or in clinical human tests.

Highlights

IntroductionThe skin is the largest organ of the body and protects it from exogenous materials
The structure of the skin and nasal membrane regulates the need for using enhanced delivery carriers to overcome these permeability barriers.The skin is the largest organ of the body and protects it from exogenous materials
The results indicated an absence of erythema signs following 12, 24 or 48 h of application of the ethosomal carrier

Summary

Introduction

The skin is the largest organ of the body and protects it from exogenous materials. The outermost layer of the skin, the stratum corneum (SC), consists of nonviable, anucleate, keratinized cells and forms an effective barrier to retain water within the body and keeps exogenous compounds out. Lipid molecules in the stratum corneum, mainly ceramides, cholesterol and fatty acids, play a major role in determining. Molecules 2020, 25, 2959 the barrier function of this layer. These lipids are packaged into small organelles to form lamellar granules which fuse in an edge-to-edge manner to form flattened lamellar disks organized in paired bilayers [1]. The main penetration pathway for molecules is the intracellular route through these lipid bilayers of the SC [2]. Viable epidermis and dermis are layered tissues containing a high-water concentration, representing a hydrophilic region for molecules to partition in their way from the SC to the blood vessels

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