Formulation of Novel Liquid Crystal (LC) Formulations with Skin-Permeation-Enhancing Abilities of Plantago lanceolata (PL) Extract and Their Assessment on HaCaT Cells.

Dóra Kósa,Judit Váradi,Ildikó Bácskay,Miklós Vecsernyés,Sándor Gonda,Pálma Fehér,Gábor Vasas,Zoltán Ujhelyi,Ágota Pető,Ferenc Fenyvesi

doi:10.3390/molecules26041023

Abstract

Exposure to reactive oxygen species can easily result in serious diseases, such as hyperproliferative skin disorders or skin cancer. Herbal extracts are widely used as antioxidant sources in different compositions. The importance of antioxidant therapy in inflammatory conditions has increased. Innovative formulations can be used to improve the effects of these phytopharmacons. The bioactive compounds of Plantago lanceolata (PL) possess different effects, such as anti-inflammatory, antioxidant, and bactericidal pharmacological effects. The objective of this study was to formulate novel liquid crystal (LC) compositions to protect Plantago lanceolata extract from hydrolysis and to improve its effect. Since safety is an important aspect of pharmaceutical formulations, the biological properties of applied excipients and blends were evaluated using assorted in vitro methods on HaCaT cells. According to the antecedent toxicity screening evaluation, three surfactants were selected (Gelucire 44/14, Labrasol, and Lauroglycol 90) for the formulation. The dissolution rate of PL from the PL-LC systems was evaluated using a Franz diffusion chamber apparatus. The antioxidant properties of the PL-LC systems were evaluated with 2,2-diphenyl-1-picrylhydrazyl (DPPH) and malondialdehyde (MDA) assessments. Our results suggest that these compositions use a nontraditional, rapid-permeation pathway for the delivery of drugs, as the applied penetration enhancers reversibly alter the barrier properties of the outer stratum corneum. These excipients can be safe and highly tolerable thus, they could improve the patient’s experience and promote adherence.

Highlights

Human skin is our main protective organ against multiple environmental insults, such as reactive oxygen species (ROS) [1]
Our results suggest that these compositions use a nontraditional, rapid-permeation pathway for the delivery of drugs, as the applied penetration enhancers reversibly alter the barrier properties of the outer stratum corneum
Besides all Plantago lanceolata (PL)-liquid crystal (LC) compositions being able to decrease MDA levels compared to the untreated and unformulated PL extract controls, we found that PL-LC composition I significantly decreased the MDA level

Summary

Introduction

Human skin is our main protective organ against multiple environmental insults, such as reactive oxygen species (ROS) [1]. The exact method of the pathogenic effect of ROS is not fully understood, their role in serious diseases, such as hyperproliferative skin disorders or skin cancer, were clearly concluded [2]. Exposure to UV rays with 200–280 nm wavelength (UV-C) could result in frequent generation of reactive oxygen species [4]. Due to the increasing ordinary UV-C exposure, source reduction seems to be an impossible mission. According to this conclusion, robust and effective antioxidant therapy seems to be the only vital tool in this contest

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