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新型液晶（LC）制剂的配方，具有（PL）提取物的皮肤渗透增强能力，及其对 HaCaT 细胞的评估。

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

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei körút 98, 4032 Debrecen, Hungary.

Doctoral School of Pharmaceutical Sciences, University of Debrecen, Nagyerdei körút 98, 4032 Debrecen, Hungary.

出版信息

Molecules. 2021 Feb 15;26(4):1023. doi: 10.3390/molecules26041023.

DOI:10.3390/molecules26041023
PMID:33672029
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7919469/
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 (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 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.

摘要

活性氧物种的暴露很容易导致严重疾病，如皮肤过度增生性疾病或皮肤癌。草药提取物被广泛用作不同成分的抗氧化剂来源。抗氧化治疗在炎症条件下的重要性增加了。创新制剂可用于提高这些植物药的效果。 （PL）的生物活性化合物具有不同的作用，如抗炎、抗氧化和杀菌的药理作用。本研究的目的是制定新的液晶（LC）组合物，以保护提取物免受水解，并提高其效果。由于安全性是药物制剂的一个重要方面，因此使用各种体外方法在 HaCaT 细胞上评估了应用赋形剂和混合物的生物学特性。根据先前的毒性筛选评估，选择了三种表面活性剂（Gelucire 44/14、Labrasol 和 Lauroglycol 90）用于配方。使用 Franz 扩散室装置评估 PL 从 PL-LC 系统中的溶解速率。使用 2,2-二苯基-1-苦基肼（DPPH）和丙二醛（MDA）评估评估了 PL-LC 系统的抗氧化性能。我们的结果表明，这些组合物使用非传统的快速渗透途径来输送药物，因为应用的渗透增强剂可逆地改变了外层角质层的屏障特性。这些赋形剂可以是安全且高度耐受的，因此可以改善患者的体验并促进其用药依从性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8420/7919469/1fa19ff261e2/molecules-26-01023-g009a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8420/7919469/33f9e46645e5/molecules-26-01023-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8420/7919469/1a5bdf37c837/molecules-26-01023-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8420/7919469/e496b545b5a9/molecules-26-01023-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8420/7919469/f85077e885bf/molecules-26-01023-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8420/7919469/a5cd33264619/molecules-26-01023-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8420/7919469/1e4e0440dc3d/molecules-26-01023-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8420/7919469/ece0f5216ac1/molecules-26-01023-g007a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8420/7919469/57e9b09aa05f/molecules-26-01023-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8420/7919469/1fa19ff261e2/molecules-26-01023-g009a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8420/7919469/33f9e46645e5/molecules-26-01023-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8420/7919469/1a5bdf37c837/molecules-26-01023-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8420/7919469/e496b545b5a9/molecules-26-01023-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8420/7919469/f85077e885bf/molecules-26-01023-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8420/7919469/a5cd33264619/molecules-26-01023-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8420/7919469/1e4e0440dc3d/molecules-26-01023-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8420/7919469/ece0f5216ac1/molecules-26-01023-g007a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8420/7919469/57e9b09aa05f/molecules-26-01023-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8420/7919469/1fa19ff261e2/molecules-26-01023-g009a.jpg

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