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用于透皮给药的改性磷脂囊泡凝胶:甘油和/或乙醇对其脂质双分子层流动性及渗透特性的影响

Modified Phospholipid Vesicular Gel for Transdermal Drug Delivery: The Influence of Glycerin and/or Ethanol on Their Lipid Bilayer Fluidity and Penetration Characteristics.

作者信息

Abdallah Marwa H, Shahien Mona M, El-Horany Hemat El-Sayed, Ahmed Enas Haridy

机构信息

Department of Pharmaceutics, College of Pharmacy, University of Ha'il, Ha'il 81442, Saudi Arabia.

Department of Pediatrics, College of Medicine, University of Ha'il, Ha'il 81422, Saudi Arabia.

出版信息

Gels. 2025 May 13;11(5):358. doi: 10.3390/gels11050358.

DOI:10.3390/gels11050358
PMID:40422378
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12110836/
Abstract

This review explores the enhanced transdermal therapy of several skin disorders with the application of carriers comprising phospholipid vesicular gel systems. Topical drug delivery has several advantages compared to other administration methods, including enhanced patient compliance, the avoidance of the first-pass impact associated with oral administration, and the elimination of the need for repeated doses. Nonetheless, the skin barrier obstructs the penetration of drugs, hence affecting its therapeutic efficacy. Carriers with phospholipid soft vesicles comprise a novel strategy used to augment drug delivery into the skin and boost therapeutic efficacy. These vesicles encompass chemicals that possess the ability to fluidize phospholipid bilayers, producing a pliable vesicle that facilitates penetration into the deeper layers of the skin. Phospholipid-based vesicular carriers have been extensively studied for improved drug delivery through dermal and transdermal pathways. Traditional liposomes are limited to the stratum corneum of the skin and do not penetrate the deeper layers. Ethosomes, glycerosomes, and glycethosomes are nanovesicular systems composed of ethanol, glycerol, or a combination of ethanol and glycerol, respectively. Their composition produce pliable vesicles by fluidizing the phospholipid bilayers, facilitating deeper penetration into the skin. This article examines the impact of ethanol and glycerol on phospholipid vesicles, and outlines their respective manufacturing techniques. Thus far, these discrepancies have not been analyzed comparatively. The review details several active compounds integrated into these nanovesicular gel systems and examined through in vitro, in vivo, or clinical human trials involving compositions with various active molecules for the treatment of various dermatological conditions.

摘要

本综述探讨了应用包含磷脂囊泡凝胶系统的载体对几种皮肤疾病进行增强透皮治疗的情况。与其他给药方法相比,局部给药具有多个优点,包括提高患者依从性、避免口服给药相关的首过效应以及无需重复给药。尽管如此,皮肤屏障会阻碍药物渗透,从而影响其治疗效果。含有磷脂软囊泡的载体是一种用于增强药物透皮递送并提高治疗效果的新策略。这些囊泡包含能够使磷脂双层流化的化学物质,形成一种柔韧的囊泡,便于渗透到皮肤深层。基于磷脂的囊泡载体已被广泛研究用于通过真皮和透皮途径改善药物递送。传统脂质体局限于皮肤角质层,无法渗透到更深层。醇质体、甘油质体和糖基醇质体分别是由乙醇、甘油或乙醇与甘油的组合组成的纳米囊泡系统。它们的组成通过使磷脂双层流化产生柔韧的囊泡,便于更深地渗透到皮肤中。本文研究了乙醇和甘油对磷脂囊泡的影响,并概述了它们各自的制备技术。到目前为止,尚未对这些差异进行比较分析。该综述详细介绍了整合到这些纳米囊泡凝胶系统中的几种活性化合物,并通过体外、体内或涉及含有各种活性分子的组合物用于治疗各种皮肤病况的临床人体试验进行了研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f97c/12110836/9517bd1da141/gels-11-00358-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f97c/12110836/3b0cbe04b134/gels-11-00358-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f97c/12110836/26afc1222291/gels-11-00358-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f97c/12110836/a42bfe0dcba3/gels-11-00358-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f97c/12110836/8091cfd93188/gels-11-00358-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f97c/12110836/87cc783fee27/gels-11-00358-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f97c/12110836/fb94843a95ca/gels-11-00358-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f97c/12110836/9517bd1da141/gels-11-00358-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f97c/12110836/3b0cbe04b134/gels-11-00358-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f97c/12110836/26afc1222291/gels-11-00358-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f97c/12110836/a42bfe0dcba3/gels-11-00358-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f97c/12110836/8091cfd93188/gels-11-00358-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f97c/12110836/87cc783fee27/gels-11-00358-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f97c/12110836/fb94843a95ca/gels-11-00358-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f97c/12110836/9517bd1da141/gels-11-00358-g007.jpg

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本文引用的文献

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Development and Evaluation of Nano-Vesicular Emulsion-Based Gel as a Promising Approach for Dermal Atorvastatin Delivery Against Inflammation.基于纳米囊泡乳液的凝胶的研制与评价:一种有前途的经皮递送阿托伐他汀治疗炎症的方法。
Int J Nanomedicine. 2024 Nov 7;19:11415-11432. doi: 10.2147/IJN.S477001. eCollection 2024.
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Preparation of Paeonol Ethosomes by Microfluidic Technology Combined with Gaussians and Evaluation of Biological Activity by Zebrafish.微流控技术结合高斯法制备丹皮酚脂质体及其斑马鱼生物活性评价
ACS Omega. 2024 Oct 21;9(44):44425-44435. doi: 10.1021/acsomega.4c05830. eCollection 2024 Nov 5.
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Synthesis of vitamin D3 loaded ethosomes gel to cure chronic immune-mediated inflammatory skin disease: physical characterization, in vitro and ex vivo studies.
载维生素 D3 的醇质体凝胶的合成治疗慢性免疫介导的炎症性皮肤病:物理特性、体外和离体研究。
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Development of Glycerosomal pH Triggered In Situ Gelling System to Ameliorate the Nasal Delivery of Sulpiride for Pediatric Psychosis.用于改善舒必利经鼻给药治疗小儿精神病的甘油体pH触发原位凝胶系统的研发
Gels. 2024 Sep 23;10(9):608. doi: 10.3390/gels10090608.
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Microfluidic technologies for lipid vesicle generation.微流控技术用于脂质体的生成。
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Plant-Based Nanovesicular Gel Formulations Applied to Skin for Ameliorating the Anti-Inflammatory Efficiency.应用于皮肤以提高抗炎效率的植物基纳米囊泡凝胶制剂。
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Formulation Development of Meloxicam Binary Ethosomal Hydrogel for Topical Delivery: In Vitro and In Vivo Assessment.用于局部给药的美洛昔康二元醇质体水凝胶的制剂开发:体外和体内评估
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