Liposomal formulations for waterproofing mucosal membranes

IF 4.3 2区医学 Q1 PHARMACOLOGY & PHARMACY

European Journal of Pharmaceutics and Biopharmaceutics Pub Date : 2025-05-26 DOI:10.1016/j.ejpb.2025.114757

Luisa Coderch , Lucia Ricci , Meritxell Martí , Saman Bagherpour , Lluïsa Pérez-García , Cristina Alonso

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Abstract

Liposome formulations consisting of lipids contained in the stratum corneum have been recently demonstrated to decrease the permeability of mucosae. The permeability barrier of the mucosa is dependent on the presence of specific lipids. The main objective of this work is to reinforce the barrier effect of the oral mucosa with liposomal formulations to decrease permeation. Due to the high similarity in composition and structure between lanolin and human stratum corneum lipids, liposomes were formed with lipids contained in the stratum corneum with two kinds of ceramide or with lanolin. Transmembrane water loss of the two formulations was assessed, obtaining an important diminution for both liposomal formulations. Caffeine, lidocaine, ketoprofen and ivermectin and a virus model were tested on mucosa and on modified mucosa to evaluate the liposomal efficacy.

A somewhat consistent permeation pattern was obtained for the different membranes: caffeine > lidocaine > ketoprofen > ivermectin. For all drugs and for the virus model, the most effective formulation was the liposomal formulation, consisting of lipids found in the horny layer of the skin. The effect of the lanolin on the transmembrane water loss is not reflected on the drug permeation. Therefore, it is demonstrated the main role of ceramides in the barrier function for drugs and a virus model. Strengthening the barrier function of the mucosa promotes the prevention or reduction of the permeation of different actives, which could be to extrapolate to harmful actives like viruses, pollutants, toxins, contaminants, etc.

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用于防水粘膜的脂质体配方

由角质层中含有的脂质组成的脂质体制剂最近被证明可以降低粘膜的通透性。粘膜的渗透性屏障依赖于特定脂质的存在。这项工作的主要目的是通过脂质体制剂来增强口腔黏膜的屏障作用，以减少渗透。由于羊毛脂与人角质层脂质在组成和结构上的高度相似，将角质层中的脂质与两种神经酰胺或羊毛脂形成脂质体。评估了两种制剂的跨膜失水，获得了两种脂质体制剂的重要减少。分别在粘膜和修饰粘膜上检测咖啡因、利多卡因、酮洛芬和伊维菌素及病毒模型，评价脂质体的疗效。不同膜的渗透模式是一致的：咖啡因；利多卡因比;ketoprofen祝辞伊维菌素。对于所有药物和病毒模型，最有效的配方是脂质体配方，由皮肤角质层中的脂质组成。羊毛脂对跨膜水分损失的影响不反映在药物渗透上。因此，证明了神经酰胺在药物屏障功能和病毒模型中的主要作用。粘膜屏障功能的增强促进了不同活性物质渗透的阻止或减少，可推断为有害活性物质如病毒、污染物、毒素、污染物等。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

European Journal of Pharmaceutics and Biopharmaceutics 医学-药学

CiteScore

8.80

自引率

4.10%

发文量

211

审稿时长

36 days

期刊介绍： The European Journal of Pharmaceutics and Biopharmaceutics provides a medium for the publication of novel, innovative and hypothesis-driven research from the areas of Pharmaceutics and Biopharmaceutics. Topics covered include for example: Design and development of drug delivery systems for pharmaceuticals and biopharmaceuticals (small molecules, proteins, nucleic acids) Aspects of manufacturing process design Biomedical aspects of drug product design Strategies and formulations for controlled drug transport across biological barriers Physicochemical aspects of drug product development Novel excipients for drug product design Drug delivery and controlled release systems for systemic and local applications Nanomaterials for therapeutic and diagnostic purposes Advanced therapy medicinal products Medical devices supporting a distinct pharmacological effect.