Liposomal Formulation Improves the Bioactivity of Usnic Acid in RAW 264.7 Macrophage Cells Reducing its Toxicity.

IF 2.8 4区医学 Q2 PHARMACOLOGY & PHARMACY

Current drug delivery Pub Date : 2024-01-01 DOI:10.2174/1567201820666230111112415

Marzia Vasarri, Linda Ponti, Donatella Degl'Innocenti, Maria Camilla Bergonzi

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引用次数: 1

Abstract

Background: Reactive oxygen species (ROS) production and oxidative stress may be responsible for the onset of several chronic diseases. Usnic acid (UA) is a natural secondary metabolite of lichens with several healthful bioactivities, including antioxidant properties. However, UA is a hydrophobic compound known for its hepatic toxicity. These aspects limit its therapeutic applications. To overcome these drawbacks and improve the pharmacological use of hydrophobic compounds, nanotechnology is widely used. Therefore, the incorporation of UA into appropriate nanocarriers could enhance the bioactivity of UA by increasing its solubility.

Objective: The aim of this work was to improve the solubility of UA and its bioactivity in the absence of cytotoxicity.

Methods: In this study, UA loaded liposomes (UA-LP) were developed. The formulations were chemically and physically characterized, and an in vitro release study was performed. Free UA and UA-LP were tested on RAW 264.7 murine macrophages in terms of cytotoxicity, intracellular ROS production, and NO release in the absence or presence of pro-oxidant LPS stimulus.

Results: UA-LP showed excellent physical and chemical stability during storage and improved solubility of UA. UA-LP showed an antioxidant effect in the absence of cytotoxicity compared with free UA on LPS-exposed macrophages.

Conclusion: For the first time, liposomal formulation improved the beneficial action of UA in terms of solubility and antioxidant activity.

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脂质体制剂提高Usnic酸在RAW 264.7巨噬细胞中的生物活性，降低其毒性。

背景：活性氧（ROS）的产生和氧化应激可能是几种慢性疾病发病的原因。Usnic acid（UA）是地衣的天然次生代谢产物，具有多种健康的生物活性，包括抗氧化特性。然而，UA是一种疏水性化合物，以其肝毒性而闻名。这些方面限制了其治疗应用。为了克服这些缺点并改善疏水性化合物的药理学用途，纳米技术被广泛使用。因此，将UA掺入合适的纳米载体中可以通过增加其溶解度来增强UA的生物活性。目的：本工作的目的是在没有细胞毒性的情况下提高UA的溶解度及其生物活性。方法：制备UA负载脂质体（UA-LP）。对制剂进行了化学和物理表征，并进行了体外释放研究。在不存在或存在促氧化LPS刺激的情况下，在RAW 264.7小鼠巨噬细胞上测试了游离UA和UA-LP的细胞毒性、细胞内ROS的产生和NO的释放。结果：UA-LP在储存过程中表现出优异的物理和化学稳定性，并提高了UA的溶解度。与游离UA相比，UA-LP对LPS暴露的巨噬细胞在没有细胞毒性的情况下表现出抗氧化作用。结论：脂质体制剂首次在溶解度和抗氧化活性方面改善了UA的有益作用。

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

Current drug delivery PHARMACOLOGY & PHARMACY-

CiteScore

5.10

自引率

4.20%

发文量

170

期刊介绍： Current Drug Delivery aims to publish peer-reviewed articles, research articles, short and in-depth reviews, and drug clinical trials studies in the rapidly developing field of drug delivery. Modern drug research aims to build delivery properties of a drug at the design phase, however in many cases this idea cannot be met and the development of delivery systems becomes as important as the development of the drugs themselves. The journal aims to cover the latest outstanding developments in drug and vaccine delivery employing physical, physico-chemical and chemical methods. The drugs include a wide range of bioactive compounds from simple pharmaceuticals to peptides, proteins, nucleotides, nucleosides and sugars. The journal will also report progress in the fields of transport routes and mechanisms including efflux proteins and multi-drug resistance. The journal is essential for all pharmaceutical scientists involved in drug design, development and delivery.