Abstract

Reactive oxygen species (ROS), including superoxide anion, hydrogen peroxide, and hydroxyl radical, can be formed as normal products of aerobic metabolism and can be produced at elevated rates under pathophysiological conditions. Overproduction and/or insufficient removal of ROS result in significant damage to cell structure and functions. In vitro studies showed that antioxidants, when applied directly and at relatively high concentrations to cellular systems, are effective in conferring protection against the damaging actions of ROS, but results from animal and human studies showed that several antioxidants provide only modest benefit and even possible harm. Antioxidants have yet to be rendered into reliable and safe therapies because of their poor solubility, inability to cross membrane barriers, extensive first-pass metabolism, and rapid clearance from cells. There is considerable interest towards the development of drug-delivery systems that would result in the selective delivery of antioxidants to tissues in sufficient concentrations to ameliorate oxidant-induced tissue injuries. Liposomes are biocompatible, biodegradable, and nontoxic artificial phospholipid vesicles that offer the possibility of carrying hydrophilic, hydrophobic, and amphiphilic molecules. This paper focus on the use of liposomes for the delivery of antioxidants in the prevention or treatment of pathological conditions related to oxidative stress.

Highlights

  • Oxidative stress (OS) is defined as an imbalance between the production of reactive oxygen species and antioxidant defenses that can lead to cellular and tissue damage [1,2,3,4,5,6,7,8]

  • Antioxidants have been defined as substances that are able to prevent, delay, or remove oxidative damage to a molecule [36] and may be categorized in the following groups: (i) those aimed at preventing the generation and distribution of reactive oxygen and nitrogen species, (ii) those aimed at reactive metabolite scavenging including the maintenance of effective levels of antioxidants, such as vitamin E, vitamin C, β-carotene, and glutathione as well as the enzyme superoxide dismutase, and (iii) those aimed at free radical repair, the maintenance of effective levels of glutathione [4, 10, 11, 36]

  • The cardiovascular effect of resveratrol can, in turn, be related with its proved capacity to act as a modulator on the metabolism of lipoproteins inhibiting the oxidation of lowdensity lipoproteins (LDLs), and inhibiting either platelet aggregation or proatherogenic eicosanoids production by human platelets and neutrophils

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Summary

Introduction

Oxidative stress (OS) is defined as an imbalance between the production of reactive oxygen species and antioxidant defenses that can lead to cellular and tissue damage [1,2,3,4,5,6,7,8]. A potential pharmacological strategy in preventing or treating oxidant-induced cellular and tissue damage involves the use of appropriate antioxidants. Antioxidants are substances which are able to prevent, delay, or remove oxidative damage to a molecule [4, 9,10,11] Their efficacy is hindered with challenges such as poor solubility, inability to cross cellmembrane barriers, extensive first-pass metabolism, and rapid clearance of antioxidants from cells [12, 13]. Encapsulation of enzymatic antioxidants (superoxide dismutase and catalase) or nonenzymatic antioxidants (glutathione, Nacetylcysteine, CoQ10, curcumin, resveratrol, α-tocopherol, and γ-tocopherol) in liposomes improves their therapeutic potential against oxidant-induced tissue injuries, because liposomes apparently facilitate intracellular delivery and prolong the retention time of entrapped agents inside the cell

Oxidative Stress and the Antioxidant Defense System
Antioxidant Therapy
Liposomes
Liposomes as an Antioxidant Delivery System
Liposomal N-Acetylcysteine
Other Liposomal Antioxidants
Liposomes Containing More than One Antioxidant
Findings
Concluding Remarks
Full Text
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