Design of liposomes as drug delivery system for therapeutic applications

Guimaraes, D; Cavaco-Paulo, A; Nogueira, E

Abstract

Liposomes are spherical vesicles consisting of one or more concentric phospholipid bilayers enclosing an aqueous core. Being both nontoxic and biodegradable, liposomes represent a powerful delivery system for several drugs. They have improved the therapeutic efficacy of drugs through stabilizing compounds, overcoming obstacles to cellular and tissue uptake and increasing drug biodistribution to target sites in vivo, while minimizing systemic toxicity. This review offers an overview of liposomes, thought the exploration of their key fundamentals. Initially, the main design aspects to obtain a successful liposomal formulation were addressed, following the techniques for liposome production and drug loading. Before application, liposomes required an extensive characterization to assurance in vitro and in vivo performance. Thus, several properties to characterize liposomes were explored, such as size, polydispersity index, zeta potential, shape, lamellarity, phase behavior, encapsulation efficiency, and in vitro drug release. Topics related with liposomal functionalization and effective targeting strategies were also addressed, as well as stability and some limitations of liposomes. Finally, this review intends to explore the current market liposomes used as a drug delivery system in different therapeutic applications.

Keywords: Liposomes; Drug delivery; Liposome production; Liposome characterization; Market liposomes

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Liposome System

Liposomes, spherical vesicles composed of one or more phospholipid bilayers, are at the forefront of drug delivery systems, revolutionizing the way therapeutics are administered. These versatile nanocarriers can encapsulate both hydrophilic and hydrophobic drugs, protecting them from degradation and enhancing their stability. The biocompatible and biodegradable nature of liposomes minimizes toxicity and adverse immune responses, making them suitable for a wide range of applications, including cancer therapy, infectious diseases, and vaccine delivery. Liposomes can be engineered to target specific tissues or cells by modifying their surface with ligands, antibodies, or peptides, ensuring precise delivery of the therapeutic agent and reducing off-target effects. Additionally, the release profiles of drugs can be finely tuned by adjusting the composition of the lipid bilayers, allowing for controlled and sustained release. This capability not only improves the therapeutic efficacy but also reduces the frequency of dosing, enhancing patient compliance. Recent advancements have also seen the development of stimuli-responsive liposomes that release their payload in response to specific triggers such as pH, temperature, or enzymes, further enhancing their effectiveness. Overall, liposomes represent a powerful and flexible platform for improving the delivery and performance of a wide array of drugs, marking a significant advancement in medical treatment.