A Review of Liposomes as a Drug Delivery System: Current Status of Approved Products, Regulatory Environments, and Future Perspectives

Abstract

Liposomes have been considered promising and versatile drug vesicles. Compared with traditional drug delivery systems, liposomes exhibit better properties, including site-targeting, sustained or controlled release, protection of drugs from degradation and clearance, superior therapeutic effects, and lower toxic side effects. Given these merits, several liposomal drug products have been successfully approved and used in clinics over the last couple of decades. In this review, the liposomal drug products approved by the U.S. Food and Drug Administration (FDA) and European Medicines Agency (EMA) are discussed. Based on the published approval package in the FDA and European public assessment report (EPAR) in EMA, the critical chemistry information and mature pharmaceutical technologies applied in the marketed liposomal products, including the lipid excipient, manufacturing methods, nanosizing technique, drug loading methods, as well as critical quality attributions (CQAs) of products, are introduced. Additionally, the current regulatory guidance and future perspectives related to liposomal products are summarized. This knowledge can be used for research and development of the liposomal drug candidates under various pipelines, including the laboratory bench, pilot plant, and commercial manufacturing.

Magnetoliposomes Containing Multicore Nanoparticles and a New Antitumor Thienopyridine Compound with Potential Application in Chemo/Thermotherapy

“…The size of a typical phospholipid bilayer is of 4.5 nm, similar to that of the liposome-like structure composed of ODA and DPPC in magnetoliposomes [ 36 ]. Considering that FRET only occurs at a donor–acceptor distances below 10 nm and that proflavine molecules were located at the flower-shaped structures surface, while the hydrophobic dye Nile Red was located within the bilayer of the liposome-like structures, this donor–acceptor distance supports the formation of a bilayer around the flower-shaped NPs and, consequently, the synthesis of magnetoliposomes [ 15 , 21 ].…”

Critical Analysis and Quality Assessment of Nanomedicines and Nanocarriers in Clinical Trials: Three Years of Activity at the Clinical Trials Office

“…Liposomes are versatile drug delivery systems, developed for various routes of administration, that have the advantage of protecting the active substance enclosed in the vesicles, prolonging its half-life in the bloodstream and enhancing bioavailability. Several liposomal products have been authorized over the course of the last two decades by the European Medicines Agency (EMA) and the Food and Drug Administration (FDA) [ 28 ]. The distribution reported in Figure 4 shows that the vast majority of nanomedicines is tested in the therapeutic area of cancer, followed by eye disease, blood and lymphatic disease, virus disease, and respiratory tract disease therapeutic areas.…”

Antiproliferative and Antimicrobial Effects of Rosmarinus officinalis L. Loaded Liposomes

“…Nano-phytomedicines represent a category of drug formulations that result from a combination of nanotechnology and herbal medicine [25]. They are modern formulations that are meant to overcome the disadvantages of vegetal medicinal products or the extracts that are obtained on their basis, which present promising in vivo and in vitro biological activities, but show at the same time significant limitations, such as poor absorption, low bioavailability, low solubility, and rapid clearance [25][26][27]. Nanotechnology has proven to be an effective tool that can be used to effectively eradicate these limitations [25,26].…”

“…Nanotechnology has proven to be an effective tool that can be used to effectively eradicate these limitations [25,26]. Liposomes are artificial vesicles of small size and spherical shape, obtained from cholesterol and non-toxic phospholipids [27,28]. Such preparations exist in the case of R. officinalis and are used to achieve more efficacy in overcoming the limitations of its phytoformulations (related to bioavailability and solubility) and to enhance its therapeutical activities [29,30].…”