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Review
. 2017 Mar 27;9(2):12.
doi: 10.3390/pharmaceutics9020012.

Liposomal Formulations in Clinical Use: An Updated Review

Upendra Bulbake  1 , Sindhu Doppalapudi  2 , Nagavendra Kommineni  3 , Wahid Khan  4
Affiliations
Review

Liposomal Formulations in Clinical Use: An Updated Review

Upendra Bulbake et al. Pharmaceutics. .

Abstract

Liposomes are the first nano drug delivery systems that have been successfully translated into real-time clinical applications. These closed bilayer phospholipid vesicles have witnessed many technical advances in recent years since their first development in 1965. Delivery of therapeutics by liposomes alters their biodistribution profile, which further enhances the therapeutic index of various drugs. Extensive research is being carried out using these nano drug delivery systems in diverse areas including the delivery of anti-cancer, anti-fungal, anti-inflammatory drugs and therapeutic genes. The significant contribution of liposomes as drug delivery systems in the healthcare sector is known by many clinical products, e.g., Doxil®, Ambisome®, DepoDur™, etc. This review provides a detailed update on liposomal technologies e.g., DepoFoam™ Technology, Stealth technology, etc., the formulation aspects of clinically used products and ongoing clinical trials on liposomes.

Keywords: clinical trials; drug delivery; liposome technology; liposomes; marketed products; nanotechnology; therapeutics.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Schematic representation showing the advantages of formulating drugs in liposomes.
Figure 2
Figure 2
Therapeutic areas covered by liposome-based products.
Figure 3
Figure 3
Pharmacokinetics of PEGylated liposomes and Non-PEGylated liposomes.
Figure 4
Figure 4
Spheroid and granular structure of a DepoFoam™ particle.
Figure 5
Figure 5
Remote loading approach of DOX into the intraliposomal aqueous phase. Liposomes are prepared at the desired concentration of ammonium sulphate. The gradient was formed by removing the ammonium sulphate from the external liposome medium. Intraliposomal NH4+ dissociates into NH3 and H+, NH3 escape from the liposome and H+ is retained in the liposome water phase. DOX HCl is added to the liposome dispersion at a temperature above the phase transition of the liposomal lipids. DOX, a cationic amphiphile, is present in equilibrium between an ionised and a non-ionised form. The latter form commutes across the liposome bilayer and becomes ionised once exposed to the internal H+ environment, and forms a salt with the SO42− anions.
Figure 6
Figure 6
Liposomes present under different phases of clinical trial investigation.
See this image and copyright information in PMC

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