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Optimizing Druggability through Liposomal Formulations: New Approaches to an Old Concept

DOI: 10.5402/2012/738432

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Abstract:

Developing innovative delivery strategies remains an ongoing task to improve both efficacy and safety of drug-based therapy. Nanomedicine is now a promising field of investigation, rising high expectancies for treating various diseases such as malignancies. Putting drugs into liposome is an old story that started in the late 1960s. Because of the near-total biocompatibility of their lipidic bilayer, liposomes are less concerned with the safety issue related to the possible long-term accumulation in the body of most nanoobjects currently developed in nanomedicine. Additionally, novel techniques and recent efforts to achieve better stability (e.g., through sheddable coating), combined with a higher selectivity towards target cells (e.g., by anchoring monoclonal antibodies or incorporating phage fusion protein), make new liposomal drugs an attractive and challenging opportunity to improve clinical outcome in a variety of disease. This review covers the physicochemistry of liposomes and the recent technical improvements in the preparation of liposome-encapsulated drugs in regard to the scientific and medical stakes. 1. Introduction Liposomes are nearly spherical, microparticulate, multilamellar or unilamellar bilayer vesicles made from lipids alternating with aqueous sections [1]. Their biochemical structure is very much similar to that of normal human cellular membranes. They also bear resemblance to micelles, although there are some key differences between them (Figure 1). They were first discovered by Dr Alec D. Bangham in 1961 at Babraham University of Cambridge [2]. Figure 1: Aspects of liposomes and micelles. A representation of the steric organization of a liposome (left) and a micelle (right). Liposomes have a lipidic bilayer (bottom) whereas micelles are constructed only by one lipid layer that has its apolar section turned inwards while its polar heads interact with the environment. As a result, the enclosed space in micelles is much more confined to that available in liposomes. Because of the aforementioned similarity to natural components as well as their ability to enfold various substances, scientists hypothesized that liposomes complied with the requirements of an almost ideal drug carrier system. So, for the last 40 years liposomes have been studied thoroughly and are actually celebrated for their biological and technological advantages as effective carriers for biologically active substances, both in vitro and in vivo. Naturally, they continue to constitute a field of intense research and are considered to be the best drug carrier system

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