Liposomal drug development

Several liposome-based drugs have been approved for clinical application [64]. One of the clinically approved liposomes is Doxil, a PEGylated liposome containing doxorubicin (DOX), which is used for the treatment of a number of diseases [65]. As shown in this case, in the field of liposome drug development, PEG is widely used to protect the liposome from recognition by opsonins, thereby reducing liposome clearance. 

Over the past 20 years, our laboratory has played a major role in the development of liposomal systems optimized for the delivery of conventional drugs, almost all of which are encapsulated by pH-gradient techniques. Our initial studies led to the development of several liposomal drug delivery systems in which uptake was driven by the citrate method of generating pH gradients (15,21-23,27,54—58). This was followed by the development of new... 

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Kumi KI, Booth BP. A regulatory view of liposomal drug product characterization. New Drug Development. Marcel Dekker, Inc., 2004. 

In many cases in drug development, the solubility of some leads is extremely low. Fast dissolution rate of many drug delivery systems, for example, particle size reduction, may not be translated into good Gl absorption. The oral absorption of these molecules is usually limited by solubility (VWIImann et al., 2004). In the case of solubility limited absorption, creating supersaturation in the Gl Luids for this type of insoluble drugs is very critical as supersaturation may provide great improvement of oral absorption (Tanno et al., 2004 Shanker, 2005). The techniques to create the so-called supersaturation in the Gl Luids may include microemulsions, emulsions, liposomes, complexations, polymeric micelles, and conventional micelles, which can be found in some chapters in the book. 

Utilizing the concept that the key function of the plasmalemma is to exclude the external environment, liposomes were developed to carry soluble as well as lipophilic drugs. 

In general, the administration route plays an important role on the impact of the therapeutic treatment, and it is chosen according to the kind or purpose of the treatment (local or systemic), toxicity, and accessibility of the diseased area. In this section specific characteristics of other routes of administration that are currently receiving attention will be emphasized and the most recent developments with respect to liposomal drug applications will be presented. 

Among the several drug delivery systems, liposomes - phospholipid nanosized vesicles with a bilayered membrane structure - have drawn a lot of interest as advanced and versatile pharmaceutical carriers for both low and high molecular weight pharmaceuticals. At present, liposomal formulations span multiple areas, from clinical application of the liposomal drugs to the development of various multifunctional liposomal systems to be used in therapy and diagnostics. This chapter provides a brief overview of various liposomal products currently under development at experimental and preclinical level. 

The development of pharmaceutical liposomes is an ever growing research area with an increasing variety of potential applications, and encouraging results ftom early clinical applications and clinical trials of different liposomal drugs. 

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