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Bioanalysis. 2011 Feb;3(3):333-44. doi: 10.4155/bio.10.204.

In vitro and in vivo characterizations of PEGylated liposomal doxorubicin.

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US Food and Drug Administration, Office of Generic Drugs, 7519 Standish Place, Rockville, MD 20855, USA.


One challenge in developing a nanoparticle drug-delivery system is understanding the critical physicochemical properties that may impact its in vivo performance and establishing analytical techniques that can adequately characterize in vitro and in vivo properties. Doxil®/Caelyx®, a PEGylated liposomal doxorubincin (PLD), is one of the leading approved nanoparticle product used in cancer therapy. In this review, we use PLD as an example to illustrate identification of key in vitro and in vivo characteristics. The following characteristics, including liposome composition, state of encapsulated drug, internal environment of liposome, liposome size distribution, lamellarity, grafted polyethylene glycol at the liposome surface, electrical surface potential or charge, and in vitro leakage, are considered critical to demonstrate the supramolecular structure of PLD and ensure consistent drug delivery to cancer tissues. Corresponding analytical techniques are discussed to determine these liposome characteristics. Furthermore, in vivo stability of the PLD can be determined by plasma pharmacokinetics of both free and liposome-encapsulated drug. A better understanding of the critical in vitro and in vivo liposome characteristics together with improvements in analytical technology will enable generic liposome product development and ensure liposome product quality.

[Indexed for MEDLINE]

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