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Liposomes - Successful Carrier Systems for Targeted Drug Delivery

Liposomes are colloidal, vesicular structures based on (phospho) lipid bilayers. Their characteristics depend on the manufacturing protocol and choice of bilayer components. They can be as small as 20nm and as large as 10Mm in diameter. The liposomes can be unilamellar (meaning only one bilayer surrounds an aqueous core) or multilamellar (several bilayers concentrically oriented around an aqueous core). Moreover, the choice of bilayer components determines the rigidity (or fluidity) and the charge of the bilayer. For example, saturated phospholipids with long acyl chains such as dipalmitoylphosphatidylcholine, form a rigid, rather impermeable bilayer structure, while the unsaturated phosphatidylcholine species from natural sources (egg or soy bean phosphatidylcholine) give much more permeable and less stable bilayers. The introduction of positively or negatively charged lipids provides the liposomes a surface charge. Liposome surfaces can be readily modified. By attaching polyethylene glycol (PEG) units to the bilayer, the circulation time of liposomes in the bloodstream is dramatically increased. Alternatively, homing molecules can be attached to liposome bilayers to make these structures target site specific. Size, lamellarity, bilayer rigidity, charge and bilayer surface modifications all determine the fate of liposomes on the shelf and in vivo. Over the years the behaviour of liposomes has been investigated in much detail (1,2) and algorithms can be used to help the pharmaceutical formulation scientist in selecting the proper liposome type.

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By Daan Crommelin and Gert Bos of OctoPlus and Gert Storm of the Utrecht Institute for Pharmaceutical Sciences, The Netherlands Professor Daan Crommelin PhD is a Professor at the Department of Pharmaceutics at Utrecht University. He is Scientific Director of the Utrecht Institute for Pharmaceutical Sciences (UIPS) and Adjunct Professor at the Department of Pharmaceutics and Pharmaceutical Chemistry at the University of Utah.
His research focuses on advanced drug delivery and drug targeting strategies. He has published over 240 articles in peer-reviewed journals. Daan is also Chief Scientific Officer of OctoPlus, a Leiden-based company specialising in the development of pharmaceutical product formulations and advanced drug delivery systems..

Gert Bos PhD obtained his masters degree in Chemical Technology in 1993 at the University of Twente. He subsequently earned his PhD in the field of Biomaterial Science from the same university.
He currently combines a postdoctoral research and development function at the faculty of Pharmaceutical Sciences of the Utrecht University (UIPS) and a business development position at OctoPlus in the Netherlands.

Professor Gert Storm PhD obtained is PhD in 1987 on a thesis entitled, Liposomes as delivery system for doxorubicin in cancer therapy. He was appointed as Professor (Drug Targeting Chair) at the University of Utrecht in 2000, and in 1999 as Adjunct Professor at the department of pharmaceutics at the Royal School of Pharmacy, Copenhagen, Denmark. His research interests are in the field of biopharmaceutics and drug targeting.
He published over 180 original articles, reviews and book chapters. He is a member of the editorial (advisory) board of the J. Drug Targeting, J. Liposome Research, S.T.P. Pharma Sciences and Eur. J. Pharm. Sciences, and is Special Features Editor of Pharm. Research. He acts as a Consultant to a number of pharmaceutical companies.

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Gert Bos
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Daan Crommelin
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Gert Storm
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