ABSTRACT

Drug delivery device (ODD) of controlled and targeted function can ideally

deliver high dose of the therapeutic agent specifically to the diseased cells

with the healthy cells less interfered, thus resulting desired pharmacokinetics

and biodistribution for higher therapeutic effect and fewer side effect. Such

kind of idea for a well-designed administration of therapeutics could be

traced back to Paul Ehrlich, the 1906 Nobel Prize Medicine Laureate, and his

concept of magic bullets. Since then it has been arousing continuous interest

in developing various advanced targeting strategies, among which ligand-

conjugated nanoparticles (including soft nanoparticles such as micelles and

liposomes and solid nanoparticles such as those of biodegradable polymers)

may be the most prospective among various targeted ODD [1-6]. Polymeric

nanoparticles (NPs) are able to dissolve hydrophobic drugs in polymeric matrix,

solving the drug solubility problem aswell as possess the advantages such as high

stability, efficient drug load, sustained drug release, enhanced circulation time in

bloodstream, and active targeting space for cancer cells [7, 8]. A good example

is the polymeric nanoparticle formulation of docetaxel, a potent anticancer drug

approved by FDA for the treatment on a wide spectrum of cancers [9], which has

aroused high attraction recently [10-13]. Among those, targeted formulations

are believed to be capable of distinguishing the cancer cells from normal cells

as well as accumulating in the cancer cells.