The potential and limitations of targeted delivery of anticancer agent
s with colloidal particulate carriers is the subject of this contribut
ion, Because over the years liposomes have gained the most attention a
s carrier system in the category of colloidal carrier systems, this pa
per focuses on the utility of the liposomal system for tumor targeting
. It is imperative that an intended therapeutic application of liposom
es should be well matched with the liposome behavior in vivo. Therefor
e, the in vivo fate of the first-generation liposomes and the more rec
ently developed second-generation liposomes (surface-modified liposome
s such as the immunoliposomes and long-circulating liposomes) is analy
zed in terms of accessibility of target sites, time-, and site-control
led drug release and potential target sites for rational targeted deli
very are discussed. A few examples of areas in cancer chemotherapy, wi
th a strong rationale for the use of liposomes, are given, It is concl
uded that, although several options are available on the drawing board
, issues such as tumor cell heterogeneity, access to the target site,
shedding of antigens, and target site-specific release of the liposome
-associated drug need to be addressed early in the development process
.