ABSTRACT

The endothelium is often regarded as a gatekeeper, playing an

important role in separating blood from the surrounding tissues and

regulating the passage of proteins and other molecules across the

blood vessels. This transport can either be transcellular or paracellu-

lar. The cytoskeletal structures of the endothelial cells play a pivotal

role in regulating this transport. This chapter attempts to discuss in

brief these two types of transport and the components and factors

governing them, an understanding ofwhich is essential for designing

more efficient drugs that can traverse the endothelium more

effectively for increased therapeutic benefits. Novel approaches for

enhancing the penetration of drugs are also reviewed here.