ABSTRACT
RUTH DUNCAN / Univers i ty of Keele, Keele, Staffordshire , England
I. Introduct ion 582
A. Definition of Endocytosis 582 B . Quantitation of Endocytosis 588 C. Design of Drug -Ca r r i e r s for Drug Delivery
via Selective Endocytosis 591
II. Mechanisms for Achieving Selective Capture 596
A. Selection According to Subs t ra te Size 596 B. Nonspecific Determinants Regulat ing
Membrane Interact ions 597 C. Cell-Specific Recognition Systems 599
III . Use of Selective Endocytosis for Drug Targe t ing 604
IV. Conclusions 606
References 607
Use of endocytic capture of macromolecules to achieve selective delivery of macromolecular drugs or drug conjugates is not new. It has been 10 years since DeDuve and colleagues [1] first coined the phase "lysosomotropic agents" to describe compounds that accumulate in the lysosomes of cells. Since then, there have been numerous attempts to devise clinically useful drug delivery systems to utilize cell-specific endocytic mechanisms for drug targeting. Although there have not yet been any significant clinical developments, considerable progress has been made in terms of a technology to produce tailor-made drug delivery systems.
