Lecture 17 Drug targeting.pdf

文档介绍：Molecular Principles of Biomaterials Spring 2003
Lecture 17: Drug targeting
Last time: Intracellular drug delivery
Today: Drug targeting
Reading: . Wickham, ‘Ligand-directed targeting of genes to the site of disease,’ Nat. Med. 9(1)
135-139 (2003)
Drug Targeting
Applications of drug targeting1
ƒ delivery of toxic drugs to tumors
o highly toxic drugs that are too dangerous to deliver in a systemic manner
ƒ . potent radionuclides, cellular toxins
ƒ allow smaller doses to be used
ƒ delivery of DNA vectors to target cell type for ic corrections
ƒ targeting to vasculature
o cancer treatment
ƒ target to neovasculature forming around tumors2
o
pulmonary, cardiovascular, and inflammatory diseases
ƒ targeting to pathogen-infected cells
o
infected cells undergo changes in cell-surface molecule expression
ƒ crossing blood-brain barrier3
Application Cellular target Molecular target Targeting ligand Ligand type
Anti-cancer therapy Various tumor cells Folate receptor Folate Protein ligand for target
EGF receptor EGF receptor preferentially
expressed on target
cells
Neovascular tissue B-FN (fibronectin anti-B-FN antibody antibody against
isoform) fibronectin isoform only
expressed during
embryonic development
and in aggressive
tumors
Anti-cancer Endothelial cells E-selectin sialyl Lew