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. Author manuscript; available in PMC: 2008 Aug 10.
Published in final edited form as: Adv Drug Deliv Rev. 2007 Jun 28;59(8):748–758. doi: 10.1016/j.addr.2007.06.008

Table 1.

Major well characterized endocytic targeting ligands for macromolecular drug delivery.

Targeting Agent Internalization Mechanism Delivery Vehicle Therapeutic Cargo
Folic Acid Caveolin-Assist1ed Ligand Alone

  1. Thymidylate Synthase Inhibitor[62]

  2. Photoactive Compound[63]
Low-Density Lipoprotein Caveolin-Assisted Nanoparticles Photodynamic Therapy Agent[64]
Cholera Toxin B Lipid Raft Associated Liposomes Saliva-Binding Region[65]
Mannose-6- Phasphate Clathrin-Dependent RME Human Serum Albumin Antifibrotic Drug[66]
Transferrin Clathrin-Dependent RME

  1. PEGylated Liposomes[67]

  2. Polymeric Chitosan Vesicles[68]

 Doxorubicin
Riboflavin Clathrin-Dependent RME Bovine Serum Albumin[69] N/A
Arg-Gly-Asp (RGD) Cell Adhesion Molecule (CAM) Directed Biocompatible Polymer Radionuclides [70]
ICAM-1 Antibody CAM Directed Nanocarriers Lysosomal Enzyme[20]
Nicotinic Acid Clathrin-Dependent RME Biotinylated Polylysine DNA[71]