Receptor-targeted nanocarriers for therapeutic delivery to cancer

Figures & data

Figure 1. A schematic diagram representing the accumulation of nanocarriers in tumor sites by passive or active targeting. Both targeted nanocarriers and non-targeted nanocarriers reach tumors selectively through the leaky vasculature in the tumors. Upon arrival at tumor sites, targeted nanocarriers can bind to the target tumor cells or enter the cells via receptor mediated endocytosis.

Figure 2. Commonly used nanocarriers.

Table I. Commonly used targeting ligands for targeted nanocarriers.

Name	Targeting ligand	Receptor	References
Small molecules	Folic acid	Folate receptor	Zhao et al. (2008), Low et al. (2008)
	Galactose	Asialoglycoprotein receptor (ASGPR)	Wu et al. (2002)
Peptides	RGD	avβ3 integrin receptor	Vives et al. (2008), Garanger et al. (2006)
	ATWLPPR (VEGF peptide)	VEGF receptor	Di Benedetto et al. (2008)
Aptamers	Pegaptanib	VEGF receptor	Ng et al. (2006)
Proteins	Transferrin	Transferrin receptor	Qian et al. (2002), Daniels et al. (2006)
	Luteinizing hormone releasing hormone (LHRH)	LHRH receptor	Leuschner et al. (2006)
Antibodies	Herceptin (Trastuzumab)	Her2/neu (Breast cancer)	Kirpotin et al. (1997), Park et al. (2002)
	Rituxan (Rituximab)	CD20 antigen (B-cell non-Hodgkin lymphoma)	Lapalombella et al. (2008)
	CD19 antibody	CD19 antigen (human B-cell lymphoma)	Lopes de Menezes et al. (1998)

Table II. Examples of novel ligands for targeted nanocarriers.

Name	Targeting ligand	Receptor	Reference
Peptides	LHDH	avβ3 integrin	Norberto and Kakar (2009), Sundaram et al. (2009)
	SP5-2 (TDSILRSYDWTY)	Non-small cell lung cancer	Chang et al. (2009)
	NGR peptide	Angiogenic endothelial cell	Negussie et al. (2010), Pastorino et al. (2003)
	iRGD (CRGDK/RGPD/EC)	Both avβ3 integrin and neuropilin-1 on tumour vessels	Sugahara et al. (2010)
Aptamers	A10 RNA aptamer	Prostate-specific membrane antigen	Farokhzad et al. (2006)
	Sgc8c DNA aptamer	Protein tyrosine kinase 7 (PTK7) receptor	Huang et al. (2009)
Antibodies	Monoclonal antibody A7	Colorectal carcinoma	Toma et al. (2005)
	Transferrin antibody	Transferrin receptor	Gosk et al. (2004)
	DI17E6	avβ3 integrin receptor	Wagner et al. (2010)
	2C5 antibody	nuclesome (NS)-restricted activity	Torchilin et al. (2003)
	5D4 antibody	Prostate cancer	Sawant et al. (2008)
	Anti- HER2 scFv	ErbB2 receptor	Laginha et al. (2008)
	Anti-VCAM-1	Vascular cell adhesion molecule-1 (VCAM-1) on activated endothelial cells	Voinea et al. (2005)
	Anti-CD22 scFv	CD22 antigen B-cell lymphomas	Loomis et al. (2010)
Other targeting molecules	Affibody	EGFR receptor	Beuttler et al. (2009)
	Avimer	Human extracellular receptor	Silverman et al. (2005)
	Nanobody	Human tumour-associated carcinoembryonic antigen	Cortez-Retamozo et al. (2004)

Figure 3. Schematic illustration of the basic intracellular targets including endo-lysosomal compartment, mitochondrion, cytoplasm, nucleus for drug, gene and oligo deliveries.

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