Gong Wu Rolf F Barth Weilian Yang Robert J Lee Werner Tjarks Marina V Backer and Joseph M Backer

6.1 Introduction 78

6.2 General Requirements for Boron Delivery Agents 78

6.3 Low-Molecular-Weight Delivery Agents 79

6.4 High-Molecular-Weight Boron Delivery Agents 79

6.5 Dendrimer-Related Delivery Agents 80

6.5.1 Properties of Dendrimers 80

6.5.2 Boronated Dendrimers Linked to Monoclonal Antibodies 80

6.5.2.1 Boron Clusters Directly Linked to mAb 80

6.5.2.2 Attachment of Boronated Dendrimers to mAb 81

6.5.3 Boronated Dendrimers Delivered by Receptor Ligands 81

6.5.3.1 Epidermal Growth Factors (EGF) 81

6.5.3.2 Folate Receptor-Targeting Agents 83

6.5.3.3 Vascular Endothelial Growth Factor (VEGF) 83

6.5.4 Other Boronated Dendrimers 85

6.6 Liposomes as Boron Delivery Agents 86

6.6.1 Overview of Liposomes 86

6.6.2 Boron Delivery by Nontargeted Liposomes 86

6.6.2.1 Liposomal Encapsulation of Sodium Borocaptate and Boronophenylalanine 86

6.6.2.2 Liposomal Encapsulation of Other Boranes and Carboranes 87

6.6.3 Boron Delivery by Targeted Liposomes 89

6.6.3.1 Immunoliposomes 89

6.6.3.2 Folate Receptor-Targeted Liposomes 90

6.6.3.3 EGFR-Targeted Liposomes 91

6.7 Boron Delivery by Dextrans 92

Experimental studies described in this report were supported by N.I.H. grants 1 R01 CA098945 (R.F. Barth), 1 R01 CA79758 (W. Tjarks), and Department of Energy grants DE-FG02-98ER62595 (R.F. Barth) and DE-FG-2-02FR83520 (J.M. Backer).

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