Highmolecularweight Boron Delivery Agents

High-molecular-weight (HMW) delivery agents usually contain a stable boron group or cluster linked via a hydrolytically stable bond to a tumor-targeting moiety, such as monoclonal antibodies (mAbs) or LMW receptor-targeting ligands. Examples of these include epidermal growth factor

FIGURE 6.1 Structures of two compounds used clinically for boron neutron capture therapy (BNCT), 4-dihy-droxyborylphenylalanine or boronophenylalanine (BPA, 1), and disodium undecahydro-closo-dodecaborate or sodium borocaptate (BSH, 2) and the isocyanato polyhedral borane (3), which has been used to heavily boronate dendrimers.

BH B

FIGURE 6.1 Structures of two compounds used clinically for boron neutron capture therapy (BNCT), 4-dihy-droxyborylphenylalanine or boronophenylalanine (BPA, 1), and disodium undecahydro-closo-dodecaborate or sodium borocaptate (BSH, 2) and the isocyanato polyhedral borane (3), which has been used to heavily boronate dendrimers.

(EGF) and the mAb cetuximab (IMC-C225) to target the EGF receptor (EGFR) or its mutant isoform EGFRvIII, which are overexpressed in a variety of malignant tumors including gliomas, and squamous-cell carcinomas of the head and neck.32 Agents that are to be administered systemi-cally should be water soluble (WS), but lipophilicity is important to cross the blood-brain barrier (BBB) and diffuse within the brain and the tumor. There should be a favorable differential in boron concentrations between tumor and normal brain, thereby enhancing their tumor specificity. Their amphiphilic character is not as crucial for LMW agents that target-specific biological transport systems and/or are incorporated into nanovehicles such as liposomes. Molecular weight also is an important factor because it determines the rate of diffusion both within the brain and the tumor. Detailed reviews of the state-of-the-art of compound development for BNCT have been published.33,34 In this review, we will focus on boron containing macromolecules and liposomes as delivery agents for BNCT, and how they can be most effectively administered.

Diabetes Sustenance

Diabetes Sustenance

Get All The Support And Guidance You Need To Be A Success At Dealing With Diabetes The Healthy Way. This Book Is One Of The Most Valuable Resources In The World When It Comes To Learning How Nutritional Supplements Can Control Sugar Levels.

Get My Free Ebook


Post a comment