Nanoparticle PEG modification with H-phosphonates

摘要

The present invention provides phosphonate conjugates and methods of preparing the phosphonate conjugates so as to allow, for example, improved methods and compounds for modifying the surface of a nanoparticle to increase in vivo circulation times and targeted delivery performance.

主权项

1. A compound of the formula: wherein each L1, L2, L3 and L4 is independently selected from the group consisting of a bond and a linking group; R1 is selected from the group consisting of a nanoparticle, an attachment component, a targeting agent, a diagnostic agent, a stealth agent, and a tetrapodal presentation component; each R2 is independently selected from the group consisting of a stealth agent, C1-C10 alkyl, a carboxylic acid or ester, a phosphonic acid or ester, a sulfonic acid or ester, and a hydroxy; each R3 and R4 is independently selected from the group consisting of H, a nanoparticle, an attachment component, a targeting agent, a diagnostic agent, and a stealth agent, wherein at least one of R3 or R4 is other than H; and n is an integer of from 0 to 2.