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. Author manuscript; available in PMC: 2013 Aug 1.
Published in final edited form as: Nanomedicine (Lond). 2012 Jun 18;7(10):1507–1519. doi: 10.2217/nnm.12.27

Figure 1. Structure and active sites of fumagillin with their sources of instability indicated (see figure on previous page).

Figure 1

Synthetic strategy for the preparation of Sn-2 fumagillin prodrug and development of site-targeted nanoparticles: saponification of fumagillin with MeOH:water (1:1), 35% NaOH; esterification with PAzPC, DCC/DMAP; preparation of a lipid-thin film from a phospholipid mixture of 98.7 mole% lecithin phosphatidylcholine, 0.15 mole% of αvβ3-ligand-conjugated lipid and 1.12 mole% of fumagillin prodrug; self-assembly by brief sonication and microfluidization, perfluorocarbon, glycerin, pH 6.5, at 20,000 psi for 4 min.

†Hydrodynamic diameter (dynamic light scattering [DLS]): 220 nm; electrophoretic potential: −17 mV; polydispersity index: 0.19.

‡Hydrodynamic diameter (DLS): 280 nm; electrophoretic potential: −22 mV; polydispersity index: 0.25.

Hydrodynamic diameter (DLS): 230 nm; electrophoretic potential: −21 mV; polydispersity index: 0.06.

§Hydrodynamic diameter (DLS): 280 nm; electrophoretic potential: −10 mV; polydispersity index: 0.08.