Selective uptake of surface-modified phospholipid vesicles by bone marrow macrophages in vivo

Advanced Drug Carriers Targeting Bone Marrow

“…The uptake of lipid-based nanoparticles by bone marrow phagocytes in rhesus monkeys, rabbits, and hamsters is induced by the incorporation of SA-lipid. PEG-DSPE enhances the uptake of the nanoparticles by bone marrow phagocytes passively by preventing the uptake by hepatic and splenic phagocytes (Sou et al 2007;2010;2011a).…”

“…Sou et al found a liposome formulation that is specifically distributed to bone marrow in rabbits and rhesus monkeys (Sou et al, 2007(Sou et al, , 2010(Sou et al, , 2011a. Figure 2 shows that the bone marrowtargeted liposomes comprise lipids of four kinds: 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC), cholesterol, L-glutamic acid, N-(3-carboxy-1-oxopropyl)-, 1,5-dihexadecyl ester (SAlipid), and poly(ethylene glycol) (PEG).…”

“…Figure 2 shows that the bone marrowtargeted liposomes comprise lipids of four kinds: 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC), cholesterol, L-glutamic acid, N-(3-carboxy-1-oxopropyl)-, 1,5-dihexadecyl ester (SAlipid), and poly(ethylene glycol) (PEG). The SA-lipid component has been identified as the active factor leading to their phagocytosis by bone marrow phagocytes, presumably macrophages in rabbits (Sou et al, 2007). Furthermore, as little as 0.6 mol% of PEG-DSPE depressed hepatic uptake but did not depress the bone marrow uptake.…”

“…Tc by a remote loading method . (B) Gamma camera images of rabbits acquired at 10 minutes and 6 hours after injection of 99m Tc-labeled bone marrow-targeted liposomes (Sou et al, 2007).…”

“…This importance suggests that the phagocytic activity of bone marrow is a potent target of nanoparticle-based drug delivery. In fact, it has been demonstrated that nanoparticles modified with a specific molecule on their surface are distributed selectively into bone marrow tissues (Harris et al 2010;Mann et al, 2011;Moghimi, 1995;Porter et al, 1992;Schettini et al, 2006;Sou et al 2007Sou et al , 2010Sou et al , 2011a. These bone marrow-specific drug carrier systems are expected to improve diagnostic and therapeutic systems to treat hematopoietic disorders.…”