Loading of curcumin into macrophages using lipid-based nanoparticles.
Curcumin (1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione, Cm) is a natural compound which possesses antioxidant, anti-inflammatory and anti-tumor ability. Here, phospholipid vesicles or lipid-nanospheres embedding Cm (CmVe or CmLn) were formulated to deliver Cm into tissue macrophages through intravenous injection. Cm could be solubilized in hydrophobic regions of these particles to form nanoparticle dispersions, and these formulations showed ability to scavenge reactive oxygen species as antioxidants in dispersions. At 6h after intravenous injection in rats via the tail vein (2mg Cm/kg bw), confocal microscopic observations of tissue sections showed that Cm was massively distributed in cells assumed as macrophages into the bone marrow and spleen. Taken together, these results indicate that the lipid-based nanoparticulates provide improved intravenous delivery of Cm to tissues macrophages, specifically bone marrow and splenic macrophages in present formulation, which has therapeutic potential as an antioxidant and anti-inflammatory.
Advanced Research Institute for Science and Engineering, Waseda University, Tokyo 169-8555, Japan.
Keitaro
K
Sou
Shunsuke
S
Inenaga
Shinji
S
Takeoka
Eishun
E
Tsuchida
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D000975:Antioxidants / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D001853:Bone Marrow / Q000378:metabolism; D002626:Chemistry, Pharmaceutical; D003474:Curcumin / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism*; D004337:Drug Carriers; D004339:Drug Compounding; D057927:Hydrophobic and Hydrophilic Interactions; D007275:Injections, Intravenous; D008264:Macrophages / Q000378:metabolism*; D008297:Male; D018613:Microscopy, Confocal; D053758:Nanoparticles; D010743:Phospholipids / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D017382:Reactive Oxygen Species / Q000378:metabolism; D012995:Solubility; D013024:Soybean Oil / Q000737:chemistry*; D013154:Spleen / Q000378:metabolism; D013678:Technology, Pharmaceutical / Q000379:methods; D013997:Time Factors
D000893:Anti-Inflammatory Agents; D000975:Antioxidants; D004337:Drug Carriers; D010743:Phospholipids; D017382:Reactive Oxygen Species; D013024:Soybean Oil; D003474:Curcumin