Nanoparticulate platinum(II) anticancer drug: synthesis and characterization of amphiphilic cyclotriphosphazene-platinum(II) conjugates.
Novel cyclotriphosphazene-platinum(II) conjugates were prepared by hydrolysis and platination of the amphiphilic cyclotriphosphazenes grafted with equimolar hydrophilic methoxy-poly(ethylene glycol) (MPEG) and hydrophobic oligopeptide. These macromolecular conjugates were found to form stable nanoparticles with a mean diameter of approximately 90-200 nm depending on the hydrophobicity of the conjugated (diamine)platinum moieties. The nanoparticulate platinum(II) conjugates have shown temperature and concentration dependent particle sizes. However, the particle sizes of the conjugates were found to decrease to a certain size as the solution concentration was decreased but remained stable even at 10 microM, which is enough for systemic delivery by injection. The conjugates exhibited lower in vitro cytotoxicity than cisplatin but reasonably good activity against selected human tumor cell lines.
Yu
Ji Young
JY
Division of Nano Science, Department of Chemistry, Ewha Womans University, Daehyun-Dong 11-1, Seodaemun-Ku, Seoul 120-750, Republic of Korea.
Jun
Yong Joo
YJ
Jang
Soo Hyun
SH
Lee
Hwa Jeong
HJ
Sohn
Youn Soo
YS
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D009682:Magnetic Resonance Spectroscopy; D036103:Nanotechnology; D009944:Organoplatinum Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D010316:Particle Size; D010984:Platinum / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry
D000970:Antineoplastic Agents; D009944:Organoplatinum Compounds; D011092:Polyethylene Glycols; D010984:Platinum