Cationic polyaspartamides including poly-α,β-[N'-(2-aminoethyl)-L-aspartamide] (PAEA), poly-α,β-[N'-(4- aminobutyl)-L-aspartamide] (PABA), poly-α,β-[N'-(6-aminohexyl)-L-aspartamide] (PAHA), poly-α,β-[N'-(5-amino- 3-azapentyl)-L-aspartamide] (PAAPA) and poly-α,β-[N'-(8-amino-3,6-diazaoctyl)-L-aspartamide] (PADAOA) were synthesized from polysuccinimide. Their properties were evaluated by ^1H NMR, IR, GPC, fluorescence measurement and in vitro cytotoxicity assays. The molecular weights per primary amine charge group of PAEA(1) (Mn= 2229), PAAPA and PADAOA are 212, 279, and 226. Polyaspartamides including PAEA(1), PAAPA, PADAOA and low molecular weight PAHA are markedly less toxic than poly(ethyleneimine) and poly(L-lysine), however, PABA and higher molecular weight PAHA are slightly less toxic than poly(L-lysine). Cell cytotoxicity of PAHA was seen to decrease with increasing molecular weight of PAHA, due to water solubility reduction. The negatively charged plasmid DNA has been found to be completely neutralized and complexed by the cationic polyaspartamides at an N/P ratio of 5 : 1 to 10 : 1, forming self-assembled polyplexes via ionic interactions. These polyaspartamide/DNA complexes possess stable zeta potentials and mean particle diameters of about 180 nm for PAEA (1)/DNA and PAAPA/DNA complexes and 280 nm for PADAOA/DNA complexes.
Magnetic resonance imaging (MRI) is a clinical diagnostic modality, which has become popular in hospitals around the world. Approximately 30% of MRI exams include the use of contrast agents. The research progress of the paramagnetic resonance imaging contrast agents was described briefly. Three important approaches in the soluble paramagnetic resonance imaging contrast agents design including nonionic, tissue-specific and macromolecular contrast agents were investigated. In addition, the problems in the research and development in future were discussed.
Diethylenetriaminepentaacetic dianhydride was co-polymerized with dodecyl ester and benzyl ester of lysine,and octodecyl ester and benzyl ester of lysine respectively to give two terpolymers. These two terpolymer ligands were reacted with GdCl 3 to afford amphiphilic oligomers of Gd(Ⅲ) complexes. These new ligands and Gd(Ⅲ) complexes were characterized by IR, 1H NMR and elemental analysis. The oligomeric complexes show a higher relaxivity as compared to that of Gd(DTPA) which is widely used in clinic diagnoses. The Gd(Ⅲ) complex derived from octodecyl ester demonstrated liver-selective enhancement for MR imaging of Wistar rat. The ratios of signal to noise ( S/N ) in the proton intensity imaging were enhanced,respectively,by 15%,27%,and 36% at the time of 5,30 and 45 min after injection of this complex.