Thiele Carolin, Loretz Brigitta, Lehr Claus-Michael
Department of Drug Delivery, Helmholtz-Institute for Pharmaceutical Research Saarland, Helmholtz-Centre for Infection Research Braunschweig, Saarland University, Campus, Building E8.1, 66123, Saarbrücken, Germany.
Department of Pharmacy, Saarland University, Saarbrücken, Germany.
Drug Deliv Transl Res. 2017 Apr;7(2):252-258. doi: 10.1007/s13346-016-0333-8.
Regioselective oxidation of water-soluble starch and conversion with alkyl diamines resulted in defined cationic starch derivatives. Those were assessed in their potential for polyplex formation, biocompatibility, and transfection efficacy. The new polymers have the advantage of being biodegradable, being not cytotoxic at rather high concentrations (LC > 400 μg/ml) for C2 substitution, and reach transfection efficiencies comparable to commercial transfection reagents. The polymer with the highest transfection efficacy is a C12 substituted polymer (degree of substitution = 30 %) at N/P 3. The LC value of that highly modified polymer is still one order of magnitude lower than that of PEI 25 kDa.
水溶性淀粉的区域选择性氧化以及与烷基二胺的转化产生了特定的阳离子淀粉衍生物。对这些衍生物在形成多聚体的潜力、生物相容性和转染效率方面进行了评估。这些新型聚合物具有可生物降解的优点，对于C2取代，在相当高的浓度（LC>400μg/ml）下无细胞毒性，并且转染效率与市售转染试剂相当。转染效率最高的聚合物是N/P为3时的C12取代聚合物（取代度=30%）。那种高度修饰聚合物的LC值仍比25kDa的聚乙烯亚胺低一个数量级。
