Department of Pharmaceutical Technology, Institute of Pharmacy, Friedrich-Schiller University Jena, Jena, Germany.
Macromol Biosci. 2012 Jul;12(7):986-98. doi: 10.1002/mabi.201200017. Epub 2012 May 30.
Limitations of PEG in drug delivery have been reported from clinical trials. PEtOx (0.4-40 kDa) as alternative is synthesized by a living, microwave-assisted polymerization, and is directly compared to PEG of similar molar mass regarding cytotoxicity and hemocompatibility. In short-term treatments, both types of polymers are well tolerated even at high concentrations. Moderate concentration and molar mass dependent cytotoxic effects occurred only after long-term incubation at concentrations higher than therapeutic doses. PEtOx possesses not only an easy route of synthesis and beneficial physicochemical characteristics such as low viscosity and high stability, which are advantageous over PEG, but additionally in vitro toxicology comparable to PEG.
临床研究报道了 PEG 在药物输送方面的局限性。PEtOx（0.4-40 kDa）作为替代品，通过活的微波辅助聚合合成，并在细胞毒性和血液相容性方面与类似摩尔质量的 PEG 进行直接比较。在短期治疗中，即使在高浓度下，这两种类型的聚合物也都能很好地耐受。只有在长期孵育浓度高于治疗剂量时，才会出现中等浓度和摩尔质量依赖性的细胞毒性作用。PEtOx 不仅具有合成路线简单和低粘度、高稳定性等有益的物理化学特性，这些特性优于 PEG，而且体外毒理学与 PEG 相当。
