Preparation of PEGylated liposomes incorporating lipophilic lomeguatrib derivatives for the sensitization of chemo-resistant gliomas.

@article{Signorell2018PreparationOP,
  title={Preparation of PEGylated liposomes incorporating lipophilic lomeguatrib derivatives for the sensitization of chemo-resistant gliomas.},
  author={Rea Deborah Signorell and Alexandros Papachristodoulou and Jiawen Xiao and Bianca Arpagaus and Tommaso Casalini and Joanes Grandjean and Jana Thamm and Frank Steiniger and Paola Luciani and Davide Brambilla and Beat Werner and Ernst Martin and Michael Weller and Patrick Roth and Jean-Christophe Leroux},
  journal={International journal of pharmaceutics},
  year={2018},
  volume={536 1},
  pages={
          388-396
        }
}
Liposomal delivery is a well-established approach to increase the therapeutic index of drugs, mainly in the field of cancer chemotherapy. Here, we report the preparation and characterization of a new liposomal formulation of a derivative of lomeguatrib, a potent O6-methylguanine-DNA methyltransferase (MGMT) inactivator. The drug had been tested in clinical trials to revert chemoresistance, but was associated with a low therapeutic index. A series of lomeguatrib conjugates with distinct alkyl… CONTINUE READING