Xin Guo

University of the Pacific
Trans-2-aminocyclohexanol-based lipids as pH-sensitive conformational switches in liposomes for drug delivery

It was a great pleasure to present the progress of our TEVA project, “trans‐2‐Aminocyclohexanol-based Lipids as pH‐Sensitive Conformational Switches in Liposomes for Drug Delivery” at the ACS meeting. Over the past three years, we have designed and prepared a variety of trans-2-aminocyclohexanol (TACH) lipids as molecular switches of liposomes. Our NMR, fluorometric and EM studies have demonstrated that the drop of pH triggers the conformational flip of the trans-2-aminocyclohexanol lipids, which in turn destabilizes liposome membranes. For pharmaceutical applications, PEGylated liposomes consisting of the TACH lipids (fliposomes) enhanced the anticancer effect of methotrexate and TACH lipids enhanced the gene transfection of cationic lipoplexes by up to 100-fold in cultured cells.

We enjoyed the presentations of the other TEVA recipients and the discussions with scientists from TEVA and from ACS at the symposium. We thank TEVA and ACS, who supported this exciting project, which opens many doors for the TACH lipids and liposomes to benefit modern medicine.