Tianmin Zhu
Zhejiang Hisun pharmaceutical Co., Ltd., P R China
Title: A prodrug approach for drug delivery of everolimus
Biography
Biography: Tianmin Zhu
Abstract
A novel water-soluble everolimus prodrug, glutathione-everolimus, was designed and synthesized by introducing an endogenous tripeptide with an acetyl as a linker. The improvement in water solubility allows the conjugate to be developed into an injectable drug. The results of biological evaluation in vitro and in vivo suggest that the prodrug is more effective and long acting than everolimus. Meanwhile, the pharmacokinetics study in vivo (both in mice and machine) confirmed that the delivery of everolimus through the injection of the prodrug overcome the low bioavailability of oral everolimus.
