SEMINAR ANNOUNCEMENT

PhD Thesis Defence Seminar

Development of a Novel Drug Delivery System
-Lipid Microemulsion of Tributyrin

by

Mr. SU Jie
Department of Pharmacy
National University of Singapore

on

Abstract:

Tributyrin, as a prodrug of butyric acid has been shown to be an effective anti-tumor agent alone or in combination with other chemotherapeutic agents in vitro. As tributyrin exists as a triglyceride-typed oil, it could be formulated as an emulsion to facilitate its delivery. The aim of this project was to develop a lipid microemulsion of tributyrin with affinity to low-density lipoprotein (LDL) or apolipoprotein(s) and evaluate its in vitro cellular activity and in vivo pharmacokinetic properties. The microemulsion monolayer prepared was proved to bind effectively with LDL and apolipoprotein(s) in vitro, which depended on the component of the monolayer as well as the size of the emulsion particles. In vivo, the pharmacokinetic properties of tributyrin were changed after incorporated into emulsion due to uptake via the LDL-receptor mediated pathway. The selective uptake of the emulsion by the cellular LDL receptors was further confirmed by testing the cellular viability in the presence of competing LDL. The tributyrin emulsion was used as a carrier for ATRA, and studies were conducted and proved to enhance the drug effect by reducing the clearance and increasing the in vitro activity.

Keywords: Tributyrin, Lipid microemulsion, Lipoprotein, Pharmacokinetics, Carcinoma cells, ATRA

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