Preparation of tributyrin emulsion and characterization of the binding of the emulsion particles to low-density lipoprotein in vitro.
Tributyrin has been shown to be an effective antitumor agent alone or in combination with other chemotherapeutic agents in vitro. Because tributyrin exists as an oil, it could be formulated as an emulsion to facilitate its delivery. The aim of this study was to develop a tributyrin emulsion with affinity to low-density lipoprotein (LDL). The tributyrin emulsion was prepared by sonication. Sizes of the different fractions of the emulsion particles separated by ultracentrifugation were determined. Cholesterol was found to decrease the particle size slightly because of its condensing effect. The emulsion monolayer prepared was proved to bind effectively with LDL in vitro. The dissociation constant and binding maximum to LDL of the emulsion fraction 1 with smaller particle sizes were 0.1236 microM and 0.4140 mmol/mol, and that of the fraction 2 with larger particle sizes were 0.0635 microM and 0.2654 mmol/mol, respectively. These results suggested that the binding ability of tributyrin emulsion depended on the component of the monolayer as well as the size of the emulsion particles. The potential pharmaceutical applications of this tributyrin emulsion are discussed.
Su
Jie
J
Department of Pharmacy, National University of Singapore, 18 Science Drive 4, Singapore 117543.
Ho
Paul C
PC
D008078:Cholesterol, LDL / Q000737:chemistry / Q000378:metabolism*; D004655:Emulsions; D010316:Particle Size; D011485:Protein Binding / Q000502:physiology; D014280:Triglycerides / Q000138:chemical synthesis* / Q000378:metabolism*
D008078:Cholesterol, LDL; D004655:Emulsions; D014280:Triglycerides; C005830:tributyrin