The composition of oil phase modulates venous irritation of lipid emulsion-loaded diallyl trisulfide.

INTRODUCTION

In this study, a nanoemulsion system (LE) was investigated for intravenous delivery of diallyl trisulfide (DT), which was a lipophilic and venous irritant drug for systemic therapy of bacterial and fungal infection.

METHODS

Egg phospholipid was chosen as the only emulsifier, soybean oil, medium chain triglyceride (MCT), and olive oil were used as the oil phases, forming stable DT LEs (o/w) with small particle sizes. The venous irritation of DT LEs was evaluated by in vitro human umbilical cord endothelial cells (HUV-EC CRL 1730) tolerance model with the intracellular ATP and GTP concentrations as the indices.

RESULTS

The intracellular ATP and GTP reduction changed with the incorporation of a variety of oils, which were strongly related with the free DT concentration of DT LEs.

DISCUSSION: It was deduced that the free DT concentrations of LEs made of various oils depended on the particle sizes of the DT LEs. In conclusion, the oil phases modulated the free DT concentrations by forming DT LEs with different particle sizes, and optimization of the oil phase was an effective method to alleviate the venous irritation of DT LEs.