Emulsifiers' composition modulates venous irritation of the nanoemulsions as a lipophilic and venous irritant drug delivery system.
In this study, a nanoemulsion (NE) system was investigated for intravenous delivery of lipophilic and venous irritant drugs. NEs were prepared to deliver diallyl trisulfide (DT) for systemic therapy of bacterial and fungal infection, egg phospholipid was chosen as the main emulsifier, and two co-emulsifiers were also incorporated, including Poloxamer 188 (P188) and Solutol HS 15 (S15). Soybean oil was used as the dispersed phases, forming stable DT NEs with small particle sizes. The venous irritation of DT NEs was evaluated by in vitro human umbilical cord endothelial cells (CRL 1730) compatibility model with the intracellular adenosine triphosphate (ATP) and guanosine triphosphate (GTP) concentrations as the indices. The intracellular ATP and GTP reduction changed with the incorporation of a variety of co-emulsifiers, which varied in a free DT concentration-dependent manner. It was deduced that the free DT concentrations of NEs containing co-emulsifiers were determined by the partition coefficient of DT between oil and surfactant buffer solution. In conclusion, NE was an appropriate delivery system for lipophilic and venous irritant drug, and optimization of the composition of emulsifiers was an effective method to alleviate the venous irritation of DT NEs.
Mao
Chengwen
C
College of Life Science and Technology, Huazhong University of Science and Technology, Wuhan, People's Republic of China.
Wan
Jiangling
J
Chen
Huabing
H
Xu
Huibi
H
Yang
Xiangliang
X
D000255:Adenosine Triphosphate / Q000378:metabolism; D001808:Blood Vessels / Q000473:pathology*; D002478:Cells, Cultured; D002851:Chromatography, High Pressure Liquid; D016503:Drug Delivery Systems; D004563:Electrochemistry; D004655:Emulsions / Q000737:chemistry* / Q000633:toxicity*; D042783:Endothelial Cells / Q000187:drug effects; D006160:Guanosine Triphosphate / Q000378:metabolism; D006801:Humans; D007509:Irritants; D008055:Lipids / Q000737:chemistry; D053758:Nanoparticles; D009821:Oils / Q000737:chemistry; D010316:Particle Size; D020442:Poloxamer; D011092:Polyethylene Glycols / Q000737:chemistry; D013229:Stearic Acids / Q000737:chemistry; D013501:Surface-Active Agents
D004655:Emulsions; D007509:Irritants; D008055:Lipids; D009821:Oils; D013229:Stearic Acids; D013501:Surface-Active Agents; D020442:Poloxamer; D011092:Polyethylene Glycols; C067028:Solutol HS 15; D006160:Guanosine Triphosphate; D000255:Adenosine Triphosphate