Cellular Uptake and Metabolism of Soluplus-based Scopoletin Micelles in Caco-2 Cells
- Author:
Ying-Chun ZENG
1
Author Information
- Publication Type:Journal Article
- Keywords: Caco-2 cells; LC-MS/MS; Micelle; Scopoletin; Soluplus
- From: Chinese Pharmaceutical Journal 2018;53(23):2029-2033
- CountryChina
- Language:Chinese
- Abstract: OBJECTIVE: To develop an analytical method for the quantification of scopoletin (Sco) and investigate the cellular uptake and metabolism of polyvinylcaprolactam-polyvinyl acetate-polyethylene glycol (soluplus)-based Sco micelles (Sco-Ms) in Caco-2 cells, as well as exploring the possible mechanisms involved in the oral absorption of Sco-Ms.METHODS: Combined with enzymatic hydrolysis for pretreatment, a liquid chromatography-electrospray ionization-tandem mass spectrometric (LC-MS/MS) method was developed for the quantification of Sco and its corresponding metabolite. Then, cellular uptake efficiency and metabolic rate of Sco were calculated.RESULTS: This method was proven to be linear over the concentration range of 5-1 000 ng•mL-1. Cellular uptake of Sco-Ms increased significantly compared with that of free Sco at various time points. Meanwhile, Sco-Ms inhibited the enzymatic degradation of Sco. Sco-Ms were primarily internalized into enterocytes via macropinocytosis and clathrin-dependent pathways.CONCLUSION: Enhanced cellular uptake and decreased metabolic rate are pivotal mechanisms by which Sco-Ms promotes oral absorption of Sco.
