Abstract
Genipin has attracted much attention for its hepatoprotective, anti-inflammatory, and neuroprotection activities. However, poor water solubility and active chemical properties limit its application in food and pharmaceutical industries. This article aimed to develop a lipid-based microemulsion delivery system to improve the stability and bioavailability of genipin. The excipients for a genipin microemulsion (GME) preparation were screened and a pseudo-ternary phase diagram was established. The droplet size (DS), zeta potential (ZP), polydispersity index (PDI), physical and simulated gastrointestinal digestion stability, and in vitro drug release properties were characterized. Finally, the effect of the microemulsion on its cellular uptake by Caco-2 cells and the protective effect on PC12 cells were investigated. The prepared GME had a transparent appearance with a DS of 16.17 ± 0.27 nm, ZP of −8.11 ± 0.77 mV, and PDI of 0.183 ± 0.013. It exhibited good temperature, pH, ionic strength, and simulated gastrointestinal digestion stability. The in vitro release and cellular uptake data showed that the GME had a lower release rate and better bioavailability compared with that of free genipin. Interestingly, the GME showed a significantly better protective effect against amyloid-β (Aβ1-42)-induced PC12 cell cytotoxicity than that of the unencapsulated genipin. These findings suggest that the lipid-based microemulsion delivery system could serve as a promising approach to improve the application of genipin.
Highlights
medium chain triglycerides (MCT), isopropyl myristate (IPM), and ethyl oleate (EO) were chosen as the oil phases for the construction of the pseudo-ternary phase diagrams
The results indicated that the genipin microemulsion (GME) had small droplets with homogeneous dispersibility
The results indicated that the GMEs had good stability under different pH, temperature, and ionic strength environments
Summary
Its ripe fruit has been used as yellow natural colorants and in Chinese traditional medicine for thousands of years [1,2]. As an important Chinese traditional medicine, G. jasminoides’. Fruit has been used to treat many different diseases due to its hepatoprotective, cholagogic, sedative, anti-hypertension, hemostasis, and detumescence properties [2]. Geniposide, an iridoid glucoside, is one of the major bioactive compounds in this medicinal plant and its content is used as the quality control marker of crude G. jasminoides fruit in Chinese. Multiple pharmacological activities of geniposide and its aglycone genipin have been reported, including its hepatoprotective effect [3], hypoglycemic [4] and antiinflammatory activity [5], protection of cerebral ischemic injury [6], neuroprotection [7], and anti-depressant effects [8]. Geniposide has been widely considered as the main active component, some studies suggested that genipin was a more active ingredient [9–11]
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