纳米晶自稳定Pickering乳液促进葛根素口服吸收的机制研究

Translated title of the contribution: Study on oral absorption mechanisms of puerarin in nanocrystals self-stabilized pickering emulsion

Yan Hua Wang, Xin Ye, Fan Jing Meng, Tao Yi, Ji Fen Zhang

Research output: Contribution to journalArticlepeer-review

3 Citations (Scopus)

Abstract

Nanocrystals self-stabilized Pickering emulsion (NSSPE) is a new kind of emulsion where only nanocrystals of poorly soluble drugs are used as stabilizers. Our previous study showed that NSSPE with Ligusticum chuanxiong oil as the main oil phase can significantly promote oral absorption of puerarin. The present study aimed to explore its absorption mechanism in oral administration. The in vitro dissolution test was carried out to study the effect of NSSPE on release of puerarin. The effects and mechanism of NSSPE on uptake and transport of puerarin across Caco-2 cell were investigated. The results showed that the drug release rate of NSSPE was similar to that of nanocrystals, with their cumulative dissolution of puerarin not affected by pH of releasing mediums, both significantly higher than that of crude material. The uptake of puerarin in NSSPE was concentration-dependent and significantly higher than that of solution or surfactant stabilized emulsion. Genistein and indomethacin, inhibitors of lipid rafts / caveolin, could significantly reduce the uptake of puerarin in NSSPE. Compared with solution, NSSPE and surfactants stabilized emulsion obviously increased transport rate Ka and apparent permeability coefficient Papp of puerarin in AP → BL direction, but there was no significant difference in BL → AP direction. It could be inferred that there were both passive and active transport mechanisms, as well as lipid raft / caveolin mediated endocytosis for absorption of NSSPE. The promoted oral absorption of puerarin in NSSPE was mainly related to the existing nanocrystal form which could promote dissolution, puerarin as well as Ligusticum chuanxiong oil which could promote drug transmembrane transport and inhibit drug efflux. It is the unique structure and composition of the compound NSSPE that promoted the oral absorption of puerarin.

Translated title of the contributionStudy on oral absorption mechanisms of puerarin in nanocrystals self-stabilized pickering emulsion
Original languageChinese (Traditional)
Pages (from-to)2051-2060
Number of pages10
JournalZhongguo Zhongyao Zazhi
Volume46
Issue number8
DOIs
Publication statusPublished - 15 Apr 2021

Keywords

  • Caco-2 cell
  • Dissolution
  • Ligusticum chuanxiong oil
  • Nanocrystals
  • Oral absorption
  • Pickering emulsion
  • Puerarin

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