Honokiol/magnolol-loaded self-assembling lecithin-based mixed polymeric micelles (lbMPMs) for improving solubility to enhance oral bioavailability

Hong Liang Lin, Wen Ting Cheng, Ling Chun Chen, Hsiu O. Ho, Shyr Yi Lin, Chien Ming Hsieh

Research output: Contribution to journalArticlepeer-review

Abstract

Objective: This study was intended to utilize lecithin-based mixed polymeric micelles (lbMPMs) for enhancing the solubility and bioavailability of honokiol and magnolol to resolve the hindrance of their extreme hydrophobicity on the clinical applications. Methods: Lecithin was selected to increase the volume of the core of lbMPMs, thereby providing a greater solubilization capacity. A series of amphiphilic polymers (sodium deoxycholate [NaDOC], Cremophor®, and Pluronic® series) were included with lecithin for screening and optimization. Results: After preliminary evaluation and subsequentially optimization, two lbMPMs for- mulations composed of honokiol/magnolol:lecithin:NaDOC (lbMPMs[NaDOC]) and hono- kiol/magnolol:lecithin:PP123 (lbMPMs[PP123]) in respective ratios of 6:2:5 and 1:1:10 were optimally obtained with the mean particle sizes of 80-150 nm, encapsulation efficacy (EEs) of >90%, and drug loading (DL) of >9.0%. These lbMPMs efficiently stabilized honokiol/ magnolol in phosphate-buffered saline (PBS) at room temperature or 4 °C and in fetal bovine serum or PBS at 37 °C. PK study demonstrated that lbMPMs[NaDOC] showed much improvement in enhancing bioavailability than that by lbMPMs[PP123] for both honokiol and magnolol. The absolute bioavailability for honokiol and magnolol after intravenous administration of lbMPMs[NaDOC] exhibited 0.93- and 3.4-fold increases, respectively, compared to that of free honokiol and magnolol. For oral administration with lbMPMs[NaDOC], the absolute bioavailability of honokiol was 4.8%, and the absolute and relative bioavailability of magnolol were 20.1% and 2.9-fold increase, respectively. Conclusion: Overall, honokiol/magnolol loaded in lbMPMs[NaDOC] showed an improve- ment of solubility with suitable physical characteristics leading to enhance honokiol and magnolol bioavailability and facilitating their wider application as therapeutic agents for treating human disorders.

Original languageEnglish
Pages (from-to)651-665
Number of pages15
JournalInternational Journal of Nanomedicine
Volume16
DOIs
Publication statusPublished - 2021

Keywords

  • Honokiol
  • Lecithin
  • Magnolol
  • Mixed polymeric micelles
  • Pluronic
  • Sodium deoxycholate

ASJC Scopus subject areas

  • Biophysics
  • Bioengineering
  • Biomaterials
  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry

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