Improving cellular uptake and synergetic anti-tumor effects of magnolol and Brucea javanica oil through self-microemulsion

Abstract

Objective

Magnolol (MG) and Brucea javanica (L.) Merr. oil (BJO) possess synergetic anti-tumor effects, but have poor water solubility and stability, which results in low oral bioavailability.

Significance

The MG loaded self-microemulsion drug delivery system (MG-SMDDS) with BJO as oil phase component was utilized to improve the cellular uptake and synergetic anti-tumor effects.

Methods

Compatibility study and pseudoternary phase diagram (PTPD) were respectively employed to screen for the composition and proportion of oil phase in the formulation. Central composite design-effect surface method was applied to optimize proportion of each formulation condition. The droplet size, ζ-potential, colloid stability, encapsulation rate (ER) and in vitro dissolution rate of MG-SMDDS were evaluated. Furthermore, cellular uptake and cytotoxicity of the microemulsion on HepG2 cells were assessed.

Results

The optimal composition of MG-SMDDS was: MG (9.09%), castor oil (7.40%), BJO (2.47%), Cremophor EL 35 (54.04%) and 1, 2-propanediol (27.01%). The MG-SMDDS exhibited satisfactory droplet size, ζ-potential, colloid stability and ER, as well as faster dissolution rate than free MG. More importantly, SMEDDS containing BJO could enhance the cellular uptake and cytotoxicity of free BJO and free MG on tumor cells.

Conclusions

The BJO self-microemulsion delivery technique can provide an idea for design of oral delivery vehicles based on BJO.

Keywords:

• Magnolol
• Brucea javanica oil
• self micro-emulsifying system
• dissolution rate
• anti-tumor

Acknowledgement

The authors have acknowledged the published paper (Zhang, H., Wei, S., Zhang, Y., Pan, A., Adu-Frimpong, M., Sun, C., & Qi, G. (2022). Improving cellular uptake and bioavailability of periplocy­marin-linoleic acid prodrug by combining PEGylated liposome. Drug delivery, 29(1), 2491–2497)

Disclosure statement

No potential conflict of interest was reported by the author(s).

Additional information

Funding

This work was supported by Natural Science Foundation of China [Grant No.82104104], School-level research projects of Yancheng Institute of Technology [grant no. xjr2020018].