Honokiol Loaded Mixed Micelles Fororal Delivery Using Novel F127 and TPGS as Carriers
10.14148/j.issn.1672-0482.2021.0376
- VernacularTitle:负载和厚朴酚F127/TPGS二元混合胶束的制备及促进其口服生物利用度研究
- Author:
Xiao-Qing CHEN
1
,
2
;
Ping-Gang DING
;
Ru-Ling XU
;
Hui-Min DONG
;
Zhi-Chao QI
;
Jian-Ming JU
Author Information
1. 南京中医药大学附属中西医结合医院,江苏南京 210028
2. 江苏省中医药研究院中药质量和代谢组研究室,江苏南京 210028
- Keywords:
honokiol;
F127;
TPGS;
micelles;
Caco-2 cell;
oral bioavailability;
anti-tumor
- From:
Journal of Nanjing University of Traditional Chinese Medicine
2021;37(3):376-382
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE The purpose of this research was to develop a self-assembled micelle using biocompatible copoly-mers Pluronic F127 (F127) and Vitamin E d-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS) to enhance the oral bio-availability and anti-cancer efficiency of honokiol (HK). METHODS The optimized prescription honokiol micelle (HK-M) was prepared by an ethanol solvent evaporation method. HK-M was characterized by transmission electron microscopy(TEM) and HPLC. The dialysis bag method was used to assesse the cumulative amount of HK released from the HK-M. Caco-2 cells were applied to measure the permeability of HK-M. The bioavailability and in vivo anti-tumor effect were also evaluated. RE-SULTS At the ratio of 4:1 (F127:TPGS), the HK-M was transparent and colourless with a small size (23.28 ± 2.01)nm and a spherical shape. The apparent solubility of HK in HK-M was dramatically increased to 4.76 mg/mL, suggesting that HK-M had good stability. Furthermore, encapsulation in micelles led to a sustained release of HK. HK-M enhances HK's per-meability across Caco-2 cell monolayer. Compared with free HK, there was a 1.17-fold increase in the relative oral bioavail-ability for HK-M. Moreover, HK-M achieved a higher inhibition rate on tumor volume (35.17％) than HK group (14.86％). CONCLUSION These findings present an oral HK micelle formulation containing F127 and TPGS, with improved solubility,increased oral bioavailability, and enhanced anti-cancer activity.
