Abstract: In the past decades, many materials have been studied as carriers for targeted drug delivery. However, there is a need for utilizable and selective carrier materials with few side effects.  Here, the magnetic Ganoderma Lucidum Spores (mGLS) as a highly efficient targeted drug delivery carrier were explored. Then the regulatable targeted drug delivery system was verified by loading and releasing of the 5-Fluorouracil (5-FU). The results showed that the maximum of the loaded 5-FU reached 250.23 mg·g?1 in the mGLS. The cumulative release of the 5-FU for the drug delivery system could reach 80.11% and 67.14% in the PBS and HCl after 48 h, respectively. In addition, this system showed the good pharmacokinetic properties in vivo. After 12 h, the blood concentration in the 5-FU@mGLS group kept at 5.3 μg·mL?1 and was four times higher than that in the 5-FU group. In summary, the GLS as a natural microscale core-shell structures appears the striking application in carrier material for oral drug delivery.

Key words: Magnetic Ganoderma Lucidum Spores (mGLS), sustained release, 5-FU, drug delivery