Title:Assessment of Amentoflavone Loaded Sub-Micron Particle Preparation using
Supercritical Antisolvent for its Antitumor Activity
Volume: 19
Issue: 1
Author(s): Shulei Duan, Jing fu Jia, Biao Hong, Jie Zhou, Yi Zhang, Fahuan Ge*Ming Li
Affiliation:
- School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, PR China
Keywords:
Amentoflavone, zein, sub-micron particles, supercritical antisolvent, antitumor activity, drug release.
Abstract: Introduction: The amentoflavone (AMF) loaded polymeric sub-micron particles were
prepared using supercritical antisolvent (SAS) technology with the aim of improving the anticancer
activity of AMF.
Methods: Zein and phospholipid mixtures composed of Hydrogenated Phosphatidylcholine (HPC)
and egg lecithin (EPC) were used as carrier materials and, the effects of carrier composition on the
product morphology and drug release behavior were investigated. When the mass ratio of Zein/HPC/
EPC was 7/2/1, the AMF loaded particles were spherical shape and sub-micron sized around
400 nm, with a drug load of 4.3±0.3 w% and entrapment efficacy of 87.8±1.8%. The in vitro drug
release assay showed that adding EPC in the wall materials could improve the dispersion stability
of the released AMF in an aqueous medium, and the introduction of HPC could accelerate the drug
release speed.
Results: MTT assay demonstrated that AMF-loaded micron particles have an improved inhibitory
effect on A375 cells, whose IC50 was 37.39μg/ml, compared with that of free AMF(130.2μg/ml).
Conclusion: It proved that the AMF loaded sub-micron particles prepared by SAS were a prospective
strategy to improve the antitumor activity of AMF, and possibly promote the clinical use of
AMF preparations.