Preparation, characterization, and sonodynamic antitumor effect of the folate receptor targeted FA-EN-β-CD containing...

To improve water solubility, reduce phototoxicity and increase the tumor-targeting ability of hematoporphyrin (Hp) as a sonosensitizer for sonodynamic therapy under ultrasonic conditions, a novel folate receptor (FR)-targeted, folate-conjugated ethylenediamine-β-cyclodextrin (FA-EN-β-CD) containing Hp (FA-EN-β-CD-Hp) was constructed. β-Cyclodextrin containing Hp (β-CD-Hp) was also established as a nontargeted control. The inclusion efficiencies of Hp in FA-EN-β-CD-Hp and β-CD-Hp were determined to be 90.4 ± 2.7% (wt/wt) and 92.5 ± 3.4% (wt/wt), respectively. Growth inhibition rates in HepG-2 cells in vitro were assessed upon ultrasound exposure. The results indicated that the growth inhibition rates of FA-EN-β-CD-Hp, β-CD-Hp, and F-Hp (Hp: 150 μg/ml) reached 96.4 ± 3.6%, 53.4 ± 3.4%, and 48.2 ± 2.8%, respectively. These results indicated that FA-EN-β-CD-Hp is a promising drug delivery system in the field of sonodynamic cancer therapy.