Preparation, characterization, and sonodynamic antitumor effect of the folate receptor targeted FA‐EN‐β‐CD containing hematoporphyrin in vitro

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.