Preparation of hydroxy genkwanin nanosuspensions and their enhanced antitumor efficacy against breast cancer.

Preparation of hydroxy genkwanin nanosuspensions and their enhanced antitumor efficacy against breast cancer. Drug Deliv. 2020 Dec;27(1):816-824 Authors: Ao H, Li Y, Li H, Wang Y, Han M, Guo Y, Shi R, Yue F, Wang X Abstract Hydroxy genkwanin (HGK), a flavonoid compound from natural resources, showed good inhibition against the growth of breast tumor cells. However, the poor solubility restricted the further study and the in vivo drug delivery of HGK. We prepared HGK nanosuspensions by antisolvent precipitation method and investigated their characterization, stability, hemolysis probability, release behavior in vitro, antitumor activity in vitro and in vivo, and preliminary safety through acute toxicity experiments. The resultant HGK nanosuspensions (HGK-NSps) showed an average diameter of (261.1 ± 4.8 nm), a narrow particle size distribution (PDI of 0.12 ± 0.01), spherical morphology, high drug-loading content (39.9 ± 2.3%, w/w), and good stability in various physiological media. HGK-NSps was safe for intravenous injection at low concentration and HGK was slowly released from the obtained nanosuspensions. HGK-NSps showed stronger cytotoxicity than free HGK against many tumor cells in vitro. Especially against MCF-7 cells, the IC50 value was decreased to 1.0 μg/mL, 5-fold lower than the HGK solution. In the in vivo antitumor activity study HGK-NSps (40 mg/kg) displayed a similar therapeutic effect to that o...
Source: Drug Delivery - Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research