Preparation, characterization, and pharmacokinetics study of a novel genistein-loaded mixed micelles system

Drug Development and Industrial Pharmacy
Hongxue ShenJian-Ming Ju

Abstract

Genistein (GEN), is a natural dietary isoflavone, has been reported to show anticancer activities. However, its poor aqueous solubility and oral bioavailability limit its clinical application. We designed a novel genistein-loaded mixed micelles (GEN-M) system composed of Soluplus® and Vitamin E d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) were prepared by organic solvent evaporation aimed to overcome the challenges of GEN's poor solubility and then further improve its oral bioavailability. The optimized, spherical-shaped GEN-M was obtained at a ratio of 10:1 (Soluplus®:TPGS). The mean particle size of GEN-M was 184.7 ± 2.8 nm, with a narrow polydispersity index (PDI) of 0.162 ± 0.002. The zeta potential value of GEN-M was -2.92 ± 0.01 mV. The micelles solutions was transparent with blue opalescence has high the entrapment efficiency (EE) and drug loading (DL) of 97.12 ± 2.11 and 3.87 ± 1.26%, respectively. GEN-M was demonstrated a sustained release behavior when formed micelles shown in drug release in vitro. The solubility of GEN in water increased to 1.53 ± 0.04 mg/mL after encapsulation. The permeability of GEN across a Caco-2 cell monolayer was enhanced, and the pharmacokinetics study of GEN-M showed a 2.42-fold...Continue Reading

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Citations

May 6, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Vieri PiazziniMaria Camilla Bergonzi
May 29, 2020·Drug Development and Industrial Pharmacy·Chengying ShenXiaofang Li
Oct 1, 2020·Antioxidants·Josipa GrgićAna Bucić-Kojić
Jul 4, 2020·Signal Transduction and Targeted Therapy·Zhe ZhangCanhua Huang
Nov 19, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Wamidh H TalibAsma Ismail Mahmod

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