Preparation and Characterization of PEG-PLA Genistein Micelles Using a Modified Emulsion-Evaporation Method

• Published in: Journal of nanomaterials Vol. 2020; no. 2020; pp. 1 - 15
• Main Authors: Wu, Jizhou, Li, Guojian, Yu, Yanhong, Qin, Wen, Cheng, Qiuchen, Zhuo, Lang
• Format: Journal Article
• Language: English
• Published: Cairo, Egypt Hindawi Publishing Corporation 2020; Hindawi; John Wiley & Sons, Inc
• Subjects: Acetone; Bioavailability; Cell cycle; Copolymers; Encapsulation; Evaporation; Experiments; Fourier transforms; Hemodialysis; Infrared analysis; Micelles; Morphology; Muscles; Nanomaterials; Nanoparticles; Polydispersity; Polyethylene glycol; Polylactic acid; Polyvinyl alcohol; Solubility; Trehalose; Beijing China; United Kingdom > UK; United States > US; China
• ISSN: 1687-4110; 1687-4129
• DOI: 10.1155/2020/3278098

The objective of this study is to improve the bioavailability of genistein by encapsulation with polyethylene glycol-polylactic acid (PEG-PLA) copolymers. Genistein micelles (GMs) prepared using a modified emulsion-evaporation method were more stable than those made with the original method. The effect of polyvinyl alcohol, Tween 80, sonication time, PEG-PLA/genistein ratio, and organic phase (acetone)/H2O ratio on the size, polydispersity index, encapsulation efficiency, and drug loading efficiency of GMs was investigated. GMs were obtained and characterized under optimal experimental conditions. For long-term storage, GMs were lyophilized by freeze drying with trehalose to produce genistein lyophilized powder (GLP). The analysis of GLP by Fourier-transform infrared spectroscopy and differential scanning calorimetry showed that genistein was successfully incorporated into the micellar structure. In vitro release experiments revealed that the incorporation of genistein into PEG-PLA copolymers significantly improved its solubility and bioavailability. GLP was more potent in inhibiting the proliferation of HSC-T6 cells than genistein. Treatment with GLP at 10–20 μg/mL for 48 h significantly inhibited the protein expression of α-smooth muscle actin and collagen I in HSC-T6 cells compared with the control. These data demonstrated that the improved solubility and bioavailability of genistein in the form of GLP enhanced its antifibrotic effect in vitro.