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

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 eff...

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Published inJournal 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
LanguageEnglish
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
Online AccessGet full text

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Abstract 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.
AbstractList 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.
Author Li, Guojian
Qin, Wen
Zhuo, Lang
Wu, Jizhou
Cheng, Qiuchen
Yu, Yanhong
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  fullname: Zhuo, Lang
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CitedBy_id crossref_primary_10_3390_pharmaceutics15122653
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SubjectTerms 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
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Title Preparation and Characterization of PEG-PLA Genistein Micelles Using a Modified Emulsion-Evaporation Method
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