Preparation of copolymer 7-hydroxyethyl chrysin loaded PLGA nanoparticles and the in vitro release

• Published in: Zhejiang da xue xue bao. Journal of Zhejiang University. Medical sciences. Yi xue ban Vol. 53; no. 1; pp. 116 - 125
• Main Authors: WANG, Xiaojuan, YANG, Baole, MA, Chuan, HE, Lei, JING, Linlin, HUANG, Qiong, MA, Huiping
• Format: Journal Article
• Language: Chinese; English
• Published: China 05.02.2024
• Subjects: Drug Carriers; Flavonoids; Lactic Acid; Nanoparticles; Particle Size; Polyglycolic Acid; Polylactic Acid-Polyglycolic Acid Copolymer; In vitro release; Formulation optimization; Poly (lactic-co-glyconlic acid) nanoparticles; 7-hydroxyethyl chrysin; Emulsion solvent evaporation method
• ISSN: 1008-9292
• DOI: 10.3724/zdxbyxb-2023-0233

To prepare 7-hydroxyethyl chrysin (7-HEC) loaded poly (lactic-co-glycolic acid) (PLGA) nanoparticles and to detect the release. The 7-HEC/PLGA nanoparticles were prepared by emulsification solvent volatilization method. The particle size, polydispersity index (PDI), encapsulation rate, drug loading and zeta potential were measured. The prescription was optimized by single factor investigation combined with Box-Behnken response surface method. Mannitol was used as protectant to prepare lyophilized powder, and the optimal formulation was characterized and studied for the release. The optimal formulation of 7-HEC/PLGA nanoparticles was as follows: drug loading ratio of 2.12∶20, oil-water volume ratio of 1∶14.7, and 2.72% soybean phospholipid as emulsifier. With the optimal formulation, the average particle size of 7-HEC/PLGA nanoparticles was (240.28±0.96) nm, the PDI was 0.25±0.69, the encapsulation rate was (75.74±0.80)%, the drug loading capacity was (6.98±0.83)%, and the potentiostatic potential was (－18.17±0.17) mV. The cumulative release reached more than 50% within 48 h. The optimized formulation is stable and easy to operate. The prepared 7-HEC/PLGA nanoparticles have uniform particle size, high encapsulation rate and significantly higher dissolution rate than 7-HEC.