Characterization and cytotoxicity of PLGA nanoparticles loaded with formononetin cyclodextrin complex

• Published in: Journal of drug delivery science and technology Vol. 41; pp. 375 - 383
• Main Authors: Guo, Bohong, Xu, Danqiao, Liu, Xiaohong, Liao, Cancheng, Li, Shengbin, Huang, Zexian, Li, Xiaofang, Yi, Jun
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 01.10.2017
• Subjects: 2-Hydroxypropyl-β-cyclodextrin; Cytotoxicity; Formononetin; Inclusion complex; PLGA nanoparticles; 2-Hydroxypropyl-β-cyclodextrin; Cytotoxicity; Formononetin; PLGA nanoparticles; Inclusion complex
• ISSN: 1773-2247
• DOI: 10.1016/j.jddst.2017.08.010

The study aimed to prepare and characterize the formononetin-2-hydroxypropyl-β-cyclodextrin inclusion complex loaded PLGA nanoparticles (FMN-2-HPβ-CD-NP). The neutralization agitation method was used to prepare FMN-2-HPβ-CD inclusion complex. Phase solubility study demonstrated the formation of AL type inclusion complex. The inclusion stability constant was 2116 ± 73 M−1. The PLGA nanoparticles were prepared by solid/oil/water (S/O/W) technology and theirs in vitro properties were studied. Experiments of NMR, FTIR, XRD and SEM confirmed the formation of FMN-2-HPβ-CD inclusion complex. Transmission electron microscopy (TEM) showed the spherical morphology of FMN-2-HPβ-CD-NP. The average particle size was 210.23 ± 3.4 nm, the polydispersity index was 0.108 ± 0.02, the Zeta potential was −26.25 ± 0.42 mV and the mean encapsulation efficiency was 91.97± 0.79%. The in vitro release study indicated that FMN-2-HPβ-CD-NP had a sustained release effect. The in vitro cytotoxicity showed that FMN-2-HPβ-CD-NP remained anticancer activity in Hela and MCF-7 tumor cells compared to free FMN. In conclusion, the novel delivery system of drug-in-cyclodextrin-in-nanoparticles was a promising carrier for poor lipophilic and poor hydrophilic drugs. [Display omitted]