ABSTRACT
This study aims to improve the solubility and bioavailability of daidzein by preparing the ß-cyclodextrin-daidzein/PEG_(20000)/Carbomer_(940) nanocrystals. Specifically, the nanocrystals were prepared with daidzein as a model drug, PEG_(20000), Carbomer_(940), and NaOH as a plasticizer, a gelling agent, and a crosslinking agent, respectively. A two-step method was employed to prepare the ß-cyclodextrin-daidzein/PEG_(20000)/Carbomer_(940) nanocystals. First, the insoluble drug daidzein was embedded in ß-cyclodextrin to form inclusion complexes, which were then encapsulated in the PEG_(20000)/Carbomer_(940) nanocrystals. The optimal mass fraction of NaOH was determined as 0.8% by the drug release rate, redispersability, SEM morphology, encapsulation rate, and drug loading. The inclusion status of daidzein nanocrystals was determined by Fourier transform infrared spectroscopy(FTIR), thermogravimetric analysis(TGA), and X-ray diffraction(XRD) analysis to verify the feasibility of the preparation. The prepared nanocrystals showed the average Zeta potential of(-30.77±0.15)mV and(-37.47±0.64)mV and the particle sizes of(333.60±3.81)nm and(544.60±7.66)nm before and after daidzein loading, respectively. The irregular distribution of nanocrystals before and after daidzein loading was observed under SEM. The redispersability experiment showed high dispersion efficiency of the nanocrystals. The in vitro dissolution rate of nanocrystals in intestinal fluid was significantly faster than that of daidzein, and followed the first-order drug release kinetic model. XRD, FTIR, and TGA were employed to determine the polycrystalline properties, drug loading, and thermal stability of the nanocrystals before and after drug loading. The nanocrystals loaded with daidzein demonstrated obvious antibacterial effect. The nanocrystals had more significant inhibitory effects on Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa than daidzein because of the improved solubility of daidzein. The prepared nanocrystals can significantly increase the dissolution rate and oral bioavailability of the insoluble drug daidzein.
Subject(s)
Acrylic Resins , Nanoparticles , Sodium Hydroxide , Escherichia coliABSTRACT
Three different methods, including autoclaving, autoclaving-debranching, and purification, were used to prepare Kudzu-resistant starch (KRS) from Kudzu starch (KS). The physicochemical properties, such as thermodynamic properties, pasting properties, solubility, swelling, and coagulability, as well as the in vitro digestive characteristics of the three kinds of KRS were studied. The results showed that the morphology of starch granules of KRS prepared by autoclave, autoclave enzymatic hydrolysis, and purification methods was changed and the relative crystallinity was significantly decreased compared with the original starch. X-ray diffraction (XRD) showed that KRS exists in the form of C and C+V crystalline form. There was a significant increase in the pasting temperature and a remarkable decrease in the peak viscosity and the expansion degree of the KRS prepared by all three methods. The solubility of the resistant starch (RS) obtained by autoclaving-debranching and that by purification were both increased compared to that of native KS, while the solubility of the RS obtained by autoclaving was decreased. Meanwhile, the retrogradation of the three RS was also improved to varying degrees. The contents of RS in the samples were: P-KRS (71%) > DA-KRS (43%) > A-KRS (42%) > KS (9%). Simulated human in vitro digestion experiments showed that RS has stronger antidigestibility properties than native starch. Among them, the RS prepared by the purification method has stronger antidigestive properties, and it is predicted that it may have a better potential value in regulating blood glucose. These results indicated that the processing properties of KRS, especially the digestibility, are significantly improved and can be used as a new functional food ingredient, which deserves thorough study.
