In the present paper, the effect of β-cyclodextrin (β-CD) inclusion complexation on the solubility and enzymatic hydrolysis of naringin was investigated. The inclusion complex of naringin/β-CD at the molar ratio of 1:1 was obtained by the dropping method and was characterized by differential scanning calorimetry. The solubility of naringin complexes in water at 37 ± 0.1 °C was 15 times greater than that of free naringin. Snailase-involved hydrolysis conditions were tested for the bioconversion of naringin into naringenin using the univariate experimental design. Naringin can be transformed into naringenin by snailase-involved hydrolysis. The optimum conditions for enzymatic hydrolysis were determined as follows: pH 5.0, temperature 37 °C, ratio of snailase/substrate 0.8, substrate concentration 20 mg·mL⁻¹, and reaction time 12 h. Under the optimum conditions, the transforming rate of naringenin from naringin for inclusion complexes and free naringin was 98.7% and 56.2% respectively, suggesting that β-CD complexation can improve the aqueous solubility and consequently the enzymatic hydrolysis rate of naringin.

The purpose of this work was to research the enhancement of Epimedium fried with suet oil based on the in vivo formation self-assembled flavonoid nanomicelles. Taking icariin as the representative, under the action of suet oil, self-assembled nanomicelles were prepared under simulated gastrointestinal tract conditions and were characterized by dynamic light scattering and transmission electron microscopy (TEM). The experiments with icariin self-assembled nanomicelles without suet oil were done according to the above. The influence of suet oil on the transportation of icariin across Caco-2 cell monolayers and the absorption in rat intestine of self-assembled nanomicelles were evaluated. The particle size of icariin self-assembled nanomicelles with suet oil was smaller than without suet oil. The nanomicelles seemed to be monodisperse spherical particle with smooth surfaces. The icariin entrapment efficiency of self-assembled nanomicelles with suet oil was increased from 43.1% to 89.7%. In Caco-2 cell monolayers, the absorptive permeability, secretory permeability and efflux ratio of icariin self-assembled nanomicelles with suet oil was 1.26 × 10^{−6 cm/s, 5.91 × 10−6 cm/s and 4.69, respectively, while that of icariin self-assembled nanomicelles without suet oil was 0.62 × 10−6 cm/s, 3.00 × 10−6} cm/s, and 4.84, respectively. In rat intestinal perfusion experiments, the permeability coefficient of icariin self-assembled nanomicelles with suet oil in duodenum was higher than the value of icariin self-assembled nanomicelles without suet oil (p < 0.05). With the action of suet oil, icariin self-assembled nanomicelles were more stable and the entrapment efficiency was higher than that without suet oil, which could increase the solubility of icariin and improve its intestinal absorption. Therefore, suet oil plays a role in its enhancement.

The root of Paeonia lactiflora Pall. (Chishao, CS) and Ligusticum chuanxiong Hort. (Chuanxiong, CX) were widely used as a drug pair in Chinese Medicine, and the combination of CS and CX showed a more significant inhibition on neuronal apoptosis in our previous study. In the present study, total paeony glycosides (TPGs) from CS and total ligustici phenolic acids (TLPAs) from CX were combined to evaluate the synergistic effects against focal cerebral ischemia both in vitro and in vivo. The combination of TPGs and TLPAs at 7:3 had the best anti-oxidative stress and anti-inflammatory effect on OGD-induced HUVEC. Additionally, the infarction area proportion and neuron apoptosis of rats by TPGs:TLPAs (7:3) was significantly lower than their alone in MCAO rats. Moreover, TPGs: TLPAs of 7:3 showed a more significant effect on decreasing the expression of MMP-2 and MMP-9, and increasing the protein expression or mRNA level of TIMP-1 than other combinations. The optimal ratio of TPGs and TLPAs at 7:3 could bring more remarkable protective effects against focal cerebral ischemia in MCAO rats by alleviating oxidative stress, inflammatory and neuronal apoptosis to protect the blood-brain barrier. Overall, the present study provided benefical evidence for clinical application of CS and CX as a “drug pair”.