RESUMO
Objective To prepare formononetin-2-hydroxypropyl-β-cyclodextrin (FMN-2-HP-β-CD) inclusion complex and to explore its inclusion behavior. Methods The preparation method of FMN-2-HP-β-CD inclusion complex was optimized by comparing kneading method, stirring method, and ultrasonic method. The content of FMN was assayed by HPLC. The preparation technology of FMN-2-HP-β-CD inclusion complex was optimized by orthogonal design taking drug loading capacity as index. The inclusion complex was characterized by scanning electronic microscopy (SEM) and X-ray diffractometry (XRD). Phase solubility method was used to calculate the molar ratio between host and guest molecules and the related thermodynamic parameter. The molecular simulation was processed to investigate the inclusion behavior of FMN and 2-HP-β-CD. Results Using acid-base neutralization agitation method, the optimum inclusion conditions were: the molar ratio of FMN with 2-HP-β-CD 1∶1, inclusion temperature 50 ℃, and 2-HP-β-CD concentration 5 g/L. The drug loading capacity was (9.42 ± 0.25)%. The phase solubility curve was AL type and the stability constants decrease with the increasing temperature. The thermodynamic parameters showed that the inclusion of FMN and 2-HP-β-CD is a process of exothermic and entropy decreasing with enthalpy change as the main driving force. Molecular simulation showed that the 7-OH of the FMN takes the lead from the wider rim of 2-HP-β-CD into the cavity, and forms a hydrogen bond with the oxygen atom on the 2-HP-β-CD. Conclusion The FMN-2-HP-β-CD inclusion complex prepared by the optimumprocess conditions has good repeatability, which can improve the solubility of FMN. Molecular simulation of FMN and 2-HP-β-CD inclusion behavior was consistent with the relevant thermodynamic parameters.
RESUMO
OBJECTIVE:To study the effect of HP-β-CD on solubility of 1,8-oxido-p-menthane in volatile oil of magnoliae flos,and optimize the extraction technology of Xinzhi nasal drops. METHODS:Steam distillation method was adopted to extract the volatile oil in magnoliae flos. Using the content of 1,8-oxido-p-menthane in volatile oil of magnoliae flos as index,HPLC was adopted to determine the effects of HP-β-CD with different concentration on solubility of 1,8-oxido-p-menthane in volatile oil of magnoliae flos. Using the comprehensive scores of imperatorin and extract yield as indexes,orthogonal test was used to optimize the amount of ethanol,volume fraction and extraction time in extraction technology of Xinzhi nasal drops. Verification test was car-ried out. RESULTS:50% HP-β-CD aqueous solution can improve the solubility of 1,8-oxido-p-menthane to 7.6 times. The optimal extraction technology of Xinzhi nasal drops was as follow as 10-fold 80% ethanol,extracting twice,1 h every time. In verification test,the average content of imperatorin was 0.078%(RSD=2.01%,n=3),and extract yield was 10.80%(RSD=1.85%,n=3). CONCLUSIONS:HP-β-CD shows good solubilization effect on the 1,8-oxido-p-menthane in volatile oil of magnoliae flos,and the optimized extration technology for Xinzhi nasal drops is feasible.
RESUMO
A novel hydrophobic ferrocene polymer ( P-Fc) was synthesized successfully. Taken the advantage of 2-hydroxypropyl-β-cyclodextrin ( HP-β-CD ) with hydrophilic outside and hydrophobic inside, P-Fc was successfully enveloped in the cavity of HP-β-CD to form macromolecular vesicle by a self-assembly process. The structure and morphology of the macromolecular vesicle was characterized by FTIR, 1HNMR, SEM and CV. Rhodamine 6G (R6G) and doxorubicin hydrochloride (DOX) was used as target drugs and loaded in the vesicles successfully. After added the oxidant, ferrocene was oxidized to dicyclopentadienyl iron, which destroyed the vesicles successfully. The rapid directional release of the drugs was realized. The maximum loading values of R6G and DOX were 6. 89 and 39. 06 μg/mg, respectively. The release rates were 73. 7%and 88. 2%, respectively. It would increase the utilization level of the drugs and enhance their efficiency.