Objective Daidzein solid dispersions were prepared by solid dispersion technology to improve in vitro dissolution rate. Methods Daidzein solid dispersions were prepared by solvent method using polyvinyl pyrrolidone K30 ( PVP K30) as carrier.The in vitro dissolution characteristics of solid dispersions were evaluated,and the properties were detected by IR and XRD. Results The dissolution rates of different mass ratio of daidzein-PVP solid dispersion were significantly improved compared with that of daidzein API.The cumulative dissolution of solid dispersion with mass ratio of 1∶6 within 30 minutes was up to 87.8%,equivalent to six times of API. The in vitro drug release kinetics were fitted mathematically to Korsemeyer-Peppas model. Conclusion Solid dispersion with PVP K30 as carrier could significantly improve dissolution rate of daidzein.

Objective To prepare and characterize glycyrrhetinic acid cationic liposomes.Methods Liposomes were prepared by ethanol injection technique.An orthogonal test was utilized to optimize the formulation and preparation of glycyrrhetinic acid liposomes.The unencapsulated glycyrrhetinic acid and liposomes were separated by Sephadex gel G-50,the encapsulation efficiency was detected by HPLC.The morphological examination of glycyrrhetinic acid liposomes was performed using transmission electron microscopy.The particle size and Zeta potential of the liposomes were measured.The release rate of glycyrrhetinic acid from liposomes was tested.Results The liposomes with spherical or ellipsoidal shape and better stability featured the encapsulation efficiency of(91.61?1.16)%,the mean partical size of(141?10)nm,and Zeta potential of(35.9?5)mV.The in vitro release kinetics were consistent with Higuchi equation.The stability of glycyrrhetinic acid liposomes was better.Conclusion The selected formulation and preparation technic of glycyrrhetinic acid liposomes could be rational,stable,and with a sustained feature in vitro release.

Objective To determine the encapsulation efficiency of glycyrrhetinic acid(GA) liposomes and to study the release of GA from the liposomes in vitro.Methods GA liposomes were prepared by ethanol injection.The unencapsulated glycyrrhetinic acid and liposomes were separated by sephadex gel G-50,and the encapsulation efficiency was detected by HPLC.The release behavior of the drug was studied by the third method for dissolution issued in Chinese pharmacopoeia(published in 2005).Results The encapsulation efficiency of liposomes was 91.61%,and the in-vitro drug-release curve was accorded with Higuchi equation.Conclusion The GA liposomes have high encapsulation efficiency and sustained-release effect.

Objective: To prepare the compound Yuxingcao dispersible tablets and investigate the dissolution of baicalin in vitro. Methods: The formulation of dispersible tablets was optimized by an orthogonal design test in terms of disinterating time.Results: The optimal disintegrants were composed of CMS-Na 5%,MCC 20%,L-HPC 10%,and disintegration time of prepared compound Yuxingcao dispersible tablets followed the quality specification of dispersible tablet in Chinese Pharmacopoeia 2005. The in vitro dissolution test indicated that more than 95% of baicalin dissolved in 3 minute from dispersible tablets. Concolusion: The formulation and preparation process of compound Yuxingcao dispersible tablets were simple and feasible.

Objective To investigate the method for preparing oridonin-single-walled carbon nanotubes ( ORI-SWCNTs) nanocomposite and study its adsorption kinetics. Methods ORI-SWCNTs nanocomposite was prepared by using the method of solution mixing. The synthesized ORI-SWCNTs nanocomposite was characterized by using Laser particle size analyzer, Fourier transform infrared, DSC analysis, powder X-ray diffraction and electron microscopy techniques. Results The encapsulation efficiency and loading capacity of ORI in SWCNTs-COOH nanocarrier was estimated to be about (70.23±2.1) %and (27.29±1.2) %, respectively. The Zeta potential was (-34.29±1.2) mV, partical size was about (458±18) nm. The absorption of ORI on SWCNTs-COOH could be explained by pseudo-second-order model. Conclusion The established preparation process of ORI-SWCNTs nanocomposite by solution mixing is feasible, with higher loading efficiency and encapsulate efficiency..

OBJECTIVE: To prepare Formononetin (FMN) inclusion compound liposome and evaluate its quality. METHODS: FMN inclusion compound liposome was prepared by film dispersion method. The morphology, particle size, Zeta potential, encapsulation efficiency and in vitro release properties were studied. RESULTS: The particle size, Zeta potential and encapsulation efficiency of prepared FMN inclusion compound liposome were (255. 34 ± 12. 87) nm, (25. 32 ± 3. 51) mV, (81. 63 ± 0. 79)％, respectively (n=3). The 24 h accumulative release rate of prepared FMN inclusion compound liposome was 56. 12％. CONCLUSIONS: FMN inclusion compound liposome with good sustained-release effect is prepared successfully and in line with related quality standard.

OBJECTIVETo synthesize compounds based on imidazo-fused heterocycles and evaluate their anti-tumor activity against breast cancer.

METHODSThe compounds 1a-1e, 2a and 2b were synthesized by aerobic copper-catalyzed halocyclization of methyl N-heteroaromatics with aliphatic amines; 3a and 3b were generated by sonogashira reaction and Suzuki reaction, respectively; the compounds 4a-4c were obtained by Buchwald-Hartwig reaction of the corresponding amines and 1e. The effects of these compounds against breast cancer cells and their nephrotoxicity were determined using MTT assay. Annexin VFITC/PI apoptosis detection kit was used to assess the apoptosis-inducing effects of these compounds in breast cancer cells. With normal saline as the control, the safety and anti-tumor activity of the compound 2a (daily dose of 10 mg/kg for 14 days) was tested in a mouse model bearing human breast cancer xenografts.

RESULTSThe compounds 2a, 4a, 4b and 4c all showed obvious anti-tumor activities. Among these compounds, 2a showed the most potent anti-tumor effect against breast cancer cells with an IC of 9.77 ± 2.32 μmol/L, similar to that of cisplatin (IC=8.96 ± 2.35 μmol/L); 2a also showed a slightly lower nephrotoxicity than cisplatin, and their CC was 10.79±0.87 μmol/L and 8.45±0.68 μmol/L, respectively. 2a obviously promoted apoptosis of breast cancer cells and caused a moderate suppression of the breast cancer growth in the tumor-bearing mouse models without producing serious adverse effects.

CONCLUSIONSFour compounds synthesized based on imidazo-fused heterocycles have anti-tumor activities against breast cancer. The compound 2a is capable of dose-dependently promoting apoptosis of breast cancer cells and has a good safety and a moderate efficacy for suppressing tumor growth in mouse models bearing human breast cancer xenografts.