1.In vitro and in vivo Antitumor Effect of Lentinan Combined with 5-FU
China Pharmacist 2015;(3):400-403
Objective:To study the in vitro and in vivo anti-tumor effect of lentinan combined with 5-FU. Methods:MTT method was used to determine the proliferation of H22 in vitro, and the cell cycle changes were analyzed by a flow cytometry. The in vivo anti-tumor effect was evaluated in Kunming mice. The tumor inhibitory rate, thymus/spleen index, IL-2, IL-6 and TNF-α were deter-mined. Results:The in vitro results revealed that lentinan had no obvious effect on the inhibitory rate and cell cycle of the cells treated with 5-FU. In vivo results showed that lentinan at the dosage of 25 and 50 mg·kg-1 could obviously enhance the anti-tumor effect of 5-FU(P<0. 05). Furthermore, lentinan could increase the thymus/spleen index of the tumor-bearing mice. Conclusion:Lentinan com-bined with 5-FU has synergistic effects on anti-tumor activity through nonspecific immune stimulation rather than the direct killing of tumor cells.
2.Preparation and Release Behavior in vitro of Memantine Hydrochloride Sustained-release Pellets
China Pharmacist 2015;(2):233-237
Objective:To prepare sustained-release pellets of memantine hydrochloride and investigate the in vitro drug release be-havior. Methods:The drug-loaded pellets were prepared by a fluid bed coating technology, the sustained-release pellets were prepared with Eudragit RL 30D and Eudragit RS 30D as the coating materials, and in vitro drug release behavior of the sustained-release pellets was studied. Results:The in vitro drug release was steady and complete in 24h, which fit a zero-order kinetics model. Conclusion:The memantine hydrochloride sustained-release pellets has the sustained-release property.
3.In vitro Dissolution of Olanzapine Pamoate Long-acting Injections
China Pharmacist 2014;(12):2053-2056
Objective:To develop a dissolution method for olanzapine pamoate long-acting injections. Methods:The in vitro dis-solution profile of olanzapine pamoate was detected by an oar method and an HPLC method. The stirring speed respectively was 25, 50 and 75 r·min-1, and 500 ml of sodium lauryl sulfate simulated muscle fluid [0.5% , with pH of (7.0 ±0.05)] at (37 ±0.5)℃was used as the bio-relevant dissolution media. Results: The linearity between the peak areas and the concentrations was observed within the range of 2. 15-107. 40 mg·L-1(r=0. 999 9) for pamoate and 1. 75-87. 40 mg·L-1(r=0. 999 9) for olanzapine, respec-tively, and the average recovery of olanzapine pamoate was 99. 80%(RSD=0. 55%, n=9). The f2 for the dissolution in the dissolu-tion medium of shelf-prepared products and the innovation preparations was 70. 80. Conclusion:The dissolution method can be utilized to control the quality of olanzapine pamoate long-acting injections.
4.Inhibition of MCF-7/ADR cells by DOX-loaded pluronic-attached PAMAM dendrimer conjugate.
Zhuojun GU ; Meng WANG ; Qiongyan FANG ; Chengrun WANG ; Huaiyu ZHENG
Acta Pharmaceutica Sinica 2014;49(8):1188-93
Pluronic modified polyamidoamine (PAMAM) conjugate (PF127-PAMAM) was prepared and the inhibiting effect of MDR against MCF-7/ADR was investigated with doxorubicin (DOX) as model drug. 1H NMR and FTIR spectra showed that the conjugate was synthesized successfully. Element analysis accurately measured that 27.63% amino of per PAMAM was modified by pluronic (PAMAM : PF127, 1 : 35.37 mole ratio). PF127-PAMAM showed an increased size and a reduced zeta potential compared to PAMAM. PF127-PAMAM had lower hemolytic toxicity and cytotoxicity due to the reduced zeta potential and the protection of PF127. Each PF127-PAMAM molecular could load 19.58 DOX molecules, and the complex exhibited sustained and pH-sensitive release behavior. PF127-PAMAM/DOX exhibited weaker cytotoxicity than free DOX in MCF-7 cells; while the complex showed much stronger reverse effect of drug resistance in MCF-7/ADR cells, and resistance reversion index (RRI) was as high as 33.15.