目的:探讨髓鞘形成相关N-甲基-D-天冬氨酸受体(NMDA-R)亚基在MK-801诱导的精神分裂症小鼠模型大脑中的变化.方法:35只雄性C57BL//6J小鼠,随机分为:对照组(control)和地卓西平马来酸盐处理组(MK-801),利用旷场实验、探孔实验及高架十字迷宫检测小鼠行为学改变,免疫荧光染色观察小鼠大脑NMDA-R亚基NR1的表达,real time RT-PCR检测髓鞘形成相关NMDA-R亚基NR1、NR2C和NR3A mRNA的表达.结果:与对照组小鼠相比,MK-801处理组在旷场内10 min总运动路程较对照组显著增加;3 min及5 min内探孔次数较对照组显著降低;模型组小鼠在开臂内停留总时间较对照组显著降低.NR1在小鼠神经细胞胞膜、轴突周围和髓鞘部位均有表达.大脑皮层、海马内的NMDA-R亚基NR1,NR2C及NR3A mRNA的表达在两组间均无显著差异;胼胝体区域NR1和NR2C mRNA表达在两组间同样无显著差异;但相较于对照组,MK-801慢性给药组小鼠胼胝体区域NMDA-R亚基NR3A mRNA表达显著上调.结论:NMDA-R在少突胶质细胞、髓鞘等部位确有表达;胼胝体部位NR3A亚基上调可能在MK-801诱导的精神分裂症中发挥作用.

Objective :To optimize the formula and preparation technique of doxorubicin liposome, and to e-valuate its cytotoxicity on human ovarian cancer HO8910 cells in vitro with rhythmical low-dosage admin-istration. Methods:Doxorubicin liposome was prepared by the (NH4 )2SO4-gradient method. The opti-mum formation was selected by means of the orthogonal design of experiment .The in vitro drug release behavior of liposome was evaluated by the dialysis method. MTT assay was applied to investigate the cyto-toxicity of doxorubicin liposome and free doxorubicin with common administration after 24h and rhythmi-cal low-dosage administration after 144h on HO8910 cells .Results :The optimum formula was as follows :the ratio of lecithin to cholesterol was 3∶1, (NH4)2SO4 concentration was 155 mmol/L ,drug∶lecithin was 1∶10 ,temperature was 60 ℃ .The average entrapment efficiency for doxorubicin was 92.86% .The release of liosome was relatively slow. The cytotoxicity test showed that IC50 of free doxorubicin and doxo-rubicin liposomes were 0.62 μg/mL and 0.46 μg/mL respectively at 24h and 0.06 μg/mL and 0.01 μg/mL at 144h .Conclusion :The selected formulation and preparation technique of doxorubicin liposome is reasonable in prescription ,practicable in techniques and high in encapsulation efficiency. MTT indicated that the inhibition rates of free doxorubicin and doxorubicin liposomes with rhythmical low-dosage admin-istration were much higher than those with MTD chemotherapy administration, and rhythmical low-dos-age administration had much higher inhibition rate for HO 8910 cells than free drug .

Objective: To develop a GC method to determine the menthol quickly in productions with mint. Methods: We bought two kinds peppermint and one kind mouthwash from the market, chose n-hexaneas the suitable extractant, use the AT. OV-1301 capillary column for separating the menthol. The best chromatographic operating condition was chosen. Split stream sampling was 2 μL, split ratio was 10:1, injector temperature was 220 ℃, detection temperature: 220 ℃, oven temperature: 110 ℃ for 2 min, stepped temperature: 5 ℃/min to 150 ℃, maintain for 5 min, determinated by FID. Results: Menthol have good linearity within the range of 5.0~1500 μg/mL. Within-day precisions of the method were 1.30%~1.80%. The recovery ratio of the three sample was 103.44%, 101.87% and 107.26% respectively, and the content of the three samples was (4.09±0.24) mg/g, (3.78±0.21) mg/g and (0.41±0.01) mg/mL respectively. Conclusion: The method is fast, simple and accurate in the determination of menthol.

Objective To preparare hyaluronic acid-curcumin-liposome(HA-CUR-L)and to investigate the encapsulation rate and the quality evaluation.Methods HA-CUR-L was prepared by the reversed-phase evaporation method,and the encapsulation rate,HA-binding rate,form distribution,particle size and in vitro release were detected.Results The average entrapment rate of HA-CUR-L was 88.75%,the binding rate of HA was 71.69% and the particle size was 160 nm.The total accumulative in vitro release amount was 82.26% after 36 h.Conclusion Selecting the reversed-phase evaporation method for optimizing HA-CUR-L is reasonable in prescription,convinient and feasible technology with high encapsulation rate.

Curcumin liposomes modified with vitamin A were prepared by reverse-phase evaporation vesicles.Orthogonal test was adopted to optimize the formulation with encapsulation efficiency and binding rate as the evaluation parameters.Encapsulation efficiency,binding rate,particle size and in vitro release were investigated.The ratio of the liposomes of less than 1.58 μm was 57%.The encapsulation efficiency and vitamin A binding rate of curcumin liposomes modified with vitamin A were 89.3% and 61.3%.

Objective:To prepare curcumin liposome and investigate its stability.Methods:Curcumin liposome was prepared by the reversed-phase evaporation method and purified by exclusion chromatography with Sephadex-50.The optimum formation was selected by means of orthogonal design of experiment;Centrifugal acceleration experiment and determination of leakling ration were served to proved the liposome stability.Results:The optimum formula was as follows:the ratio of lecithin to drug was 60∶1;lecithin:cholesterol was 4∶1;pH of PBS was 6.5,ultrasonic time was 5min.The average entrapment efficiency for curcumin was 95.06%.Conclusion:The selected formulation and preparation technique of curcumin liposome is reasonable in prescription,practicable in techniques,high in encapsulation efficiency and good in stability.

OBJECTIVE To prepare prodrug 5′-palmitoyl-5- fluorouridine (5-FURP) liposome and to evalutate its toxicity in vitro. METHODS The orthogonal design was used to screen the optimal formation and preparation process.The 5-FURP liposome was prepared by the reverse-phase evaporation vesicles(REV),and its encapsulation efficiency and physicochemical property was determined. The cytotoxicity of 5-FURP liposome was investigated by human breast cancer of MCF-7cell line,human nasopharyngeal carcinoma of CNE-1 cell line,human nasopharyngeal carcinoma of HEP-2 cell line. RESULTS encapsulation efficiency of the 5-FURP liposome was 94.35%. The stability of 5-FURP liposome was valuated with the entrapment efficiency and the change of EPC value in 4,25 ℃ for 1 month. The results showed that the 5-FURP liposome stored in 4 ℃ would keep stable. The results of cell toxicity in vitro showed that the liposomes encapsulated with 5-FURP inhibited human breast cancer of MCF-7 cell line,human nasopharyngeal carcinoma of CNE-1 cell line,human nasopharyngeal carcinoma of HEP-2 cell line was higher than that of the free drug.The IC50 of 5-FURP liposome was higher(5.0,3.4,2.6 times) for the MCF-7,CNE-1,HEP-2 than for free 5-FUR. CONCLUSION 5-FURP was encapsulated in liposomes can inhance corpuscular uptake and promote therapeutic effect of medicine.

OBJECTIVE:To determine the content of IL-2 in IL-2 targeting liposomes of 5-FURP.METHODS:The sample solution was stained by Coomassie brillant blue G-250 solution.Using blank liposome as blank.the absorbability of the IL-2 was determined by ultraviolet spectrophotometry at a wavelength of 595 nm:meanwhile its content was determined.RESULTS:The linear range of IL-2 was 1～100μg·mL~(-1)(r=0.999 7)and the average recovery rate was 99.26%(RSD=0.59%,n=5).CONCLUSION:The method was proved to be simple,rapid,sensitive and reproducible,and it iS applicable for the determination of IL-2 in liposome of 5-FURP.