黄芪多糖脂质体的制备

采用逆相蒸发法和薄膜法制备黄芪多糖脂质体,并对脂质体的包封率进行了测定.结果表明,逆相蒸发法制备的为大单层脂质体,其包封率为44.32%;薄膜法制备的为复层脂质体,其包封率为36.28%,逆相蒸发法操作简单,所需仪器设备为常规仪器,再加上其制备的大单层脂质体包封容积大,包封率高,因此是一种黄芪多糖脂质体制备的理想方法.     

番茄红素脂质体的制备工艺

采用逆相蒸发法和薄膜法两种方法制备番茄红素脂质体.筛选出制备高包封率脂质体的工艺为:卵磷脂与胆固醇之比为3:1,温度为35℃,番茄红素与磷脂比例为1:6,旋转速度为200r/min,此条件下番茄红素脂质体的最高包封率可达71.26%.     

基于超临界流体技术制备葡萄糖脂质体的实验研究

脂质体由于其特殊的结构和性能,是一种很有发展潜力的药物载体,在医药和化妆品等行业具有广阔的应用前景。超临界逆向蒸发法是用超临界流体代替有机溶剂制备脂质体的方法,具有对水溶性药物脂质体制备过程简单、包覆率高等特点。以葡萄糖为模型药物,利用该方法制备出了葡萄糖脂质体,并详细考察了不同工艺条件对脂质体粒径和包覆率的影响。结果表明:用超临界逆向蒸发法可成功地制备出最小粒径为290nm、包覆率最高可达41.3%的葡萄糖脂质体。压力、温度和平衡时间对粒径和包覆率都有较大的影响。压力在10~30MPa时,随压力的增加,脂质体粒径显著减小至某一值后,基本趋于稳定,而包覆率逐渐增加,达到25.7%~27.5%,随后包覆率逐渐减小;温度在35~65℃时,随温度的增加粒径显著减小至最小值,然后逐渐增大,而包覆率一直增大,最高可达41.3%;平衡时间在15~45min时,随平衡时间的增加,粒径相对稳定,而包覆率显著增加,超过45min之后,粒径显著增加,包覆率显著下降。     

高压微射流制备纳米中链脂肪酸脂质体的研究

以中链脂肪酸(MCFA)为模型材料,比较了高压微射流(HPM)、超声波和微孔过滤3种方法处理后的MCFA脂质体,着重研究了HPM的处理压力和处理次数对脂质体的平均粒度、包封率和稳定性的影响。结果表明:相比超声波和微孔过滤法,HPM处理后的MCFA脂质体的平均粒度最小、包封率最高、稳定性良好;在120 MPa压力条件下处理6次时,MCFA脂质体的平均粒度达到最小,为(73.9±10.2)nm,包封率为(52.20±9.57)%;在120 MPa压力条件下处理4次时,包封率和载药量达到最高,分别为(70.64±11.25)%和(9.42±0.83)%,稳定性系数最高,为0.9990±3.6951,平均粒度为(78.9±21.5)nm。     

异烟肼乳酸-乙醇酸共聚物磁性微球的制备和体外释放

采用化学共沉法制备磁性Fe3O4纳米粒,再采用W/O/W复乳-溶剂挥干法制备异烟肼乳酸-乙醇酸共聚物[Poly(lactide-co-glycolide),PLGA]磁性微球(INH-PLGA-MMS);电镜考察INH-PLGA-MMS形态、激光粒径分析仪考察粒径分布、磁场计测定磁感应强度、高效液相色谱法(HPLC)测定包封率、载药量及其释放度。结果表明,W/O/W复乳-溶剂挥干法制得的INH-PLGA-MMS外观圆整、表面光滑,平均粒径为3.02μm,磁感应强度为11.403emu/g,平均包封率为62.52%,平均载药量为9.21%,体外释放表明该制剂具有明显的缓释功能,外加振荡磁场可以增加磁性微球中药物的释放。     

吴茱萸碱与脂质体模拟生物膜的相互作用:FTIR和DSC研究

药物与生物膜相互作用的研究对于了解药物药效和改善其生物性能具有重要的意义。但生物膜的组成复杂,直接研究药物活性成分与生物膜的相互作用比较困难。以脂质体作为生物膜模型,研究了吴茱萸碱与脂质体的相互作用,分析了吴茱萸碱分子在脂质体中的包封位置,探讨了吴茱萸碱抗炎作用可能的作用机制。以二棕榈酰磷脂酰胆碱（DPPC）为膜材,应用薄膜分散法制备含有不同摩尔百分比（x）的吴茱萸碱脂质体,应用傅立叶变换红外光谱（FTIR）和差示扫描量热（DSC）技术分析随着脂质体中药物摩尔百分比的增大,DPPC分子各红外特征吸收峰频率、峰形及量热参数的变化情况,从而探讨药物在脂质体中的包封位置及吴茱萸碱分子对脂质体膜流动性的影响。实验数据表明,在0＜x＜10 mol%的浓度范围内,DPPC头部区域磷酸基团的不对称伸缩振动频率没有明显变化,脂质体相变温度和相变焓均随药物摩尔百分比的增大而减小。在0＜x＜5 mol%浓度范围内,DPPC界面区域的水化的羰基峰的吸收波数由1 726.0 cm-1增加到1 731.8 cm-1,当x=10 mol%时,该波数又减小到1 728.0 cm-1。在10 mol%≤x＜20 mol%浓度范围内,磷酸基团的不对称伸缩振动的波数由1 242.0 cm-1减小为1 236.3 cm-1,水化的羰基峰的吸收频率没有明显变化,脂质体相变温度和相变焓均随药物摩尔百分比的增大而增大。纯DPPC脂质体中亚甲基的对称伸缩振动波数为2 848.4 cm-1,载药后该波数都增大到2 850.3 cm-1。这些结果表明吴茱萸碱在脂质体中的包封位置具有浓度依赖性：在0＜x＜10 mol%浓度范围内,吴茱萸碱主要作用于DPPC分子的疏水尾链区域,少部分药物分子作用于DPPC分子的界面区域。在10 mol%≤x＜20 mol%浓度范围内,吴茱萸碱分子则主要作用于DPPC分子的头部区域,少部分药物分子作用于DPPC分子的疏水尾链区。所有载药脂质体的相变温度均低于纯DPPC脂质体的相变温度,即不同浓度的吴茱萸碱均可以使脂质体的膜流动性增加,并且,当药物摩尔百分比为10 mol%时,吴茱萸碱对生物膜流动性的增加效应最为明显。研究工作对于进一步揭示吴茱萸碱与生物膜的相互作用机制具有重要意义。     

反透析法测定阿奇霉素囊泡的包封率

建立阿奇霉素囊泡的包封率测定方法.以紫外分光光度法为分析手段,采用反透析法测定阿奇霉素囊泡的包封率.反透析法透析平衡时间为8h,游离药物的绝对回收率符合要求.该方法测得自制阿奇霉素囊泡的平均包封率为92.51％±0.56％,10h内没有渗漏,方法重现性好.该法操作准确、简便,可用于测定阿奇霉素囊泡的包封率.     

主动靶向氧化苦参碱脂质体包封率的测定

建立高效液相色谱法测定主动靶向氧化苦参碱脂质体包封率.主动靶向氧化苦参碱脂质体经洗脱柱分离后进行HPLC分析,以0.01mol/L醋酸铵(pH=7.0)∶乙腈=90∶10(V/V)为流动相,色谱柱为Agilent C18柱(5μm,4.6mm×150mm),柱温30℃;流速为1mL/min;紫外检测波长为215nm.氧化苦参碱在0.5-50μg/mL范围内线性关系良好(n=5,r=0.9997),最低定量浓度为0.5μg/mL(S/N＞ 10),回收率为98.5％,氧化苦参碱的低、中、高日内精密度与日间精密度RSD均小于3％.本法准确、灵敏,能较好的应用于主动靶向制剂氧化苦参碱脂质体包封率的测定.     

超声增强脂质体与细胞相互作用的研究

理论及实验研究了超声增强脂质体与细胞的相互作用.实验制作了包裹荧光素的脂质体,利用1 MHz聚焦超声增强脂质体与乳癌细胞的相互作用,采用荧光显微镜观察与荧光素结合前后细胞的变化,流式细胞仪定量检测细胞中包含的荧光素.结果表明,在声压幅度为0.24 MPa超声作用40 s后,细胞吸收荧光素能力比对照组（无超声作用）有8.78％的提高.理论讨论了超声增强脂质体与细胞相互作用的可能物理机制,指出超声诱发的脂质体运动及脂质体的粒径变化是超声增强脂质体与细胞相互作用的原因. 关键词： 脂质体 药物传递 超声辐射力     

包层氚增殖球床不同装载方案的有效热导率研究

针对聚变堆固态包层的产氚载体中锂陶瓷颗粒组成的氚增殖球床,建立了基于离散元-计算流体力学(DEM-CFD)方法的球床传热分析模型,进行了离散元(DEM)几何模型有效性验证、网格敏感性分析和计算流体力学(CFD)传热模型有效性验证。用该模型模拟计算了粒径分布球床、不同粒径的一元球床、二元球床的有效热导率,研究了相同填充率下,粒径分布、不同粒径及粒径混合对球床有效热导率的影响。研究结果表明,对于填充率相近的钛酸锂球床,粒径分布球床与一元等效粒径球床的有效热导率结果相差不大;在辐射换热可以忽略的情况下,粒径尺寸对一元球床有效热导率的影响可以忽略不计;二元混合钛酸锂球床相较于一元钛酸锂球床有更高的球床填充率和有效热导率。     

蟾毒灵对脂质体双分子层结构的影响:31P NMR研究

应用³¹P NMR方法研究了蟾毒灵(BF)对脂质体双分子层结构的影响.研究结果表明对于未经超声波处理的卵磷脂(PC),BF对磷脂双分子层膜具有稳定作用.另一方面,当PC经过超声波处理后,首次观测到纯PC的双分子层膜转变为胶束或微胞,后者的比例随着超声波处理的时间的增加而增加;而BF的存在可加速PC由双分子层结构向胶束相的转变.     

RSM and ANN modeling-based optimization approach for the development of ultrasound-assisted liposome encapsulation of piceid

Piceid, a naturally occurring derivative of resveratrol found in many plants, has recently been considered as a potential nutraceutical. However, its poorly water-soluble property could cause a coupled problem of biological activities concerning drug dispersion and absorption in human body, which is still unsolved now. Liposome, a well-known aqueous carrier for water-insoluble ingredients, is commonly applied in drug delivery systems. In this study, a feasible approach for solving the problem is that the targeted piceid was encapsulated into a liposomal formula as aqueous substrate to overcome its poor water-solubility. The encapsulation process was assisted by ultrasound, with investigation of lipid content, ultrasound power and ultrasound time, for controlling encapsulation efficiency (E.E%), absolute loading (A.L%) and particle size (PS). Moreover, both RSM and ANN methodologies were further applied to optimize the ultrasound-assisted encapsulation process. The data indicated that the most important effects on the encapsulation performance were found to be of lipid content followed by ultrasound time and ultrasound power. The maximum E.E% (75.82%) and A.L% (2.37%) were exhibited by ultrasound assistance with the parameters of 160 mg lipid content, ultrasound time for 24 min and ultrasound power of 90 W. By methodological aspects of processing, the predicted E.E% and A.L% were respectively in good agreement with the experimental results for both RSM and ANN. Moreover, RMSE, R² and AAD statistics were further used to compare the prediction abilities of RSM and ANN based on the validation data set. The results indicated that the prediction accuracy of ANN was better than that of RSM. In conclusion, ultrasound-assisted liposome encapsulation can be an efficient strategy for producing well-soluble/dispersed piceid, which could be further applied to promote human health by increased efficiency of biological absorption, and the process of ultrasound-mediated liposome encapsulation can be well established by a methodological approach using either RSM or ANN, but it is worth mentioning that the ANN model used here showed the superiority over RSM for predicting and optimizing encapsulation.     

液晶态油酸脂质体与生物膜相互作用的理化特性

用小角Ｘ射线散射用法和 ^３１Ｐ核磁共振技术，对抗癌新药——液晶态油酸多相脂质体的结构进行了研究。实验结果表明：胆固醇、油酸、非离子表面活性剂均对ＰＥ脂质体液晶态的结构有显著的影响。在含有高效分散剂的磷酸盐缓冲溶液中制成的液晶态油酸多相脂质体由片层六角相和片层立方相组成。电子自旋共振研究表明，这种结构的脂质体与Ｅ_ｃ腹水肝癌细胞相互作用的结果使Ｗ／Ｓ值增加。 关键词：     

Liposome Encapsulation of Thiol-Capped CdTe Quantum Dots for Enhancing the Intracellular Delivery

Although water soluble thiol-capped quantum dots (QDs) have been widely used as photoluminescence (PL) probes in various applications, the negative charges on thiol terminals limit the cell uptake hindering their applications in cell imaging. The commercial liposome complex (Sofast®) was used to encapsulate these QDs forming the liposome vesicles with the loading efficiency as high as about 95%. The cell uptakes of unencapsulated QDs and QD loaded liposome vesicles were comparatively studied by a laser scanning confocal microscope. We found that QD loaded liposome vesicles can effectively enhance the intracellular delivery of QDs in three cell lines (human osteosarcoma cell line (U2OS); human cervical carcinoma cell line (Hela); human embryonic kidney cell line (293 T)). The photobleaching of encapsulated QDs in cells was also reduced comparing with that of unencapsulated QDs, measured by the PL decay of cellular QDs with a continuous laser irradiation in the microscope. The flow cytometric measurements further showed that the enhancing ratios of encapsulated QDs on cell uptake are about 4–8 times in 293 T and Hela cells. These results suggest that the cationic liposome encapsulation is an effective modality to enhance the intracellular delivery of thiol-capped QDs.     

提高叶片局部粗糙度对风机效率影响的实验研究

通过对三种风机在叶片上进行了加大局部粗糙度的实验,研究了风机叶片上不同位置的粗糙度变化对风机效率的影响,发现风机叶片内弧尾缘加大粗糙度时风机的效率会提高。实验得到了通过增加叶片局部粗糙度提高风机效率的粗糙带最佳宽度及其位置,并对不同的粗糙度对效率的影响进行了初步的探讨。本工作为风机节能开辟了一条新路。     

维生素C对生物膜流动性的影响的ESR波谱的研究

本文使用TEMPO和脂肪酸氮氧自由基自旋标记脂质体和正常的与癌变的鼠肝细胞膜,研究了V_c对膜流动性的影响,探讨有关V_c抗肿瘤作用的机理。实验表明:V_c可以影响膜类脂和膜蛋白的运动,提高癌变细胞膜的流动性,并随V_c浓度的增加其作用速度加快,但对正常肝细胞膜流动性则无明显影响。此外,在一定浓度范围内,V_c对正常的与癌变的肝细胞膜的掺入能力有显著差异。     

药型罩材料的晶粒度对射流性能的影响

 通过对紫铜药型罩的静破甲威力实验和脉冲X射线照像，研究了药型罩材料的晶粒度对射流性能的影响。研究结果表明，药型罩材料的晶粒度对射流动态延伸特性有重要影响。罩材料的晶粒细化可以增加有效连续射流的长度，推迟射流断裂的时间，提高静破甲威力水平。最后讨论了晶粒度对射流性能影响的机理。     

热传导对微型涡轮动叶性能影响的数值模拟

为了探求热传导对微型燃气轮机性能的影响,使用CFX对某微型燃气轮机涡轮动叶的流动特性和换热性能进行了数值模拟并提出了考虑热传导损失的轮周效率的计算方法.通过计算发现热传导对流动和涡轮动叶的性能的影响不可忽略,热传导使动叶输出功和效率明显降低.考虑顶部间隙后,热传导的影响更加显著.     

新型高效汽水分离器的试验研究

汽水分离装置是核电站蒸汽发生器净化蒸汽的重要部件,其性能不仅会影响蒸汽发生器的上筒体尺寸、水循环性能及水位的稳定性,而且还会影响汽轮机的正常运行。由于波形板内的两相流动过程很复杂,目前国外对汽水分离器的研究仍以实验为主。本文则针对冷态条件下新型波形板汽水分离器的分离性能进行了试验研究,验证了二次携带现象的存在,并测量了双钩波形板汽水分离器的分离效率和压降,分析了挡板对分离效率的影响,获得了计算双钩波形板分离效率的经验公式,为波形板分离器的优化设计奠定了基础。     

SOME ASPECTS OF THE INVESTIGATION OF RANDOM VIBRATION INFLUENCE ON RIDE COMFORT

Contemporary vehicles must satisfy high ride comfort criteria. This paper attempts to develop criteria for ride comfort improvement. The highest loading levels have been found to be in the vertical direction and the lowest in lateral direction in passenger cars and trucks. These results have formed the basis for further laboratory and field investigations. An investigation of the human body behaviour under random vibrations is reported in this paper. The research included two phases; biodynamic research and ride comfort investigation. A group of 30 subjects was tested. The influence of broadband random vibrations on the human body was examined through the seat-to-head transmissibility function (STHT). Initially, vertical and fore and aft vibrations were considered. Multi-directional vibration was also investigated. In the biodynamic research, subjects were exposed to 0·55, 1·75 and 2·25 m/s² r.m.s. vibration levels in the 0·5- 40 Hz frequency domain. The influence of sitting position on human body behaviour under two axial vibrations was also examined. Data analysis showed that the human body behaviour under two-directional random vibrations could not be approximated by superposition of one-directional random vibrations. Non-linearity of the seated human body in the vertical and fore and aft directions was observed. Seat-backrest angle also influenced STHT. In the second phase of experimental research, a new method for the assessment of the influence of narrowband random vibration on the human body was formulated and tested. It included determination of equivalent comfort curves in the vertical and fore and aft directions under one- and two-directional narrowband random vibrations. Equivalent comfort curves for durations of 2·5, 4 and 8 h were determined.