黄芩苷脂质体制备及包封率测定

采用逆相蒸发法,利用卵磷脂制备黄芩苷脂质体,以紫外法测定黄芩苷浓度,透析法测定黄芩苷包封率。结果表明：卵磷脂：胆固醇（m／m）为4：1,有机相：水相为3：1,黄芩苷浓度1．5mg／mL,所制得黄芩苷脂质体粒径均匀、制备量大,包封率达40．4％。     

聚乙烯醇脂质体的制备及性能研究

以大豆卵磷脂为包封材料,用反相蒸发法制备脂质体,同时用不同浓度的聚乙烯醇(PVA)进行包覆。实验结果表明,PVA在脂质体外形成了一层膜,而且包覆量随其浓度的增加而增加。相比较于未包覆的脂质体,PVA包覆的脂质体具有较高的包封率和较小的泄露率。当ρ(PVA)=3g/L时,脂质体的包封率最高为58%,当ρ(PVA)=4g/L时,脂质体的泄漏最慢。     

芦丁脂质体的制备与药物包封率的测定

采用薄膜分散法,制备包封率高、粒径均匀、稳定性好的芦丁脂质体,并建立芦丁脂质体中芦丁含量和包封率的测定方法。以包封率为主要指标,通过正交设计优化芦丁脂质体的制备工艺,同时采用反相高效液相色谱法进行芦丁含量和包封率测定。结果表明,薄膜分散法制备的脂质体平均包封率为66.50%,外观均匀、稳定性良好。建立的反相高效液相色谱法能将芦丁与辅料分离良好,芦丁浓度在4～40μg/L范围内与峰面积呈现良好的线性关系（r=0.999 2,n=5）,平均回收率为99.0%,可用于测定芦丁脂质体的药物含量与包封率。     

基于迷迭香精油温敏脂质体的温度响应型控释抗氧化复合膜制备

以合成磷脂DPPC和胆固醇为膜材，采用乙醚注入法制备迷迭香精油温敏脂质体，将温敏脂质体添加到壳聚糖-普鲁兰多糖溶液中，以BOPP为基膜制备抗氧化复合膜。对迷迭香温敏脂质体进行包封率、粒径分布、多分散性指数（PDI）、相变温度和原子力显微镜的测定，测定薄膜中精油释放速率，验证薄膜温度响应特性。结果表明，制备温敏脂质体平均包封率为65.6%，平均粒径为164.8nm，多分散性指数（PDI）平均值为0.163，相变温度为38.5℃和41.8℃。抗氧化复合膜在42℃条件下7天内释放量为94.1%，具有显著的温度响应控制释放作用。     

脂质体载药性能与卵磷脂的关系

探讨了卵磷脂对脂质体载药性能的影响。用逆相蒸发法制备阿糖胞苷脂质体,通过测定脂质体的包封率、平均粒径和药物渗漏量,考察了蛋黄卵磷脂、大豆卵磷脂及猪脑卵磷脂对脂质体载药性能的影响。实验结果表明,在n(PC)∶n(CHOL)=1∶1的条件下,蛋黄卵磷脂脂质体的平均粒径为2.59μm,包封率为(17.02±0.21)%,在37℃经40 h温育后,平均粒径增加0.53μm,药物渗漏量为(0.18±0.01)mg/h。平均粒径和包封率均高于大豆卵磷脂脂质体及猪脑卵磷脂脂质体,平均粒径增加值低于大豆卵磷脂脂质体及猪脑卵磷脂脂质体,渗漏速度高于猪脑卵磷脂脂质体,但低于大豆卵磷脂脂质体。对比实验证明,蛋黄卵磷脂脂质体的载药性能较好。     

大豆磷脂阿奇霉素脂质体的制备及包封率测定

采用逆相蒸发法,利用大豆粉状磷脂制备阿奇霉素脂质体。以高效液相色谱法为分析手段,采用反透析法测定阿奇霉素脂质体的包封率。研究了阿奇霉素脂质体配方中不同成分的比例,以及水合介质对脂质体包封率的影响。阿奇霉素脂质体的最佳制备条件为:温度40℃,m(阿奇霉素)∶m(磷脂)=1∶25,m(阿奇霉素)∶m(胆固醇)=1∶2,水合介质为pH=6.8的磷酸盐缓冲溶液〔V(NaH2PO40.01 mol/L)∶V(Na2HPO40.01 mol/L)=3∶2〕,加入的磷酸盐缓冲溶液为20 mL(相对于20 mg阿奇霉素),在该条件下,阿奇霉素脂质体的包封率为72%。     

紫甘薯花青素脂质体制备工艺的优化

以大豆卵磷脂、胆固醇为膜材,采用逆相蒸发法制备紫甘薯花青素脂质体,以凝胶柱层析法测定脂质体中紫甘薯花青素的包封率,得出制备紫甘薯花青素脂质体的最优工艺条件为:胆固醇与大豆卵磷脂物质的量比为1∶2,紫甘薯花青素水溶液(0.250 mg·m L-1)与乙醚的体积比为1∶4,逆相蒸发时间为30min,上述条件制备的脂质体平均包封率为76.61%。     

盐酸托泊替康脂质体包封率影响因素的考查

利用脂质体为药物载体，制备抗癌药盐酸托泊替康脂质体，并进一步探究影响盐酸托泊替康脂质体包封率的因素，筛选得到较优的制备工艺。以HSPC、DSPE-MPEG和Chol为包封材料，采用主动载药法—硫酸铵梯度法进行脂质体的制备，研究空白脂质体的pH、硫酸铵浓度、药磷比和孵育时间对盐酸托泊替康脂质体包封率的影响。空白脂质体的pH和孵育时间对包封率无显著影响，硫酸铵浓度为0.35 mol·L^-1,API/P=3.5，空白脂质体pH=5.0，包封率>95%。硫酸铵浓度和药磷比为影响盐酸托泊替康脂质体包封率的最主要因素，两者可进一步提高盐酸托泊替康脂质体的包封率。     

禽传染性支气管炎病毒脂质体核酸疫苗的制备

目的制备禽传染性支气管炎病毒脂质体核酸疫苗,并优化其制备工艺。方法采用逆向蒸发法制备禽传染性支气管炎病毒脂质体核酸疫苗,通过正交试验进行制备条件的优化,用荧光法测定脂质体的包封率。筛选制备高包封率脂质体核酸疫苗的最佳条件,测定脂质体粒径,并对疫苗免疫效果进行检测。结果制备高包封率的禽传染性支气管炎病毒脂质体核酸疫苗的工艺为:卵磷脂、胆固醇的比例为2∶1(摩尔比),转速为150r/min,温度为45℃,包封率可达80.31%。脂质体粒径平均为149nm,脂质体核酸疫苗显著提高了疫苗的免疫效果。结论按本工艺制备的禽传染性支气管炎病毒脂质体核酸疫苗包封率高,脂质体粒径均一,免疫效果良好。     

类脂囊泡作为头孢唑啉钠药物载体的研究

实验以司盘（span）和胆固醇（CH）为主要原料,通过薄膜分散法法制备了头孢唑啉钠囊泡。用透射电镜考察了囊泡的形态和构造,并对可能影响包封的各种实验条件进行了优化。实验表明：在50℃超声40min的条件下,Span40与CH用量比为4：3时形成的囊泡对1．0mg／mL的注射用头孢唑啉钠平均包封率达50％以上,而且制备的头孢唑啉钠囊泡在模拟胃流体和模拟肠流体中均有缓释作用。     

复相乳化法制备聚乳酸/水杨酸钠微囊

以W/O/W复相乳化法,聚乳酸为壁材、水杨酸钠为芯材,制备聚乳酸/水杨酸钠微囊。聚乳酸/水杨酸钠微囊的工艺条件为:水杨酸钠溶液浓度为40 mg/mL,聚乳酸溶液浓度为25mg/mL,聚乙烯醇溶液浓度为2mg/mL,内水相水杨酸钠体积为2mL,油相聚乳酸溶液体积为10mL,外水相聚乙烯醇溶液体积为60mL,即内水相与油相比为1∶5,油相与外水相体积比为1∶6。聚乳酸/水杨酸钠微囊的包封率为75.70%。     

Chitosan and marine phospholipids reduce matrix metalloproteinase activity in myeloma SP2 tumor‐bearing mice

An animal experiment was conducted to assess the antitumor effects of chitosan‐coated liposomes on myeloma SP2. The animal experimental groups designed for myeloma SP2 tumor‐bearing BALB/c mice were provided with five different drinks: (I) control (double‐distilled water); (II) squid phospholipid liposomes alone 1.0 mg/mL; (III) chitosan alone 5.0 mg/mL; (IV) squid phospholipid liposomes 1.0 mg/mL with chitosan 5.0 mg/mL in the form of a simple mixture; and (V) squid phospholipid liposomes 1.0 mg/mL coated with chitosan 5.0 mg/mL. At 20 days after implantation of the myeloma SP2 cells into mice, oral administration of the experimental drinks was provided for 35 days. There was significant suppression of tumor growth when chitosan and squid phospholipids were administered simultaneously in a simple mixture or as chitosan‐coated liposomes. Matrix metalloproteinase (MMP)‐2 and MMP‐9 activity was significantly less in the serum of mice that consumed chitosan‐coated liposomes than in control mice. We found that decreased tumor burden was related to MMP secretion. Therefore, chitosan‐coated marine phospholipid liposomes might be useful as potential agents for the treatment of myeloma SP2.     

利用牙膏中甘油含量鉴别牙膏种类

建立了气相色谱法定量分析牙膏中甘油含量来鉴别牙膏种类的方法。以正十四烷作为内标,采用DB-FFAP毛细管柱分离样品,氢火焰离子化检测器(FID)测定牙膏中甘油的含量。线性方程为Y=0.3847C-0.0095,相关系数r=0.9996,线性范围为0.01~3.0 mg/mL,最低检测浓度为2.58μg/mL,平均回收率为96.2%,相对标准偏差1.29%。该方法具有操作简便,灵敏、准确、重现性好等特点,适用于公安基层办案工作的需要。     

气相色谱测定消心痛中有机溶剂的残留量

建立了C．C测定消心痛原料药中氯仿、乙酸、乙酸乙酯残留量的方法。采用色谱柱为PEG-20M不锈钢柱(4m×2mm),柱温采用程序升高,起始柱温50℃维持3 min,然后以10℃/min的速率升至180℃维持5 min,再以10℃/min的速率升至280℃维持10 min。FID检测器,检测器温度320℃,进样口温度320℃,氮气为载气,流速50mL/min,氢气流速30 mL/min。空气流速400 mL/min。可使三种有机溶剂完全分离,氯仿在0．0005～0．003 mg/mL的浓度范围内呈良好的线性关系(r=0．9994),回收率为100．3％(RSD＜1．0％)；乙酸乙酯在0．005～0．03 mg/mL的浓度范围内呈良好的线性关系(r=0．9999),回收率为100．5％,(RSD＜1．0％)；乙酸在0．005～0．03 mg/mL的浓度范围内呈良好的线性关系(r=0．9997),回收率为98．7％,(RSD＜1．0％)。     

利用牙膏中薄荷醇含量鉴别牙膏种类

建立了气相色谱法定量分析牙膏中薄荷醇含量来鉴别牙膏种类的方法。以正十四烷作为内标,采用DB-FFAP毛细管柱分离样品,氢火焰离子化检测器(FID)测定牙膏中薄荷醇的含量。线性方程为Y=1.1137C-0.0087,相关系数r=0.9991,线性范围为0.01~0.20 mg/mL,最低检测浓度为2.61μg/mL,平均回收率为94.3%,相对标准偏差1.66%。该方法具有操作简便,灵敏、准确、重现性好等特点,适用于公安基层办案工作的需要。     

Ternary Copper(II) Complexes With Indomethacin, a Potent Non-Steroidal Antiinflammatory Drug. Crystal Structure of Bis (Dimethylformamide)-Tetrakis[1-(4-Chlorobenzoyl)-5-Methoxy-2-Methyl-1-H-Indole-3-Acetato]Dicopper(II). Antiinflammatory Properties and Prevention of Gastrointestinal Side Effects by Nanocapsules

Two ternary copper(ll) complexes of indomethacin [1-(4-chlorobenzoyl)-5-methoxy-2- methyl-1-H-indole-3-acetic acid] called hereafter lndo, were prepared and characterized by single crystal X-ray diffraction. The first complex Cu(2)(Indo)(4)(DMF)(2) I crystallizes in space group P-1 (a = 10.829(2), b = 13.379(2), c = 16.491(3) A; alpha = 105.58(2), beta = 101.06(2), gamma = 106.96(2) degrees ; V= 2104.6(6) A(3), Z= 1). The title molecule is a centrosymmetric binuclear complex, with Cu atoms bridged by the carboxylate moieties of four indomethacinate ligands. The four nearest O atoms around each Cu atom form a square planar arrangement with the square pyramidal coordination completed by the O atom of N,N'-dimethylformamide. Daily administration for seven days of 1 mg/kg of indomethacin, I and I encapsulated into liposomes induces a weak inflammation of rat gastrointestinal tract. I was less inflammatory than indomethacin but the better protection was brought by encapsulation of the compound. This might be of interest in sustained therapies of chronic inflammatory diseases.     

锶渣处理含铬废水的研究

利用二次锶渣处理含铬废水,研究了各工艺因素对六价铬去除率的影响。结果表明,活化二次锶渣提高了六价铬的处理效率,随着二次锶渣粒径的减小,六价铬的去除率增大。二次锶渣对六价铬的吸附具有分形动力学特征。活化二次锶渣处理含铬废水的适宜条件为：吸附剂用量为含铬废水与二次渣的体积质量比为25 mL/g,pH=10,温度为40 ℃,处理时间为60 min,此时六价铬去除率可达到82.5%。     

Development and characterization of lactoferrin nanoliposome: cellular uptake and stability

Lactoferrin was purported in consumer literature to enhance and support the immune system response through their antioxidant, antibacterial, and anticarcinogenic properties. To improve the effectiveness of lactoferrin, liposomes were used as a carrier in this study. The main purpose of this study was to compare three different methods to prepare the lactoferrin nanoliposomes based on the encapsulation efficiency and size distribution and evaluate the stability and cellular uptake of lactoferrin nanoliposomes. Encapsulation efficiency and size distribution indicated the reverse-phase evaporation method was fit for preparing the lactoferrin nanoliposomes. The stabilities of lactoferrin nanoliposomes in simulated gastrointestinal juice, sonication treatment time and lipoperoxidation extent of storage time were evaluated. The lactoferrin nanoliposomes showed an acceptable stability in simulated gastrointestinal juice at 37°C for 4 h and short treatment times were required to achieve nano-scaled liposomes. Furthermore, the viability of cells was decreased by increasing the concentration of the various lactoferrin nanoliposomes. The methyl thiazolyl tetrazolium results demonstrated that Lf nanoliposomes and Lf activated in the cells in a manner of dose-effect relation and Lf nanoliposomes had a statistically significantly different (p<0.01) between the concentration 5 and 10 mg/mL. According to the results, nanoliposomes may be fit for the oral administration of lactoferrin and could be useful approach for lactoferrin availability in tumor cells.     

Optimization on condition of epigallocatechin-3-gallate (EGCG) nanoliposomes by response surface methodology and cellular uptake studies in Caco-2 cells

The major component in green tea polyphenols, epigallocatechin-3-gallate (EGCG), has been demonstrated to prevent carcinogenesis. To improve the effectiveness of EGCG, liposomes were used as a carrier in this study. Reverse-phase evaporation method besides response surface methodology is a simple, rapid, and beneficial approach for liposome preparation and optimization. The optimal preparation conditions were as follows: phosphatidylcholine-to-cholesterol ratio of 4.00, EGCG concentration of 4.88 mg/mL, Tween 80 concentration of 1.08 mg/mL, and rotary evaporation temperature of 34.51°C. Under these conditions, the experimental encapsulation efficiency and size of EGCG nanoliposomes were 85.79% ± 1.65% and 180 nm ± 4 nm, which were close with the predicted value. The malondialdehyde value and the release test in vitro indicated that the prepared EGCG nanoliposomes were stable and suitable for more widespread application. Furthermore, compared with free EGCG, encapsulation of EGCG enhanced its inhibitory effect on tumor cell viability at higher concentrations.