前列腺素E_1冻干隐形脂质体包封率的测定

目的评价前列腺素E1(PGE1)冻干隐形脂质体的质量,测定PGE1冻干隐形脂质体的包封率.方法用超滤法分离脂质体和游离药物;采用Hypersil C18柱(250 mm×4.6 mm,5μm),流动相:pH 4.9的磷酸二氢钾溶液.乙腈(3:2),流速1.0 mL·min-1,检测波长210 nm,测定药物含量,计算包封率.结果超滤法能很好的分离脂质体与游离药物,PGE1在1～50 mg·L-1内线性关系良好(r=0.999 3),平均包封率为93.02%.结论超滤-HPLC法测定PGE1冻干隐形脂质体包封率方法简便、准确.     

两种胡桃醌脂质体包封率测定方法研究

目的:建立两种胡桃醌脂质体包封率的测定方法,并对测定结果进行比较。方法:分别采用透析法和葡聚糖凝胶色谱柱法对脂质体中的游离药物进行分离,然后使用紫外分光光度计对脂质体包封的药物进行测定进而计算包封率。结果:透析法透析14h达到稳定;葡聚糖凝胶色谱柱法在30min内即将游离药物与脂质体进行有效的分离。胡桃醌测定波长为425nm,在0.005~0.04mg/m L的浓度范围内,线性关系良好,经回收率实验、精密度及重现性实验证实两种方法可行。结论:对比两种方法可知透析法耗时较长测定的包封率值偏低,葡聚糖凝胶色谱柱法测定所需时间更短,更便捷,测出的包封率更接近真实值。     

维生素E脂质体的制备工艺筛选、优化及其性质研究

目的优化维生素E（VE）脂质体的制备工艺并考察其性质。方法采用乙醇注入法、乙醚注入法、逆相蒸发法、薄膜水化法和复乳法分别制备v。脂质体,以包封率和保留率为考察指标,选择最优制备方法;经L9（3^4）正交试验设计优化选择,确定脂质体的最佳配方。结果薄膜水化法制备所得的VE脂质体包封率最高,VE保留率较高;用薄膜水化法制备脂质体的最佳配方为磷脂：VE：胆固醇=20：0．8：1．5;用透射电镜观察最佳实验组VE脂质体发现其具有指纹状结构,Zeta电位为．30．9±0．9mV,平均粒径为33．7nm。结论薄膜水化法制得的V。脂质体具有包封率高,VE保留率高,粒径均匀等特点。     

杨梅苷脂质体的薄膜超声法制备工艺研究

目的:为了充分发挥杨梅苷的药理作用和提高其稳定性,本实验制备杨梅苷脂质体并优化其制取工艺和考察其质量稳定性.方法:采用薄膜超声法制备杨梅苷脂质体,采用冷冻离心法分离脂质体和游离药物,采用高效液相色谱法测定脂质体中药物含量并计算其包封率,采用激光粒度仪测定脂质体的平均粒径.结果:采用薄膜超声法制备杨梅苷脂质体的最佳处方和工艺为:杨梅与卵磷脂的比例为1:7,卵磷脂与胆固醇的比例为4:1,磷酸盐缓冲溶液的pH值为7.0,浓度为0.005mol·L-1,超声时间为3min左右.结论:在最佳处方和工艺条件下制备的杨梅苷脂质体包封率较高、粒径分布良好,重现性亦较好,冷藏下渗漏率较低,稳定性较强.     

中链脂肪酸-维生素C冻干脂质体的制备研究

以脂溶性药物中链脂肪酸（MCFAs）和水溶性药物维生素C（Vit.C）为模型药物,采用复乳-高压法制备中链脂肪酸-维生素C复方脂质体,并用冷冻干燥技术制备成固体脂质体。通过研究脂质体的形态、粒径分布和包封率,对预冻温度、预冻时间、干燥时间、适宜的冻干保护剂种类、冻干保护剂与卵磷脂的质量比分别进行单因素考察。优选脂质体适宜的预冻温度为-80℃,预冻时间为5h,总干燥时间48h,适宜的冻干保护剂为蔗糖,蔗糖与卵磷脂的质量比为1.5∶1。最优冻干工艺条件下制得的中链脂肪酸-维生素C复合脂质体的维生素C包封率为62.25%,MCFAs包封率为46.30%,平均粒径为115.5nm。并考察了复方脂质体冻干前后粒径、Zeta电位、颗粒形态变化,发现粒径和Zeta电位变化不大,表明复方脂质体具有较好的物理稳定性。     

大豆磷脂阿奇霉素脂质体的制备及稳定性研究

利用大豆粉状磷脂,采用逆相蒸发结合冻融法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38℃,阿奇霉素：磷脂为1：20（质量比）,阿奇霉素：胆固醇为1：2．5（质量比）,最佳的水合介质是pH6．8的磷酸盐缓冲溶液,加入的磷酸盐缓冲溶液为20ml。在此条件下,阿奇霉素脂质体的包封率为72．86％。该方法准确,可用于大豆磷脂阿奇霉素脂质体的制备,并且制备的脂质体稳定。     

HPLC测定雷帕霉素聚乳酸-聚乙醇酸纳米粒的包封率

目的建立用HPLC法测定雷帕霉素聚乳酸．聚乙醇酸纳米粒包封率的方法。方法用超速离心法分离游离的雷帕霉素与包封药物的纳米粒,以HPLC为分析方法测定评价雷帕霉素聚乳酸．聚乙醇酸纳米粒的包封率。用Venusil XBP C18柱,以乙腈为流动相,流速0．8mL／min,检测波L6．277nm。结果雷帕霉素峰与辅料峰分离良好。雷帕霉素浓度在2．5-100μg/mL范围内线性关系良好,r=0．9998,平均回收率在98．3％～101．2％之间,日内精密度和日间精密度RSD均小于2％（n=5）。结论本法操作简单,准确可靠,可用于测定雷帕霉素聚乳酸-聚乙醇酸纳米粒药物的包封率。     

猪用外源生长激素(PST)脂质体的研制

通过薄膜法制备ＰＳＴ脂质体,并用过滤凝胶柱法分离脂质体及测定其包封率,在ＰＳＴ浓度为０．２mg/ml,卵磷脂：胆固醇为５：２时,包封率为２６．７％,通过４℃下冷藏测定发现包封率无明显变化,故其稳定性较即。另外 用扫描电镜观察了ＰＳＴ脂质体的结构与形态。     

HPLC-大孔树脂法测定芝麻素脂质体包封率

本实验对芝麻素脂质体进行质量评价,测定芝麻素脂质体的包封率.采用大孔树脂分离脂质体与游离药物,用高效液相色谱检测药物含量,计算包封率.该方法在5～200μg/ml范围之间线性良好(r=0.9999),RSD小于1.47%,加样回收率为98.18%.预饱和大孔树脂柱对空白脂质体的平均回收率为100.35%,且能很好的保留溶液中及脂质体制剂中的游离药物.此方法操作简单,重现性较好.     

葛根素壳聚糖纳米粒的制备

目的制备葛根素壳聚糖纳米粒,研究其理化性质。方法利用离子交联法制备葛根素壳聚糖纳米粒,以正交试验优化制备工艺,超滤法分离游离药物,紫外分光光度法测定包封率;电镜观察纳米粒的微观形态,光散射测定仪测定纳米粒的粒径分布。结果成功制备了稳定的含药纳米粒混悬液,包封率为5 0.8%。结论离子交联法适用于葛根素壳聚糖纳米粒的制备。     

HPLC法测定蓝莓中绿原酸的含量

建立了高效液相色谱法对蓝莓中绿原酸含量的测定方法,采用Aglient C18(250mm×4.6mm,5um)色谱柱;流动相为乙腈:0.4%磷酸溶液为13:87;流速为1.0mL/min;检测波长:327nm。结果显示,绿原酸在浓度为3.3×10-3—40×10-3mg/mL范围内,线性关系良好(Y=61.07x+8.896,R2=0.99996),精密度RSD为3.33%,平均回收率为106.01%,RSD为1.22%。本方法简便,结果准确,重现性好,可以作为蓝莓中绿原酸含量检测的良好方法。     

莪术醇长循环脂质体的制备及体外抗乳腺癌作用研究

目的:制备莪术醇长循环脂质体并对其体外性质进行初步研究。方法:用薄膜分散法制备莪术醇长循环脂质体,对其形态、粒径和电位分布,包封率,体外释放和放置稳定性测定,并考察体外细胞摄取和细胞毒性。结果:制备得到的莪术醇长循环脂质体粒径为(150.3±4.0) nm,PDI为0.197±0.009,zeta电位(-24.5±0.7) mV。莪术醇长循环脂质体平均包封率为80.24%,在4 ℃条件下存放2个月粒径和含药量无明显变化。细胞摄取实验中载香豆素-6长循环脂质体可增强MDA-MB231细胞的摄取。莪术醇长循环脂质体对MDA-MB231细胞具有较强细胞毒性作用,且作用强于莪术醇普通脂质体和游离莪术醇。结论:制备的莪术醇长循环脂质体包封率高,稳定性好,莪术醇长循环脂质体可增强乳腺癌MDA-MB231细胞的摄取及体外细胞毒性。     

Development of chitosan-coated liposomes for sustained delivery of tamarind fruit pulp's extract to the skin

In this study, chitosan-coated liposomes were developed. To entrap lyophilized tamarind extract containing alpha-hydroxy acids (AHAs) together with tartaric acid, the reverse phase evaporation method was used to obtain well-formed liposomes loaded with the extract. The highest entrapment efficiency of 68.3 ± 3.0% into the liposomes was obtained with liposomes consisting of phosphatidylcholine and cholesterol in a molar ratio of 2 : 1 after the extrusion process. The average particle size of the prepared liposomes was 158 ± 26 nm showing a negative zeta potential of −6 mV. For the preparation of the chitosan-coated liposomes, two selected independent parameters were varied: chitosan concentrations of 0.1, 0.5 and 1.0% w/v and volumes of the chitosan solutions of 1, 2 and 3 mL, to study the effects of such parameters on the entrapment efficiency of the extract-loaded liposomes. Variation in the volumes of the chitosan solution did not affect the entrapment efficiency of the liposomes. However, the entrapment efficiency of the AHAs in the chitosan-coated liposomes significantly increased with increasing chitosan concentrations. The size of the chitosan-coated liposomes was in the range of 200–300 nm with a positive zeta potential in the range of 6–29 mV. An in vitro release study using dialysis technique was performed to evaluate the release profile of the tartaric acid from the chitosan-coated liposomes. The obtained results showed the effect of the chitosan-coated liposomes on the lower release rate and on the amount of tartaric acid in comparison with that of the uncoated liposomes. The study in an in vitro skin cell model indicated that the developed system could enhance the potential of tamarind's AHAs on the stimulation of human keratinocyte proliferation being two-fold higher than the solution of the tamarind extract.     

白藜芦醇固体脂质体制备工艺研究

采用乙醇注入法制备白藜芦醇脂质体,用冷冻干燥技术制备固体脂质体。以包封率为考察指标,对芯材与壁材的配比、乳化剂的种类和用量、冻干保护剂甘露醇使用量、油水相之比分别进行单因素考察。结果表明：最优制备工艺条件为m(卵磷脂):m(胆固醇):m(白藜芦醇)=10:2:1、乳化剂Tween 80、乳化剂用量0.2%(m/m)、冻干保护剂甘露醇使用量2%(m/m)、油水相体积比为1:10。最优工艺制得的白藜芦醇固体脂质体的包封率为84.68%,采用乙醇注入法可制得包封率高的白藜芦醇固体脂质体,且方法简便易行。     

水杨酸铬(Ⅲ)配合物对肥胖小鼠肠道菌群的影响

目的探讨水杨酸铬(Ⅲ)配合物{[Cr(Ⅲ)(5-Cl-SA)(en)2]Cl·2H2O·2CH3OH}对肥胖小鼠的减肥效果和对小鼠肠道菌群结构的影响。方法昆明种小鼠随机分为正常组、模型组和药物组,定期称重并收集其粪便;给药9周后,解剖小鼠并测定多项生理生化指标;提取粪便微生物总DNA,PCR扩增16S rDNA V3可变区,并行变性梯度凝胶电泳(DGGE),分析肠道微生物多样性,利用主成分分析(PCA)研究肠道微生物群落组成的变化。结果水杨酸铬(Ⅲ)配合物可显著控制小鼠体重增长,且有减肥功效;给药9周后,小鼠各项生理指标均趋于正常。PCR-DGGE指纹图谱分析结果显示,高脂饲料和受试药物对肠道微生物的多样性影响不大,但对菌群结构影响显著。结论本研究为开发新型减肥药物提供了依据。     

羧甲基壳聚糖包裹椰子油脂质体制备的工艺优化

通过薄膜-超声分散法制备羧甲基壳聚糖包裹的椰子油脂质体,以大豆卵磷脂和氢化大豆卵磷脂为膜材,包封率为主要评价指标,采用单因素和正交实验对薄膜-超声分散法制备羧甲基壳聚糖包裹的椰子油脂质体的工艺和配方进行优化,并对所制备脂质体的微观形态、包封率、丙二醛(malondialdehyde,MDA)含量和体外释放度进行分析。结果表明:最佳制备条件为羧甲基壳聚糖与磷脂比为1:16,磷脂与胆固醇比为8:1,椰子油与磷脂比为3:1,pH为4.5,超声强度750 W,超声时间20 min,此条件下实际包封率为96.94%±0.20％。羧甲基壳聚糖包裹椰子油脂质体在0.9%氯化钠中,24 h的释放度为41.28%±0.30%。椰子油脂质体的包封率高和累积释放度高,稳定性好,可实现延缓释放和靶向给药。     

Functionality of porcine skin hydrolysates produced by hydrothermal processing for liposomal delivery system

Porcine skin proteins were hydrolyzed using hydrothermal processing (HTP) and fractionated by membrane ultrafiltration (UF) into peptides with different molecular weights (1–10 kDa). The porcine skin hydrolysates (PSHs) were analyzed for their antioxidant, antiaging, and skin permeation properties. Additionally, the PSHs were incorporated into liposomes with different charges to maintain and/or enhance their beneficial effect. The results showed that both HTP and UF‐II (1–3 kDa) had significantly high antioxidant and antiaging effects and good skin permeability. Based on the results for PSH‐loaded liposomes, the best carrier for incorporating PSHs was a positively charged liposome that had been prepared using positively charged lipid. PSH loaded with positively charged liposomes (PSH/LIP‐P) had the following droplet properties: 71.11 nm, 0.208 PDI (polydispersity index), and 38.37 mV. PSH/LIP‐P also had an incorporation efficiency of 70.72%, and the liposomes maintained their physical droplet stability during storage.

Practical applications

The findings of this study highlighted porcine skin hydrolysates (PSH) produced by hydrothermal processing and membrane ultrafiltration with high antioxidant and antiaging effects and good skin permeability. PSH‐loaded liposome capsules maintained a small size and high incorporation efficiency for PSH. The PSHs and PSH‐loaded liposomes could be tested further for their in vivo functionality as nutraceutical or cosmeceutical ingredients. Hence, the finding could be useful information for developing potential commercial products in the food, cosmetics, and related industries.     

一株产L-赖氨酸菌株发酵培养基的响应面优化

本试验优化了一株黄色短杆菌HXLl09的发酵培养基以提高L．赖氨酸的产量。在研究葡萄糖、硫酸铵、豆饼水解液、KH2P04·3H20、MgS04·7H20、FeS04·7H20、MnSO4·H2O4＋单因素实验的基础上,DesignExpert软件的Box-BehnkenDesign（BBD）建立响应面模型。结果表明：HXL109最佳产酸条件为：葡萄糖89.48g／L,豆饼水解液30．77g／L,硫酸铵20．89g／L,KH2P04·3H204．5g／L。在此条件下L．赖氨酸的产量为142．65g门L,与预测值（143．67g／L）吻合度较高。通过发酵对比实验可见,用响应面分析法对该L-赖氨酸产生菌发酵培养基进行优化,可获得最佳的工艺条件。     

血红素铁脂质体的制备

目的：制备血红素铁脂质体。方法：采用乙醇注入法及旋转薄膜- 超声法制备,再经过不同孔径的滤膜得到不同粒径的血红素铁脂质体,在原有技术的基础上优化血红素铁脂质体各组分的制备工艺,应用紫外分光光度计测定血红素铁的含量,计算出血红素铁脂质体的包封率,用差示扫描量热法检测血红素铁脂质体各组成物质的相变过程。结果：两种方法都能够得到较为理想的脂质体,血红素铁:胆固醇:卵磷脂质量比范围为(0.1～200):(1～10):(10～100)。结论：所得血红素铁脂质体呈均一大单室型,通过0.8μm 的滤膜后有效粒径为0.804μm,最大包封率36%。     

芹黄素类脂纳米囊的制备与理化性质考察

目的制备芹黄素类脂纳米囊并考察其理化性质。方法选择聚乙二醇单硬脂酸酯、卵磷脂作为表面活性剂,中链甘油三酯为油相,采用相转化法制备芹黄素类脂纳米囊;并初步研究其理化性质。结果按照优化处方制得的芹黄素类脂纳米囊载药量为1.26%,包封率为95.7%,平均粒径为46.1 nm,透射电镜下呈类球形,Zeta电位为-28.18 mV。结论该纳米囊制备方法简单,包封率较高,粒径较小。