布洛芬磁性固体脂质纳米粒的制备

背景：布洛芬因溶解度和溶血问题,目前仍无注射给药剂型上市。 目的：将自制的磁流体载入固体脂质纳米粒中,制备布洛芬磁性固体脂质纳米粒。 方法：以包封率为指标,用正交设计确定布洛芬固体脂质纳米粒的最优处方。以共沉淀法制备Fe3O4磁流体作为磁性材料,采用乳化分散-超声法,按照最优处方制备布洛芬磁性固体脂质纳米粒。观察其表面形态、粒径大小、分布和Zeta电位、饱和磁化强度、包封率及体外释放特征。 结果与结论：通过正交实验得最优处方为布洛芬0.05 g、F-68 0.2 g、吐温80 0.05 g、卵磷脂0.1 g、单硬脂酸甘油酯0.05 g、磁流体2.5 mL。用该工艺和处方制备的布洛芬磁性固体脂质纳米粒粒子呈均匀球形;平均粒径、zeta电位为(122±16) nm和(-13.3±6.94) mV;药物包封率和Fe3O4铁包封率分别为84.15%和83.19%;布洛芬在给定介质中36 h释放较完全,符合制剂学性质要求。     

改良自乳化溶剂扩散法制备MePEG-PLA纳米粒对成骨细胞的毒性

背景：两亲性嵌段聚合物由于其较强的载药能力强、纳米级大小、血液中长循环等优点在载药系统中得到广泛的应用。 目的：评估改良自乳化溶剂扩散法制备的甲氧基封端的聚乙二醇-聚乳酸 (MePEG-PLA)纳米粒对人骨肉瘤细胞MG63的毒性。 方法：通过改良自乳化溶剂扩散法制备MePEG-PLA纳米粒,MTS法测定纳米粒培养1,2,3 d后对MG63的毒性。激光粒度分析仪测定纳米颗粒的粒径大小、粒径分布及Zeta电位;透射电镜表征纳米胶束外观形态;酶标仪检测培养1,2,3 d细胞吸光度值。 结果与结论：MePEG-PLA纳米粒的平均粒径为25.7 nm,分布均匀,呈球形,Zeta电位为-8.06 mV,MePEG-PLA毒性为 0级。提示改良自乳化溶剂扩散法制备纳米粒简单易行,制备的纳米粒无毒,具有良好的应用前景。     

阳离子载基因MePEG-PLGA纳米粒的制备及优化处方的筛选

目的 建立纳米粒沉淀法制备阳离子甲氧基封端的聚乙二醇-聚乳酸聚乙醇酸嵌段聚合物(MePEG-PLGA)纳米粒的方法.方法 本研究利用单因素设计和正交实验选定最优实验方案,并对纳米粒的物理性质如表面形态,粒径分布、Zeta电位、DNA结合率,保护DNA能力进行考察.结果 最优条件制备得到的纳米粒粒径大小为89.7 nm,...     

固体脂质体纳米粒制备方法的研究进展

固体脂质纳米粒（solid lipid nanoparticles,SLN）又称固体脂质体,是一种室温下为固态的天然或合成的脂质体或类脂纳米粒子。SLN的研究始于20世纪90年代,是一种以硬脂酸、卵磷脂、三酰甘油等脂类原料为基质,将药物包裹于类脂核中制成50~1000nm粒径的固体脂质粒子给药体系[1-2]。SLN常温下为固态,具有以下四方面特点：①良好的生物兼容性;②能有效地控制药物释放,并可有效避免药物的降解和泄漏;③适合于多种给药途径;     

中心组合设计法优化雌二醇PEG-PLA微球制备工艺研究

利用中心组合设计法优化雌二醇聚乙二醇-聚乳酸微球制备工艺,提高微球制备质量,并对其特性进行预测。采用油/水乳剂溶剂挥发法制备微球。自变量为水相聚乙烯醇浓度、有机相聚乙二醇-聚乳酸浓度和理论载药量,以微球产率、包封率、平均粒径和跨距为因变量,对各自变量的各水平进行多元线性回归和二项式拟合,根据因变量面法选择较佳工艺条件并对优化区间进行预测。结果表明,产率、包封率、平均粒径和跨距用二项式模型拟合较好,复相关系数R分别为0.912 6、0.964 2、0.963 2和0.962 8,包封率、平均粒径和跨距的预测值与实测值的偏差分别为2.84%、7.56%和8.58%。中心组合设计法优化处方和制备工艺,方法简便,可对多因素和多指标的实验进行综合优化筛选,对试验结果预测较准确,是进行处方和制备工艺优化筛选的较佳方法。     

盐酸表阿霉素纳米靶向制剂的缓释效应

背景：盐酸表阿霉素是一种广谱抗生素,目前临床使用的不足多为药物释放快、目标组织药物浓度低,静脉给药后广泛分布于体内各种组织器官,不良反应明显。 目的：针对盐酸表阿霉素临床应用的不足,制备盐酸表阿霉素纳米靶向注射制剂。 方法：以叶酸偶联牛血清白蛋白为载体,采用乳化-高压匀质法,制备盐酸表阿霉素纳米靶向注射制剂,以激光粒度分析仪测定纳米颗粒的粒径大小、粒径分布及Zeta电位,扫描电镜观察纳米颗粒的表面形态,高效液相色谱法分析白蛋白负载盐酸表阿霉素纳米制剂的包封率、载药量和释药性能。 结果与结论：制备的盐酸表阿霉素纳米粒外观呈均匀球型,粒径分布较窄,平均粒径为(157.73±     0.40) nm,平均 Zeta 电位为(-30.85±0.43) mV,载药量 22.78%,包封率可达96.24%。体外模拟释药结果表明药物释放曲线分为两个阶段,突释阶段微球释药量在24 h内达42.6%,缓释阶段纳米粒释药持续时间长,在112 h 时释药量达 84.1%,载药纳米粒的药物释放速率持续稳定。结果表明乳化结合高压匀质法制备的盐酸表阿霉素纳米靶向制剂粒径均匀,粒径范围分布窄,载药量和包封率高,具有一定的缓释作用。     

Pharmacokinetic and Anti-inflammatory Effects of Sanguinarine Solid Lipid Nanoparticles

The sanguinarine (SG) was studied for its pharmacokinetic and anti-inflammatory activities with prepared solid lipid nanoparticles (SLNs). The sanguinarine solid lipid nanoparticles (SG-SLNs) were prepared by film-ultrasonic dispersion method and the entrapment efficiency of SG was higher at 75.6 %. The drug release profile of SG was examined in pH 7.4 PBS and 85 % of the SG loaded in SLNs was gradually released during 24 h. We used mice endotoxin shock model which was induced by lipopolysaccharide (1 mg/kg) to examine the anti-inflammatory function of SG-SLNs. Healthy Kunming mice were administered orally with saline, SG (10 mg/kg), and SG-SLNs (10 mg/kg), respectively, at 12 and 1 h before lipopolysaccharide (LPS) injection. Mice were sacrificed at 1 and 6 h, respectively, and blood was collect through the venous sinus to access inflammatory mediators. Pharmacokinetic studies proved that the AUC_0→24 and C _max of SG-SLNs were significantly increased compared that of SG. SG-SLNs revealed significant anti-inflammatory effects through inhibition of LPS-induced tumor necrosis factor-alpha level, interleukin 6 level, and nitric oxide production in serum. Therefore, it can be concluded that SG-SLNs led to a better oral bioavailability.     

Attenuation of Carbon Tetrachloride-Induced Hepatic Injury with Curcumin-Loaded Solid Lipid Nanoparticles

Background and Objectives

Curcumin, an established pleiotropic agent, has potential for hepatoprotection owing to its powerful antioxidant, anti-inflammatory, and antifibrogenic properties. However, its poor bioavailability limits its use in therapeutics. In this study, we aimed to package curcumin into solid lipid nanoparticles (C-SLNs) to improve its bioavailability and compare the efficacy of C-SLNs with that of free curcumin and silymarin, a well-established hepatoprotectant in clinical use, against carbon tetrachloride (CCl₄)-induced hepatic injury in rats, post-induction. A self-recovery group to which no treatment was given was also employed for quantifying self-healing of hepatic tissue, if any.

Material and Methods

C-SLNs (particle size 147.6 nm), prepared using a microemulsification technique, were administered to rats post-treatment with CCl₄ (1 ml/kg body weight [BW] twice weekly for 2 weeks, followed by 1.5 ml/kg BW twice weekly for the subsequent 2 weeks). The extent of liver damage and repair in terms of histopathology and levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), oxidative stress markers (malondialdehyde, superoxide dismutase, and reduced glutathione) and a pro-inflammatory response marker, tumor necrosis factor (TNF)-α, were determined in both the CCl₄ group and the treatment groups.

Results

C-SLNs (12.5 mg/kg) significantly (p < 0.001–0.005) attenuated histopathological changes and oxidative stress, and also decreased induction of ALT, AST, and TNF-α in comparison with free curcumin (100 mg/kg), silymarin (25 mg/kg), and self-recovery groups.

Conclusion

Curcumin could be used as a therapeutic agent for hepatic disorders, provided it is loaded into a suitable delivery system.     

载药纳米微球的制备和评价

含有有效药物的载药纳米粒子是一种新型的缓释系统,可改变常规的给药方式,有极广阔的发展前景。我们用超声的方法结合了不同的药物制成作用不同的纳米粒子,验证了纳米粒子对局部给药治疗的有效性,建立了良好的动物动脉摄取模型,为继续研究奠定了坚实的基础。     

Synthesis of Au@SiO2 Core/Shell Nanoparticles and their Dispersion into an Acrylic Photocurable Formulation: Film Preparation and Characterization

Au core/silica shell (Au@SiO₂) nanoparticles were synthesized by coating gold NPs with sol/gel silica in alcoholic solution. The alcoholic dispersion was added, in the range of 1–5 wt.‐%, to TPGDA and photocured by means of UV light. Transparent coatings were obtained and they can find suitable applications. It was shown that the NPs can restrict the segmental motion and decrease the free volume of the polymer network, with a consequent increase in glass transition temperature. TEM analysis put in evidence that the particles are well dispersed without any macroscopic agglomeration, and many particles are present as isolated particles.

     

Biodegradable Nanoparticles for Protein Delivery: Analysis of Preparation Conditions on Particle Morphology and Protein Loading,Activity and Sustained Release Properties

Abstract

PLGA particles have been extensively used as a sustained drug-delivery system, but there are multiple drawbacks when delivering proteins. The focus of this work is to address the most significant disadvantages to the W/O/W double emulsion procedure and demonstrate that simple changes to this procedure can have significant changes to particle size and dispersity and considerable improvements to protein loading, activity and sustained active protein release. A systematic approach was taken to analyze the effects of the following variables: solvent miscibility (dichloromethane (DCM), ethyl acetate, acetone), homogenization speed (10 000–25 000 rpm), PLGA concentration (10–30 mg/ml) and additives in both the organic (sucrose acetate isobutyrate (SAIB)) and aqueous (bovine serum albumin (BSA)) phases. Increasing solvent miscibility decreased particle size, dispersity and protein denaturation, while maintaining adequate protein loading. Increasing solvent miscibility also lowered the impact of homogenization on particle size and dispersity and protein activity. Changes to PLGA concentration demonstrated a minimum impact on particle size and dispersity, but showed an inverse relationship between protein encapsulation efficiency and particle protein weight percent. Most particles tested provided sustained release of active protein over 60 days. Increasing solvent miscibility resulted in increases in the percent of active protein released. When subjected to synthesis conditions with DCM as the solvent, BSA as a stabilizer resulted in the maximum stabilization of protein at a concentration of 100 mg/ml. At this concentration, BSA allowed for increases in the total amount of active protein delivered for all three solvents. The benefit of SAIB was primarily increased protein loading.     

Experiments on Alcocytes Containing Enzyme Nanoparticles for Reducing Toxic Blood Concentration of Ethanol

We developed a method of introduction of alcohol dehydrogenase and aldehyde dehydrogenase into mouse and human erythrocytes. The possibility of using erythrocytes loaded with the two enzymes (alcocytes) for reducing ethanol concentration in animal blood was studied. Injection of alcocytes to mice led to accelerated decrease in ethanol concentration as soon as after 5 min and this capacity of alcocytes persisted for at least 2 h. Alcocytes prepared from fresh or preserved human blood did not survive in mice. Thus autologous alcocytes is functionally active and can be used as a protective system in acute alcohol intoxication. The developed method can be regarded as a new medical biotechnology.     

mPEG-PLGA-mPEG纳米粒的体外降解规律的研究

通过开环共聚方法合成了具有不同组份的丙交酯 /乙交酯 /聚乙二醇 (LA/GA/PEG)共聚物 (PLGA PEG ,PELGA) ,并进一步偶联制得三嵌段共聚物 (mPEG PLGA mPEG ,简称PELGE)。采用超声乳化—溶剂蒸发法 (O/W )制备PELGE纳米粒 ,用紫外分光光度法测定乳酸含量的方法研究了PELGA、PELGE纳米粒体外降解规律 ,体外降解实验表明 :共聚物分子量增加 ,降解减慢 ;共聚物中GA含量增加 ,即LA/GA比例减小 ,降解加快 ;PEG含量增加 ,降解加快 ;LA/GA和PEG含量相同的PELGE比PELGA的降解速度快。证明了可通过改变LA/GA的比例或PEG的含量来调节聚合物的降解速率。