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??OBJECTIVE To prepare smart & site-specific drug carrier for controlled release purpose and study the bio-compatibilities and release performance.METHODS By using high pressure thermo-heat method in autoclave, superparamagnetic core was obtained and further coated by SiO₂ and MCM-41, therefore the ??core-shell?? structure was formed. To make the carrier ??smart?? and thus responsive to stimuli which was light in this research, the tunnels of the molecular sieve were grafted with gating molecules, 4,5-diazafluoren-9-one (indicated in the paper as DAFO). For bio-compatibilities testing, MTT in-vitro experiment was conducted. Cytarabine was used as test drug to preliminarily evaluate the controlled release performance of the drug carrier in vitro.RESULTS The Fe₃O₄ nano-particles synthesized via high-pressure hydro-thermo procedure exhibited superparamagnetic with mean diameter of 280 nm. After SiO₂ & molecular sieve coating steps and ligand grafting steps, the particles grew to 540 nm. The sub-structure of the carrier was confirmed by scanning/transmission electron microscope(SEM & TEM) and nitrogen adsorption/desorption. Our ??smart?? carrier was able to be guided to the sites or organs with magnetic field and more importantly it was able to unload drug molecules under 510 nm light irritation that could flip the gating-molecule. Furthermore, the drug carrier illustrated bio-compatibility and showed obvious cytotoxicity.CONCLUSION The novel nanocomposites developed in this study can be used as targeted drug carrier.     

柚皮素-PLGA纳米粒的制备及其体内药动学研究

目的 制备柚皮素-PLGA纳米粒,并考察其体内药动学.方法 纳米沉淀法制备PLGA纳米粒,在单因素试验基础上采用正交试验优化处方,测定包封率、载药量、粒径、Zeta电位、体外释药.大鼠分别灌胃给予柚皮素及其PLGA纳米粒混悬液(40 mg/kg)后采血,HPLC法测定柚皮素血药浓度,计算主要药动学参数.结果 最佳处方为...     

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??OBJECTIVE To prepare calcitonin/puerarin-PLGA-dual-loaded nanoparticles modified by chitosan, and investigate theirin vitro release behavior.METHODS CS-CT/PR-NPs were prepared by the double emulsion solvent evaporation technique with PLGA as a carrier material; the formulation of CS-CT/PR-NPs was optimized by orthogonal design; the morphology of CS-CT/PR-NPs was observed by transmission electron microscope;the mean particle size,particle size distribution and Zeta potential were measured by laser particle size analyzer; the entrapment efficiency and drug loading were measured by ultracentrifugation; the in vitro release behavior was studied by dialysis. RESULTS CS-CT/PR-NPs were spherical in shape with the mean particle size of(190??2.65) nm, particle size distribution of (0.117??0.027) and Zeta potentialof(16.5??1.08) mV. The entrapment efficiency was (75.7??1.15)%, and the drug loading of CT was (3.47??0.31)%, while those of PR were (50.9??1.08)% and (4.68??0.19)%, respectively. The profiles of in vitro release had the features of sustained-release. CONCLUSION CS-CT/PR-NPs are prepared successfully and show a sustained-release characteristic with high entrapment efficiency, which may improve the oral bioavailability of CT and provide the experimental reference for preparing the dual-loaded nanoparticles.     

2种方法制备丹参酮ⅡA-PLGA纳米粒的比较

目的：考察并优化丹参酮Ⅱ_A-PLGA纳米粒的制备工艺,比较2种制备方法对纳米粒成型及其质量的影响。方法：采用纳米沉淀法和乳化溶剂蒸发法制备纳米粒,并对制得的纳米粒进行质量评价及比较,包括粒径、形态、载药量、包封率、药物利用率、晶型及体外释放行为。结果：沉淀法和乳化溶剂蒸发法制备的纳米粒平均粒径分别为225 nm和183 nm,包封率分别为95.49%和87.99%、载药量分别为2.03%和0.16%、药物利用率分别为38.42%和17.59%。结论：沉淀法制备丹参酮Ⅱ_A-PLGA纳米粒的效果优于乳化溶剂蒸发法。     

溴化双十二烷基二甲基铵修饰的载汉防己甲素聚乳酸-羟基乙酸共聚物纳米粒制备及体外评价

目的 制备溴化双十二烷基二甲基铵(DMAB)修饰的载汉防己甲素(Tet)的聚乳酸-羟基乙酸共聚物(PLGA)纳米粒(DMAB-Tet-PLGA-NPs),考察其制备的影响因素,优化制备工艺,并对其理化性质、细胞毒性及细胞摄取进行研究。方法 采用乳化分散溶剂挥发法制备DMAB-Tet-PLGA-NPs,运用均匀设计试验优化制备工艺,通过包封率、载药量、累积释药量等指标考察其载药特性;采用MTT比色法考察DMAB-Tet-PLGA-NPs对人肺腺癌细胞株A549的细胞毒性;采用定量定性法评价DMAB-Tet-PLGA-NPs细胞摄取率。结果 制备的DMAB-Tet-PLGA-NPs平均粒径为(205.40±2.66)nm,表面带正电,呈规则的球形及椭圆形。药物包封率和载药量分别为(50.780±3.253)%和(2.130±0.035)%。体外释放实验显示DMAB-Tet-PLGA-NPs缓慢释药,48 h累积释药量64.56%。MTT实验表明DMAB-Tet-PLGA-NPs细胞毒性呈剂量及时间依赖性。定性定量细胞摄取实验证实DMAB-Tet-PLGA-NPs能较好地被细胞摄取。结论 DMAB-Tet-PLGA-NPs粒径大小均一,包封率高,体外释药表现出较好的缓释效果,易被细胞摄取,对A549细胞的活性有明显的抑制作用。     

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??Multidrug resistance (MDR) is one of the major obstacles for successful chemotherapy in cancer. Inorganic material-based nanoparticles provide a novel choice to effectively circumvent the intrinsic drawbacks of traditional organic materials in overcoming the multidrug resistance (MDR) of cancer cells due to their unique structural and compositional characteristics,for example,high stability,large surface area,tunable compositions,abundant physicochemical multifunctionalities,and specific biological behaviors. In this work,the recent advances of inorganic materials-based nanoparticles to overcome MDR of cancer cells were reviewed. And the advantage and mechanism of inorganic materials-based nanoparticles to overcome MDR were summarized. The recent development of inorganic materials-based nanoparticles (mesoporous SiO₂,Au,TiO₂,magnetic Fe₃O₄,Ag,combinations of inorganic materials-based nanoparticles with traditional overcoming MDR strategy etc.),to overcome the MDR were also discussed. And the future developments of these inorganic materials-based nanoparticles are suggested. These elaborately designed inorganic materials-based nanoparticles offer an unprecedented opportunity and show the encouraging bright future for overcoming the MDR of tumors.     

基于PEG-PLGA和CMCS载体制备白藜芦醇纳米粒在结肠癌治疗中的应用＊

目的 为了提高白藜芦醇（Resveratrol，RES）的生物利用度,将其制备成纳米粒子，并研究其体外抗结肠癌的作用。方法 分别以聚乙丙交酯聚乙二醇共聚物（PEG-PLGA）和羧甲基壳聚糖（Carboxymethyl chitosan，CMCS）作为药物载体，采用纳米沉淀法和乳化交联法分别制备了PEG-PLGA共载白藜芦醇纳米粒（RES-PEG-PLGA NPs）和CMCS共载白藜芦醇纳米粒（RES-CMCS NPs），利用紫外分光光度计、激光粒度分析仪和透射电子显微镜等仪器对纳米粒的理化性质进行表征；采用CCK-8检测法测定纳米粒对人结肠癌细胞（SW480）的抗增殖活性，并通过荧光显微镜考察了纳米粒在SW480细胞中的摄取。结果 RES-PEG-PLGA NPs粒径为78.67 ± 1.0 nm，包封率为87%；RES-CMCS NPs粒径为231 ± 1.6 nm,包封率为60%。结论 两种纳米粒在模拟肿瘤微环境下均能实现白藜芦醇的缓释，都可以有效地被SW480细胞摄取，并且对SW480细胞表现出较高的抑制作用。     

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??OBJECTIVE To establish a method for determination of the entrapment efficiency of coumarin 6-loaded PLGA nanoparticles by high-speed centrifugation. METHODS The nanoparticle suspensions were diluted by different vehicles, and free drugs were then separated by high-speed centrifugation. The separation effect for free drug and nanoparticles as well as the effect of diluting solvent on nanoparticles morphology were observed by scanning electron microscopy. The method was validated and the determination condition was optimized. RESULTS The calibration curve for coumarin 6 had good linearity in the range of 0.8-100 ng(r=1.000 0), and the precision were high with RSD??1.28%. After diluting the nanoparticle suspensions with 1% TPGs, high-speed centrifugation could effectively separate the free drug from nanoparticles. The recovery of free drug was 99.25%-103.00%. The average entrapment efficiencies of coumarin 6-loaded nanoparticles was 88.74% with RSD of 0.65%. CONCLUSION The method is rapid, accurate and feasible. It can be used to determine the entrapment efficiency of coumarin 6-loaded PLGA nanoparticles.     

Composition of eye cosmetics (kohls) used in Oman

A total of 47 kohl samples, primarily used as traditional eye cosmetics, were analyzed using X-ray powder diffraction (XRPD) and scanning electron microscopy (SEM). It was found that, of the 18 Omani-made kohls, the main component of five was galena (PbS). Of the other 13, 12 were based on amorphous carbon and one on hematite (Fe₂O₃). The remaining samples were made in other countries and were found to contain one of the following as the main component: galena, minium (Pb₃O₄), amorphous carbon, magnetite (Fe₃O₄), zincite (ZnO), calcite (CaCO₃) or sassolite (H₃BO₃).     

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??OBJECTIVE To synthesize immunomagnetic nanoparticles with uniform particle size, strong superamagnetism as well as strong immune activity which can be specifically and sensitively combined with circulating tumor cells in peripheral blood of patients with breast cancer.METHODS Superparamagnetic oxide iron nanoparticles containing active carboxyl groups (SMNP-COOH) were synthesized by polyol methods, thermogravimetric analysis was used to determine the amount of carboxyl groups on the surface of SMNP-COOH, while the content of iron was determined by o-phenanthroline. Mediated by 1-ethyl-3,3-dimethylaminopropyl carbodiimide(EDC) and N-hydroxysuccinimide (NHS), immunomagnetic nanoparticles(IMNP) against human breast carcinoma cell line were constructed by binding the monoclonal antibodies against hMAM with SMNP-COOH. X-Ray diffraction was used to confirm their synthesis,meanwhile,transmission electron microscope (TEM), dynamic light scattering (DLS), and vibrating sample magnetometry (VSM) were applied to characterize their physicochemical properties. The conjugation amount of the antibodies and the activity of IMNPs were evaluated by enzyme linked immunosorbent assay (ELISA).RESULTS X-Ray diffraction showed that the chracteristic peaks of the crystalline powder of SMNP-COOH and IMNP agreed with the Fe₃O₄ standard. The concentration of iron in SMMP-COOH and IMNP were 0.205 and 0.164 mol??L^-1, respectively.TEM showed that both synthesized SMNP-COOH and IMNP were almost spherical or ellipsoidal. The sizes of SMNP-COOH and IMNP were (13.7??3.6) and (15.4??4.5) nm, respectively. Dynamic light scattering(DLS) demonstrated the intensity particle size and polydispersity index (PDI) of SMNP-COOH and IMNP were 23.4 nm and 0.303, and 71.2 nm and 0.175,respectively. VSM results showed that both SMNP-COOH and IMNP had strong superamagnetism, and the saturation magnetization of SMNP-COOH and IMNP were 71.37 and 67.68 emu??g^-1Fe, respectively, which confirmed antibody binding may reduce the magnetism of SMNP-COOH. The ELISA results showed the conjugation amount of antibody was about 93 ??g on 1 mg SMNP-COOH by covalent bond. The obtained immunomagnetic nanoparticles (IMNP) which were bound with the hMAM monoclonal antibodies could specifically and sensitively combine with breast cancer cell line MDA-MB-415.CONCLUSION IMNP with strong superparamagnetic property,excellent stability and perfect antibody activity were successfully synthesized, which demonstrate the potential to magnetically separate circulating tumor cells in peripheral blood from patients with breast cancer, thus providing a favorable weapon to accurately detect CTCs in breast tumor patients.