肝素/碳酸钙微囊的制备及其药物缓释性能

以药物HEP为有机基质,在CaCl2、Na2 CO3常温水溶液体系中制备碳酸钙微囊.分别采用SEM、流式细胞仪和紫外分光光度计等测试技术对微囊的形貌和结构进行了观察和表征.SEM结果表明,制备的HEP/CaCO3微囊平均直径为1.5μm,球形,分散性好;紫外分光光度法检测表明,微囊具有较高的药物装载量,肝素的包封率为80％;药物体外释放实验表明,HEP/CaCO3微囊的缓释性能受pH值的影响,在pH=1的PBS溶液中有明显的释放作用,随着释放溶液中pH值的减小,微囊的缓释效果越明显.本实验方法操作简单,所制备的药物微囊装载量高,在药物控释领域具有潜在的应用价值.     

碳酸钙纳米结构多孔空心微球的制备及其药物缓释性能研究

以CaCl2和Na2CO3为反应物,十二烷基硫酸钠(SDS)为表面活性剂,在室温水溶液中制备了纳米结构碳酸钙空心球.用TEM和SEM对其进行形貌观察发现,所制备的碳酸钙空心球的球壁由纳米粒子组成,具有多孔形貌特征.分别在模拟胃液(pH＝1.2)以及模拟肠液(pH＝7.4)中对制备的纳米结构碳酸钙空心球进行了药物装载和缓释性能的研究,选用的药物为布洛芬(IBU).研究结果表明,IBU/CaCO3多孔空心微球药物传输体系具有较高的药物装载量和良好的药物缓释性能,纳米结构碳酸钙空心球中IBU的装载量可以达到195mg/g,且连续释药时间能持续53h以上;除去表面活性剂后,载体中IBU的装载量可达到130mg/g,药物释放率为100%时,持续释药时间可达到40h.纳米结构碳酸钙多孔空心球作为药物载体材料在药物缓释体系中具有潜在的应用前景.     

Preparation and In Vitro Evaluation of Chitosan Microspheres Containing Prednisolone: Comparison of Simple and Conjugate Microspheres

The purpose of the present study was to obtain a novel microparticulate formulation of prednisolone, which was adequate for the treatment of inflammatory bowel disease (IBD). The formulations prepared were evaluated in vitro. Two types of chitosan microspheres containing prednisolone, named Ch-Pred and Ch-SP-MS, were prepared by an emulsification-solvent evaporation method using a chitosan-prednisolone mixture and a chitosan-succinyl-prednisolone conjugate (Ch-SP), respectively. Ch-Pred and Ch-SP-MS were obtained in almost spherical shape. Ch-Pred showed a relatively high drug content of 13.2% (w/w), but the particle size was distributed from 10 to 45 µm, and a large initial burst release of approximately 60% was observed. On the other hand, although Ch-SP-MS exhibited a fairly low drug content of 3.5% (w/w), their particle size ranged from several hundred nanometers to 20 µm, with the mean diameter of 5 µm, and a gradual drug release profile was achieved. These characteristics on particle size and in vitro release suggested that Ch-SP-MS should have good potential as a microparticulate system for the treatment of IBD.     

SA／GT／CS复合水凝胶载药微球的制备与药物释放性能研究

将海藻酸钠/明胶/盐酸四环素共混液滴入含有CaCl2的壳聚糖醋酸溶液中,制备出SA/GT质量配比分别为10/0.6、10/0.8、10/1.0的SA/CS/GT复合水凝胶载药微球,考察了模拟肠液和胃液中不同原料配比对载药性能的影响.结果表明,在配比为10/0/8下微球具有最大载药量,模拟肠液中水凝胶微球释放药物周期较长.因此,SA/CS/GT三元复合水凝胶微球由于其良好的控制释放和降解性能,将是口服释药系统的一种优良载体.     

静电喷雾法制备壳聚糖/康普瑞丁载药微球

本研究采用静电喷雾法,以壳聚糖为基质材料,康普瑞丁为模型药物制备微球。实验中采用AcOH/H2O和AcOH/H2O/EtOH两种溶剂,分析了微球形貌和粒径分布的影响因素,并且对CS-CA4微球的缓释性能进行了测定。结果表明,壳聚糖浓度、溶剂配比及乙醇和康普瑞丁的加入会使壳聚糖微球呈球状、中间塌陷的类球状、棒状等不同形貌,微球粒径存在较大差异;通过AcOH/H2O/EtOH复合溶剂将疏水性药物康普瑞丁载入壳聚糖微球,制备出的壳聚糖/康普瑞丁载药微球分散性好,粒径分布均匀,平均粒径仅为0.27μm;使用戊二醛蒸汽交联48h的微球缓释效果明显。     

4-羧酸正辛酯基-4′-正辛氧基偶氮苯液晶的性能研究

以4-羧基-4′-羟基偶氮苯为母体,与正溴辛烷同时发生酯化和醚化反应,合成了一种新型偶氮苯液晶化合物——4-羧酸正辛酯基-4′-正辛氧基偶氮苯,其结构采用红外光谱(FT-IR)和核磁共振氢谱(1 H NMR)进行表征。采用360nm和440nm的紫外-可见光交替照射,该偶氮苯液晶在乙醇溶液中能够发生顺反光异构化反应,经重复照射10次,其紫外吸收峰均能回复至最初状态。通过差示扫描量热仪(DSC)和偏光显微镜(POM)研究发现,该偶氮苯液晶为热致互变液晶,显示扇形织构的近晶相,并且易于汇集形成马尔他十字液晶相。     

Carnauba Wax Microspheres Loaded with Valproic Acid: Preparation and Evaluation of Drug Release

Abstract

To minimize unwanted toxic effects of valproic acid (1) by the kinetic control of drug release, gastroresistant carnauba wax microspheres loaded with the antiepileptic agent were prepared. The preparation was based on a technique involving melting and dispersion of drug-containing wax in an aqueous medium. The resulting emulsion after cooling under rapid stirring produced solid, discrete, reproducible free flowing microspheres which converted the liquid drug droplets into solid material. About 94% of the isolated microspheres were of particle size range 200-425 μm. The microspheres were analyzed to determine the drug content in various particle size range and to characterize the in vitro release profile. The average drug content was 26% w/w. The intestinal drug discharge of 1 from the carnauba wax microspheres was studied and compared with the release patterns observed for white beeswax and hexadecanol microspheres previously described. The drug release performance was greatly affected by the material used in the microencapsulation process. In the intestinal environment carnauba wax microspheres exhibited more rapid initial rate of release and about 80% of the entrapped drug was discharged in 120 min while complete release occurred in about 8 h.     

Carnauba Wax Microspheres Loaded with Valproic Acid: Preparation and Evaluation of Drug Release

To minimize unwanted toxic effects of valproic acid (1) by the kinetic control of drug release, gastroresistant carnauba wax microspheres loaded with the antiepileptic agent were prepared. The preparation was based on a technique involving melting and dispersion of drug-containing wax in an aqueous medium. The resulting emulsion after cooling under rapid stirring produced solid, discrete, reproducible free flowing microspheres which converted the liquid drug droplets into solid material. About 94% of the isolated microspheres were of particle size range 200-425 μm. The microspheres were analyzed to determine the drug content in various particle size range and to characterize the in vitro release profile. The average drug content was 26% w/w. The intestinal drug discharge of 1 from the carnauba wax microspheres was studied and compared with the release patterns observed for white beeswax and hexadecanol microspheres previously described. The drug release performance was greatly affected by the material used in the microencapsulation process. In the intestinal environment carnauba wax microspheres exhibited more rapid initial rate of release and about 80% of the entrapped drug was discharged in 120 min while complete release occurred in about 8 h.     

壳聚糖微球的制备及其对防污剂Sea-Nine 211缓释性能的研究

采用乳化交联法中的复乳法(o/w/o型)制备负载Sea-Nine 211的壳聚糖(CS)微球,并用扫描电镜和红外光谱对其结构及形貌进行了表征。应用正交试验设计,考察了壳聚糖浓度、投料比、交联剂浓度对微球制备的影响。载有疏水性防污剂Sea-Nine 211的壳聚糖微球的包覆率和缓释性能都比较良好,缓释的防污剂对海洋硅藻三角褐指藻的生长有抑制作用。     

壳聚糖/PHB复合缓释微包囊的制备与体外释药评价

用疏水性聚酯PHB外包覆壳聚糖-三聚磷酸钠-阿斯匹林药物缓释体(CPA)制备了壳聚糖/PHB复合缓释微包囊(CPAB),以克服CPA遇酸不稳定的释药特点.用傅立叶红外分光光度计、激光粒度仪、扫描电镜表征了CPAB的组成、粒径及表面形貌.结果显示,CPAB粒径在50～100nm和载药率18.5%时,表面有不均匀的空隙.体外释药评价证实CPAB能有效解决CPA在酸性下的不稳定性,具有长效缓释作用.     

PLLA-PEG-PLLA/Fe_3O_4磁性微球的制备及性能

以聚乙二醇为引发剂,L-丙交酯为单体,开环聚合得到聚乳酸-聚乙二醇三嵌段共聚物(PLLA-PEG-PLLA),采用溶剂挥发法制备了PLLA-PEG-PLLA/Fe_3O_4磁性微球,并通过扫描电镜对其形态进行了表征。利用振动样品磁强计和Tg研究了微球的磁含量和磁性能,结果发现,相同粒径不同磁含量的磁性微球,磁含量越高,升温速率越快,当磁含量为70.57%时,升温速率最快,能达到磁热疗的有效温度42℃。对于磁含量相同,粒径不同的微粒,粒径越小,升温速率越快,粒径约为10μm时升温速率最快。     

壳聚糖水凝胶的制备及其在药物释放中的应用

水凝胶作为性能良好的载体,在药物的控释、组织工程等领域有着广泛的应用。壳聚糖是一类天然的带正电荷的碱性多糖,由其形成的水凝胶具有较好的生物相容性、生物降解性、抗菌和低细胞毒性,因此,壳聚糖水凝胶有着良好的生物应用前景。本文综述了壳聚糖水凝胶的制备方法(包括物理交联法和化学交联法),在物理交联法部分着重介绍了离子化合物及聚电解质分子与壳聚糖通过离子交联形成水凝胶,以及利用分子链间的疏水作用形成壳聚糖水凝胶的方法;而在化学交联法部分介绍了合成壳聚糖水凝胶的化学手段,包括交联剂、光照辐射和酶的使用。继而概述了壳聚糖水凝胶在药物缓释应用方面的研究进展,包括温度、pH值和电场响应的药物控释体系。最后展望了壳聚糖水凝胶未来的发展前景。     

预交联法制备海藻酸钠复合微球及其缓释性能

采用预交联法制备海藻酸钠(SA)/凹土(ATP)复合微球(PCM)以克服常规制备方法导致微球交联不均匀的缺陷,从而改善微球的缓释性能。将ATP先与Ca~(2+)进行部分离子交换制备Ca~(2+)-ATP,然后在与SA复合过程中同时进行预交联形成交联密度有所提高的微球内核,再采用滴注法制备该复合微球。利用红外光谱、扫描电镜和电子照片对微球结构和形貌进行表征,考察了Ca~(2+)浓度对PCM力学强度、溶胀率、载药和缓释性能的影响。结果表明,PCM在1h的累计释放率由预交联前的68%降为50%,显著改善了微球的"突释"。释放动力学研究表明,微球的释药可用Ritger-Peppas方程很好地拟合,释药速率受骨架溶蚀和药物扩散双重控制。     

负载对苯二酚的聚苯乙烯-二乙烯苯交联微球的制备及缓释行为(英文)

采用超声波改进的二步种子溶胀法制备粒径2.4～9μm的多孔聚苯乙烯-二乙烯苯微球,单分散的聚苯乙烯微球由分散聚合制备并以其作为种球。论文考察了种球类型、超声分散时间、种球和溶胀剂以及交联单体比率等因素对多孔微球形貌及孔结构的影响,并采用扫描电镜、BET等手段对微球性能进行了表征。研究发现超声辅助分散的引入可使产物的粒径分布更窄并将第一步溶胀时间由传统的24h缩短至10h。实验结果表明:种球的单分散性对最终产物的形貌有决定性影响,它的任何形貌缺陷都将在最终产物中被扩大;随着溶胀剂/种球比率和交联单体/种球比率的增加,最终产物的粒径和比表面积增大,孔径减小。以对苯二酚为模型组分,考察其在制得的多孔微球上的缓释行为,发现制得的多孔聚合物微球在用作化妆品活性组分载体时,表现出良好的缓释性能。     

单分散聚(苯乙烯-丙烯酰胺)高分子微球的制备及性能

以苯乙烯和丙烯酰胺为单体,过硫酸钾为引发剂,采用乳液聚合法,制备了单分散表面富含酰胺修饰的苯乙烯聚合物功能微球(PSAM),采用红外光谱(FT-IR)、热重分析(TGA)和透射电镜(TEM)对样品进行表征,并研究了微球的制备条件以及形成和热稳定性增强机理。结果表明,产物微球表面富含氨基功能基团,通过乳液聚合,可制得粒径分散均一、表面光滑和热稳定性较高的单分散功能高分子微球。     

Effect of fullerene intercalation on the conformation and packing of poly-(2-methoxy-5-(3'-7'-dimethyloctyloxy)-1,4-phenylenevinylene)

Photoluminescence (PL) and resonance Raman spectroscopy are used to track changes in the conformations and packing of poly-(2-methoxy-5-(3'-7'-dimethyloctyloxy)-1,4-phenylenevinylene) (MDMO-PPV) chains with the addition of [6,6]-phenyl-C(61)-butyric acid methyl ester (PCBM) molecules. PL lineshapes of MDMO-PPV thin films as a function of annealing time were first measured to determine the spectroscopic signatures of chain conformations and packing in the absence of PCBM. Annealing results in enhanced interchain interactions leading to red-shifts of PL 0-0 transitions by up to ～300 cm(-1) and apparent increases of the line shape Huang-Rhys factors. Wavelength-dependent PL lifetimes of as-cast and films annealed for short times (～30 s) are nonexponential with an instrument-limited component of ～100 ps and a ～350 ps component. With longer annealing times, decays become single exponential with an average lifetime of ～1 ns indicating that all excitations efficiently funnel to strongly coupled interchain sites. Addition of PCBM disrupts MDMO-PPV interchain interactions causing PL 0-0 transitions to blue-shift, increases in line width, and decreases in apparent Huang-Rhys factors. Resonance Raman spectra of MDMO-PPV/PCBM thin films with variable PCBM weight fractions (～50:1 up to 1:8 w/w) were then measured using short (488 nm) and long (568 nm) excitation wavelengths. The out-of-plane vinylene C-H wag mode of MDMO-PPV (～964 cm(-1)) showed pronounced increases in intensity of up to ～30% and red-shifts of up to 5 cm(-1) with increasing PCBM content. These changes result from a decrease of planarity between chain segments that suppresses interchain interactions. Furthermore, red-shifts of up to ～4 cm(-1) were observed for the C═C symmetric stretch of the MDMO-PPV vinylene group (～1625 cm(-1)) with 488 nm excitation. The sensitivity of the MDMO-PPV vinylene group vibrations with PCBM indicates preferential interactions between these two molecules and is consistent with intercalation of PCBM into the polymer structure. This assignment was confirmed by thermally annealing of MDMO-PPV/PCBM films to remove intercalated PCBM molecules, which partially restores interchain interactions as seen from smaller intensity increases (～15%) and red-shifts (～2 cm(-1)) of the ～964 cm(-1) mode. Overall, the spectroscopic results show that MDMO-PPV chains adopt distorted conformations (i.e., less intrachain order and shorter conjugation lengths) that have important implications for explaining the structural origins for large improvements in charge mobilities in MDMO-PPV/PCBM blends.     

Phen-Fe_3O_4/PLA-PEG-PLA微球的制备、表征及体外释放行为

采用微波合成的PLA-PEG-PLA和单微乳法制备的纳米Fe3O4为载体,以邻菲罗啉(1,10-Phenanthro-line,Phen)为释放模型药物,通过乳化-溶剂挥发法制备了Phen-Fe3O4/PLA-PEG-PLA微球。通过傅里叶变换红外光谱(FT-IR)、核磁共振波谱(1 H-NMR)、X射线衍射(XRD)、扫描电子显微镜(SEM)对PLA-PEG-PLA及磁性微球的结构进行了表征分析。结果表明,微波法合成的PLA-PEG-PLA是一种三嵌段共聚物,载药微球呈规则球形,表面光滑,粒径分布较均匀。体外释放行为表明PLA-PEG-PLA作为载药基质具有明显的缓释性能。     

红色荧光粉BaZn2(PO4)2:Eu3+的制备及其光谱特性

采用高温固相法制备了BaZn2(PO4)2:Eu3+红色荧光材料.测量了BaZn2(PO4)2:Eu3+材料的激发与发射光谱,激发峰位于360-400nm之间,发射光谱主峰位于595nm处.研究了BaZn2(PO4)2:Eu3+材料在595nm的主发射峰强度随Eu3+浓度的变化,发射峰强度先随Eu3+浓度的增加而增大;...     

聚乳酸多孔微球的制备及释药性能

将聚乳酸(PLLA)/四氢呋喃(THF)溶液分散在甘油(连续相)中,通过自乳化结合热致相分离(TIPS)制备一系列PLLA多孔微球,微球由捆束状纳米纤维组成。通过改变PLLA浓度、(PLLA/THF)∶甘油比值、溶剂种类以及淬火温度等条件研究所得多孔微球结构与形貌。结果表明,PLLA的质量分数为2%~5%、m(PLLA/THF)∶m(甘油)=1∶3、-20℃和-196℃淬火均能得到形状规整的PLLA多孔微球。多孔微球孔隙率和比表面积最高可达95.44%和32.53m2/g。PLLA多孔微球对牛血清蛋白的药载量为0.355 mg/mg,30 h内释放率达到59.8%,是一种非常良好的药物缓释载体。