载表阿霉素聚乳酸微球的制备及性质研究

表阿霉素是广谱的抗肿瘤药物,为了减少给药量,降低药物的毒副作用,并达到缓慢释放的目的,本研究以Span-80和Tween-80复合乳化剂为初乳乳化剂,以聚乙烯醇水溶液为复乳乳化剂,采用复乳-溶剂挥发法制备了聚乳酸载药微球,并分别用激光粒度分析仪,光学显微镜,透射电子显微镜,扫描电子显微镜以及激光共聚焦显微镜对微球微观形态进行了表征.通过优化实验,所得载表阿霉素聚乳酸微球粒径2-5μm,载药率最高可达到4.39%,包封率达37.2%,72h体外累积释放量为34.9%,具有明显的缓释效果.本研究制备了表阿霉素缓释新剂型,为进一步的动物实验、临床实验和临床应用提供了有价值的参考数据,有很好的应用前景.     

洛伐他汀聚乳酸缓释微球的制备及其体外释药

采用油/水型乳化溶剂挥发法制备了洛伐他汀聚乳酸缓释微球,通过正交试验筛选最优制备工艺;考察了微球的粒径,形态,及载药量、包封率等特征,采用透析法进行微球体外释药研究。结果表明由最佳工艺制备的洛伐他汀聚乳酸微球形态圆整,粒径分布较为均匀。分子量5万聚乳酸制备的微球,载药量32.28%,包封率81.81%,平均粒径65.8μm ;分子量3万聚乳酸制备的微球,载药量27.66%,包封率60.84%,平均粒径63.3μm。二者在10d内体外累积释放率分别为34.81%和40.96%,释药动力学符合Higuchi方程。     

硫酸庆大霉素聚乳酸微球的制备及其体外缓释度的测定

以硫酸庆大霉素为囊心物质,采用复乳法制备了硫酸庆大霉素-聚乳酸微球（gentamycin sulfate-polylactic acid-microspheres,GTMS-PLA-MS）,比较了不同制备条件下所得微球的差异.扫描电镜（SEM）测试表明微球外观呈球形并且多孔,两种条件下制备的微球平均粒径分别为6.67 μm和11.70μm,药物包封率分别为37.52%和49.19%.用差热分析法（DTA）分析微球得知,硫酸庆大霉素与聚乳酸两种物质相互融为一体.以pH=7.4的磷酸盐缓冲溶液为释药介质,用紫外分光光度法（UV）对载药微球的体外释药过程进行了试验.结果表明,微球在最初20 min有突释效应,此后是缓慢释药,最终累积释药量达95%以上.     

改良复乳法（W/O/W）制备聚乳酸载药微球

在复乳法的基础上,研究了渗透压在制备微球过程中对微球形貌、突释效应和释药性能的影响.扫描电子显微镜(SEM)、结果表明,PLA-CEZ呈现完整的球形.体外释药曲线显示,表面多孔的载药微球具有明显的突释效应,此后是缓慢释放阶段.因此,可以通过改变微球的结构来控制头孢唑啉钠的释放.     

小檗碱聚乳酸微球的制备工艺及特性研究

采用溶剂挥发法制备小檗碱聚乳酸微球, 选择小檗碱与聚乳酸的投料比、二氯甲烷与水的体积比和乳化剂PVA的质量分数3个因素为实验因素,以包封率和载药量为优化指标, 采用L9(3⁴)正交试验优选最佳处方和制备工艺,测定微球的粒径分布、包封率,并进行体外释药试验。小檗碱聚乳酸微球的算术平均粒径为(53.0±3.5)μm(n=500),载药量为(8.96±0.3)%(n=3),药物包封率为(83.4±0.5)%(n=3),37℃时30d内微球体外累积释药量为82.03%。小檗碱聚乳酸微球球形圆整,释放良好,分子量2.5万左右的聚乳酸较适宜制作微球。     

聚乳酸头孢唑啉钠微球的制备及其释药性能

采用复乳法制备了聚乳酸--头孢唑啉钠(PLA-CEZ)微球.扫描电子显微镜(SEM)、差热分析(DTA)和红外光谱(FT-IR)的实验结果表明,PLA-CEZ呈现完整的球形且聚乳酸和模型药物能够有机地结合为一体.同时,探讨了聚乳酸分子量大小及释药介质对载药微球释放速率的影响.     

卡马西平微胶囊的超临界制备及溶出性能研究

为提高卡马西平药物的溶出性能,基于超临界流体注入(SFI)技术,先后开展了聚乳酸-羟基乙酸(PLGA)、聚乙二醇单甲醚-聚乳酸-羟基乙酸(MPEG-PLGA)聚合物包裹卡马西平的微胶囊制备实验。结合差示扫描量热法和红外光谱分析,探讨了卡马西平在微胶囊中的形态及其与聚合物分子间的作用,同时实测了相应的药物体外溶出性能。结果表明:该文所制PLGA及MPEG-PLGA载药微胶囊中,卡马西平药物分子均呈无定形状态,均匀分散于包裹剂中;MPEG-PLGA载药微胶囊内药物与聚合物分子间有较强的相互作用,其塑性优于PLGA载药微胶囊;以MPEG-PLGA为聚合物基体的微胶囊的药物溶出速率明显高于单纯以PLGA为基体的微胶囊,且外加的MPEG分子量越小、相应PLGA中n(LA):n(GA)越低越利于药物溶出速率的提高;为提高药物溶出速率,进行SFI时也可适当增加微胶囊的载药量,但不宜过高,当载药量从9.8%、28.3%升至35.8%时,卡马西平药物的溶出速率依次增大,但当载药量达45.2%时,对应微胶囊的溶出速率不升反降。     

白蛋白聚乳酸缓释微球的制备及体外释放研究

文章研究了复乳法制备聚乳酸-白蛋白复合微球和白蛋白的体外释放。以包封率为指标,通过正交实验优化制备工艺条件;对复合微球的大小、形态、负载率和体外释药进行了研究。结果表明制备的复合微球外观圆整,粒径主要分布在10~40μm,白蛋白的包封率为(85.25±2.5)%,负载率为(14.52±0.42)%。该复合微球在体外缓释白蛋白达27 d以上,主要通过扩散控释机制,缓释曲线符合Higuchi方程。     

透析法制备载羟基喜树碱-聚乳酸纳米粒及其理化性质研究

采用直接透析法制备载羟基喜树碱-聚乳酸(HCPT-PLA)纳米粒并研究其理化性质、体外释放和细胞毒性.以HCPT-PLA纳米粒的载药率为评价标准,通过正交设计考察PLA浓度、HCPT与PLA的质量比和不同截留分子质量透析袋对其指标的影响.利用Malvern nano-zs粒度测定仪、XRD、DSC和激光共聚焦显微镜(CLSM)对HCPT-PLA纳米粒的理化性质进行表征.薄膜透析法考察体外释药特性;MTT试验检测细胞毒作用.在优化条件下制备的载药纳米粒为实心球形,平均粒径为226.8 nm,多分散系数为0.270,载药率为7.49%.HCPT是以晶体状态均匀分布于PLA纳米粒中.药物体外释药符合Higuchi方程Q=2.000 6X1/2-2.593 4,r=0.989 2.MTT试验显示HCPT-PLA纳米粒呈现明显细胞毒作用.透析法制备HCPT-PLA纳米粒,粒径小且分布均匀,具有较好的缓释特性;细胞毒性试验表明HCPT-PLA纳米粒具有较强的抑瘤作用且抑瘤效果优于HCPT.     

血管内皮生长因子受体靶向的紫杉醇胶束的制备及其缓释效果

利用PLGA-PEG嵌段聚合物的两亲性质制备了3种不同PEG分子量的内部包载药物的血管内皮生长因子受体靶向胶束APRPG-PEG-M。通过对制剂粒径分布、zeta电位、包封率及载药量等方面的考察,确定处方和制备工艺,并考察其制剂学性质。制备的靶向胶束呈球形或类球形,粒径109.7~119.9nm、包封率89.2%~91.5%,在体外释药试验中48h累积释放量为47.8%~60.0%,表现出明显的缓释效果。制备的紫杉醇靶向胶束在体外对药物释放具有良好的缓释效果。     

聚乳酸-聚乙二醇嵌段共聚物及其交联聚氨酯弹性体的性能研究

通过改变聚乙二醇的用量,将丙交酯与聚乙二醇共聚制成嵌预聚体,用二苯基甲烷二异氰酸酯扩链后再用三羟甲基丙烷交联,制得系列聚氨酯型新颖性体。通过对其性能研究表明,随着ＰＥＧ含量的增加,共聚物的特性粘度降低,玻璃化转变温度降低,拉伸强度先升后降;聚氨酯弹性体的玻璃化转变温度降低,拉伸强度降低,而降解速度去加快。     

P(MMA-CO-BA)热敏型微胶囊的制备及性能研究

采用乳液聚合法,以染料隐色体为芯材,交联聚(甲基丙烯酸甲酯-丙烯酸丁酯)(P(MMA-CO-BA))为壁材,通过调整BA在共聚单体中的质量分数制备了具有不同玻璃化温度的交联P(MMA-CO-BA)热敏型微胶囊.利用粒度分布仪、扫描电镜(SEM)、热重分析(TG)仪、差示扫描量热(DSC)仪表征了微胶囊的粒径分布、形貌、热稳定性和玻璃转化温度.结果表明:所得微胶囊具有良好的热稳定性;微胶囊粒子分布均匀,呈规则的球形;共聚单体中BA质量分数增加,微胶囊的平均粒径减小;BA在共聚单体中质量分数为5.0%,10.0%和15.0%时,所得微胶囊的玻璃化温度分别为115.0,110.3和94.3 ℃.     

聚丙交脂-乙交酯纤维的温压成形

通过溶液沉析纺丝法制备聚丙交酯-乙交酯(PLGA)纤维,观察纤维的形貌并对其进行XRD和SEM表征.采用纤维温压成形法控制压力和温度得到条形的PLGA材料结合试样断口分析,研究成型压力与温度对PLGA材料的力学性能的影响.研究结果表明:非晶多孔结构的PLGA纤维可通过溶液沉析纺丝的方法获得,其孔径为0.1～ 1.0 μm;压制压力和压制温度对材料的力学性能影响较大,材料的抗弯强度、剪切强度和抗弯模量均随着温度和压力的增大而先增大后降低;在压制压力为105 MPa,压制温度为160 ℃时,试样的力学性能比较理想,此时,其抗弯强度可达到187.3 MPa,剪切强度达到100.1 MPa,抗弯模量达到2.5 GPa,可望作为非承重部位骨折愈合内固定材料.     

聚乳酸-聚扁桃酸共聚物的合成与表征

合成乳酸OCA和扁桃酸OCA单体,用DMAP引发乳酸OCA和扁桃酸OCA开环共聚合成可生物降解的聚乳酸-聚扁桃酸共聚物,通过调节聚合共聚单体的比例,可得到分子量从3 620¹1 800 g/mol不等的共聚物,实现了分子量可控的目的.使用1H NMR、GPC、DSC、TEM、XRD等手段对共聚物进行了表征,所得共聚物的热力学性能、降解性能等均得到改善.并对轮状病毒进行负载制备成载药微球,对其降解行为进行研究,为药物控制释放提供一类新的载体材料.     

用低聚乳酸作尿素缓释膜的研究

以乳酸合成的低聚乳酸作为包膜材料采用物理法对尿素进行包裹 ,制作包膜尿素 .介绍了低聚乳酸的合成原理、制备方法和分析测试方法 ,并讨论加热时间对数均分子量的影响 .浸泡实验结果表明 ,聚乳酸的分子量越高 ,缓释放效果越好 .     

Study of Synthesis of Copoly （lactic acid／glycolic acid） by Direct Melt Polycondensation

A two steps direct copolymerisation process was developed. The first step is to produce oligomer and then the oligomer of lactic acid/glycolic acid (90/10) is polymerized with binary catalyst tin chloride dihydrate/ptoluenesulfonic acid. In this way, the direct synthesis of copoly (lactic acid/glycolic acid) without any organic solvent was investigated. The properties and structures of products were characterized by nuclear magnetic resonance (NMR), differential scanning calorimetry (DSC), X-ray diffraction and so on. The results show that comparatively high molecular weight copolymer of lactic acid and glycolic acid can be prepared by direct processing under appropriate technological conditions.     

Electrochemical behavior of different shelled microcapsule composite copper coatings

Copper/liquid microcapsule composite coatings with polyvinyl alcohol (PVA), gelatin or methyl cellulose (MC) as shell materials were prepared by electrodeposition. The influence of shell materials on the corrosion resistance of the composite coatings in 0.1 M H₂SO₄ was investigated by means of electrochemical techniques, scanning electron microscopy (SEM), and energy dispersion spectrometry (EDS). The results show that the participation of microcapsules can enhance the corrosion resistance of the composite coatings compared with the traditional copper layer. Based on the analysis of electrochemical test results, the release ways of microcapsules were deduced. Gelatin and MC as the shell materials of microcapsules are easy to release quickly in the composite coating. On the contrary, the releasing speed of PVA microcapsules is relatively slow due to their characteristics.     

悬浮载体复合膜生物反应器过滤特性及滤饼层微结构特征

为研究悬浮载体复合式膜生物反应器(SCMBR)的膜过滤特性和膜表面滤饼层的微观结构特征,对SCMBR和传统膜生物反应器(CMBR)膜污染表面进行了对比分析.阻力构成分析表明,SCMBR滤饼层阻力所占总阻力比率在相同运行时间(15%,10 kPa,34 h)和跨膜压力(45%,30 kPa,89 h)下均小于CMBR(63.33%,34 h,30 kPa).污染膜表面扫描电镜分析表明,SCMBR反应器内膜表面滤饼层结构较疏松,孔隙较大.通过ISA3D软件对共聚焦显微镜图像进行分析,确定了滤饼层微观结构参数,结合Carman-Kozeny方程研究了SCMBR滤饼层阻力减小的机理.     

A new gelator based on tetraphenylethylene and diphenylalanine: Gel formation and reversible fluorescence tuning

A new gelator 1 based on tetraphenylethylene(TPE) and diphenylalanine was designed and synthesized.Compound 1 was non-emissive in solution,but its fluorescence turned on after the formation of gels,due to the aggregation-induced emission(AIE) feature of TPE.Interestingly,the fluorescence was reversibly switched "on-off" upon the "gel-sol" transition.Scanning electron microscope(SEM),confocal laser scanning microscope(CLSM) and X-ray diffraction(XRD) were employed to study the gels.     

Novel PLGGE graft polymeric micelles for doxorubicin delivery

Novel poly{(lactic acid)-co-[(glycolic acid)-alt-(L-glutamic acid)]}-g-monomethyl poly(ethylene glycol) (PLGGE) micelles were prepared and used as carriers for anti-tumor drug delivery. Three PEGylated PLGG copolymers (PLGGE2000, PLGGE1100 and PLGGE500) were characterized by XRD, TG and DSC. The critical micelle concentrations (CMCs) of the amphiphilic copolymers were 1.04, 0.55 and 0.13 μg/mL, respectively. The TEM, AFM and DLS measurements revealed that the micelles were homogeneous spherical nanoparticles with the diameters ranged from 50 to 150 nm when THF was used as solvent in the preparation of the micelles. Interestingly, extended cylindrical micelles were obtained using CHCl 3 as solvent. The micelles could trap doxorubicin (DOX) in the core with the highest drug loading content up to 23.7%. The mean diameter of drug loaded micelles was much bigger than that of blank micelles. The in vitro drug release of the micelles was diffusion-controlled release within the first 36 h and initial burst release was not obvious. However, after 36 h, the release rate in pH 5.0 was faster than that in pH 7.4 due to the degradation. The PLGGE micelles were nontoxic to both NIH 3T3 fibroblasts and HepG2 cells. The in vitro cytotoxicity against HepG2 cells demonstrated that the drug loaded micelles exhibited high inhibition activity to cancer cells. CLSM observation of HepG2 cells showed that DOX released from the micelles could be delivered into cell cytoplasm and cell nuclei. PLGGE micelles are potential promising carriers for anti-tumor drug delivery.