Preparation and Characterization of Carboxymethyl Chitosan and β-Cyclodextrin Microspheres by Spray Drying

Three kinds of carboxymethyl chitosan/β-cyclodextrin microspheres loaded with theophylline were prepared by spray drying intended for pulmonary delivery. Mucociliotoxicity, permeation rate, and drug release characteristics of the product were investigated. The microspheres obtained by spray drying were found to be spherical with smooth or wrinkled surfaces. The mean particle size was between 3.39 and 6.06 µm. The microspheres demonstrated high product yield (43.7–50.2%), high drug loading (13.7–38.1%), and high encapsulation efficiency (86.9–92.8%). FT-IR indicated that there were interactions of theophylline with carboxymethyl chitosan matrix. Further studies on mucociliotoxicity and permeation confirmed that microspheres had better adaptability and high permeation rate. In vitro drug release from the microspheres was not related to the drug/polymer ratios.     

Formulating Drug Delivery Systems by Spray Drying

The knowledge of the potential use of the spray-drying technology to prepare microparticulate drug delivery systems—microspheres and microcapsules—has been strongly improved over the last years. Various microparticulate spray drying systems used as vehicles for drug encapsulation and delivery that have been investigated for different purposes are presented here, including spray-dried powders formulated with hydrophilic polymers allowing controlled drug release, biodegradable microspheres prepared from aqueous systems, and spray-dried silica gel microspheres.     

羧甲基壳聚糖的制备与性能研究

以壳聚糖为原料制备了羧甲基壳聚糖,考察了NaOH用量、一氯乙酸用量、反应时间和反应温度对羧甲基壳聚糖取代度的影响,得出羧甲基化的最佳条件为：壳聚糖／一氯乙酸／氢氧化钠（m／m）=1：3．2：4,反应时间为3h,反应温度为60℃,制得产物的水溶性有较大提高,并利用红外光谱对产物结构进行了表征。     

Drug Release Kinetics of Spray-Dried Chitosan Microspheres

The aim of this article was to investigate the drug release kinetics of spray-dried chitosan microspheres using various kinetic models. The mean particle size and encapsulation efficiency of cross-linked chitosan microspheres was between 3.8 and 4.2 μm and 96.3 and 98.7%, respectively. Spray-dried chitosan microspheres were spherical in shape with smooth surface. The surface morphology of spray-dried chitosan microspheres was affected by the crystallinity of the loaded drug and cross-linking agent. The release data of the spray-dried chitosan microspheres were treated with zero-order, first-order, Higuchi, Korsmeyer, and Kopcha kinetic models and best fit was observed with Higuchi model, indicating the release of drug from spray-dried chitosan microspheres followed Fick's law of diffusion.     

Drug Release Kinetics of Spray-Dried Chitosan Microspheres

The aim of this article was to investigate the drug release kinetics of spray-dried chitosan microspheres using various kinetic models. The mean particle size and encapsulation efficiency of cross-linked chitosan microspheres was between 3.8 and 4.2 μm and 96.3 and 98.7%, respectively. Spray-dried chitosan microspheres were spherical in shape with smooth surface. The surface morphology of spray-dried chitosan microspheres was affected by the crystallinity of the loaded drug and cross-linking agent. The release data of the spray-dried chitosan microspheres were treated with zero-order, first-order, Higuchi, Korsmeyer, and Kopcha kinetic models and best fit was observed with Higuchi model, indicating the release of drug from spray-dried chitosan microspheres followed Fick's law of diffusion.     

Fe_3O_4/羧甲基壳聚糖磁性载药微球的制备及释药性能

通过乳化交联法制备了负载有抗癌药物5-氟尿嘧啶的Fe3O4/羧甲基壳聚糖磁性载药微球。利用红外光谱(IR)和扫描电镜(SEM)对载药微球的结构与形貌进行了表征,研究了影响载药微球载药和释药性能的因素。IR测试显示载药微球中含有磁性Fe3O4;SEM照片显示载药微球尺寸均一,表面光滑。确定制备磁性载药微球的最佳条件为:5-氟尿嘧啶0.5g、磁性Fe3O40.2g、戊二醛8mL;磁性载药微球在温度为35~40℃、pH值为5.2的缓冲溶液中释药量达到峰值,适用于人体十二指肠肿瘤的治疗。     

羧甲基壳聚糖对Fe2+的络合及光谱分析

本文研究羧甲基壳聚糖对Fe^2＋的吸附性能,探讨了时间、PH值等对吸附性质的影响.PH=6时羧甲基壳聚糖对Fe^2＋最大吸附量为0.7mmol/g.并通过IR和UV光谱证实了羧甲基壳聚糖对Fe^2＋的络合作用.     

Manufacturing Drug Loaded Chitosan Microspheres by Spray Drying: Development, Characterization, and Potential Use in Dentistry

The aim of this work was to determine specifications for spray-drying manufacturing of sustained-release drug-loaded microparticles with potential application in dentistry. Chitosan was used as the microencapsulation polymer and ketoprofen as the model drug. A 1:1 chitosan/ketoprofen suspension was spray-dried under different operating conditions. The size distribution, morphology, total drug load, and release profile of the powders were characterized. In vitro release studies were performed with the powder samples entrapped in cellulose dialysis tubes. The microparticles produced had a narrow size distribution (mean diameter ranging from 2.11 to 3.27 µm), good sphericity, and a smooth surface. In vitro release studies showed a linear drug dissolution behavior.     

Manufacturing Drug Loaded Chitosan Microspheres by Spray Drying: Development,Characterization, and Potential Use in Dentistry

The aim of this work was to determine specifications for spray-drying manufacturing of sustained-release drug-loaded microparticles with potential application in dentistry. Chitosan was used as the microencapsulation polymer and ketoprofen as the model drug. A 1:1 chitosan/ketoprofen suspension was spray-dried under different operating conditions. The size distribution, morphology, total drug load, and release profile of the powders were characterized. In vitro release studies were performed with the powder samples entrapped in cellulose dialysis tubes. The microparticles produced had a narrow size distribution (mean diameter ranging from 2.11 to 3.27 µm), good sphericity, and a smooth surface. In vitro release studies showed a linear drug dissolution behavior.     

羧甲基壳聚糖的制备及在水处理中的应用研究进展

主要介绍了壳聚糖水溶性衍生物—羧甲基壳聚糖的制备方法及在水处理中的应用研究,羧甲基壳聚糖在水处理方面有广泛的应用前景。     

叶酸修饰聚碳酸酯磁性载药微球的制备及其性能

通过十六醇(CA)引发2,2-二甲基三亚甲基环碳酸酯(DTC)开环聚合合成了聚碳酸酯(CA-PDTC),CAPDTC进一步与叶酸(FA)通过酯化反应合成了叶酸修饰的聚碳酸酯(CA-PDTC-FA)。采用FTIR、1HNMR和UVvis证实了所得产物的结构。以吲哚美辛(IMC)为模型药物,Fe_3O_4粒子为磁源,通过乳化法制备了叶酸修饰的聚碳酸酯磁性载药微球(CA-PDTC-FA@Fe_3O_4)。经X射线粉末衍射仪(XRD)、热重分析仪(TG)、动态光散射仪(DLS)和振动样品磁强计(VSM)测试,结果发现:质量分数为9.5%的Fe_3O_4粒子被包裹在聚合物微球中,微球粒径约为320 nm,具有超顺磁性,且对IMC的包载率为4.6%,载药微球在模拟人体环境(pH=7.4,37℃)下36 h后的累积释药量为20.0%,具有缓释效果。     

喷雾干燥法制备1型糖尿病反义肽噬菌体壳聚糖微球疫苗

目的制备1型糖尿病反义肽噬菌体壳聚糖微球疫苗,并观察其热稳定性。方法采用水溶性壳聚糖、海藻糖、甘氨酸作为保护剂,通过喷雾干燥技术制备1型糖尿病反义肽噬菌体壳聚糖微球疫苗,扫描电镜下观察其形态及粒径大小,并检测入口温度及海藻糖浓度对壳聚糖微球疫苗活性的影响。将喷雾干燥样品置37℃放置6d,检测其热稳定性。结果通过喷雾干燥法制备的1型糖尿病反义肽噬菌体壳聚糖微球疫苗电镜下呈不规则的球形,粒径大小为20μm左右。喷雾干燥后样品的滴度与喷雾干燥前的疫苗原液相比均降低,且随着入口温度的升高而先升高后降低;喷雾干燥后的样品随着海藻糖浓度的增加,滴度也相应升高。与喷雾干燥前的疫苗原液相比,壳聚糖微球疫苗具有更好的热稳定性。结论已成功制备了1型糖尿病反义肽噬菌体壳聚糖微球疫苗,其具有良好的热稳定性。     

壳聚糖-琼胶复合微球的制备及其药物释放性能

采用小分子离子交联法制备了pH值敏感的壳聚糖-琼胶复合微球,对壳聚糖-琼胶复合微球的粒径、形貌、pH值敏感性等进行了表征.以茶碱为模型药物研究了壳聚糖-琼胶复合微球的药物释放性能,结果发现一定量琼胶的引入有助于改善壳聚糖微球的药物缓释性能.     

壳聚糖缓释微球的制备与表征

以壳聚糖(Chitosan)、戊二醛(Glutaraldehyde)、尿素(Urea)为主要原料,采用乳化-化学交联法制备尿素-壳聚糖缓释微球.通过红外光谱测试,分析缓释微球的结构特征;通过扫描电镜测试,观察微球的微观形貌;通过交联度测试确定戊二醛的最佳用量;通过缓释测试,测定壳聚糖微球的缓释效果.结果表明:采用乳化-...     

羧甲基纤维素-壳聚糖LbL空腔微胶囊的制备

微胶囊技术现已广泛应用于生物医药,环境保护,日用化工,农业科学及航空航天等领域,随着应用范围扩大,开发新技术与新方法制备微胶囊,使其具有更精确可控的结构已成为微胶囊技术发展的重大课题之一。选择两种生物相容性较好的天然聚电解质—羧甲基纤维素(CMC)和壳聚糖(CS),作为制备新型微胶囊的原料,利用聚阴离子羧甲基纤维素和聚阳离子壳聚糖之间的静电结合,成功制备出一种具有新结构的中空聚电解质微胶囊并初步研究了其形貌能基本性能。     

海藻酸盐/壳聚糖复合微球的制备及其控制释放作用

采用喷雾干燥法将活性成分包载到海藻酸钠微凝胶中,再经钙离子和壳聚糖交联得到复合微球。以维生素B₂为模型药物探讨了微球的控制释放效果和机理。扫描电镜分析表明海藻酸钠微凝胶经复合交联后形成了团聚体结构。与单一钙离子交联的海藻酸盐微球相比,复合微球对维生素B₂释放更慢,半数释放时间(t₅₀)延长约6倍,且交联时间越长、交联剂用量越高,维生素B₂释放越慢。当载药量介于16.0%～35.6%时,维生素B₂释放时间达24 h以上,释放过程主要受费克扩散控制。     

羧甲基壳聚糖的制备及应用研究

用一氯乙酸对壳聚糖进行化学改性,制备了羧甲基壳聚糖(CMCH),探讨了影响取代度和水溶性的因素,并用红外光谱(IR)表征其结构。结果表明,制备水溶性好的CMCH的条件为:ω(NaOH)为42%,氢氧化钠与一氯乙酸的质量比为1 20∶1,反应温度为55℃。测定了CMCH的保湿性,含CMCH的定型剂有较好的卷曲保持率,达到82 6%。     

壳聚糖/聚丙烯酸共聚物微球的制备及性能

以环己烷为油相,壳聚糖溶液为水相,运用反相乳液聚合法制得了具有pH敏感性的壳聚糖/聚丙烯酸共聚物微球。讨论了微球在pH=1～10缓冲溶液中的溶胀率变化,研究表明,微球在强酸性(pH≈1)和碱性(pH>7)条件下,溶胀率均在10倍以上;而在pH=2～6时溶胀较差,当pH=4时出现最低值,溶胀率低于1倍。光学显微镜所观察到的微球粒径均在40μm以内,且大小均匀。采用傅里叶红外光谱仪分析了不同配比样品特征峰的峰值和峰面积的变化。用722光栅分光光度计研究了共聚物微球包埋考马斯亮蓝的溶胀释放过程。     

β-Cyclodextrin/Triclosan Complex-Grafted Methacrylated Glycol Chitosan Hydorgel by Photocrosslinking via Visible Light Irradiation for a Tissue Bio-Adhesive

Accelerating wound healing with minimized bacterial infection has become a topic of interest in the development of the new generation of tissue bio-adhesives. In this study, we fabricated a hydrogel system (MGC-g-CD-ic-TCS) consisting of triclosan (TCS)-complexed beta-cyclodextrin (β-CD)-conjugated methacrylated glycol chitosan (MGC) as an antibacterial tissue adhesive. Proton nuclear magnetic resonance (¹H NMR) and differential scanning calorimetry (DSC) results showed the inclusion complex formation between MGC-g-CD and TCS. The increase of storage modulus (G’) of MGC-g-CD-ic-TCS after visible light irradiation for 200 s indicated its hydrogelation. The swollen hydrogel in aqueous solution resulted in two release behaviors of an initial burst and sustained release. Importantly, in vitro and in vivo results indicated that MGC-g-CD-ic-TCS inhibited bacterial infection and improved wound healing, suggesting its high potential application as an antibacterial tissue bio-adhesive.     

羧甲基壳聚糖席夫碱的制备及抗菌性能研究

在超声波作用下,以自制的低分子量羧甲基壳聚糖与香草醛为原料,制备了低分子量羧甲基壳聚糖香草醛席夫碱。利用FI-IR对其结构进行了表征,研究了香草醛与羧甲基壳聚糖中氨基的反应摩尔比、反应温度、反应时间及超声波功率对产物氨基取代度的影响。结果表明：当香草醛与羧甲基壳聚糖中氨基的摩尔比为1∶0.8、反应时间为3 h、反应温度为70℃、超声波作用功率为70 W时,羧甲基壳聚糖香草醛席夫碱的氨基取代度可达到82.5%;将羧甲基壳聚糖席夫碱与羧甲基壳聚糖的抗菌性能进行了比较,发现羧甲基壳聚糖香草醛席夫碱对金黄葡萄球菌和大肠埃希菌的抑菌圈宽度分别比羧甲基壳聚糖的抑菌圈宽0.7 mm和0.5 mm。