纳米磁性壳聚糖载药体的制备与体外释药评价

以自制Fe3O4磁性纳米为磁性靶向核,在乳液体系中制备壳聚糖／三聚磷酸钠／5-Fu磁性壳聚糖纳米载药体（TCF）,经一定比例的PHB和PEG混合外包覆,得到载药率为16．56％的磁性纳米微囊（PTCF）,通过红外光谱、x-射线粉末衍射、透射电镜和振动磁强计表征,结果显示,TCF、PTCF分别为粒径15nm和20nm均匀颗粒,25℃时的矫顽力和剩磁均趋于零,表现出超顺磁性;体外释药行为显示,PTCF无突释现象,释药速率随PHB和PEG用量可控,具备磁靶向控释药物的潜在性质。     

壳聚糖靶向缓释功能高分子载药微球及其特性研究

采用壳聚糖作为载体,通过分子结构设计,以叶酸靶向受体改性壳聚糖,然后选择5-氟尿嘧啶为模型药物,采用复凝聚法制备新型壳聚糖靶向缓释功能高分子载药微球。通过红外光谱和1 H-NMR核磁共振分析确定了叶酸改性壳聚糖化学结构,并通过扫描电镜、激光粒度分析仪、激光共聚焦显微镜及紫外光谱等现代仪器和分析方法对载药微球的形貌结构、粒径、包埋率、载药量和体外药物释放特性等进行研究。结果表明,模型药物被成功包埋到叶酸改性后的壳聚糖微球中,包埋率E和载药量L最高可达86.5%和32.7%,载药微球的平均粒径为5.251μm,多分散系数(PDI)为0.056,球形度、分散性良好;激光共聚焦显微镜结果显示微球为核壳结构;体外释放实验表明壳聚糖靶向缓释功能高分子载药微球具有持久的缓释作用,24h后载药微球在模拟胃液(pH值=1.2)中释放率为70%,在模拟肠液(pH值=7.4)中释放率为40%,释药速度与释放介质的pH值密切相关。     

壳聚糖-固态分散体载药微球的制备及性能研究

首先采用不同分子量的壳聚糖通过乳化-化学交联法制备了4种不同的壳聚糖载药微球。通过对微球的粒径、溶胀率、载药率、包封率等指标检测以及缓释性能的研究,发现分子量为240kDa的壳聚糖制备的载药微球缓释效果明显,载药率、包封率均较高,综合性能优于其它分子量壳聚糖制备的微球。利用该分子量壳聚糖包埋固态分散体制备了壳聚糖-固态分散体载药微球,改善了药物的溶解性并具有药物缓释作用。因此,壳聚糖-固态分散体载药微球是一种理想的药物缓释体系,可以用于包埋溶解性差,生物半衰期短,对胃肠刺激性强的药物。     

聚L-谷氨酸/壳聚糖纳米凝胶的制备与表征EI北大核心CSCD

以纳米SiO_2为模板,在其表面接枝聚L-谷氨酸(PLGA),以壳聚糖(CS)为大分子交联剂,构建了PLGA/CS化学交联中空纳米凝胶,研究了纳米SiO_2粒子表面接枝,纳米凝胶制备、微观形貌以及pH响应行为。以水溶性盐酸米托蒽醌(MTX)为模型药物,研究了PLGA/CS纳米凝胶的载药与释药性能。结果表明,PLGA在SiO_2表面成功接枝;PLGA/CS纳米凝胶呈球形,平均粒径为365 nm。冻干后纳米凝胶尺寸收缩至100 nm左右;PLGA/CS纳米凝胶具有pH响应性,随pH的提高,PLGA/CS纳米凝胶粒径先减小后增大;PLGA/CS纳米凝胶对MTX有良好的负载能力,最高载药量达41.4%。载MTX的PLGA/CS纳米凝胶在起始阶段存在一定程度突释,随后释药速度明显变缓,直到7 d后达到释放平衡,药物缓释效果良好。     

壳聚糖-聚羟基丁酸酯共混膜的体外血液相容性评价

制备了壳聚糖(CTS)/聚(R)-3-羟基丁酸酯(PHB)二元系列膜,扫描电镜(SEM)分析检测其表面形貌.体外评价了不同比例共混复合物的溶血率、动态凝血、复钙化时间及血小板粘附.结果表明,二元共混膜较之原料壳聚糖相比,溶血率下降,复钙化时间延长,动态凝血曲线变化缓慢.SEM显示共混膜材料表面的血小板粘附现象明显少于壳聚糖.组成为C1B1的共混材料表现突出.通过与PHB简单共混的方法可以有效改善壳聚糖的血液相容性能.     

聚L-谷氨酸/壳聚糖纳米凝胶的制备与表征

以纳米SiO_2为模板,在其表面接枝聚L-谷氨酸(PLGA),以壳聚糖(CS)为大分子交联剂,构建了PLGA/CS化学交联中空纳米凝胶,研究了纳米SiO_2粒子表面接枝,纳米凝胶制备、微观形貌以及pH响应行为。以水溶性盐酸米托蒽醌(MTX)为模型药物,研究了PLGA/CS纳米凝胶的载药与释药性能。结果表明,PLGA在SiO_2表面成功接枝;PLGA/CS纳米凝胶呈球形,平均粒径为365 nm。冻干后纳米凝胶尺寸收缩至100 nm左右;PLGA/CS纳米凝胶具有pH响应性,随pH的提高,PLGA/CS纳米凝胶粒径先减小后增大;PLGA/CS纳米凝胶对MTX有良好的负载能力,最高载药量达41.4%。载MTX的PLGA/CS纳米凝胶在起始阶段存在一定程度突释,随后释药速度明显变缓,直到7 d后达到释放平衡,药物缓释效果良好。     

羟基喜树碱叶酸-壳聚糖纳米粒的制备及其性能研究

为了提高羟基喜树碱对肿瘤组织的靶向性,增强其抗肿瘤活性,延长其在体内的作用时间,以壳聚糖为药物载体,叶酸为肿瘤靶向配体,三聚磷酸钠为聚阴离子,利用静电相互作用的原理,通过离子交联法合成载羟基喜树碱的叶酸-壳聚糖(FA-CTS/HCPT)纳米粒。利用动态光散射、透射电镜以及红外等技术对纳米粒的结构、平均粒径及粒径分布、形态特征、表面电位、稳定性、对药物的包封率及载药量、体外释放等特点进行了初步研究。结果表明,所制得的纳米粒平均粒径为150nm;粒子形态圆整,大小均匀;表面电位+50.1mV;放置数十天纳米粒粒径几乎无变化,纳米粒具有很好的粒度稳定性;对羟基喜树碱包封率最高为89.9%,载药量最高为19.8%;在人工体液pH值为7.4条件下具有很好的缓释作用,用Higuchi方程拟合其体外释放曲线,得Higuchi方程:Q=14.529t1/2+8.3589(R2=0.9247),说明HCPT在人工体液的释放量与时间的平方根成直线关系,符合水不溶性骨架的释药性能。     

壳聚糖/羟基磷灰石-庆大霉素缓释材料的抗菌性能研究及AFM观察

制备壳聚糖/羟基磷灰石-庆大霉素(CS/HA-G)缓释材料,评价其抗茵性能在骨髓炎的治疗中的应用前景;并从微观角度初步探讨药物对大肠杆菌的作用机制.对CS/HA-G缓释材料进行体外缓释行为研究及抗茵实验;并以原子力显微镜(AFM)观察大肠杆茵在药物作用前后表面形态结构的变化.CS/HA-G对大肠杆茵的抑茵效果显著,维持有效释药时间长达30d以上.AFM观察显示药物作用于大肠杆菌后菌体高度和表面平均粗糙度(Ra)均下降,有内容物渗漏.CS/HA是一种理想的庆大霉素载体材料.CS/HA-G的缓释作用和缓释规律显示出该材料在大肠杆菌引发的骨髓炎的防治中具有极大的临床应用潜能.     

磁性壳聚糖-5-氟尿嘧啶纳米粒的制备及体外释药性能

采用交联-聚合法在超声波的作用下,制备了磁性壳聚糖-5-氟尿嘧啶纳米粒(M CN-Fu)。透射电子显微镜(TEM)和红外光谱(IR)等分析结果表明,M CN-Fu粒子外形规整,分散性好,粒径主要在50 nm~60 nm之间。紫外-可见光谱分析结果表明,M CN-Fu的载药量为21.3%,在磷酸盐缓冲溶液(pH=7.2)中,30 h的累积释药率为67.6%,具有良好缓释性能,并具有良好磁响应性能。     

壳聚糖胃滞留-漂浮微球体外释药的高精度组合建模法研究

以牛血清白蛋白(BSA)为模型药物,壳聚糖(CS)和海藻酸钠(SA)为壁材,采用锐孔凝固浴法制备了壳聚糖胃滞留-漂浮微球(CGRM).建立零级释放动力学模型(ZODM)、Higuchi模型和Ritger-Peppas(RPcppas)模型对CGRM的释药性能进行了模拟和预测研究,并在此基础上构建了一种高精度的组合建模法.组合模型的模拟和预测精度均有一定提高,表明该组合建模法是一种模拟长效药物缓释体系释药规律的有力工具.     

Effect of Process Variables on Drug Release from Microparticles Containing A Drug-Resin Complex

Abstract

Microparticles consisting of dextromethorphan-resin complex (resinate) coated with a cellulose derivative were prepared by a modified emulsion-solvent evaporation method. Adjustment of the release rate was achieved by varying resinate (core) to polymer (coat) ratio or by using additives. Higher ratios of resinate to polymer gave faster release of the drug. Polyethylene glycol (PEG) 4000 also increased the release rate. Increasing core to coat ratio also increased average particle size. Placing the emulsifying agent in different phases of the emulsion in the fabrication process also affected the particle size distribution. The microparticles showed good sustained release of the drug     

Investigation of Hypromellose Particle Size Effects on Drug Release from Sustained Release Hydrophilic Matrix Tablets

Selected combinations of six model drugs and four hypromellose (USP 2208) viscosity grades were studied utilizing direct compression and in vitro dissolution testing. Experimental HPMC samples with differing particle size distributions (coarse, fine, narrow, bimodal) were generated by sieving. For some formulations, the impact of HPMC particle size changes was characterized by faster drug release and an apparent shift in drug release mechanism when less than 50% of the HPMC passed through a 230 mesh (63 μm) screen. Within the ranges studied, drug release from other formulations appeared to be unaffected by HPMC particle size changes.     

Mathematical Modeling of Magnesium Oxide Release from Granules Produced by Laboratory Fluidization

The particle size usually has an important effect on the rate of drug liberation from sustained release systems. The nature of that effect depends on the geometry of the system and the mechanism of the drug release (1). The aim of the present study was to characterize the relationship between the drug release projile of granules produced by luboratory fluidization and their particle size. The magnesium oxide release from granules-which are of two different particle sizes and contain Eudragit polymer-was investigated both experimentally and with mathematical models. First-order, cube root, square root, and two-thirds root models were applied for the evaluation of the drug release data. Changes in the particle size of the investigated granules altered the drug release profile     

异噻唑啉酮微胶囊的制备表征及释放行为

以二异氰酸酯(TDI)、聚乙二醇4000(PEG)、二羟甲基丙酸(DMPA)和三乙胺(TEA)为原料,制备可水乳化的聚氨酯(WPU).以合成的WPU为囊壁、以异噻唑啉酮衍生物(Sea-nine 211)为囊芯,通过乳化自组装得到防污剂Sea-nine 211微胶囊,用红外光谱、粒径分布和扫描电镜对胶囊进行表征,并采用分...     

Surfactant‐mediated synthesis of polyhydroxybutyrate (PHB) nanoparticles for sustained drug delivery

In this study, polyhydroxybutyrate (PHB) nanoparticles were synthesised following nanoprecipitation method having different solvents and surfactant (Tween 80) concentrations. In this study, PHB nanoparticles were encapsulated with curcumin and subjected for sustained curcumin delivery. Both the curcumin loaded and unloaded PHB nanoparticles were characterised using FTIR, SEM, and AFM. Sizes of the particles were found to be between 60 and 300 nm. The drug encapsulation efficiency and in vitro drug release of the nanoparticles were analysed. Antibacterial activity and anticancer activity were also evaluated. The LC₅₀ values of most of the nanoparticles were found to be between 10 and 20 µg/100 µl, anticancer activity of curcumin loaded PHB nanoparticles were further confirmed by AO/PI staining and mitochondrial depolarisation assay.Inspec keywords: encapsulation, cancer, scanning electron microscopy, nanoparticles, surfactants, drugs, nanofabrication, antibacterial activity, biomedical materials, drug delivery systems, polymers, nanomedicine, Fourier transform infrared spectra, precipitation (physical chemistry), atomic force microscopy, particle sizeOther keywords: surfactant‐mediated synthesis, polyhydroxybutyrate nanoparticles, sustained drug delivery, surfactant concentrations, PHB nanoparticles, sustained curcumin delivery, drug encapsulation efficiency, anticancer activity, in vitro drug release, nanoprecipitation method, Tween 80, FTIR spectra, SEM, AFM, particle sizes, antibacterial activity, AO‐PI staining, mitochondrial depolarisation assay     

Preparation and Evaluation of Controlled Release Propranolol Hydrochloride Beads

Conventional pan coating method was utilized to prepare propranolol-HCl sustained release coated beads. Eudragit RS 100 was used as release controlling materials. Overcoating of the beads with beeswax was also investigated. The beads were characterized for their particle size distribution, drug loading efficiency and their dissolution behaviour in 0.1N HCl, Most of the finished beads (72.4%) fall in the particle size range 800-1700 um. The actual drug content, calcu-lated as opposed to the theoretical drug content were 77.6% and 74.2% of the drug for the beads having particle size range 1700-1250 um and 1250-800 um respectively, The coating level of the polymer, the particle size of the beads and overcoating with beeswax play a major role in determining the release rate of the drug from the coated beads.     

Preparation and Evaluation of Controlled Release Propranolol Hydrochloride Beads

Abstract

Conventional pan coating method was utilized to prepare propranolol-HCl sustained release coated beads. Eudragit RS 100 was used as release controlling materials. Overcoating of the beads with beeswax was also investigated. The beads were characterized for their particle size distribution, drug loading efficiency and their dissolution behaviour in 0.1N HCl, Most of the finished beads (72.4%) fall in the particle size range 800–1700 um. The actual drug content, calcu-lated as opposed to the theoretical drug content were 77.6% and 74.2% of the drug for the beads having particle size range 1700–1250 um and 1250–800 um respectively, The coating level of the polymer, the particle size of the beads and overcoating with beeswax play a major role in determining the release rate of the drug from the coated beads.     

Sustained Release Microspheres of Diclofenac Sodium Using PEGylated Rosin Derivatives

The PEGylated derivatives of rosin-PD-1 and PD-2 synthesized and characterized earlier () were investigated as potential materials for sustained release microsphere prepared by emulsion solvent evaporation method using diclofenac sodium (DCS) as model drug. All the microspheres exhibited smooth surfaces intercepted by pores; their sizes (d₉₀) ranged between 11–24 μm. The entrapment efficiency (< 80%) of the microspheres increased proportionally with derivative concentration. Presence of solvent like isopropyl alcohol or dichloromethane rendered the microspheres with large sizes but with reduced drug entrapment. Microspheres with small size were obtained at an optimum viscosity of liquid paraffin; any change lead to increase in the particle size. Magnesium stearate was found to be most suitable detackifier in the present system. The drug release was directly related to the particle size—small sized microspheres released drug at a faster rate. The dissolution data complied with Higuchi equation while the mechanism of drug release was Fickian diffusion (n ～ 0.5). Controlled inhibition of edema, as tested by hind paw edema method, was observed for 10 h when the microspheres were administered intraperitoneally. The present study found the derivatives as promising materials for preparing microspheres for sustained delivery of DCS.     

载紫杉醇聚乳酸-羟基乙酸纳米粒的体外释药研究

以生物可降解材料聚乳酸-羟基乙酸(PLGA)为载体制备了载紫杉醇纳米粒,重点考察了纳米粒的体外释放特性.采用乳化-溶剂挥发法制备了载紫杉醇PLGA纳米粒,其平均粒径为200nm,载药量为21%,包封率为89.44%;体外释药符合Higuchi方程:Q=3.8796t1/2+30.4649(r=0.9397),同时载紫杉醇纳米粒具有一定的缓释作用.