静电喷雾法制备羧甲基纤维素/壳聚糖液芯微胶囊

以羧甲基纤维素(CMC)和壳聚糖(CS)聚合物为原料,采用静电喷雾技术制备了CMC/CS液芯微胶囊。研究了制备条件对微胶囊成型和尺寸的影响,并用激光扫描共聚焦显微镜、扫描电子显微镜和倒置显微镜进行了表征。将四环素与CMC溶液共混,以Al3+-CS作为凝固浴,在电压10 kV、液面距离20 mm、流速10 mL/h的条件下,制备了载药微胶囊。微胶囊的药物包封率随壳聚糖浓度增大而提高,在1.5%时达到99.5%。药物释放实验结果表明CMC/CS液芯微胶囊的释放率与pH有关,控释性能良好。     

聚氨基酸复合微胶囊对Hb的控制释放

以生物相容性好、价格低廉的海藻酸钠(ALG)为聚阴离子芯材,通过静电液滴装置制备了平均粒径在290 μm左右、球形度好、表面光洁的海藻酸钙胶珠;再将生物可降解、具有介入治疗作用的聚精氨酸(PLA)与聚组氨酸(PLH)的混合物作为聚阳离子壁材,在海藻酸钙胶珠表面覆上一层高分子聚合膜以制备聚氨基酸复合微胶囊;并以牛血红蛋白Hb为药物模型,对微胶囊的控制释放性能进行了考察并将其初步应用于体外模拟口服给药。结果表明:聚氨基酸复合微胶囊在前0.5 h的累积释放量均低于40％,溶出结束时累积释放量均达到80%以上;ALG/(PLA-PLH)复合微胶囊和ALG/PLH微胶囊的药物释放速率均低于ALG/PLA微胶囊;于10 min成膜时间内制备的微胶囊具有较高的载药量、包封率和缓释性能;以pH 4.6 HAc-NaAc缓冲液为成膜溶媒制备的微胶囊,Hb持续释放时间和残留量均高于蒸馏水组;前2 h在模拟胃液的pH 1.2 HCl溶媒中累计释放的Hb不超过10％且绝大部分是在模拟肠液环境即pH 6.8 PBS 溶媒中释放的;壳聚糖的引入能在一定程度上延长药物释放时间。聚氨基酸复合微胶囊具备一定的缓释性、pH响应性和生理黏附性,有望成为一种口服给药系统用药物载体。      

基于聚碳酸亚丙酯载体的农药微胶囊制备与表征

采用阴离子配位聚合法,以高聚物负载型双金属氰化物复合体(DMC)作为催化剂,合成了二氧化碳、环氧丙烷二元共聚物:聚碳酸亚丙酯(PPC)。并以聚乙烯醇PVA-1788为水相稳定剂,采用乳化溶剂挥发法制备毒死蜱微胶囊。采用土壤悬浊拟环境培养实验法评价了PPC的降解性能。通过光学显微镜(OM)、扫描电子显微镜(SEM)、广角X射线衍射(W-XRD)、高效液相色谱(HPLC)等表征农药微胶囊的性能。结果表明,PPC具有生物可降解性,所得的PPC-毒死蜱微胶囊球形规整,表面光滑。95%的微胶囊粒径在3～10μm范围内,载药量和包封率分别达到16.75%和89.34%。微胶囊释药性能研究表明,PPC-毒死蜱微胶囊具有明显的缓释效应,其释放可分为前期快速释放和中后期稳定释放2个阶段。释放27d,PPC微胶囊累积释药量达86.87%。     

毒死蜱/脲醛树脂微胶囊的制备工艺优化及缓释动力学

随着人们健康与环保意识的不断加强,农药施用量大、效率低、高残留等问题日益受到人们的重视,对农药进行微胶囊化,有助于有效解决当前农药使用过程中所面临的问题。采用脲醛树脂作为壁材,以十二烷基硫酸钠为乳化剂,采用原位聚合法制备毒死蜱/脲醛树脂微胶囊。研究了乳化剂种类和用量、pH值、酸化时间对微胶囊粒径及其分布的影响,并进一步探讨微胶囊的载药量、包封率及释放动力学。结果表明,采用3%(质量分数)的十二烷基硫酸钠为乳化剂,在酸化时间为90min、酸化终点pH值为2.5、搅拌速度为1 200r/min、芯壁比为1∶3、固化温度为60℃时,所制备的毒死蜱/脲醛树脂微胶囊的粒径分布窄,平均粒径约为113μm,载药量达53%以上,包封率达62%以上。毒死蜱/脲醛树脂微胶囊的缓释性能及动力学研究结果显示,所制备的毒死蜱/脲醛树脂微胶囊的缓释效果明显,10天内能释放90%的药物,释放过程遵循Fick扩散机理。可见,制备的毒死蜱/脲醛树脂微胶囊具有较高的载药量、较好的包封率以及缓释性能,可进一步开发为新型的农药制剂,并为开发缓释农药新剂型提供理论支持与实践参考。     

聚乳酸/辣椒素复合载药薄膜的制备及药物释放

利用静电纺丝法和溶液法分别制备了具有微纳米纤维结构、串珠结构和较密实结构的聚乳酸/辣椒素复合载药薄膜(分别称为薄膜Ⅰ、薄膜Ⅱ和薄膜Ⅲ)。研究了不同载药量(5%、10%和15%,质量分数)和不同微结构对药物释放行为的影响。药物释放研究表明:PLA/Cap复合载药薄膜的微结构和载药量都对药物释放行为有重要的影响。当载药量为5%和10%(质量分数)时,药物释放行为主要受载药薄膜的微结构影响,释放速度由快到慢为:薄膜I、薄膜Ⅱ、薄膜Ⅲ;随着载药量的增加药物释放速度加快,且3种载药薄膜的辣椒素释放速度之间的差别减小。当载药量达15%(质量分数)时,载药量对药物释放行为的影响较微结构的影响更加显著,3种载药薄膜的药物释放行为接近。     

载γ-球蛋白微包纳载体的制备与性能

为了结合不同载体的特点从而实现更佳的性能,载体的集成化研究已日益成为研究者关注的热点。为了延长微胶囊的释放时间,构筑了新型的微包纳载体形式并用于大分子药物γ-球蛋白的包埋及释放。所制备的微包纳胶囊表面光洁,球形度较好,胶囊之间无粘连,分散性较好,粒度分布均匀。几丁聚糖分子量、浓度及药物初始浓度对载药量及体外释放影响不一。与单纯微胶囊相比,微包纳胶囊能够显著延长药物的释放时间,从而为该新型载体在大分子药物释放的应用方面提供了实验依据。     

多孔P(NIPAm-co-AAm)水凝胶对蛋白质控制释放的研究

采用冷冻聚合法制备了多孔结构的P(NIPAm-co-AAm)智能水凝胶,选用牛血清白蛋白(BSA)为模型药物分子,通过后包裹技术负载蛋白质药物,考察了多孔水凝胶中蛋白质药物的载药量和体外释放行为,研究了不同干燥处理方法对载药后水凝胶的药物控释性能的影响,并且与传统方法制备的P(NIPAmco-AAm)水凝胶进行了药物控释性能对比实验。实验结果表明,在凝胶中引入多孔结构使得P(NIPAm-coAAm)水凝胶的药物载药量和释放量得到了显著的提高。不同的干燥处理方法对多孔P(NIPAm-co-AAm)水凝胶的药物释放影响很大,载药后的凝胶采用冰箱冷冻干燥处理,可使蛋白质药物有较好的缓释效果。     

多孔P(NIPAm-co-AAm)水凝胶对蛋白质控制释放的研究

采用冷冻聚合法制备了多孔结构的P(NI-PAm-co-AAm)智能水凝胶,选用牛血清白蛋白(BSA)为模型药物分子,通过后包裹技术负载蛋白质药物,考察了多孔水凝胶中蛋白质药物的载药量和体外释放行为,研究了不同干燥处理方法对载药后水凝胶的药物控释性能的影响,并且与传统方法制备的P(NIPAm-co-AAm)水凝胶进行了药物控释性能对比实验。实验结果表明,在凝胶中引入多孔结构使得P(NIPAm-co-AAm)水凝胶的药物载药量和释放量得到了显著的提高。不同的干燥处理方法对多孔P(NIPAm-co-AAm)水凝胶的药物释放影响很大,载药后的凝胶采用冰箱冷冻干燥处理,可使蛋白质药物有较好的缓释效果。     

甘草次酸(β)海藻酸钠-羧甲基壳聚糖复合凝胶珠的制备及体外释放

以海藻酸钠-羧甲基壳聚糖(ALG-CMC)为载体材料,甘草次酸(β)(GA)为模型药物,采用滴制法制备了ALG-CMC负载GA的复合凝胶珠。采用体视显微镜与扫描电镜(SEM)观察了凝胶珠的外观形貌,考察了凝胶珠的溶胀性能和体外释药行为,以及CaCl2浓度对凝胶珠的包封率和载药量的影响。结果表明,湿态凝胶珠形态规整、粒径分布均匀,平均粒径约2900μm,包封率最高达85.7%,载药量为18.0%;CaCl2浓度对包封率和载药量几乎无影响;在pH=1.2的HCl溶液中凝胶珠溶胀率小、累积释放率低;在pH=7.4的磷酸盐缓冲(PBS)溶液中凝胶珠溶胀率大、累积释放率高。滴制法制备ALG-CMC凝胶珠条件温和、不接触有机溶剂,凝胶珠具有pH敏感性且能有效载药。该体系有可能成为GA的给药载体材料。     

广藿香油缓释微胶囊的制备及其性能分析

以广藿香油为芯材,壳聚糖和阿拉伯胶为壁材,采用复凝聚法对广藿香油进行包埋,制备广藿香油微胶囊。利用扫描电子显微镜、激光粒度仪、红外光谱和紫外光谱等分析方法研究各因素对微胶囊形成的影响。确定制备广藿香油微胶囊的最佳条件:采用中低粘度的壳聚糖,壳聚糖浓度为0.5%,阿拉伯胶浓度为4%,芯壁比为1∶2,复凝聚pH值为4.5,搅拌转速为2000r/min。红外光谱分析表明广藿香油包埋成功,其载药量和包封率分别为20.75%和67.2%。微胶囊缓释性能测试结果表明微胶囊具有良好的缓释效果,在25℃条件下,微胶囊释放150h后,累计释放率为33%,即微胶囊保留率为67%。     

Preparation of embolic NEMs loading capecitabine

The nanoparticles-embedded microcapsules (NEMs) with smooth surface, good sphericity, excellent dispersivity and uniform particle size distribution were prepared by emulsification combined with electrospraying to extend the sustained release performance of the embolic microcapsules loading capecitabine (CAP). The sodium alginate and chitosan with good biocompatibility were used as the materials and CAP as a small-molecule model drug. The drug loading, encapsulation efficiency and drug release of CAP in the NEMs were investigated. The results showed that the drug-loading and encapsulation efficiency both increased with the increment of chitosan and CAP concentration. The maximum values of drug loading and encapsulation efficiency were 1.97 and 18.01 % respectively when initial CAP concentration was 5.0 g/L and chitosan molecular weight 100 kDa. The cumulative release rate of CAP released from the NEMs was lower than 30 % in 0.5 h, which indicated that there was no obvious initial burst release behavior. In the subsequent 240 h, the release results confirmed that the NEMs had better sustained release properties compared to pure microcapsules, and it might be a new anticancer drug delivery system in the future studies.     

Calcium alginate/dextran methacrylate IPN beads as protecting carriers for protein delivery

In the present study, mechanical and protein delivery properties of a system based on the interpenetration of calcium-alginate (Ca-Alg) and dextran-methacrylate (Dex-MA) networks are shown. Interpenetrated hydrogels beads were prepared by means of the alginate chains crosslinking with calcium ions, followed by the exposure to UV light that allows the Dex-MA network formation. Optical microscope analysis showed an average diameter of the IPN beads (Ca-Alg/Dex-MA) of 2?mm. This dimension was smaller than that of Ca-Alg beads because of the Dex-MA presence. Moreover, the strength of the IPN beads, and of their corresponding hydrogels, was influenced by the Dex-MA concentration and the crosslinking time. Model proteins (BSA and HRP) were successfully entrapped into the beads and released at a controlled rate, modulated by changing the Dex-MA concentration. The enzymatic activity of HRP released from the beads was maintained. These novel IPN beads have great potential as protein delivery system.     

海藻酸钙/聚精氨酸微胶囊的制备及其生物相容性

以海藻酸盐、 聚精氨酸为壁材, 采用高压静电法制备了球形度好、 表面光洁、 粒径均匀的新型药物载体——海藻酸钙/聚精氨酸微胶囊。参照医疗器械生物学评价标准, 对其生物相容性进行了研究。细胞毒性试验结果显示, 当海藻酸钙/聚精氨酸微胶囊的含量为0.1、 0.5、 1.0 mg/mL时, 微胶囊对L929细胞生长无明显抑制作用, 海藻酸钙/聚精氨酸微胶囊浸提产物在10.0 mg/mL时仍无细胞毒性作用。海藻酸钙/聚精氨酸微胶囊不引起急性全身毒性反应, 不引起溶血反应。通过本组试验可见, 采用高压静电法制备的药物载体——海藻酸钙/聚精氨酸微胶囊具有较好的生物相容性, 具有开发和应用价值。     

Release of Theophylline from Ethyl Cellulose Mecrocapsues Alone and in Conjuction with Fat Embedded (Precirol®) Granules and Hydroxypropyl Methycellulose

Abstract

Microcapsules of theophylline with ethyl cellulose were prepared by coacervation technique using cabosil® (silicon dioxide) as separant. Tablets were prepared from microcapsules, microcapsules + theophylline fat embedded granules, and microcapsules and hydroxypropyl methylcellulose 4000 (HPMC). Release was studied in vitro by the rotating basket method. Prolonged release of theophylline was observed from microcapsules with no drug dumping. The release from microcapsules was of first-order whereas that from all the tablet formulation was diffusion controlled according to the Higuchi model. Good correlation was found between release rate and core:wall ratio for all the systems. Decrease in hardness of tablets made from microcapsules alone decreased the release rate, indicating damage of microcapsules during compression. The tablets compressed from fat embedded granules, microcapsules with fat embedded granules, and microcapsules with HPMC gave a desired release for a 74 hour sustained release preparation.     

Effects of crosslinking ratio,model drugs,and electric field strength on electrically controlled release for alginate-based hydrogel

The drug release characteristics of calcium alginate hydrogels, (Ca-Alg), under an electric field assisted transdermal drug delivery system were systematically investigated. The Ca-Alg hydrogels were prepared by the solution-casting using CaCl₂ as a crosslinking agent. The diffusion coefficients and the release mechanism of the anionic model drugs, benzoic acid and tannic acid, and a cationic model drug, folic acid on the Ca-Alg hydrogels were determined and investigated using a modified Franz-Diffusion cell in an MES buffer solution of pH 5.5, at a temperature of 37°C, for 48 h. The influences of the crosslinking ratio, —the mole of the crosslinking agent to the mole of the alginate monomer—mesh size, model drug size, drug charge, electric field strength, and electrode polarity were systematically studied. The drug diffusion coefficient decreased with an increasing crosslinking ratio and drug size for all of the model drugs. The drug diffusion coefficient is precisely controlled by an applied electric field and the electrode polarity depending on the drug charge, suitable for a tailor-made transdermal drug delivery system.     

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...     

TiO2前驱体微胶囊型缓蚀剂的制备与性能研究

随着火炮初速、膛压、射速的提高, 炮膛的烧蚀磨损逐渐变得严重, 对高效缓蚀剂的需求越来越迫切。本研究以聚乙烯醇(PVA)为壁材, 在W/O/W复乳体系中利用界面交联法制备了TiO₂前驱体微胶囊, 探讨了微胶囊的形成机理。扫描电镜观察表明微胶囊呈现出球形形貌, 分散性好, 囊壁致密、包覆完整, 粒径分析显示其平均粒径在10 μm左右; 红外分析进一步证实微胶囊是由醇醛树脂层包覆TiO₂前驱体形成; 热分析表明微胶囊中固体TiO₂含量约为35%。利用烧蚀管试验法测试其降烧蚀性能, 结果表明TiO₂前驱体微胶囊型缓蚀剂不影响发射药的燃烧规律, 在相对于发射药质量2.5wt%的添加量下, 降烧蚀效率达到35%左右。     

环氧树脂包覆聚磷酸铵微胶囊的制备及其对聚丙烯的阻燃效果

为了探究环氧树脂包覆聚磷酸(EP@APP)微胶囊对聚丙烯(PP)的阻燃效果,首先,采用原位聚合法以EP为外壳包覆APP,制备了EP@APP微胶囊,并将其与PP进行复合,制备了EP@APP/PP复合材料。然后,测试了EP@APP微胶囊的溶解性,探讨了工艺参数对溶解性的影响;考察了EP@APP微胶囊的耐水性,并借助红外光谱分析了EP@APP微胶囊的表面官能团。最后,测试了PP复合材料的极限氧指数、拉伸强度和热重曲线,并分析了PP复合材料的热分解动力学。结果表明:当EP的加入量为APP的10wt%、固化剂加入量为EP加入量的15wt%时,采用先于40℃下维持1h、再于70℃下维持1h的阶跃升温方法可制备包覆完全的EP@APP微胶囊;该种微胶囊在水中溶解度低,且具有良好的耐水性。在PP中添加EP@APP微胶囊后,PP复合材料的极限氧指数为35.5%,达到V-0燃烧等级,燃烧后的残炭量增多,成炭效果明显优于直接添加APP的PP复合材料。与APP相比,EP@APP微胶囊对PP拉伸强度的破坏程度明显降低。EP@APP微胶囊的加入使PP复合材料的表观活化能由100.8kJ/mol提高到127.5kJ/mol,改变了PP复合材料的热降解氧化过程,且生成的残炭形成了稳定的保护炭层。研究结果表明EP@APP微胶囊可有效提高PP复合材料的阻燃性能。     

Drug Release Properties of the Microcapsules of Adriamycin Hydrochloride with Ethylcellulose Prepared by a Phase Separation Technique

Adriamycin hydrochloride was microencapsulated with ethylcellulose by a phase separation method to develop a prolonged release dosage form. Polyisobutylene (PIB) was used as a coacervation-inducing agent to control the particle size and drug release rate of the resultant microcapsules. With increasing the concentration of PIB (1 to 3 %) the average diameter of the microcapsules decreased, due to the fact that the microcapsules were discreted to a single microcapsule. At low concentration of PIB, the resultant microcapsules were agglomerated, which resulted in increasing the size. The microcapsules prepared with PIB 2 % prolonged desirably the drug release from the microcapsules. A little size effects of the microcapsules on the drug release rate was found for the microcapsules with PIB 2 % and 3 %.     

层层自组装法制备肝素微囊及其性能研究

以海藻酸钙微核为模板,采用带正电荷的聚稀丙基铵盐酸盐(PAH)和带负电荷的肝素钠(HEP),通过层层自组装(Layer-by-layer,LbL)技术构建具有多层膜结构和抗凝血活性的药物微囊.采用荧光倒置显微镜、SEM、动态光散射仪、Zeta电位仪和抗凝血仪等进行表征.结果表明,制备的海藻酸钙微核粒径约为1.5μm,尺寸均匀、分散性佳;以ALG为模板制得的LbL微囊具备典型的核壳式结构;Zeta电位检测表明,随包膜层数的增加,微囊的电位呈正负交替的变化趋势;通过体外凝血时间(PT、APtt、TT)检测微囊抗凝血活性,比较了分别以PAH和HEP作为最外层时的生物活性,其中以HEP为最外层的显著增强了材料的抗凝血性能,同时随着组装层数的增加,也提高了微囊的抗凝血性能.