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Xian Zhu Can Zhang Xiaoli Wu Xiaoyan Tang Qineng Ping 《Drug development and industrial pharmacy》2013,39(1):2-9
The objective of this study is to find out an optimized formulation of water insoluble anticancer drug gambogic acid (GA)-loaded chitosan derivatives micelles. After preliminary test, four factors (the amount of N-octyl-O-sulfate chitosan (AOSC), the amount of GA, volume of ethanol, and dialysis temperature) and three levels for each factor that might affect the formation of micelles were selected and arranged in L9 (34) orthogonal experimental design to optimize the formulation of GA-loaded micelles. To compare each of the micellar formulations quantitatively, an overall desirability function was defined and calculated based on three assessment indices (drug content, loading efficiency, and entrapping efficiency of micelles). The optimized formulation was 8 mg of GA dissolved in 0.3 mL of ethanol, 12 mg of AOSC dissolved in 2 mL of H2O, respectively. The drug solution and blank micellar solution were mixed, followed by dialysis against water at 25°C. The mean size of micelle was 100 nm approximately. Lyophilized samples could keep stable for at least 2 months when it was stored at 4°C. These data suggest that the amphiphilic chitosan derivative may improve the water solubility of GA and thus be used as its nano-carrier. 相似文献
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Fan Yu Chenghua He Ayman Y. Waddad Were L. L. Munyendo 《Drug development and industrial pharmacy》2014,40(6):774-782
Context: Gambogic acid (GA) can inhibit the growth of various cancer cells. However, the low bioavailability caused by insolubility, limits its clinical application. L-arginine is always used with GA to form a complex to obtain the higher solubility. Moreover, guanidyl group from arginine, which can facilitate the cellular uptake, was identified.Objective: In this study, L-arginine and chitosan (CS) were used for the first time to prepare N-octyl-N-arginine CS (OACS), a novel amphiphilic carrier for GA with solubility- and absorption-enhancing functions; the characterization of the GA loaded OACS micelles (GA-OACS) and its absorption-enhancing effect were also investigated.Materials and methods: GA-OACS were prepared by the dialysis method. The formed micelles were characterized and evaluated by atomic force microscope (AFM), dynamic light scattering, differential scanning calorimeter (DSC), solubility test, in vitro release and in situ intestinal perfusion.Results: The GA-OACS micelles were successfully prepared attaining a 35.3% drug loading and 82.2% entrapment efficiency. GA-OACS had a homogeneous particle size of 160.3?nm; +21.8?mv zeta potential with smooth continuous surface was observed by using AFM. DSC diagram suggested that GA was encapsulated in the micelles. Meanwhile, GA encapsulated in micelles exhibited a desirable slow release in vitro experiment. The solubility of GA in OACS micelles was increased up to 3.16?±?0.13?mg/mL, 2320 times than that of free GA. The single pass perfusion showed that the absorption of GA-OACS micelles was enhanced 3.6-fold, 2.1-fold and 2.2-fold for jejunum, ileum and colon, respectively.Discussion and conclusion: OACS provided excellent ability of drug loading, increasing solubility and enhanced absorption for GA, which indicated that OACS micelles as an oral drug delivery carrier may have potential research and application values. 相似文献
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聚乙烯醇/壳聚糖共混膜的制备及表征 总被引:7,自引:1,他引:7
用溶液共混法制备聚乙烯醇/壳聚糖(PVA/CS)共混膜,对共混膜进行了IR、DSC表征和吸水率、透光率、力学性能等进行测定.结果表明: PVA与CS分子链间在共混膜中有一定的相互作用,相容性好;CS的引入有利于改善PVA的吸水性、透光率和综合力学性能,但热稳定性有所降低. 相似文献
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叶酸受体靶向的聚乳酸共聚物胶束的制备及性质研究 总被引:1,自引:0,他引:1
叶酸偶联的羟脯氨酸-乳酸共聚物(PLLA-PHpr-FA)是一种新型的叶酸受体靶向生物降解聚合物,研究PLLA-PHpr-FA自组装形成胶束的能力及胶束的性质。临界胶束浓度(CMC)用芘荧光探针测定,结果表明,CMC很低并依赖于乳酸/羟脯氨酸的比例。透射电子显微镜(TEM)显示共聚物胶束呈现典型的核/壳结构。动态激光光散射(DLS)测定粒径及粒径分布结果显示,粒径受乳酸/羟脯氨酸比例和丙酮量调控,但粒子几乎不受稀释的影响。用紫外分光光度法测定胶束的载药量和包封率表明,共聚物胶束对疏水性药物的包载较好。因此,PLLA-PHpr-FA胶束可以作为肿瘤靶向的药物载体。 相似文献
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壳聚糖(chitosan,CTS)与氯乙醇反应制备羟乙基壳聚糖(hydroxyethyl chitosan,HECTS),并接合琥珀酸酐合成N-琥珀酰羟乙基壳聚糖(N-succinyl-hydroxyethyl chitosan,Suc-HECTS),考察琥珀酰化度的影响因素确定最适反应条件。用FT-IR对产物进行结构表征,1 H NMR测定脱乙酰度和琥珀酰化度,元素分析法测定羟乙基取代度,并评价了HECTS和Suc-HECTS的细胞毒性。结果表明HECTS与Suc-HECTS均无细胞毒性。在生物医药和药物载体方面的应用提供了一定的理论基础。 相似文献
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用RAFT活性可控聚合法合成了全水亲性嵌段共聚物聚(N-乙烯基吡咯烷酮)-b-聚(2-丙烯酰胺-2-甲基丙磺酸)(PVP-b-PAMPS)和聚(N-乙烯基吡咯烷酮)-b-聚甲基丙烯酸二甲氨基乙酯(PVP-b-PD-MAEMA).二者在水溶液中复合即可形成聚离子复合物(PIC)胶束,并利用动态光散射法(DLS)和透射电镜(TEM)表征了该胶束的粒径、粒径分布以及形貌.研究结果表明,所制备的胶束外形大致呈球状,粒径在155nm左右,且粒径分布较窄.以辅酶A为模型分子,负载在胶束内进行药物控制释放.研究结果表明,辅酶A的释放受溶液pH的影响,该聚离子复合物胶束可以用作药物控释载体. 相似文献
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橡胶硫化剂N,N'-间苯撑双马来酰亚胺的合成 总被引:1,自引:0,他引:1
研究了以乙酸做溶剂,以马来酸酐和间苯二胺为主要原料合成间苯撑双马来酰亚胺的合成方法;通过正交试验,找出了反应的优化条件;通过熔点仪、红外光谱仪、高效液相色谱仪对合成产品进行定性和定量分析.结果表明:溶剂乙酸的用量为间苯二胺质量的3倍,反应容易操作进行;催化剂与间苯二胺的摩尔比为0.05~0.3;马来酸酐与间苯二胺的摩尔比为2.1/1,在此优化条件下产物的得率为90.2%;红外光谱图与标准图谱一致,合成产物的含量为96%. 相似文献
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壳聚糖中空纤维膜的制备及其结构研究 总被引:1,自引:0,他引:1
采用干湿相转化成膜的方法,纺制了壳聚糖中空纤维膜,研究了干燥方法及成膜条件对膜结构的影响.实验发现自然干燥导致膜的严重收缩,最终形成整体致密的膜结构;采用乙醇-正己烷液-液交换干燥,能够有效地避免膜结构的完全致密化,最终形成整体非对称的膜结构.成膜条件的研究结果表明,壳聚糖浓度的提高,更易形成致密层增厚的膜结构;而凝胶温度及凝胶液组成中氢氧化钠浓度的升高,有利于形成致密层更薄,支撑层孔径更大的整体非对称膜结构.进一步的研究表明,整体非对称结构的壳聚糖中空纤维膜可以应用于渗透汽化分离碳酸二甲酯/甲醇混合物,突破恒沸组成的限制,具有较好的应用前景. 相似文献
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羧甲基壳聚糖因其具有良好的水溶性和生物相容性,被广泛应用于生物医学领域。以天然可降解高分子羧甲基壳聚糖为载体,在引发剂过硫酸钾的作用下,通过自由基组合法将N-异丙基丙烯酰胺接枝到羧甲基壳聚糖上,然后在香草醛的交联作用下,采用乳化交联法制备一种负载光敏剂吲哚菁绿(ICG)的新型光热敏感型羧甲基壳聚糖微球,通过傅里叶红外(FT-IR)、核磁(1H-NMR)及扫描电镜(SEM)对共聚物结构及微球形貌进行表征,考察了油水比、转速、香草醛、乳化时间对该纳米微球包载阿霉素载药量的影响,并研究了其光热性能。结果表明,FT-IR和1H-NMR分析证明,N-异丙基丙烯酰胺成功接枝到羧甲基壳聚糖上;SEM分析可知,纳米微球外观呈球状,分布均匀,平均粒径为143 nm。油水比为20∶1,转速为600 r/min,香草醛量为1 mL,乳化时间3 h的微球载药量最高为19.32%。同时,通过改变外界环境条件,纳米微球能缓慢靶向释放药物,具有良好的光热敏感性,该纳米微球在药物控释及药物载体等领域有广泛的应用前景。 相似文献
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以壳聚糖为原料,首先合成N,N-双长链烷基壳聚糖(DACS),溶于四氢呋喃(THF)中用NaH活化后与1,3-丙烷磺内酯反应,制得N,N-双烷基-3,6-O-磺丙基壳聚糖(SPDACS)两亲性衍生物。用FT-IR、1 H-NMR、EA和溶解性实验等对产物进行表征,并研究其在水溶液中的自组装行为。结果表明,SP-DACS能溶于酸性、中性和碱性水溶液中,在水溶液中形成的自组装纳米聚合物胶束为球形结构。随着烷基链长度的增加(8、10、12),临界胶束浓度(CMC)从0.014mg/mL减小到0.006mg/mL,平均粒径从169.4nm减小到117.0nm。甲苯胺蓝变色实验结果表明SPDACS具有类肝素结构,有望成为血液相容性良好的药物载体。 相似文献
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壳聚糖修饰银纳米颗粒的制备及抗菌性能研究 总被引:2,自引:0,他引:2
采用液相化学还原法,以壳聚糖为修饰剂,硼氢化钠为还原剂,制备了壳聚糖修饰银纳米颗粒(chitosan-Ag NPs)。通过X射线粉末衍射仪、透射电子显微镜、傅立叶变换红外光谱仪等对所制备样品的结构和形貌进行了表征。结果表明,所制备纳米颗粒具有面心立方Ag的晶型结构,壳聚糖通过氨基和羟基中的N、O原子与Ag+的化学键合作用修饰在纳米颗粒表面,起到了限制颗粒粒径长大和防止其团聚的作用。采用肉汤连续稀释法检测了样品对大肠杆菌和金黄色葡萄球菌的抑菌杀菌性能,结果表明chitosan-Ag NPs具有优异的抗菌性,抗菌性能受到粒径大小的影响。 相似文献
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采用碱液置换丙二醇的方法制备物理交联壳聚糖水凝胶,研究了碱液浓度及三聚磷酸钠(TPP)离子交联预处理对凝胶结构和力学性能的影响。SEM观察结果表明水凝胶微观结构为富有纳米纤维的三维网络结构,且离子交联预处理在一定程度上会影响水凝胶内部结构的形成。无侧限压缩测试和动态力学分析(DMA)结果显示,未经离子交联的水凝胶在NaOH溶液浓度≤4mol/L时,力学性能随碱溶液浓度增大而增加,在NaOH溶液浓度为4mol/L时获得最优的力学性能;TPP交联后再经NaOH溶液处理的水凝胶其力学性能有所下降,当NaOH溶液浓度为2mol/L时可获得最优的力学性能。采用的2种物理交联方式在水凝胶形成过程中具有竞争关系。 相似文献
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将聚阳离子壳聚糖(CS)与聚阴离子甲基丙烯酰氧乙基磷酰胆碱-甲基丙烯酸二元共聚物(poly(MPC-co-MA),PMA30)进行静电复合,制备CS/PMA30聚离子水凝胶,并用红外(IR)、扫描电镜(SEM)分别对其特征官能团、表面形貌进行表征。然后,以中性红为模型药物对CS/PMA30水凝胶的控释性能进行研究。结果表明,CS/PMA30体系是通过静电作用形成的物理交联水凝胶,对模型药物中性红具有明显的控释性和pH值响应性。该水凝胶具有良好生物相容性有望在药物控释、组织工程等领域具有巨大的应用前景。该研究为进一步提高水凝胶的生物相容性提供了一个新的途径。 相似文献
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