β-环糊精载药纳米纤维的制备及其缓释行为研究
发布时间：2018-12-29 09:11
【摘要】：β-环糊精(β-CD),一种生物相容性极好的超分子材料,由于其特殊的几何结构,具有亲水的外围和疏水的内腔,可以与大多数尺寸合适的分子形成主客体包合结构,赢得了极大关注。β-环糊精能够改善包合物的化学和物理性质,包括防止客体分子受到外界条件的破坏、提升溶解性以及提高客体分子稳定性的特点,为制备复合材料提供了良好的属性,近年来被广泛应用于药物辅料。本文以β-环糊精为添加物,以生物相容性良好的有机物作为基材,制得了三种复合载药纳米纤维,再对其性能和应用进行了研究,主要内容如下:(1)采用玉米醇溶蛋白(Zein)与β-CD在乙酸体系中通过静电纺丝得到Zein/β-CD复合纳米材料。DSC表明,通过加入β-CD,Zein的玻璃化转变温度迁移到了更高的温度。之后,抗真菌药物灰黄霉素(GSV)与β-CD形成包合结构,从而加载到复合材料中,制成载药纳米纤维,其热学性能随着差示扫描量热法(DSC)进行了研究,结果证实了包合结构的存在。紫外光谱分析表明,载药纳米纤维最终的累积释药百分率超过60%,并且前期(8 h-48 h)的药物释放行为有一定的缓释效果。(2)为了提高基材醋酸纤维素(CA)的可纺性,通过在N,N-二甲基乙酰胺(DMAc)中加入β-环糊精(β-CD),成功制备了不同配比的CA/β-CD复合纳米纤维。之后,抗真菌药物灰黄霉素(GSV)加载到复合基材中,制成载药纳米膜,DSC结果表明,β-CD包合了药物GSV,使其具有较高的热稳定性。紫外光谱分析表明,载药纳米纤维最终的累积释药百分率超过75%,包合结构的存在使载药纳米纤维在药物释放的前期有有一定的缓释效果。(3)生物相容性良好的聚乙烯醇-苯乙烯吡啶(PVA-SbQ)被用作基础聚合物交联剂,结合了β-环糊精(β-CD)通过静电纺制备了纳米复合材料。FTIR证实β-CD的存在。复合纳米材料的形貌和平均纤维直径也通过SEM进行了分析。此外,TGA分析得知PVA-SbQ/β-CD复合纳米纤维的热学性能得到了改善。而且发现交联后的复合纳米材料具有明显的高拉伸强度(TS)以及更大的断裂伸长率(EB)。最终,抗真菌药物灰黄霉素(GSV)在水溶液中与β-CD形成包合结构,从而加载到复合纳米纤维中。紫外光谱分析表明,载药纳米纤维最终的累积释药百分率超过90%,表现出一定的缓释效果。
[Abstract]:尾-cyclodextrin (尾-CD),) is a supermolecular material with excellent biocompatibility. Because of its special geometric structure, 尾-cyclodextrin has hydrophilic periphery and hydrophobic inner cavity, which can form a host and guest inclusion structure with most molecules of suitable size. 尾 -cyclodextrin can improve the chemical and physical properties of inclusion compounds, including the characteristics of preventing guest molecules from being destroyed by external conditions, enhancing solubility and enhancing the stability of guest molecules. It provides good properties for the preparation of composite materials and has been widely used in pharmaceutical excipients in recent years. In this paper, three kinds of composite drug-loaded nanofibers were prepared by using 尾 -cyclodextrin as additive and organic compounds with good biocompatibility as substrate, and their properties and applications were studied. The main contents are as follows: (1) Zein/ 尾-CD composite nanomaterials were prepared by electrostatic spinning of Zein (Zein) and 尾-CD in acetic acid system. DSC showed that 尾-CD, was added to the composite nanomaterials. The glass transition temperature of Zein migrated to a higher temperature. After that, the antifungal drug Grysoflavin (GSV) and 尾-CD formed inclusion structure, and then loaded into the composite to make drug-loaded nanofibers. Its thermal properties were studied with differential scanning calorimetry (DSC). The results confirm the existence of inclusion structure. UV spectrum analysis shows that the final cumulative drug release percentage of drug-loaded nanofibers exceeds 60%. In order to improve the spinnability of cellulose acetate (CA), the drug release behavior in the early stage (8 h-48 h) was controlled. 尾 -cyclodextrin (尾 -cyclodextrin) was added into N-dimethylacetamide (DMAc) to prepare CA/ 尾-CD nanofibers with different ratios. After that, the antifungal drug, Grysoflavin (GSV), was loaded into the composite substrate to make the drug-loaded nano-film. The DSC results showed that 尾-CD encapsulated the drug GSV, and made it have higher thermal stability. UV spectrum analysis showed that the final cumulative drug release percentage of the drug-loaded nanofibers was more than 75%. Due to the existence of inclusion structure, the drug-loaded nanofibers have a slow release effect in the early stage of drug release. (3) Polyvinyl alcohol and styrene pyridine (PVA-SbQ), which has good biocompatibility, is used as the basic polymer crosslinking agent. Nanocomposites were prepared by electrospinning with 尾-cyclodextrin (尾-CD). The presence of 尾-CD was confirmed by FTIR. The morphology and average fiber diameter of the nanocomposites were also analyzed by SEM. In addition, TGA analysis showed that the thermal properties of PVA-SbQ/ 尾-CD nanofibers were improved. It was also found that the crosslinked composite nanocomposites had obvious high tensile strength (TS) and greater elongation at break (EB). Finally, the antifungal drug Grysoflavin (GSV) formed inclusion structure with 尾-CD in aqueous solution, and then loaded into composite nanofibers. UV spectrum analysis showed that the final cumulative drug release percentage of drug-loaded nanofibers exceeded 90%, showing a certain sustained release effect.
【学位授予单位】：江南大学
【学位级别】：硕士
【学位授予年份】：2017
【分类号】：TQ342.8
本文编号：2394634
[Abstract]:尾-cyclodextrin (尾-CD),) is a supermolecular material with excellent biocompatibility. Because of its special geometric structure, 尾-cyclodextrin has hydrophilic periphery and hydrophobic inner cavity, which can form a host and guest inclusion structure with most molecules of suitable size. 尾 -cyclodextrin can improve the chemical and physical properties of inclusion compounds, including the characteristics of preventing guest molecules from being destroyed by external conditions, enhancing solubility and enhancing the stability of guest molecules. It provides good properties for the preparation of composite materials and has been widely used in pharmaceutical excipients in recent years. In this paper, three kinds of composite drug-loaded nanofibers were prepared by using 尾 -cyclodextrin as additive and organic compounds with good biocompatibility as substrate, and their properties and applications were studied. The main contents are as follows: (1) Zein/ 尾-CD composite nanomaterials were prepared by electrostatic spinning of Zein (Zein) and 尾-CD in acetic acid system. DSC showed that 尾-CD, was added to the composite nanomaterials. The glass transition temperature of Zein migrated to a higher temperature. After that, the antifungal drug Grysoflavin (GSV) and 尾-CD formed inclusion structure, and then loaded into the composite to make drug-loaded nanofibers. Its thermal properties were studied with differential scanning calorimetry (DSC). The results confirm the existence of inclusion structure. UV spectrum analysis shows that the final cumulative drug release percentage of drug-loaded nanofibers exceeds 60%. In order to improve the spinnability of cellulose acetate (CA), the drug release behavior in the early stage (8 h-48 h) was controlled. 尾 -cyclodextrin (尾 -cyclodextrin) was added into N-dimethylacetamide (DMAc) to prepare CA/ 尾-CD nanofibers with different ratios. After that, the antifungal drug, Grysoflavin (GSV), was loaded into the composite substrate to make the drug-loaded nano-film. The DSC results showed that 尾-CD encapsulated the drug GSV, and made it have higher thermal stability. UV spectrum analysis showed that the final cumulative drug release percentage of the drug-loaded nanofibers was more than 75%. Due to the existence of inclusion structure, the drug-loaded nanofibers have a slow release effect in the early stage of drug release. (3) Polyvinyl alcohol and styrene pyridine (PVA-SbQ), which has good biocompatibility, is used as the basic polymer crosslinking agent. Nanocomposites were prepared by electrospinning with 尾-cyclodextrin (尾-CD). The presence of 尾-CD was confirmed by FTIR. The morphology and average fiber diameter of the nanocomposites were also analyzed by SEM. In addition, TGA analysis showed that the thermal properties of PVA-SbQ/ 尾-CD nanofibers were improved. It was also found that the crosslinked composite nanocomposites had obvious high tensile strength (TS) and greater elongation at break (EB). Finally, the antifungal drug Grysoflavin (GSV) formed inclusion structure with 尾-CD in aqueous solution, and then loaded into composite nanofibers. UV spectrum analysis showed that the final cumulative drug release percentage of drug-loaded nanofibers exceeded 90%, showing a certain sustained release effect.
【学位授予单位】：江南大学
【学位级别】：硕士
【学位授予年份】：2017
【分类号】：TQ342.8
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