紫檀芪纳米载体的制备与表征

论文总字数：24791字

摘 要

紫檀茋（Pterostilbene）是白藜芦醇的结构同系物，具有抗氧化、抗菌和抗癌等多种功效。但由于其在光照下不稳定，易变色，高温制备条件下含量就会减小，而且由于其微溶于水，还存在生物利用度较低等技术问题。如何提高紫檀茋的稳定性，提高该成分的生物利用度还是亟待解决的问题。本研究的意义在于通过载体对紫檀茋进行包裹，实现它在真皮应用中的潜在优势，并通过后期评价和表征，进一步证明载体包裹的优势，另外为紫檀茋的产业化应用提供铺垫。

本文首先通过脂质筛选和乳化剂筛选，考察了不同脂质含量、乳化剂含量以及甘油和水的比例对体系的影响，得到了紫檀茋类脂纳米囊的最佳配方，通过不同制备参数的考察，确定了制备紫檀茋类脂纳米囊的最佳工艺参数。

实验制备得到的紫檀茋类脂纳米囊中紫檀茋的含量为4.5±0.05%（w/w），包封率为99.5±0.1%，粒径为48nm，pH8.20，随后考察了体系的物理稳定性和化学稳定性，结果表明体系的稀释稳定性、离心稳定性和长期储存稳定都很好，而在过酸过碱环境中颗粒会发生聚集，在光照条件下一个月含量明显下降，表明在实际应用中要注意pH的调节，储存和运输过程中要注意避光。

最后，对所得到的的体系进行了体外释放和体外透皮性能研究。体外释放结果表明，紫檀茋能从纳米载体系统中完全释放出来，发挥其应有的功效。体外透皮实验结果表明，相比于未经过包裹的紫檀茋，经过类脂纳米囊包裹的紫檀茋具有更好的渗透性能，在兔皮内的积累量明显高于对照组，能够有效促进紫檀茋的生物利用；而透过皮肤的紫檀茋含量明显低于对照组，表明体系具有更低的系统毒性。

关键词：紫檀茋 ；纳米载体； 稳定性； 化妆品

Abstract

Pterostilbene is a structural homologue of resveratrol,it Has many effects such as antioxidant, antibacterial and anticancer.However, due to its instability in the light, volatile color, the content of the high temperature preparation conditions can be reduced, and because of its micro soluble in water, there are still lower bioavailability and lower technology issues.How to improve the stability of pterostilbene, improve the degree or problems of the composition of biological utilization. The significance of this study lies in the fact that through the carrier of pterostilbene package to realize its potential advantages in application of dermal, and through the late evaluation and characterization, further evidence of the advantages of parcel carriers, also for the industrial application of pterostilbene to pave the way.

Firstly through lipid screening and emulsifier screening, investigating the effect of different lipid content and emulsifier content and glycerol and water ratio of the system, has been the best formula of pterostilbene lipid nanocapsules, through different system parameters for preparation of investigation to determine the optimal process parameters of the preparation of pterostilbene lipid nanocapsules.

Experimental preparation of pterostilbene lipid nanocapsules of pterostilbene content is 4.5 0.05% (w / W), encapsulation rate was 99.5 0.1%, the particle size is 48nm, pH8.20. Then they examine physical and chemical stability of a system, results show that the system stability of dilution, centrifugal stability and long-term storage stability are good, and in too acid alkali environment particles aggregation occurs in light conditions a month was significantly decreased, indicating that should pay attention to in the practical application of pH regulation, storage and transportation process should pay attention to avoid light.

Finally, the release and transdermal properties of the obtained system were studied in vitro.. In vitro experiments showed that, pterostilbene can come out completely from the nano carrier system release, to play its due effect. In vitro transdermal experiment results show that compared to after the package of pterostilbene. After lipid nanocapsules coated pterostilbene has better permeability properties, in the rabbit accumulation were significantly higher than that of control group, can effectively promote the use of pterostilbene biology; and through the skin of the purple Tan stilbene content was significantly lower than that of the control group, shows that the system has lower systemic toxicity.

Keywords: pterostilbene; nanoparticles; stability; cosmetics

目录

摘要…………………………………………………………………………………………………………I

关键词…………………………………………………………………………………………II

第一章 绪论 引言…………………………………………………………………………………………1

1.1紫檀茋简介及在化妆品领域的应用…………………………………………………1

1.2脂质纳米载体技术 ………………………………………………………………1

1.2.1纳米乳液……………………………………………………………………2

1.2.2纳米脂质体……………………………………………………………………2

1.2.3脂质纳米粒……………………………………………………………………2

1.2.4环糊精………………………………………………………………………3

1.2.5类脂纳米囊乳液………………………………………………………………3

1.3本研究的主要目的………………………………………………………3

第二章 材料与方法………………………………………………………………………4

2.1实验材料 ……………………………………………………………………………4

2.2实验仪器 ……………………………………………………………………………4

2.3实验方法 ……………………………………………………………………………4

2.3.1脂质筛选……………………………………………………………………4

2.3.2乳化剂筛选……………………………………………………………………4

2.3.3配方和制备参数的确定…………………………………………………………4

2.3.3.1脂质含量对配方的影响…………………………………………………4

2.3.3.2乳化剂含量对配方的影响………………………………………………5

2.3.3.3甘油和水的比例对配方的影响…………………………………………5

2.3.3.4制备温度和制备时间的影响………………………………………5

2.3.4含量和包封率的测定……………………………………………………………5

2.3.4.1标准曲线的绘制………………………………………………5

2.3.4.2含量和包封率的测定……………………………………………………5

2.3.5配方的物理化学稳定性考察……………………………………………………5

2.3.5.1离心稳定性考察…………………………………………………………5

2.3.5.2稀释稳定性考察…………………………………………………………5

2.3.5.3 PH稳定性考察……………………………………………………………6

2.3.5.4表面活性剂耐受性考察…………………………………………………6

2.3.5.5长期稳定性考察…………………………………………………………6

2.3.5.6紫檀茋含量稳定性考察…………………………………………………7

2.3.6配方的功效表征……………………………………………………7

2.3.6.1体外释放研究……………………………………………………7

2.3.6.2经皮行为研究……………………………………………………7

第三章 结果与讨论…………………………………………………………………………8

3.1脂质筛选结果 ……………………………………………………………………………8

3.2乳化剂筛选结果 ………………………………………………………………………8

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