EGCG-CS-PAA納米粒的制備及其生物活性研究
發(fā)布時間：2018-10-19 10:41
【摘要】：EGCG陛質很不穩(wěn)定,易受光、氧、溫度、pH、金屬離子等外界因素的影響從而嚴重限制了其應用的前景。在參考前人研究的基礎上,發(fā)現(xiàn)殼聚糖納米技術能較好的保護EGCG免于遭受惡劣環(huán)境的破壞。殼聚糖納米粒包埋EGCG后,由于納米粒的優(yōu)越特性,使得EGCG生物功效得到提高,同時EGCG的釋放也變緩,從而提高了EGCG的利用效率。 在本研究中,利用殼聚糖CS和聚天冬氨酸PAA之間離子交聯(lián)制備CS-PAA納米粒載體,以此裝載EGCG,然后對EGCG-CS-PAA納米粒的穩(wěn)定性和生物活性等做了相關研究。研究發(fā)現(xiàn),不同的制備參數(shù)能顯著影響納米粒的粒徑、分散指數(shù)和Zeta電位等特性。當質量比(CS/PAA)為1.0、pH為3.5、反應時間為60min、CS分子量為3-5KDa和PAA分子量為30-50KDa時,制備出的殼聚糖納米粒的粒徑和表面電荷等物理特征為最佳。同時,在該制備參數(shù)下制備出的EGCG-CS-PAA納米粒的包封率達到25%,載藥量為344.1mg/kg,且其粒徑比未包埋EGCG的CS-PAA納米粒大些。 EGCG-CS-PAA納米粒的體外釋放研究表明在模擬胃環(huán)境(pH=2.5-4.0)下從納米粒中釋放出來的EGCG含量較少；在模擬腸環(huán)境(pH=6.0-7.4)下,納米顆粒容易發(fā)生降解從而迅速釋放EGCG。通過采用FRAP和DPPH法對EGCG-CS-PAA納米粒的抗氧化活性進行分析,兩者都顯示納米體系對EGCG的抗氧化活性具有良好的保護作用。同時EGCG-CS-PAA納米體系能在高溫、堿性等惡劣環(huán)境下對EGCG起到較好的保護作用。 白兔體內試驗結果顯示,相比于自由的EGCG, EGCG-CS-PAA納米粒在預防白兔動脈粥樣硬化及其降血脂功效方面得到明顯的提高。在EGCG納米粒小鼠急性試驗中,在實驗最大劑量(60mL/kg)范圍內,雌雄小鼠均未出現(xiàn)死亡及異常情況,且給藥后對小鼠的體重也無顯著影響。同時,細胞毒性試驗結果也表明EGCG-CS-PAA納米粒及所制備的材料均為無毒安全的。 本研究結果表明,CS-PAA納米體系可以作為如EGCG等不穩(wěn)定功能性藥物的載體,有效保護其生物穩(wěn)定性,為EGCG在醫(yī)藥食品等領域的應用開拓新的途徑。
[Abstract]:EGCG is unstable and vulnerable to light, oxygen, temperature, pH, metal ions and other external factors, which seriously limits its application prospects. On the basis of previous studies, it was found that chitosan nanotechnology could protect EGCG from severe environmental damage. After EGCG was encapsulated by chitosan nanoparticles, because of the superior properties of nanoparticles, the biological efficacy of EGCG was improved, and the release of EGCG was slowed down, thus improving the utilization efficiency of EGCG. In this study, the carrier of CS-PAA nanoparticles was prepared by ion crosslinking between chitosan CS and polyaspartic acid PAA, and then the stability and bioactivity of EGCG-CS-PAA nanoparticles were studied by loading EGCG,. It is found that different preparation parameters can significantly affect the particle size, dispersion index and Zeta potential. When the mass ratio (CS/PAA) is 1.0 渭 g pH is 3.5, the reaction time is 60 min CS molecular weight is 3-5KDa and PAA molecular weight is 30-50KDa, the size and surface charge of the prepared chitosan nanoparticles are the best. meanwhile The encapsulation efficiency of EGCG-CS-PAA nanoparticles prepared under this preparation parameter is 25mg / kg, the drug loading is 344.1 mg / kg, and its diameter is larger than that of CS-PAA nanoparticles without EGCG. The in vitro release study of EGCG-CS-PAA nanoparticles shows that under simulated gastric environment (pH=2.5-4.0), The content of EGCG released from nanoparticles was less. Under simulated intestinal environment (pH=6.0-7.4), nanoparticles are liable to degrade and release EGCG. rapidly. The antioxidant activity of EGCG-CS-PAA nanoparticles was analyzed by FRAP and DPPH. Both of them showed that the nanoparticles had good protective effect on the antioxidant activity of EGCG. At the same time, EGCG-CS-PAA nanosystem can protect EGCG in high temperature and alkaline environment. The results showed that compared with the free EGCG, EGCG-CS-PAA nanoparticles, the effect of preventing atherosclerosis and lowering blood lipids in white rabbits was significantly improved. In the acute test of EGCG nanoparticles mice, in the range of maximum experimental dose (60mL/kg), there was no death and abnormality in both male and female mice, and there was no significant effect on the body weight of mice after administration of the drug. At the same time, the results of cytotoxicity test also showed that the EGCG-CS-PAA nanoparticles and the prepared materials were nontoxic and safe. The results show that CS-PAA nanosystem can be used as a carrier of unstable functional drugs such as EGCG, protect its biological stability effectively, and open up a new way for the application of EGCG in the field of medicine and food.
【學位授予單位】：浙江工商大學
【學位級別】：碩士
【學位授予年份】：2015
【分類號】：TQ460.1;TB383.1
本文編號：2280886
[Abstract]:EGCG is unstable and vulnerable to light, oxygen, temperature, pH, metal ions and other external factors, which seriously limits its application prospects. On the basis of previous studies, it was found that chitosan nanotechnology could protect EGCG from severe environmental damage. After EGCG was encapsulated by chitosan nanoparticles, because of the superior properties of nanoparticles, the biological efficacy of EGCG was improved, and the release of EGCG was slowed down, thus improving the utilization efficiency of EGCG. In this study, the carrier of CS-PAA nanoparticles was prepared by ion crosslinking between chitosan CS and polyaspartic acid PAA, and then the stability and bioactivity of EGCG-CS-PAA nanoparticles were studied by loading EGCG,. It is found that different preparation parameters can significantly affect the particle size, dispersion index and Zeta potential. When the mass ratio (CS/PAA) is 1.0 渭 g pH is 3.5, the reaction time is 60 min CS molecular weight is 3-5KDa and PAA molecular weight is 30-50KDa, the size and surface charge of the prepared chitosan nanoparticles are the best. meanwhile The encapsulation efficiency of EGCG-CS-PAA nanoparticles prepared under this preparation parameter is 25mg / kg, the drug loading is 344.1 mg / kg, and its diameter is larger than that of CS-PAA nanoparticles without EGCG. The in vitro release study of EGCG-CS-PAA nanoparticles shows that under simulated gastric environment (pH=2.5-4.0), The content of EGCG released from nanoparticles was less. Under simulated intestinal environment (pH=6.0-7.4), nanoparticles are liable to degrade and release EGCG. rapidly. The antioxidant activity of EGCG-CS-PAA nanoparticles was analyzed by FRAP and DPPH. Both of them showed that the nanoparticles had good protective effect on the antioxidant activity of EGCG. At the same time, EGCG-CS-PAA nanosystem can protect EGCG in high temperature and alkaline environment. The results showed that compared with the free EGCG, EGCG-CS-PAA nanoparticles, the effect of preventing atherosclerosis and lowering blood lipids in white rabbits was significantly improved. In the acute test of EGCG nanoparticles mice, in the range of maximum experimental dose (60mL/kg), there was no death and abnormality in both male and female mice, and there was no significant effect on the body weight of mice after administration of the drug. At the same time, the results of cytotoxicity test also showed that the EGCG-CS-PAA nanoparticles and the prepared materials were nontoxic and safe. The results show that CS-PAA nanosystem can be used as a carrier of unstable functional drugs such as EGCG, protect its biological stability effectively, and open up a new way for the application of EGCG in the field of medicine and food.
【學位授予單位】：浙江工商大學
【學位級別】：碩士
【學位授予年份】：2015
【分類號】：TQ460.1;TB383.1
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