柚皮素固体脂质纳米粒的制备及体内外初步评价
发布时间：2019-05-07 01:52
【摘要】：目的:制备柚皮素固体脂质纳米粒(NRG-SLN),并对其体外和体内的性质进行初步评价。方法:采用溶剂注入法制备NRG-SLN,并对其包封率、载药量、粒径、Zeta电位和体外释放率等性质进行考察,同时采用人肺癌细胞系Calu-3细胞和SD大鼠分别进行细胞毒性、细胞摄取和药动学研究。结果:NRG-SLN为椭圆形大小均匀的粒子,平均粒径、Zeta电位、包封率和载药量分别为(103.9±2.2)nm(PDI=0.226±0.02),(-31.3±3.1)m V,(82.13±3.44)%和(8.31±0.21)%。体外释放表明NRG溶液在5 h内基本释放完全,而NRG-SLN混悬液释放了约35%,24 h累积释放达到80%,有明显的缓释效果。DSC分析表明药物以无定型形式存在。细胞实验说明固体脂质纳米粒载体没有细胞毒性,粒径小、摄取效果较好。体内试验表明NRG-SLN口服生物利用度(AUC0~∞)比NRG原料药高了约2.93倍(P0.05)。结论:本实验成功制备了无细胞毒性的NRG-SLN,提高了NRG的水溶性和体内生物利用度。
[Abstract]:Aim: to prepare naringin solid lipid nanoparticles (NRG-SLN) and evaluate its properties in vitro and in vivo. Methods: NRG-SLN, was prepared by solvent injection method and its encapsulation efficiency, drug loading, particle size, Zeta potential and in vitro release rate were investigated. At the same time, human lung cancer cell line Calu-3 cells and SD rats were used for cytotoxicity. Cellular uptake and pharmacokinetic studies. Results: NRG-SLN was an elliptical particle with uniform particle size, average particle size, Zeta potential, entrapment efficiency and drug loading of (103.9 卤2.2) nm (PDI= 0.226 卤0.02), (- 31.3 卤3.1) m V, respectively). (82.13 卤3.44)% and (8.31 卤0.21)%. The release in vitro showed that the NRG solution was basically completely released within 5 hours, while the NRG-SLN suspension released about 35%, and the cumulative release reached 80% at 24 h. DSC analysis showed that the drug existed in an amorphous form. Cell experiment showed that solid lipid nanoparticles had no cytotoxicity, small particle size and good uptake. The oral bioavailability (AUC0~ 鈭，
本文编号：2470671
[Abstract]:Aim: to prepare naringin solid lipid nanoparticles (NRG-SLN) and evaluate its properties in vitro and in vivo. Methods: NRG-SLN, was prepared by solvent injection method and its encapsulation efficiency, drug loading, particle size, Zeta potential and in vitro release rate were investigated. At the same time, human lung cancer cell line Calu-3 cells and SD rats were used for cytotoxicity. Cellular uptake and pharmacokinetic studies. Results: NRG-SLN was an elliptical particle with uniform particle size, average particle size, Zeta potential, entrapment efficiency and drug loading of (103.9 卤2.2) nm (PDI= 0.226 卤0.02), (- 31.3 卤3.1) m V, respectively). (82.13 卤3.44)% and (8.31 卤0.21)%. The release in vitro showed that the NRG solution was basically completely released within 5 hours, while the NRG-SLN suspension released about 35%, and the cumulative release reached 80% at 24 h. DSC analysis showed that the drug existed in an amorphous form. Cell experiment showed that solid lipid nanoparticles had no cytotoxicity, small particle size and good uptake. The oral bioavailability (AUC0~ 鈭，
本文编号：2470671
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