【摘要】：目的:制備柚皮素固體脂質(zhì)納米粒(NRG-SLN),并對(duì)其體外和體內(nèi)的性質(zhì)進(jìn)行初步評(píng)價(jià)。方法:采用溶劑注入法制備NRG-SLN,并對(duì)其包封率、載藥量、粒徑、Zeta電位和體外釋放率等性質(zhì)進(jìn)行考察,同時(shí)采用人肺癌細(xì)胞系Calu-3細(xì)胞和SD大鼠分別進(jìn)行細(xì)胞毒性、細(xì)胞攝取和藥動(dòng)學(xué)研究。結(jié)果:NRG-SLN為橢圓形大小均勻的粒子,平均粒徑、Zeta電位、包封率和載藥量分別為(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)%。體外釋放表明NRG溶液在5 h內(nèi)基本釋放完全,而NRG-SLN混懸液釋放了約35%,24 h累積釋放達(dá)到80%,有明顯的緩釋效果。DSC分析表明藥物以無定型形式存在。細(xì)胞實(shí)驗(yàn)說明固體脂質(zhì)納米粒載體沒有細(xì)胞毒性,粒徑小、攝取效果較好。體內(nèi)試驗(yàn)表明NRG-SLN口服生物利用度(AUC0~∞)比NRG原料藥高了約2.93倍(P0.05)。結(jié)論:本實(shí)驗(yàn)成功制備了無細(xì)胞毒性的NRG-SLN,提高了NRG的水溶性和體內(nèi)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 鹵2.2) nm (PDI= 0.226 鹵0.02), (- 31.3 鹵3.1) m V, respectively). (82.13 鹵3.44)% and (8.31 鹵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，

本文編號(hào)：2470671