Department of Chemical Engineering and Materials Science, University of Minnesota, Minneapolis, Minnesota 55455, USA.
J Pharm Sci. 2010 Oct;99(10):4295-306. doi: 10.1002/jps.22090.
Polyelectrolyte protected beta-carotene nanoparticles (nanosuspensions) with average diameter of <100 nm were achieved by turbulent mixing and flash nanoprecipitation (FNP). Three types of multi-amine functional polyelectrolytes, epsilon-polylysine (epsilon-PL), poly(ethylene imine) (PEI), and chitosan, were investigated to electrosterically protect the nanoparticles. Particle size and distribution were measured by dynamic light scattering (DLS); particles were imaged via scanning electron microscopy (SEM) and cryogenic transmission electron microscopy (cryo-TEM). Low pH and high polyelectrolyte molecular weight gave the smallest and most stable particles. High drug loading capacity, >80 wt%, was achieved by using either PEI or chitosan. X-ray diffraction (XRD) patterns showed that beta-carotene nanoparticles were amorphous. These findings open the way for utilization of FNP for preparation of nanoparticles with enhanced bioavailability for highly water insoluble drugs.
通过湍流混合和闪蒸纳米沉淀（FNP）技术制备了平均直径小于 100nm 的聚电解质保护的β-胡萝卜素纳米粒子（纳米悬浮液）。研究了三种多胺功能型聚电解质，即ε-聚赖氨酸（ε-PL）、聚乙烯亚胺（PEI）和壳聚糖，以静电方式保护纳米粒子。通过动态光散射（DLS）测量粒径和分布；通过扫描电子显微镜（SEM）和低温透射电子显微镜（cryo-TEM）对颗粒进行成像。低 pH 值和高聚电解质分子量可获得最小且最稳定的颗粒。使用 PEI 或壳聚糖可实现高载药量，>80wt%。X 射线衍射（XRD）图谱表明β-胡萝卜素纳米粒子为无定形。这些发现为利用 FNP 制备具有高水不溶性药物增强生物利用度的纳米粒子开辟了道路。
