Department of Pharmaceutics, School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 210203, PR China.
Int J Pharm. 2010 Sep 15;397(1-2):155-63. doi: 10.1016/j.ijpharm.2010.06.030. Epub 2010 Jun 25.
A bioadhesive drug delivery system, wheat germ agglutinin (WGA)-grafted lipid nanoparticles, was developed for the oral delivery of bufalin (a hydrophobic active component extracted from the traditional Chinese medicine Chan'su). The lipid nanoparticles associated with poly(vinyl alcohol) (PVA) were prepared by high-pressure homogenization. WGA was coupled to lipid nanoparticles by activating the hydroxyl group using glutaraldehyde, and then conjugating the nanoparticles with WGA. WGA-grafted lipid nanoparticles with a mean particle size of 164 nm and zeta potential of -10.6 mV were obtained with bufalin encapsulation of 68.2%. The amount of bound WGA was approximately 28.9% of the amount of WGA initially added. The association study between fluorescent 6-coumarin-loaded WGA-grafted lipid nanoparticles and Caco-2 monolayers showed that WGA enhanced the cellular uptake of nanoparticles compared with WGA-free lipid nanoparticles. These results suggest that WGA-grafted lipid nanoparticles could be a promising carrier to enhance cellular uptake. They could also improve drug bioavailability through the oral route.
一种生物黏附型药物传递系统，即麦胚凝集素（WGA）接枝脂质纳米粒，被开发用于蟾酥（一种从传统中药蟾酥中提取的疏水性活性成分）的口服给药。脂质纳米粒与聚乙烯醇（PVA）通过高压匀质法结合。WGA 通过戊二醛激活其羟基与脂质纳米粒结合，然后将纳米粒与 WGA 连接。用 WGA 接枝脂质纳米粒包裹蟾酥，得到平均粒径为 164nm、Zeta 电位为-10.6mV 的 WGA 接枝脂质纳米粒，蟾酥包封率为 68.2%。结合的 WGA 量约为初始添加 WGA 量的 28.9%。荧光 6-香豆素负载的 WGA 接枝脂质纳米粒与 Caco-2 单层之间的结合研究表明，与不含 WGA 的脂质纳米粒相比，WGA 增强了纳米粒的细胞摄取。这些结果表明，WGA 接枝脂质纳米粒可能是一种很有前途的载体，能够增强细胞摄取。它们还可以通过口服途径提高药物的生物利用度。
