Li Feng-Qian, Su Hua, Wang Jing, Liu Ji-Yong, Zhu Quan-Gang, Fei Yi-Bo, Pan Yong-Hua, Hu Jin-Hong
Department of Pharmaceutical Sciences, Changhai Hospital, Second Military Medical University, Shanghai 200433, China.
Int J Pharm. 2008 Feb 12;349(1-2):274-82. doi: 10.1016/j.ijpharm.2007.08.001. Epub 2007 Aug 11.
Sodium ferulate (SF) loaded nanoparticles were prepared by desolvation procedure and subsequent cross-linking of the wall material of bovine serum albumin (BSA). Several factors in the nanoencapsulation process, such as the addition rate of the desolvation agent, composition of BSA and SF solution, amount of the cross-linker glutaraldehyde, were investigated to elucidate their influences on the particle size, zeta potential, drug loading and encapsulation efficiency of the resulted nanoparticles. The obtained spherical nanoparticles were negative charged with zeta potential from -20 to -40 mV, and characterized between 100 and 200 nm with a narrow size distribution. In the condition of introducing 1.0 mL 8% glutareldehyde per mg of BSA, the drug entrapment efficiency (EE) of 80% (w/w) and loading capacity of about 16% (w/w) could be achieved for the cross-linked BSA nanoparticles with SF encapsulated (SF-BSA-NP). And the drug EE was decreased along with the increasing amount of glutareldehyde used for cross-linking. The in vitro drug release properties of SF-BSA-NP behaved with an initial burst effect and then sustained-release stage. To some extent, the drug release rate could be adjusted by cross-linking with different amount of glutaraldehyde. Compared with SF solution, SF-BSA-NP showed a much higher drug distribution into liver and a lower drug concentration in other tissues, after intravenously injected to mice. So, BSA based nanoparticles might be a suitable controlled released carrier for the freely water-soluble drug SF and further hepatic targeted drug delivery.
通过去溶剂化法并随后交联牛血清白蛋白(BSA)壁材制备了载阿魏酸钠(SF)纳米粒。研究了纳米包封过程中的几个因素,如去溶剂化剂的添加速率、BSA和SF溶液的组成、交联剂戊二醛的用量,以阐明它们对所得纳米粒的粒径、ζ电位、载药量和包封率的影响。所获得的球形纳米粒带负电荷,ζ电位为-20至-40 mV,粒径在100至200 nm之间,尺寸分布较窄。在每毫克BSA引入1.0 mL 8%戊二醛的条件下,包封SF的交联BSA纳米粒(SF-BSA-NP)的药物包封率(EE)可达80%(w/w),载药量约为16%(w/w)。并且药物EE随着用于交联的戊二醛量的增加而降低。SF-BSA-NP的体外药物释放特性表现为初始突释效应,然后是缓释阶段。在一定程度上,药物释放速率可通过与不同量的戊二醛交联来调节。与SF溶液相比,静脉注射给小鼠后,SF-BSA-NP在肝脏中的药物分布更高,在其他组织中的药物浓度更低。因此,基于BSA的纳米粒可能是水溶性药物SF合适的控释载体,可进一步实现肝靶向给药。