Florence A T, Hillery A M, Hussain N, Jani P U
Centre for Drug Delivery Research, School of Pharmacy, University of London, UK.
J Drug Target. 1995;3(1):65-70. doi: 10.3109/10611869509015936.
Quantitative and qualitative evidence from our laboratories on the absorption and translocation of polystyrene latex nanoparticles both by histological (qualitative) and analytical measurement of levels of polystyrene (quantitative) is briefly reviewed in this paper. We have previously compared the uptake of nonionized polystyrene latex ranging in size from 50nm to 3 microns, and made some comparisons of uptake between carboxylated microspheres and nonionic systems, showing the lower uptake of the former through the lymphoid tissue of the gastrointestinal tract. Size is a key parameter, uptake increasing with decreasing particle diameter. Early evidence suggested that uptake is by way of the Peyer's patches and other elements of the gut associated lymphoid tissue (GALT). Adsorption of hydrophilic block-copolymers onto polystyrene markedly reduces the uptake by intestinal GALT. Modification of the surface with specific ligands such as by covalent attachment of tomato lectin molecules has indicated widespread uptake by non-GALT tissues, following their binding to and internalisation by enterocytes. The ability to decrease and increase uptake is clear evidence of a phenomenon which has the potential for further control to allow it to be exploited fully for drug or vaccine delivery. The evidence to date with nanoparticles as carriers systems for labile drugs such as proteins by the oral route remains to be substantiated.
本文简要回顾了我们实验室关于聚苯乙烯乳胶纳米颗粒吸收和转运的定量和定性证据,这些证据来自组织学(定性)以及聚苯乙烯水平的分析测量(定量)。我们之前比较了尺寸范围从50纳米到3微米的非离子化聚苯乙烯乳胶的摄取情况,并对羧化微球和非离子系统的摄取进行了一些比较,结果表明前者通过胃肠道淋巴组织的摄取量较低。尺寸是一个关键参数,摄取量随颗粒直径减小而增加。早期证据表明摄取是通过派尔集合淋巴结和肠道相关淋巴组织(GALT)的其他成分进行的。亲水性嵌段共聚物在聚苯乙烯上的吸附显著降低了肠道GALT的摄取。用特定配体修饰表面,如通过共价连接番茄凝集素分子,表明在它们与肠细胞结合并内化后,非GALT组织广泛摄取。降低和增加摄取的能力清楚地证明了一种现象,这种现象有可能进一步控制,以便充分利用它进行药物或疫苗递送。迄今为止,纳米颗粒作为口服不稳定药物(如蛋白质)载体系统的证据仍有待证实。