Leroux J C, De Jaeghere F, Anner B, Doelker E, Gurny R
School of Pharmacy, University of Geneva, Switzerland.
Life Sci. 1995;57(7):695-703. doi: 10.1016/0024-3205(95)00321-v.
We demonstrate here that polyethylene glycol (PEG) 6,000 protects biodegradable poly(D,L-lactic acid) nanoparticles (PLA NP) from extensive uptake by monocytes in plasma. These results are in agreement with those previously obtained with PEG 20,000 which reduced the uptake of PLA NP by human monocytes in phosphate buffered saline and plasma, and prolonged the NP circulation time in vivo. The coating efficiency of PEG 6,000 and 20,000 was substantially decreased in serum. The difference between the uptake of plain and coated NP clearly reappeared for PEG 20,000-coated NP in heat inactivated serum and in IgG-depleted serum. We suggest that typical plasma proteins, heat labile serum proteins (e.g. complement components) and IgG are involved in the opsonization of plain and coated PLA NP. Other proteins previously found to adsorb onto these NP, namely albumin and apolipoprotein E, did not appear to directly influence the uptake process.
我们在此证明，聚乙二醇（PEG）6000可保护可生物降解的聚（D，L-乳酸）纳米颗粒（PLA NP）不被血浆中的单核细胞大量摄取。这些结果与先前使用聚乙二醇20000所获得的结果一致，聚乙二醇20000可减少人单核细胞在磷酸盐缓冲盐水和血浆中对PLA NP的摄取，并延长纳米颗粒在体内的循环时间。聚乙二醇6000和20000在血清中的包被效率显著降低。在热灭活血清和IgG耗尽的血清中，聚乙二醇20000包被的纳米颗粒在普通纳米颗粒和包被纳米颗粒摄取之间的差异明显再次出现。我们认为，典型的血浆蛋白、热不稳定血清蛋白（如补体成分）和IgG参与了普通和包被的PLA NP的调理作用。先前发现吸附在这些纳米颗粒上的其他蛋白质，即白蛋白和载脂蛋白E，似乎并未直接影响摄取过程。
