Champanhac Carole, Haas Heinrich, Landfester Katharina, Mailänder Volker
Max-Planck-Institute for Polymer Research, Ackermannweg 10, 55122 Mainz, Germany.
Biomater Sci. 2021 Feb 21;9(4):1227-1231. doi: 10.1039/d0bm01946a. Epub 2021 Feb 11.
Liposomal formulations are used to improve the safety and cellular absorption of conventional drugs by limiting their interaction with phagocytes. The uptake behaviour of these nanocarriers is affected by the blood composition, and accordingly the presence of an anticoagulant in the blood could have a critical impact on the efficiency of nanomedicines. For the negatively charged liposomes, such as AmBisome®, no significant change in the uptake could be observed when co-incubated with heparin and primary phagocytes. Yet, we observed that a peak of the uptake extent of cationic liposomes was reached at a clinically relevant concentration of heparin for phagocytes and cancer cells. Hence, we recommend avoiding treatment of a heparinized patient with cationic nanomedicines because unexpectedly high uptake can occur in phagocytes.
脂质体制剂通过限制传统药物与吞噬细胞的相互作用来提高其安全性和细胞吸收。这些纳米载体的摄取行为受血液成分影响，因此血液中抗凝剂的存在可能对纳米药物的效率产生关键影响。对于带负电荷的脂质体，如两性霉素B脂质体（安必素），与肝素和原代吞噬细胞共同孵育时，摄取未见明显变化。然而，我们观察到，对于吞噬细胞和癌细胞，在临床相关的肝素浓度下，阳离子脂质体的摄取程度达到峰值。因此，我们建议避免用阳离子纳米药物治疗使用肝素的患者，因为吞噬细胞中可能会意外出现高摄取情况。
