Department of Biomedical Engineering, Chung Yuan Christian University , 200 Chung Pei Road, Chung Li, 32023 ROC , Taiwan.
Langmuir. 2018 Feb 13;34(6):2324-2331. doi: 10.1021/acs.langmuir.7b04024. Epub 2018 Feb 5.
Coating liposome surfaces with human serum albumin (HSA) can improve the colloidal stability and prevent opsonization. HSA coating via specific binding with alkyl ligands is promising because although the ligand-mediated coating is relatively stable it can spontaneously exchange with fresh HSA. However, to achieve surface coating with HSA, multiple hydrophobic ligands must be exposed to an aqueous medium prior to binding with HSA. This presents a challenge, as hydrophobic ligands tend to be buried in the liposomal membrane. Here we present the first HSA modification of liposome surfaces via alkyl ligands. We found that a relatively short alkyl ligand, or a long alkyl ligand with a terminal carboxylate, could be exposed on the liposome surface without causing aggregation of the liposomes and these ligands could subsequently bind HSA. The resulting HSA-coated liposomes were as inert as conventional PEGylated liposomes in terms of macrophage recognition.
用人血清白蛋白（HSA）包覆脂质体表面可以提高胶体稳定性并防止被调理。通过与烷基配体的特异性结合来包覆 HSA 是很有前景的，因为虽然配体介导的包覆相对稳定，但它可以与新鲜的 HSA 自发交换。然而，为了实现 HSA 的表面包覆，在与 HSA 结合之前，必须将多个疏水性配体暴露于水性介质中。这是一个挑战，因为疏水性配体往往埋藏在脂质体膜中。在这里，我们首次通过烷基配体对脂质体表面进行了 HSA 修饰。我们发现，相对较短的烷基配体，或带有末端羧酸盐的长烷基配体，可以暴露在脂质体表面而不会引起脂质体聚集，并且这些配体随后可以与 HSA 结合。所得的 HSA 包覆的脂质体在巨噬细胞识别方面与常规的 PEG 化脂质体一样惰性。
