Assessing transferrin modification of liposomes by atomic force microscopy and transmission electron microscopy
Assessing transferrin modification of liposomes by atomic force microscopy and transmission electron microscopy
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DOI：
10.1016/j.ejpb.2004.12.009
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发表时间：
2005-07-01
影响因子：
4.9
通讯作者：
Ehrhardt, C
中科院分区：
文献类型：
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作者：
Anabousi, S;Laue, M;Ehrhardt, C
药物和治疗剂的位点特异性递送可以显着降低药物毒性并提高治疗效果。转铁蛋白 (Tf) 是一种适合与药物递送系统缀合以实现位点特异性靶向的配体，由于其与转铁蛋白受体 (TfR) 的特异性结合，表达了多种具有治疗意义的细胞类型。据报道，TfR 在肿瘤细胞表面高度表达，并且已充分利用 Tf 内化的充分表征和有效机制来递送抗癌药物和蛋白质。和治疗基因进入主要增殖的恶性细胞。脂质体是药物、基因和疫苗的有效载体，可以很容易地用蛋白质、抗体和其他合适的配体进行修饰，从而产生具有吸引力的靶向药物递送制剂。在本研究中，我们使用原子力显微镜（AFM）和透射电子显微镜（TEM）通过三种不同的偶联方法证实了Tf与脂质体的缀合。此外，还进行了蛋白质量 (BCA) 和磷脂含量（根据 Steward 的说法）定量的常规测定。 AFM 和 TEM 能够在脂质体表面显示 Tf 分子，并且可常规用于以快速可靠的方式获得有关蛋白质-药物载体缀合的额外视觉信息。 (c) 2005 Elsevier B.V. 保留所有权利。
Site-specific delivery of drugs and therapeutics can significantly reduce drug toxicity and increase the therapeutic effect. Transferrin (Tf) is one suitable ligand to be conjugated to drug delivery systems to achieve site-specific targeting, due to its specific binding to transferrin receptors (TfR), expressed oil several cell types of therapeutic interest. TfRs have been reported to be highly expressed on the surfaces of tumour cells and the well-characterised and efficient mechanism of internalisation of Tf has been exploited for the delivery of anticancer drugs, proteins. and therapeutic genes into primarily proliferating malignant cells. Liposomes are effective vehicles for drugs, genes and vaccines and can be easily modified with proteins, antibodies, and other appropriate ligands, resulting in attractive formulations for targeted drug delivery. In this study, we used atomic force microscopy (AFM) and transmission electron microscopy (TEM) to confirm the conjugation of Tf to liposomes by three different coupling methods. In addition, the conventional assays for quantification of protein amount (BCA) and phospholipid content (according to Steward) were performed. AFM and TEM were able to display Tf-molecules on the liposomal surfaces and can be routinely used to obtain additional visual information on the protein-drug carrier conjugation in a fast and reliable manner. (c) 2005 Elsevier B.V. All rights reserved.