Lee Na Kyeong, Wang Chi-Pin James, Lim Jaesung, Park Wooram, Kwon Ho-Keun, Kim Se-Na, Kim Tae-Hyung, Park Chun Gwon
Department of Intelligent Precision Healthcare Convergence, Sungkyunkwan University, Suwon, Gyeonggi, 16419, Republic of Korea.
Department of Biomedical Engineering, SKKU Institute for Convergence, Sungkyunkwan University (SKKU), Suwon, Gyeonggi, 16419, Republic of Korea.
Nano Converg. 2021 Aug 16;8(1):24. doi: 10.1186/s40580-021-00274-7.
Antibodies have been widely used to provide targeting ability and to enhance bioactivity owing to their high specificity, availability, and diversity. Recent advances in biotechnology and nanotechnology permit site-specific engineering of antibodies and their conjugation to the surfaces of nanoparticles (NPs) in various orientations through chemical conjugations and physical adhesions. This study proposes the conjugation of poly(lactic-co-glycolic acid) (PLGA) NPs with antibodies by using two distinct methods, followed by a comparison between the cell-targeting efficiencies of both techniques. Full-length antibodies were conjugated to the PLGA-poly(ethylene glycol)-carboxylic acid (PLGA-PEG-COOH) NPs through the conventional carbodiimide coupling reaction, and f(ab') antibody fragments were conjugated to the PLGA-poly(ethylene glycol)-maleimide(PLGA-PEG-Mal) NPs through interactions between the f(ab') fragment thiol groups and the maleimide located on the nanoparticle surface. The results demonstrate that the PLGA nanoparticles conjugated with the f(ab') antibody fragments had a higher targeting efficiency in vitro and in vivo than that of the PLGA nanoparticles conjugated with the full-length antibodies. The results of this study can be built upon to design a delivery technique for drugs through biocompatible nanoparticles.
由于抗体具有高特异性、易获得性和多样性，它们已被广泛用于提供靶向能力并增强生物活性。生物技术和纳米技术的最新进展允许对抗体进行位点特异性工程改造，并通过化学偶联和物理粘附以各种方向将其与纳米颗粒（NP）表面偶联。本研究提出通过两种不同的方法将聚乳酸-乙醇酸共聚物（PLGA）纳米颗粒与抗体偶联，然后比较这两种技术的细胞靶向效率。通过常规的碳二亚胺偶联反应将全长抗体与PLGA-聚乙二醇-羧酸（PLGA-PEG-COOH）纳米颗粒偶联，通过f(ab')片段的巯基与纳米颗粒表面的马来酰亚胺之间的相互作用将f(ab')抗体片段与PLGA-聚乙二醇-马来酰亚胺（PLGA-PEG-Mal）纳米颗粒偶联。结果表明，与全长抗体偶联的PLGA纳米颗粒相比，与f(ab')抗体片段偶联的PLGA纳米颗粒在体外和体内具有更高的靶向效率。本研究结果可为设计通过生物相容性纳米颗粒进行药物递送的技术奠定基础。
