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′)2 antibody fragments were conjugated to the PLGA-poly(ethylene glycol)-maleimide(PLGA-PEG-Mal) NPs through interactions between the f(ab′)2 fragment thiol groups and the maleimide located on the nanoparticle surface. The results demonstrate that the PLGA nanoparticles conjugated with the f(ab′)2 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.

中文翻译：

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抗体与聚合物纳米粒子表面的结合对免疫细胞靶向能力的影响

抗体由于其高特异性、可用性和多样性而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，并通过化学缀合和物理粘附以不同方向与纳米颗粒 (NP) 表面缀合。本研究提出使用两种不同的方法将聚乳酸-乙醇酸 (PLGA) 纳米颗粒与抗体结合，然后比较两种技术的细胞靶向效率。通过传统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) NP 缀合，并将 f(ab')2 抗体片段与 PLGA-聚(通过 f(ab')2 片段硫醇基团与位于纳米颗粒表面的马来酰亚胺之间的相互作用，形成乙二醇）-马来酰亚胺（PLGA-PEG-Mal）纳米颗粒。结果表明，与f(ab')2抗体片段缀合的PLGA纳米粒子比与全长抗体缀合的PLGA纳米粒子具有更高的体外和体内靶向效率。这项研究的结果可以用来设计一种通过生物相容性纳米颗粒进行药物输送的技术。