School of Pharmaceutical Sciences of Araraquara, São Paulo State University, UNESP, Department of Drugs and Medicines, Araraquara, SP, Brazil.
School of Pharmaceutical Sciences of Ribeirão Preto, São Paulo State University, USP, Department of Pharmaceutical Sciences, Ribeirão Preto, SP, Brazil.
Colloids Surf B Biointerfaces. 2017 Nov 1;159:454-467. doi: 10.1016/j.colsurfb.2017.07.085. Epub 2017 Aug 5.
Nanoparticles, especially liposomes, have gained prominence in the field of drug delivery for the treatment of human diseases, particularly cancer; they provide several advantages, including controlled drug release, protection of the drug against degradation, improved pharmacokinetics, long circulation, and passive targeting to tumors and inflammatory sites due to the enhanced permeability and retention effect. The functionalization of liposomes with monoclonal antibodies or antibody fragments to generate immunoliposomes has emerged as a promising strategy for targeted delivery to and uptake by cells overexpressing the antigens to these antibodies, with a consequent reduction in side effects. In this review, we address functionalization strategies for the non-covalent and covalent attachment of monoclonal antibodies and their fragments to liposomal surfaces. The main reaction occurs between the sulfhydryl groups of thiolated antibodies and maleimide-containing liposomes. Furthermore, we explore the main targeting possibilities with these ligands for the treatment of a variety of pathologies, including HER2- and EGFR-positive cancers, inflammatory and cardiovascular diseases, infectious diseases, and autoimmune and neurodegenerative diseases, which have not previously been reviewed together. Overall, many studies have shown selective delivery of immunoliposomes to target cells, with promising in vivo results, particularly for cancer treatment. Although clinical trials have been conducted, immunoliposomes have not yet received clinical approval. However, immunoliposomes are promising formulations that are expected to become available for therapeutic use after clinical trials prove their safety and efficacy, and after scaling issues are resolved.
纳米颗粒，特别是脂质体，在治疗人类疾病，特别是癌症的药物传递领域中备受关注；它们具有许多优点，包括控制药物释放、保护药物免受降解、改善药代动力学、长循环以及由于增强的通透性和保留效应而被动靶向肿瘤和炎症部位。通过将单克隆抗体或抗体片段功能化到脂质体上以生成免疫脂质体，已成为一种有前途的策略，可以针对过度表达这些抗体的抗原的细胞进行靶向递药和摄取，从而减少副作用。在这篇综述中，我们讨论了将单克隆抗体及其片段非共价和共价连接到脂质体表面的功能化策略。主要反应发生在巯基化抗体的巯基和含有马来酰亚胺的脂质体之间。此外，我们还探讨了这些配体的主要靶向可能性，用于治疗各种病理，包括 HER2 和 EGFR 阳性癌症、炎症和心血管疾病、传染病以及自身免疫和神经退行性疾病，这些疾病以前没有一起进行过综述。总的来说，许多研究表明免疫脂质体可以选择性地递送到靶细胞，体内结果有很大的希望，特别是在癌症治疗方面。尽管已经进行了临床试验，但免疫脂质体尚未获得临床批准。然而，免疫脂质体是很有前途的制剂，预计在临床试验证明其安全性和有效性，并解决规模化问题后，将可用于治疗。
