Kumar Parveen, Huo Peipei, Liu Bo
Laboratory of Functional Molecules and Materials, School of Physics and Optoelectronic Engineering, Shandong University of Technology, Xincun West Road 266, Zibo 255000, China.
Pharmaceutics. 2019 Aug 2;11(8):381. doi: 10.3390/pharmaceutics11080381.
The folate receptor (FR) is a tumor-associated antigen that can bind with folic acid (FA) and its conjugates with high affinity and ingests the bound molecules inside the cell via the endocytic mechanism. A wide variety of payloads can be delivered to FR-overexpressed cells using folate as the ligand, ranging from small drug molecules to large DNA-containing macromolecules. A broad range of folate attached liposomes have been proven to be highly effective as the targeted delivery system. For the rational design of folate-targeted liposomes, an intense conceptual understanding combining chemical and biomedical points of view is necessary because of the interdisciplinary nature of the field. The fabrication of the folate-conjugated liposomes basically involves the attachment of FA with phospholipids, cholesterol or peptides before liposomal formulation. The present review aims to provide detailed information about the design and fabrication of folate-conjugated liposomes using FA attached uncleavable/cleavable phospholipids, cholesterol or peptides. Advances in the area of folate-targeted liposomes and their biomedical applications have also been discussed.
叶酸受体（FR）是一种肿瘤相关抗原，它能与叶酸（FA）及其缀合物高亲和力结合，并通过内吞机制将结合的分子摄入细胞内。使用叶酸作为配体，可以将各种各样的有效载荷递送至FR过表达的细胞，从小的药物分子到含DNA的大分子。大量叶酸连接的脂质体已被证明作为靶向递送系统非常有效。由于该领域的跨学科性质，要合理设计叶酸靶向脂质体，需要从化学和生物医学角度进行深入的概念理解。叶酸缀合脂质体的制备基本上涉及在脂质体制备之前将FA与磷脂、胆固醇或肽连接。本综述旨在提供有关使用连接有FA的不可裂解/可裂解磷脂、胆固醇或肽来设计和制备叶酸缀合脂质体的详细信息。还讨论了叶酸靶向脂质体领域的进展及其生物医学应用。
