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Formulation Strategies for Folate-Targeted Liposomes and Their Biomedical Applications

Laboratory of Functional Molecules and Materials, School of Physics and Optoelectronic Engineering, Shandong University of Technology, Xincun West Road 266, Zibo 255000, China
Author to whom correspondence should be addressed.
Pharmaceutics 2019, 11(8), 381;
Received: 21 June 2019 / Revised: 22 July 2019 / Accepted: 28 July 2019 / Published: 2 August 2019
(This article belongs to the Special Issue Advances in Liposome-Based Drug Delivery Systems)
PDF [2763 KB, uploaded 2 August 2019]


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. View Full-Text
Keywords: folic acid; liposomes; folate-targeted; phospholipids; rheumatoid arthritis folic acid; liposomes; folate-targeted; phospholipids; rheumatoid arthritis

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Kumar, P.; Huo, P.; Liu, B. Formulation Strategies for Folate-Targeted Liposomes and Their Biomedical Applications. Pharmaceutics 2019, 11, 381.

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