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Overcoming the delivery barrier of oligonucleotide drugs and enhancing nucleoside drug efficiency: The use of nucleolipids
Author(s) -
Zhou Xinyang,
Wang Shuhe,
Zhu Yuejie,
Pan Yufei,
Zhang Lihe,
Yang Zhenjun
Publication year - 2020
Publication title -
medicinal research reviews
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.868
H-Index - 130
eISSN - 1098-1128
pISSN - 0198-6325
DOI - 10.1002/med.21652
Subject(s) - prodrug , nucleic acid , nucleoside , oligonucleotide , nucleotide , drug , drug delivery , chemistry , nucleoside analogue , cationic polymerization , pharmacology , biochemistry , biology , dna , organic chemistry , gene
With the rapid development of synthetic technology and biological technology, many nucleic acid‐based drugs have entered the clinical trials. However, their inherent disabilities in actively and efficiently penetrating cell membranes still severely restrict their further application. The main drawback of cationic lipids, which have been widely used as nonviral vectors of nucleic acids, is their high cytotoxicity. A series of nucleoside‐based or nucleotide‐based nucleolipids have been reported in recent years, due to their oligonucleotide delivery capacity and low toxicity in comparison with cationic lipids. Lipophilic prodrugs of nucleoside analogs have extremely similar structures with nucleolipid vectors and are thus helpful for improving the transmembrane ability. This review introduces the progress of nucleolipids and provides new strategies for improving the delivery efficiency of nucleic acid‐based drugs, as well as lipophilic prodrugs of nucleosides or nucleotides for antiviral or anticancer therapies.