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Targeted delivery of atorvastatin via asialoglycoprotein receptor (ASGPR).

ABSTRACT: Targeted drug delivery platforms can increase the concentration of drugs in specific cell populations, reduce adverse effects, and hence improve the therapeutic effect of drugs. Herein, we designed two conjugates by installing the targeting ligand GalNAc (N-acetylgalactosamine) onto atorvastatin (AT). Compared to the parent drug, these two conjugates, termed G2-AT and G2-K-AT, showed increased hepatic cellular uptake. Moreover, both conjugates were able to release atorvastatin, and consequently showed dramatic inhibition of ?-hydroxy-?-methylglutaryl-CoA (HMG-CoA) reductase and increased LDL receptors on cell surface.

SUBMITTER: Zhang Y

PROVIDER: S-EPMC6535107 | biostudies-literature | 2019 Jun

REPOSITORIES: biostudies-literature

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Targeted delivery of atorvastatin via asialoglycoprotein receptor (ASGPR).

Zhang Youxi Y Zhang Xinfu X Zeng Chunxi C Li Bin B Zhang Chengxiang C Li Wenqing W Hou Xucheng X Dong Yizhou Y

Bioorganic & medicinal chemistry 20190411 11

Targeted drug delivery platforms can increase the concentration of drugs in specific cell populations, reduce adverse effects, and hence improve the therapeutic effect of drugs. Herein, we designed two conjugates by installing the targeting ligand GalNAc (N-acetylgalactosamine) onto atorvastatin (AT). Compared to the parent drug, these two conjugates, termed G2-AT and G2-K-AT, showed increased hepatic cellular uptake. Moreover, both conjugates were able to release atorvastatin, and consequently ...[more]

PMID: 31005367

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