Targeted delivery of atorvastatin via asialoglycoprotein receptor (ASGPR) |
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| Affiliation: | 1. Allergologia e Immunologia Clinica, A.O. S. Maria degli Angeli, Pordenone, Italy;2. Division of Transplantation Immunology and Mucosal Biology, King''s College London School of Medicine at King''s College Hospital, London, UK;3. GA Generic Assays GmbH, Dahlewitz, Germany;4. Faculty of Sciences, Brandenburg University of Technology Cottbus-Senftenberg, Senftenberg, Germany;5. Department or Rheumatology, School of Health Sciences, University of Thessaly, Larissa, Greece |
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| 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 β-hydroxy-β-methylglutaryl-CoA (HMG-CoA) reductase and increased LDL receptors on cell surface. |
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| Keywords: | Atorvastatin Ligand conjugates Asialoglycoprotein receptor Targeted delivery |
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