Authors
Luyao Ren, Yuxi Qin, Hongxiao Lu, Siyu Lu, Meiying Liu, Huanhuan Zhang, Lina Guo, Guang Zhao, Yunlan Li
Published in
Regenerative biomaterials. Volume 13. Pages rbag104. Epub Jun 01, 2026.
Abstract
Metabolic dysfunction-associated steatotic liver disease (MASLD) is a widespread chronic liver disease worldwide, making efficient targeted delivery systems essential to alleviate its socioeconomic burden. Aptamers are short, single-stranded DNA or RNA oligonucleotides that bind to specific target antigens with high affinity and specificity. Compared with antibody-based therapies, aptamer-based therapies offer the advantages of small size, facile synthesis and low immunogenicity. Herein, we report a novel fatty acid translocase CD36-targeted aptamer-drug conjugate (ApDC), the NAFLD01 aptamer conjugated with 4-(4-(tert-butyl)benzoyl)-2,3-dihydroxyphenyl furan-2-carboxylate (SF), termed ASC, as a targeted delivery platform for MASLD. Results demonstrated that SF significantly reduced body weight, attenuated liver injury and ameliorated lipid accumulation in high-fat diet (HFD)-induced MASLD mice. ASC effectively reduced lipid droplet formation and hepatic injury biomarker levels, while improving antioxidant enzyme levels in MASLD cell models in vitro. A key advantage of ASC is its capacity for targeted SF delivery, which potentially reduces off-target exposure of SF to non-target organs. ASC retained the intrinsic properties of the NAFLD01 aptamer, including high binding affinity and efficient internalization by target cells. Additionally, the acid-labile hydrazone bond in ASC was cleaved in an acidic lysosomal environment. In conclusion, ASC is a promising ApDC delivery platform for MASLD.
PMID:
42371418
Bibliographic data and abstract were imported from PubMed on 29 Jun 2026.
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