ArticleAdvanced science (Weinheim, Baden-Wurttemberg, Germany)2022
Bile Acid Conjugation on Solid Nanoparticles Enhances ASBT-Mediated Endocytosis and Chylomicron Pathway but Weakens the Transcytosis by Inducing Transport Flow in a Cellular Negative Feedback Loop.
Article in Advanced science (Weinheim, Baden-Wurttemberg, Germany), 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 45 citations in OpenAlex.
- A reduction-sensitive lipophilic dihydroartemisinin prodrug in a self-microemulsifying drug delivery system for treating breast cancer lung metastasis via intestinal lymphatic transport.International journal of pharmaceutics: X · 2026Article
- Drug delivery systems incorporating bile salts: advancements since the conception of bilosomes.Therapeutic delivery · 2025Review
- Polyzwitterion-branched polycholic acid nanocarriers based oral delivery insulin for long-term glucose and metabolic regulation in diabetes mellitus.Journal of nanobiotechnology · 2025Article
- Intestinal nanoparticle delivery and cellular response: a review of the bidirectional nanoparticle-cell interplay in mucosa based on physiochemical properties.Journal of nanobiotechnology · 2024Review
- Transepithelial transport of nanoparticles in oral drug delivery: From the perspective of surface and holistic property modulation.Acta pharmaceutica Sinica. B · 2024Review
- The in vitro gastrointestinal digestion-associated protein corona of polystyrene nano- and microplastics increases their uptake by human THP-1-derived macrophages.Particle and fibre toxicology · 2024Article
- Coordinated ASBT and EGFR Mechanisms for Optimized Liraglutide Nanoformulation Absorption in the GI Tract.International journal of nanomedicine · 2024Article
- Design of chimeric GLP-1A using oligomeric bile acids to utilize transporter-mediated endocytosis for oral delivery.Biomaterials research · 2023Article
- Effect of modification of polystyrene nanoparticles with different bile acids on their oral transport.Nanomedicine : nanotechnology, biology, and medicine · 2023Article
- Bile Acid Conjugation on Solid Nanoparticles Enhances ASBT-Mediated Endocytosis and Chylomicron Pathway but Weakens the Transcytosis by Inducing Transport Flow in a Cellular Negative Feedback Loop.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2022Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
Bile acid-modified nanoparticles provide a convenient strategy to improve oral bioavailability of poorly permeable drugs by exploiting specific interactions with bile acid transporters. However, the underlying mechanisms are unknown, especially considering the different absorption sites of free bile acids (ileum) and digested fat molecules from bile acid-emulsified fat droplets (duodenum). Here, glycocholic acid (GCA)-conjugated polystyrene nanoparticles (GCPNs) are synthesized and their transport in Caco-2 cell models is studied. GCA conjugation enhances the uptake by interactions with apical sodium-dependent bile acid transporter (ASBT). A new pathway correlated with both ASBT and chylomicron pathways is identified. Meanwhile, the higher uptake of GCPNs does not lead to higher transcytosis to the same degree compared with unmodified nanoparticles (CPNs). The pharmacological and genomics study confirm that GCA conjugation changes the endocytosis mechanisms and downregulates the cellular response to the transport at gene levels, which works as a negative feedback loop and explains the higher cellular retention of GCPNs. These findings offer a solid foundation in the bile acid-based nanomedicine design, with utilizing advantages of the ASBT-mediated uptake, as well as inspiration to take comprehensive consideration of the cellular response with more developed technologies.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.