ArticleDrug delivery2018
Dipeptide-modified nanoparticles to facilitate oral docetaxel delivery: new insights into PepT1-mediated targeting strategy.
Article in Drug delivery, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
13 citing papers in PubMed, 39 citations in OpenAlex.
- Current Status and Future Prospects on Nanodelivery Systems Targeting the Small Intestine for Absorption of Bioactive Substances.Foods (Basel, Switzerland) · 2025Review
- Enhanced lymphatic transportation of SLN by mimicking oligopeptide transportation route.Asian journal of pharmaceutical sciences · 2025Article
- Molecular Insights to the Structure-Interaction Relationships of Human Proton-Coupled Oligopeptide Transporters (PepTs).Pharmaceutics · 2023Review
- αB-Crystallin Peptide Fused with Elastin-like Polypeptide: Intracellular Activity in Retinal Pigment Epithelial Cells Challenged with Oxidative Stress.Antioxidants (Basel, Switzerland) · 2023Article
- Transporter-Mediated Drug Delivery.Molecules (Basel, Switzerland) · 2023Review
- The Role of Solute Carrier Transporters in Efficient Anticancer Drug Delivery and Therapy.Pharmaceutics · 2023Review
- Transporter-Targeted Nano-Sized Vehicles for Enhanced and Site-Specific Drug Delivery.Cancers · 2020Review
- Amino acid transporters: Emerging roles in drug delivery for tumor-targeting therapy.Asian journal of pharmaceutical sciences · 2020Review
- Intestinal OCTN2- and MCT1-targeted drug delivery to improve oral bioavailability.Asian journal of pharmaceutical sciences · 2020Review
- Galactose-modified selenium nanoparticles for targeted delivery of doxorubicin to hepatocellular carcinoma.Drug delivery · 2019Article
- A novel oral prodrug-targeting transporter MCT 1: 5-fluorouracil-dicarboxylate monoester conjugates.Asian journal of pharmaceutical sciences · 2019Article
- Emerging transporter-targeted nanoparticulate drug delivery systems.Acta pharmaceutica Sinica. B · 2019Review
- Challenges and opportunities in delivering oral peptides and proteins.Expert opinion on drug deliveryReview
Corrections and comments
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Authors and funding
14 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Oligopeptide transporter 1 (PepT1) has been a striking prodrug-designing target. However, the underlying mechanism of PepT1 as a target to facilitate the oral absorption of nanoparticles (NPs) remains unclear. Herein, we modify Poly (lactic-co-glycolic acid) (PLGA) NPs with the conjugates of dipeptides (L-valine-valine, L-valine-phenylalanine) and polyoxyethylene (PEG Mw: 1000, 2000) stearate to facilitate oral delivery of docetaxel (DTX) to investigate the oral absorption mechanism and regulatory effects on PepT1 of the dipeptide-modified NPs. The cellular uptake of the dipeptide-modified NPs is more efficient than that of the unmodified NPs in the stably transfected hPepT1- Hela cells and Caco-2 cells, suggesting the involvement of PepT1 in the endocytosis of NPs. The internalization of the dipeptide-modified NPs is proved to be a proton-dependent process. Moreover, the L-valine-valine modified NPs with shorter PEG chain exhibit distinct advantages in terms of intestinal permeability and oral absorption, resulting in significantly improved oral bioavailability of DTX. In summary, PepT1 could serve as a desirable target for oral nanoparticulate drug delivery and the dipeptide-modified NPs represent a promising nanoplatform to facilitate oral delivery of hydrophobic drugs with low bioavailability.
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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.