Evidence map›Paper›PMID 29532356›Full record

ArticleDrug delivery and translational research2018

Covalently mucoadhesive amphiphilic prodrug of 5-fluorouracil for enhanced permeation and improved oral absorption.

Yan Liu, Dongyang Zhao, Mengchi Sun, Wei Wei, Yingli Wang, Jiahua Zhou, Ruoshi Zhang, Jian Wang, Haotian Zhang, Zhonggui He and 2 more

Abstract read
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Article in Drug delivery and translational research, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

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.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

5 citing papers in PubMed.

  1. Article
  2. Article
  3. Review
  4. Review
  5. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

12 authors.

Yan LiuDepartment of Pharmacy, Wuya College of Innovation, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang, 110016, China.
Dongyang ZhaoDepartment of Pharmacy, Wuya College of Innovation, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang, 110016, China.
Mengchi SunDepartment of Pharmacy, Wuya College of Innovation, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang, 110016, China.
Wei WeiDepartment of Pharmacy, Wuya College of Innovation, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang, 110016, China.
Yingli WangDepartment of Pharmacy, Wuya College of Innovation, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang, 110016, China.
Jiahua ZhouDepartment of Pharmacy, Wuya College of Innovation, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang, 110016, China.
Ruoshi ZhangDepartment of Pharmacy, Wuya College of Innovation, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang, 110016, China.
Jian WangKey Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Wenhua Road, No. 103, Shenyang, 110016, China.
Haotian ZhangDeparment of Pharmacology, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang, 110016, China.
Zhonggui HeDepartment of Pharmacy, Wuya College of Innovation, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang, 110016, China.
Qiming KanDeparment of Pharmacology, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang, 110016, China. kanqiming1@163.com.
Jin SunDepartment of Pharmacy, Wuya College of Innovation, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang, 110016, China. sunjin66@21cn.com.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

5-Fluorouracil (5-FU) is one of the important antitumor drugs and is widely used to treat various types of cancers. However, its administration is limited to intravenous route due to poor oral bioavailability. Herein, we hypothesized that the maleimide group-containing 5-FU prodrug (EMC-5-FU) could improve the intestinal mucoadhesion because the maleimide end group can covalently target thiol residues of mucin glycoprotein covering the intestinal enterocytes. In vitro bioadhesion results showed that EMC-5-FU exhibited good affinity to the cysteine-rich subdomains of mucin and NMR studies successfully verified the covalent attachment of EMC-5-FU to mucin. The intestinal perfusion study indicated that the intestinal bioadhesion and membrane permeability are greatly enhanced for EMC-5-FU, in comparison with 5-FU. Mucoadhesion investigations on rat intestine intuitively confirmed increased intestinal retention of 5-FU through maleimide-mediated mucoadhesion. Moreover, AUC

Indexed as

1-OctanolAdhesivenessAdministration, OralAnimalsAntimetabolites, AntineoplasticBiological AvailabilityFluorouracilIntestinal AbsorptionIntestinal MucosaMagnetic Resonance SpectroscopyMaleMolecular Docking SimulationMucin 5ACMucinsPermeabilityProdrugs1-OctanolAntimetabolites, AntineoplasticFluorouracilMUC5AC protein, humanMucin 5ACMucinsProdrugsSulfhydryl CompoundsWater5-FluorouracilMaleimide groupMucoadhesionOral drug deliveryProdrug

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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.