Evidence map›Paper›PMID 41570979›Full record

ArticleJournal of advanced research2026

Boosting luteolin bioavailability via P-glycoprotein efflux inhibition: a self-microemulsifying drug delivery systems.

Yimei Zheng, Boyu Chen, Xuanxiang Huang, Chao Ai, Hui Teng, Lei Chen

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of advanced research, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing 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

2 citing papers in PubMed.

  1. Review
  2. Review
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

6 authors.

Yimei ZhengCollege of Food Science and Technology, Guangdong Ocean University, Guangdong Provincial Key Laboratory of Aquatic Product Processing and Safety, Guangdong Province Engineering Laboratory for Marine Biological Products, Guangdong Provincial Engineering Technology Research Center of Seafood, Key Laboratory of Advanced Processing of Aquatic Product of Guangdong Higher Education Institution, Zhanjiang 524088, China; College of Food Science, Fujian Agriculture and Forestry University, Fuzhou, Fujian 350002, China; Fujian Province-Indonesia Marine Food Joint Research and Development Center, Fujian Polytechnic Normal University, Fuqing, Fujian 350300, China.
Boyu ChenCollege of Food Science and Technology, Guangdong Ocean University, Guangdong Provincial Key Laboratory of Aquatic Product Processing and Safety, Guangdong Province Engineering Laboratory for Marine Biological Products, Guangdong Provincial Engineering Technology Research Center of Seafood, Key Laboratory of Advanced Processing of Aquatic Product of Guangdong Higher Education Institution, Zhanjiang 524088, China.
Xuanxiang HuangCollege of Food Science and Technology, Guangdong Ocean University, Guangdong Provincial Key Laboratory of Aquatic Product Processing and Safety, Guangdong Province Engineering Laboratory for Marine Biological Products, Guangdong Provincial Engineering Technology Research Center of Seafood, Key Laboratory of Advanced Processing of Aquatic Product of Guangdong Higher Education Institution, Zhanjiang 524088, China.
Chao AiCollege of Food Science and Technology, Guangdong Ocean University, Guangdong Provincial Key Laboratory of Aquatic Product Processing and Safety, Guangdong Province Engineering Laboratory for Marine Biological Products, Guangdong Provincial Engineering Technology Research Center of Seafood, Key Laboratory of Advanced Processing of Aquatic Product of Guangdong Higher Education Institution, Zhanjiang 524088, China.
Hui TengCollege of Food Science and Technology, Guangdong Ocean University, Guangdong Provincial Key Laboratory of Aquatic Product Processing and Safety, Guangdong Province Engineering Laboratory for Marine Biological Products, Guangdong Provincial Engineering Technology Research Center of Seafood, Key Laboratory of Advanced Processing of Aquatic Product of Guangdong Higher Education Institution, Zhanjiang 524088, China. Electronic address: tenghui850610@126.com.
Lei ChenCollege of Food Science and Technology, Guangdong Ocean University, Guangdong Provincial Key Laboratory of Aquatic Product Processing and Safety, Guangdong Province Engineering Laboratory for Marine Biological Products, Guangdong Provincial Engineering Technology Research Center of Seafood, Key Laboratory of Advanced Processing of Aquatic Product of Guangdong Higher Education Institution, Zhanjiang 524088, China; College of Food Science, Fujian Agriculture and Forestry University, Fuzhou, Fujian 350002, China. Electronic address: chenlei841114@hotmail.com.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

introductionThe poor bioavailability of luteolin, a potent flavonoid with antioxidant and anti-inflammatory properties, hinders its therapeutic potential. The primary barriers to its absorption are its low solubility and active efflux by P-glycoprotein (P-gp) in the gastrointestinal tract.

objectivesTo overcome these absorption barriers, we developed a functional self-microemulsifying drug delivery system (SME) incorporating D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), aiming to simultaneously enhance solubility, inhibit P-gp efflux, and improve the oral bioavailability and therapeutic efficacy of luteolin.

methodsA TPGS-based luteolin-SME was prepared via self-assembly and characterized for particle size, stability, release profile, and antioxidant capacity. Cellular absorption mechanisms, permeability, and P-gp inhibition were evaluated using Caco-2 monolayers and molecular docking. Pharmacokinetics and biodistribution were assessed in rats, and therapeutic efficacy was examined in a lipopolysaccharide-induced inflammation model.

resultsThe optimized luteolin-SME formed uniform nanodroplets (<50 nm) with high stability and achieved a 4.3-fold higher cumulative release compared to free luteolin. In Caco-2 cells, the formulation significantly enhanced cellular uptake and permeability, primarily via clathrin- and caveolae-mediated endocytosis, and effectively inhibited P-gp efflux. Pharmacokinetically, luteolin-SME provided a 29-fold increase in relative bioavailability (AUC 247.729 vs. 8.628 mg/L·h) and a 16-fold higher Cmax (27.546 mg/L) over free luteolin. In the lipopolysaccharide-induced inflammation model, luteolin-SME markedly attenuated oxidative stress, reducing the TNF-α, IL-6, and IL-1β levels by approximately 37%, 26%, and 39%, respectively.

conclusionThe TPGS-functionalized SME effectively overcame the major absorption barriers of luteolin by integrating nanocarrier-enhanced solubilization with active P-gp inhibition. This dual strategy resulted in unprecedented oral bioavailability enhancement and potent efficacy. Our study establishes a robust and clinically promising delivery platform for luteolin and other poorly soluble, efflux-limited bioactive compounds, offering a practical approach to enhance oral therapy for inflammation-related diseases.

Indexed as

ATP Binding Cassette Transporter, Subfamily B, Member 1Drug Delivery SystemsLuteolinAdministration, OralAnimalsAnti-Inflammatory AgentsAntioxidantsBiological AvailabilityCaco-2 CellsEmulsionsHumansMaleRatsRats, Sprague-DawleySolubilityTissue DistributionAnti-Inflammatory AgentsAntioxidantsATP Binding Cassette Transporter, Subfamily B, Member 1EmulsionsLuteolintocophersolanVitamin ED-α-Tocopheryl polyethylene glycol 1000 succinateLuteolinMultifunctional nanocarrierOral bioavailabilityP-glycoproteinSelf-microemulsifying drug delivery system

Identifiers

PMID41570979
PMCPMC13669924

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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.