ArticlePharmaceutical research2016
An Assessment of the Permeation Enhancer, 1-phenyl-piperazine (PPZ), on Paracellular Flux Across Rat Intestinal Mucosae in Ussing Chambers.
Article in Pharmaceutical research, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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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.
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.
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Who cites it
9 citing papers in PubMed, 23 citations in OpenAlex.
- Piperazine-Functionalized Nanoparticles Enable Oral Insulin Delivery in Obese Mice.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Gastrointestinal Permeation Enhancers Beyond Sodium Caprate and SNAC - What is Coming Next?Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Review
- A new crystalline daidzein-piperazine salt with enhanced solubility, permeability, and bioavailability.Frontiers in pharmacology · 2024Article
- Storming the gate: New approaches for targeting the dynamic tight junction for improved drug delivery.Advanced drug delivery reviews · 2023Review
- Long-term daily oral administration of intestinal permeation enhancers is safe and effective in mice.Bioengineering & translational medicine · 2023Article
- Investigations of Piperazine Derivatives as Intestinal Permeation Enhancers in Isolated Rat Intestinal Tissue Mucosae.The AAPS journal · 2020Article
- The EXTrauterine Environment for Neonatal Development Supports Normal Intestinal Maturation and Development.Cellular and molecular gastroenterology and hepatology · 2020Article
- Anionic nanoparticles enable the oral delivery of proteins by enhancing intestinal permeability.Nature biomedical engineering · 2020Article
- Structure-Function Analysis of Phenylpiperazine Derivatives as Intestinal Permeation Enhancers.Pharmaceutical research · 2017Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purpose1-phenyl piperazine (PPZ) emerged from a Caco-2 monolayer screen as having high enhancement potential due to a capacity to increase permeation without significant toxicity. Our aim was to further explore the efficacy and toxicity of PPZ in rat ileal and colonic mucosae in order to assess its true translation potential.
methodsIntestinal mucosae were mounted in Ussing chambers and apparent permeability coefficient (Papp) values of [(14)C]-mannitol and FITC-dextran 4 kDa (FD-4) and transepithelial electrical resistance (TEER) values were obtained following apical addition of PPZ (0.6-60 mM). Exposed issues were assessed for toxicity by histopathology and lactate dehydrogenase (LDH) release. Mucosal recovery after exposure was also assessed using TEER readings.
resultsPPZ reversibly increased the Papp of both agents across rat ileal and distal colonic mucosae in concentration-dependent fashion, accompanied by TEER reduction, with acceptable levels of tissue damage. The complex mechanism of tight junction opening was part mediated by myosin light chain kinase, stimulation of transepithelial electrogenic chloride secretion, and involved activation of 5-HT4 receptors.
conclusionsPPZ is an efficacious and benign intestinal permeation enhancer in tissue mucosae. However, its active pharmacology suggest that potential for further development in an oral formulation for poorly permeable molecules will be difficult.
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