Transport Mechanisms of Solid Lipid Nanoparticles across Caco-2 Cell Monolayers and their Related Cytotoxicology

Chai, Guihong; Xu, Yingke; Chen, Shaoqing; Cheng, Bolin; Hu, Fuqiang; You, Jian; Du, Yong‐Zhong; Yuan, Hong

doi:10.1021/acsami.6b00821

Cited by 115 publications

(93 citation statements)

References 44 publications

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“…Caco-2 monolayer cell Transwell chamber model AP → BL transmembrane transport assay (Chai et al, 2016;Chen et al, 2016;Gallardo et al, 2016) was calculated according to the following formula:…”

Section: Transmembrane Transport Experimentsmentioning

confidence: 99%

Use of fluorescein isothiocyanate isomer I to study the mechanism of intestinal absorption of fucoidan sulfate in vivo and in vitro

Zhang

Chu

et al. 2018

Biopharm & Drug Disp

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A new method to label fucoidan sulfate was established with tyramine and fluorescein isothiocyanate isomer I (FITC). Fluorescence spectrophotometry and high performance liquid chromatography verified the successful labelling of fucoidan by FITC. The results of the single-pass intestinal perfusion indicated that the jejunum and ileum are the main absorption sites, and there was carrier saturation. In addition, fucoidan sulfate at 1 mg/ml had no inhibitory effect on Caco-2 cell proliferation. Studies on the transmembrane transport mechanism showed that fucoidan can be absorbed because the apparent permeability coefficient of the drugs (P ) A → B was 3.78 + 0.03 ×10 and that of B → A was 1.42 + 0.19 ×10 . The peak absorption of fucoidan occurred at 120 min after administration; moreover, the higher the concentration used, the worse the absorption was, suggesting the saturation of transport carriers. The absorption was temperature dependent: the absorption at 37°C was much better than that at 4°C. Further, the absorption of fucoidan sulfate might rely on clathrin endocytosis as chlorpromazine (10 μg/ml) significantly inhibited it.

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Section: Transmembrane Transport Experimentsmentioning

confidence: 99%

Use of fluorescein isothiocyanate isomer I to study the mechanism of intestinal absorption of fucoidan sulfate in vivo and in vitro

Zhang

Chu

et al. 2018

Biopharm & Drug Disp

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“…Additionally, Fe 3 O 4 nanoparticle-loaded NLC (NLC/Fe 3 O 4 ) was prepared to label NLC using a modified solvent diffusion method according to our previously reported method. 25 …”

Section: Preparation Of Nlc and A-317491-loaded Nlcmentioning

confidence: 99%

Effect of A-317491 delivered by glycolipid-like polymer micelles on endometriosis pain

Yuan

Ding

Meng

et al. 2017

IJN

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Endometriosis is a common gynecological disease with a lack of effective clinical treatment. Current therapy often results in endometriosis pain recurrence and serious side effects. P2X 3 receptor, an adenosine triphosphate (ATP)-gated ion channel, might be implicated in endometriosis pain. In this study, chitosan oligosaccharide-g-stearic acid (CSOSA) polymer micelles-coated nanostructured lipid carriers (NLCs) were developed as a novel delivery system for A-317491, a selective P2X 3 receptor antagonist for endometriosis pain therapy. A-317491-loaded NLC (NLC/A-317491) could be coated by CSOSA micelles to form CSOSA/NLC/A-317491 nanoparticles. Pheochromocytoma PC12 cells, which highly expressed P2X 3 receptors, were used as a cell model, and the CSOSA/NLC/A-317491 partly blocked the Ca 2+ influx induced by ATP stimulation. In nude mouse and rat endometriotic models, CSOSA/NLC could accumulate into endometriotic lesions after vein injection. In endometriotic rats, CSOSA/NLC/A-317491 reversed mechanical and heat hyperalgesia with long-term efficacy, which might be attributed to the massive CSOSA/NLC/A-317491 distribution in the endometriotic lesions. In conclusion, A-317491 delivered by CSOSA/NLC nanoparticles attenuated endometriosis pain in rats, and CSOSA/NLC/A-317491 could be used as an effective treatment strategy for P2X 3 -targeted therapy in endometriosis pain.

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“…And the classic anticancer drug DOX was used in the cell viability assay. Prior to this assay, the different concentrations of blank HMSS and HMSS-N=N-CS were employed to ascertain the biocompatibility of nanoplatform towards Caco-2 cells and normal NIH-3T3 (mouse embryo fibroblast) cells with various concentrations from 10 to 250 μg/mL by MTT assay [38,39]. As displayed in Fig.…”

Section: In Vitro Cell Viability Evaluationmentioning

confidence: 99%

Chitosan capping enzyme-responsive hollow mesoporous silica nanoplatforms for colon specific drug delivery

Cai

Han

Liu

et al. 2020

Preprint

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In summary, an enzyme-responsive colon specific drug delivery system was developed based on hollow mesoporous silica sphere (HMSS), in which the biodegradable chitosan (CS) was gated on the openings of HMSS through cleavable azo bonds (HMSS-N=N-CS). Doxorubicin (DOX) was encapsulated into the hollow cavity and mesopores of HMSS, and HMSS-N=N-CS/DOX showed a high loading amount of 35.2%. X-ray diffraction (XRD) experiment proved that the DOX loaded in the HMSS-N=N-CS was in a non–crystalline state. In vitro drug release experiments proved that HMSS-N=N-CS/DOX showed an enzyme-responsive drug release property. The grafted CS could increase the biocompatibility and stability of HMSS, and reduce the protein adsorption on the surface of HMSS. The gastrointestinal mucosa irritation and cell cytotoxicity results indicated the good biocompatibility of HMSS and HMSS-N=N-CS. The confocal laser scanning microscope (CLSM) and flow cytometry technique (FCM) results indicated that the cellular uptake of DOX was obviously increased after the HMSS-N=N-CS/DOX was preincubated with colonic enzyme mixture. Cell viability result indicated that HMSS-N=N-CS/DOX incubated with colon enzyme showed an increased cytotoxicity and the IC50 value was three time less than that of HMSS-N=N-CS/DOX group. The present work will lay the foundation for subsequent research on mesoporous carriers for oral colon-specific drug delivery.

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Transport Mechanisms of Solid Lipid Nanoparticles across Caco-2 Cell Monolayers and their Related Cytotoxicology

Cited by 115 publications

References 44 publications

Use of fluorescein isothiocyanate isomer I to study the mechanism of intestinal absorption of fucoidan sulfate in vivo and in vitro

Use of fluorescein isothiocyanate isomer I to study the mechanism of intestinal absorption of fucoidan sulfate in vivo and in vitro

Effect of A-317491 delivered by glycolipid-like polymer micelles on endometriosis pain

Chitosan capping enzyme-responsive hollow mesoporous silica nanoplatforms for colon specific drug delivery

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