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Multifunctional quercetin conjugated chitosan nano-micelles with P-gp inhibition and permeation enhancement of anticancer drug
Abstract
In this study, quercetin-chitosan conjugate (QT-CS) was synthesized for oral delivery of doxorubicin (DOX) to improve its oral bioavailability by increasing its water solubility, opening tight junction and bypassing the P-glycoprotein (P-gp). The prepared QT-CS self-assembled into micelles which could encapsulate DOX with high encapsulation rate, small particle size (136.9 nm) and strong zeta potential (+16.2 mV). QT-CS-DOX micelles displayed sustained-release profile in gastrointestinal simulation fluid (pH 1.2/pH 7.4). QT-CS micelles could promote cellular uptake of doxorubicin, which was 2.2 folds higher than that of free doxorubicin. The trans epithelial electrical resistance (TEER) value of Caco-2 monolayer cells was significantly reduced (about 57%) by drug loaded QT-CS micelles, leading to a high apparent permeability coefficient (P app) of doxorubicin, which was 10.17 folds higher than that of free doxorubicin. Above results indicate that QT-CS micelles are promising vehicles for the oral delivery of insoluble anticancer drugs.
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“In addition, QT-CS nanomicelles could encourage cellular uptake of doxorubicin that was 2.2-fold higher compared to free drug.”
From Recent Advances in Nanomicelles Delivery Systems. (2020) · cites this paper as [167]
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Metadata
- Authors
- Mu, Y., Fu, Y., Li, J., Yu, X., Li, Y., Wang, Y., Wu, X., Zhang, K., Kong, M., Feng, C., & Chen, X.
- Affiliations
- Ocean University of China (CN)
- Chinese PLA General Hospital (CN)
- Corresponding author
- Feng, Chao
- Chen, Xiguang
- Venue
- Carbohydrate Polymers
- Publisher
- Elsevier BV
- Published
- 2019-01
- Volume
- 203
- Pages
- 10-18
- ISSN
- 0144-8617 (ISSN-L)
- OpenAlex
- W2890083641
- Cited by
- 113
- References
- 31
- Citations by year
- 2026: 6 · 2025: 10 · 2024: 11 · 2023: 18 · 2022: 20 · 2021: 18 · 2020: 18 · 2019: 11
- FWCI
- 5.51
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Carbohydrate Polymers (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Natural Science Foundation of China (U1706212, 81671828)
- Applied Basic Research Plan of Qingdao (16-5-1-70-jch)
- Taishan Scholar Program
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Keywords
- doxorubicin, oral drug delivery, P-glycoprotein inhibition, self-assembly, sustained drug release, Caco-2 cell monolayers, transepithelial electrical resistance, cellular uptake, anticancer drug delivery, poorly water-soluble drugs
- MeSH terms
- Administration, Oral, Antineoplastic Agents, Doxorubicin, Drug Carriers, Humans, Micelles, Particle Size, Quercetin, ATP Binding Cassette Transporter, Subfamily B, Caco-2 Cells, Tight Junctions, Chitosan, Nanostructures, Static Electricity, Drug Liberation
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