Abstract |
Low molecular weight heparin ( LMWH) is reported to have therapeutic action on ulcerative colitis (UC). To facilitate its oral administration and improve the colon-targeting property, LMWH-loaded nanoparticles (TMC-NPs and SA-TMC-NPs) are prepared and evaluated by a series of studies, including their stabilities, drug release profiles, mucosal permeation, mucoadhesion, cytotoxicities, cellular uptake profiles, anticoagulant and anti-inflammatory activities, mucosal healing properties, biosafety and ameliorative effects on experimental colitis. Consequently, oral administration of LMWH-loaded NPs for 5 days perform significant therapeutic effects on mice, which are manifested as improved body weight gains, colon length, DAI score, MPO activity and histological characteristics. Besides, SA-TMC-NPs show better colon-targeting property than TMC-NPs that is demonstrated by lower oral absorption (ATPP 38.95 s) and stronger mucoadhesion (kcps reduces 36.46 %) to inflamed colon tissues. Therefore, TMC-based NPs are proved to be as promising oral colon-targeting drug delivery systems of LMWH and has potential application in UC treatment.
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Authors | Yan Yan, Ying Sun, Pengchong Wang, Rui Zhang, Chuanchuan Huo, Tingting Gao, Chenghua Song, Jianfeng Xing, Yalin Dong |
Journal | Carbohydrate polymers
(Carbohydr Polym)
Vol. 246
Pg. 116660
(Oct 15 2020)
ISSN: 1879-1344 [Electronic] England |
PMID | 32747292
(Publication Type: Journal Article)
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Copyright | Copyright © 2020. Published by Elsevier Ltd. |
Chemical References |
- Anti-Inflammatory Agents
- Biomarkers
- Heparin, Low-Molecular-Weight
- N-trimethyl chitosan chloride
- Trinitrobenzenesulfonic Acid
- Chitosan
- Peroxidase
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Topics |
- Administration, Oral
- Animals
- Anti-Inflammatory Agents
(metabolism, pharmacology)
- Biomarkers
(metabolism)
- Chitosan
(chemistry)
- Colitis
(chemically induced, drug therapy, metabolism, pathology)
- Colon
(drug effects, metabolism, pathology)
- Drug Delivery Systems
(methods)
- Drug Liberation
- Gene Expression
- Heparin, Low-Molecular-Weight
(metabolism, pharmacology)
- Kinetics
- Male
- Mice
- Nanoparticles
- Peroxidase
(genetics, metabolism)
- RAW 264.7 Cells
- Rats
- Rats, Sprague-Dawley
- Treatment Outcome
- Trinitrobenzenesulfonic Acid
(toxicity)
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