Deoxycholic acid-functionalised nanoparticles for oral delivery of rhein

Yao, Wenjie; Xu, Zhishi; Sun, Jiang; Luo, Jingwen; Wei, Yinghui; Zou, Jiafeng

doi:10.1016/j.ejps.2021.105713

Cited by 30 publications

(10 citation statements)

References 53 publications

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“…The plasma concentration–time curves of RH in UC rats and corresponding pharmacokinetic parameters after oral administration of different RH preparations are shown in Figure and Table , respectively. The results showed that the concentration–time curve of RH after gavage of 50 mg/kg showed a two-compartment model, which was consistent with the previous articles. − After UC rats were given different RH preparations by gavage, RH was absorbed into the blood quickly in the free-RH and RH-F-NPs groups, reaching a peak at about 0.25 h, while it reached a peak at about 2.8 h in the RH-F/C-NPs group. These results were consistent with the previous conclusion of RH release in vitro (Figure E), stating that RH loading with F/C-NPs slowed down the release rate of RH, prolonging the time of RH entering the systemic circulation.…”

Section: Results and Discussionsupporting

confidence: 89%

pH/ROS Dual-Sensitive Natural Polysaccharide Nanoparticles Enhance “One Stone Four Birds” Effect of Rhein on Ulcerative Colitis

Luo

Han

et al. 2022

ACS Appl. Mater. Interfaces

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Rhein (RH), a natural anthraquinone compound, is considered an effective treatment candidate for ulcerative colitis (UC), whose multiple biological activities contribute to UC, including anti-inflammation, antioxidation, intestinal barrier repair, and microflora regulation. However, the application of RH is severely limited by its low water solubility, low bioavailability, and poor colonic targeting. Although some nanoparticles have been developed for the oral delivery of RH, most of them mainly highlighted only one effect of some drug delivery strategies but the above multiple biological activities. Therefore, a multiple polysaccharide-based nanodelivery system, comprising chitosan (CS) and fucoidan (FU), with pH/reactive oxygen species (ROS) sensitivity and mucosal adhesion, was developed and first used to load RH as a comprehensive treatment for UC. Briefly, RH-F/C-NPs were prepared using the polyelectrolyte self-assembly method; the average size of RH-F/C-NPs was 233.1 ± 5.7 nm, and the encapsulation rate of RH was 93.67 ± 1.60%. And it could maintain gastric stability and release RH in the colon with the designed pH/ROS sensitivity contributed by the polysaccharide-based structures. Cellular uptake experiments showed that both NCM 460 cells and RAW 264.7 cells had a good uptake of RH-F/C-NPs. Importantly, the effects of RH were highlighted in in vivo experiments, the results of which showed that RH-F/C-NPs could significantly reduce DSS-induced inflammation by inhibiting the TLR4/NF-κB-mediated anti-inflammatory pathway, the Nrf2/HO-1-mediated antioxidant pathway, colonic mucosal barrier repair, and intestinal microflora regulation. In addition, pharmacokinetic studies have shown that F/C-NPs contribute to the increase in the plasma concentration and the accumulation of RH in the colon to some extent. In short, this study is the first to develop an oral multiple polysaccharide-based nanosystem with pH/ROS dual sensitivity to study the "one stone four birds" therapeutic effect of RH on UC.

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Section: Results and Discussionsupporting

confidence: 89%

pH/ROS Dual-Sensitive Natural Polysaccharide Nanoparticles Enhance “One Stone Four Birds” Effect of Rhein on Ulcerative Colitis

Luo

Han

et al. 2022

ACS Appl. Mater. Interfaces

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“…[101] Bile acids are widely used to improve drug delivery, including by improving transport across membranes, improving capsule strength and increasing drug release. [102][103][104][105][106] For example, deoxycholic acid, a secondary bile acid, has been shown to improve transport across the blood-brain barrier. [107] This may be useful in transportation across the blood labyrinthine barrier that connects the inner ear to the vasculature; to date however, this has not been established in the literature.…”

Section: Bile Acidsmentioning

confidence: 99%

Novel Nanoencapsulation Technology and its Potential Role in Bile Acid‐Based Targeted Gene Delivery to the Inner Ear

Foster

Lewkowicz

Quintas

et al. 2022

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“…Notably, RHE has unique potential for the treatment of diabetes nephropathy (diabetic complications) [51] because of its hypoglycemic and lipid-lowering activity [45], islet cell protection activity [52,53], anti-inflammatory activity [48,49,54], and renal function regulation activity [51,55,56]. According to the Biopharmaceutics Classification System (BCS) classification, RHE belongs to the BCS II class of drugs, with superior permeability and unsatisfactory solubility [57]. The unacceptably low water solubility of RHE causes the problem of low bioavailability, which greatly limits the clinical application of RHE [58].…”

Section: Introductionmentioning

confidence: 99%

Versatile Solid Modifications of Multicomponent Pharmaceutical Salts: Novel Metformin–Rhein Salts Based on Advantage Complementary Strategy Design

Liang

et al. 2023

Pharmaceutics

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This study aimed to develop an effective treatment for diabetes and diabetic complications, based on the advantage complementary strategy of drug–drug salt, by designing and synthesizing the multicomponent molecular salts containing metformin (MET) and rhein (RHE). Finally, the salts of MET–RHE (1:1), MET–RHE–H2O (1:1:1), MET–RHE–ethanol–H2O (1:1:1:1), and MET–RHE–acetonitrile (2:2:1) were obtained, indicating the polymorphism of salts formed by MET and RHE. The structures were analyzed by the combination of characterization experiments and theoretical calculation, and the formation mechanism of polymorphism was discussed. The obtained results of in vitro evaluation showed that MET–RHE had a similar hygroscopicity with metformin hydrochloride (MET·HCl), and the solubility of the component of RHE increased by approximately 93 times, which laid a foundation for improving the bioavailability of MET and RHE in vivo. The evaluation of hypoglycemic activity in mice (C57BL/6N) indicated that MET–RHE exhibited better hypoglycemic activity than the parent drugs and the physical mixtures of MET and RHE. The above findings demonstrate that this study achieved the complementary advantages of MET and RHE through the multicomponent pharmaceutical salification technique, and provides new possibilities for the treatment of diabetic complications.

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Deoxycholic acid-functionalised nanoparticles for oral delivery of rhein

Cited by 30 publications

References 53 publications

pH/ROS Dual-Sensitive Natural Polysaccharide Nanoparticles Enhance “One Stone Four Birds” Effect of Rhein on Ulcerative Colitis

pH/ROS Dual-Sensitive Natural Polysaccharide Nanoparticles Enhance “One Stone Four Birds” Effect of Rhein on Ulcerative Colitis

Novel Nanoencapsulation Technology and its Potential Role in Bile Acid‐Based Targeted Gene Delivery to the Inner Ear

Versatile Solid Modifications of Multicomponent Pharmaceutical Salts: Novel Metformin–Rhein Salts Based on Advantage Complementary Strategy Design

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