Development of melatonin loaded pectin nanoparticles for the treatment of inflammatory bowel disease: In vitro and in vivo studies

Yener, Serkan; Akbulut, K. Gonca; Karakuş, Resul; Erdoğan, Deniz; Acartürk, Füsun

doi:10.1016/j.jddst.2021.102861

Cited by 9 publications

(8 citation statements)

References 60 publications

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“…In a recent work conducted by Yener et al, 289 pectin-based nanoparticles containing melatonin ameliorated the TNBS-induced IBD in rats by decreasing colonic fibrosis, oxidative stress, and inflammatory parameters of the colon. Melatonin was used as an antioxidant, anti-inflammatory, and radical scavenger drug.…”

Section: Pectinsmentioning

confidence: 96%

“…The same study revealed that pectin nanoparticles were 40 times more adherent to the inflamed rat's colon than the healthy colon mucosa, where the drug is released. 289 The efficacy of pectin nanoparticles was further improved by adding HA in the formulation. The resulting hybrid particles (284 nm in size) were used to encapsulate Rhein as a natural anti-inflammatory ingredient.…”

Section: Pectinsmentioning

confidence: 99%

See 1 more Smart Citation

Advances in the treatment of inflammatory bowel disease: Focus on polysaccharide nanoparticulate drug delivery systems

Hadji

Bouchemal

2022

Advanced Drug Delivery Reviews

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Section: Pectinsmentioning

confidence: 96%

Section: Pectinsmentioning

confidence: 99%

Advances in the treatment of inflammatory bowel disease: Focus on polysaccharide nanoparticulate drug delivery systems

Hadji

Bouchemal

2022

Advanced Drug Delivery Reviews

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“…The ion-gelation method was successful in loading SCN within the formed pectin nanoparticles with different ratios of CaCl 2 as a cross-linker. This might be related to the positively charged CaCl 2 , which was successfully cross-linked with the negatively charged pectin molecules by an intermolecular cross-link, which is formed by electrostatic complexation interaction [ 20 ].…”

Section: Resultsmentioning

confidence: 99%

Pectin Nanoparticle-Loaded Soft Coral Nephthea sp. Extract as In Situ Gel Enhances Chronic Wound Healing: In Vitro, In Vivo, and In Silico Studies

et al. 2023

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This study shed light for the first time on the in vivo diabetic wound healing potential activity of natural marine soft coral polymeric nanoparticle in situ gel using an excision wound model. A Nephthea sp. methanol–methylene chloride extract loaded with pectin nanoparticles (LPNs) was created. For the preparation of in situ gel, ion-gelation techniques, the entrapment efficiency, the particle size, the polydispersity index, the zeta potential, the in-vitro drug release, and a transmission electron microscope were used and the best formula was selected. Using (UPLC-Q/TOF-MS), 27 secondary metabolites responsible for extract biological activity were identified. Isolation and identification of arachidic acid, oleic acid, nervonic acid, and bis-(2-ethylhexyl)-phthalate (DEHP) of Nephthea sp. was firstly reported here using NMR and mass spectral analyses. Moreover, LPN in situ gel has the best effects on regulating the proinflammatory cytokines (NF-κB, TNF-α, IL-6, and IL-1β) that were detected on days 7 and 15. The results were confirmed with an in vitro enzymatic inhibitory effect of the extract against glycogen synthase kinase (GSK-3) and matrix metalloproteinase-1 (MMP-1), with IC50 values of 0.178 ± 0.009 and 0.258 ± 0.011 µg/mL, respectively. The molecular docking study showed a free binding energy of −9.6 kcal/mol for chabrolosteroid E, with the highest binding affinity for the enzyme (GSK-3), while isogosterone B had −7.8 kcal/mol for the enzyme (MMP-1). A pharmacokinetics study for chabrolohydroxybenzoquinone F and isogosterone B was performed, and it predicted the mode of action of wound healing activity.

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“…Additionally, it is reported that there is a greater release of Qt by diffusion at pH 5.4 compared to pH 7.4 from the NEs F4Qt and P4Qt. This is explained by the loss of QPA and QP complex solubility when found at pH values (2)(3)(4)(5) close to the pI of QP and pKa of the alginate, which leads to conformational changes (helix to beta sheets) in the structure of the protein, favoring the release of Qt.…”

Section: Stem Images Of Nesmentioning

confidence: 99%

Nanoemulsions Based on Soluble Chenopodin/Alginate Complex for Colonic Delivery of Quercetin

Intiquilla,

Arazo,

Gamboa

et al. 2024

Antioxidants

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Inflammatory bowel disease (IBD) is an autoimmune disorder caused by uncontrolled immune activation and the subsequent destruction of the colon tissue. Quercetin (Qt) is a natural antioxidant and anti-inflammatory agent proposed as an alternative to mitigate IBD. However, its use is limited by its low oral bioavailability. This study aimed to develop nanoemulsions (NEs) based on a soluble chenopodin/alginate (QPA) complex and Tween 80 (T80), intended for the colonic release of Qt, activated by the pH (5.4) and bacteria present in the human colonic microbiota. NEs with different ratios of QPA/Tw80 (F1-F6) were prepared, where F4Qt (60/40) and F5Qt (70/30) showed sizes smaller than 260 nm, PDI < 0.27, and high encapsulation efficiency (>85%). The stability was evaluated under different conditions (time, temperature, pH, and NaCl). The DSC and FTIR analyses indicated hydrophobic and hydrogen bonding interactions between QPA and Qt. F4Qt and F5Qt showed the greater release of Qt in PBS1X and Krebs buffer at pH 5.4 (diseased condition), compared to the release at pH 7.4 (healthy condition) at 8 h of study. In the presence of E. coli and B. thetaiotaomicron, they triggered the more significant release of Qt (ƒ2 < 50) compared to the control (without bacteria). The NEs (without Qt) did not show cytotoxicity in HT-29 cells (cell viability > 80%) and increased the antioxidant capacity of encapsulated Qt. Therefore, these NEs are promising nanocarriers for the delivery of flavonoids to the colon to treat IBD.

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Development of melatonin loaded pectin nanoparticles for the treatment of inflammatory bowel disease: In vitro and in vivo studies

Cited by 9 publications

References 60 publications

Advances in the treatment of inflammatory bowel disease: Focus on polysaccharide nanoparticulate drug delivery systems

Advances in the treatment of inflammatory bowel disease: Focus on polysaccharide nanoparticulate drug delivery systems

Pectin Nanoparticle-Loaded Soft Coral Nephthea sp. Extract as In Situ Gel Enhances Chronic Wound Healing: In Vitro, In Vivo, and In Silico Studies

Nanoemulsions Based on Soluble Chenopodin/Alginate Complex for Colonic Delivery of Quercetin

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