Beta-Sitosterol-Conjugated Sinapic Acid-Engineered Nanoliposome: Biomucoadhesive and Enzyme-Responsive Targeted Oral Therapy in Ulcerative Colitis

ACS Applied Materials & Interfaces, Год журнала: 2025, Номер unknown

Опубликована: Апрель 29, 2025

Developing oral drug delivery systems is promising for ulcerative colitis (UC). However, the key challenges, including formulation degradation under harsh gastric conditions, poor targeting efficiency, and limited colonic residence, lead to therapeutic efficacy that still needs be tackled. Effective treatment requires a safe, efficacious, enzyme- pH-responsive, biomucoadhesive system overcome these challenges. Therefore, we have developed chitosan-armored 1,2-dimyristoyl-sn-glycero-3-phosphoglycerol (DMPG) nanoliposomes amalgamated with synthesized beta-sitosterol-sinapic acid (Be-S) conjugate, further encapsulated 3,4-methylenedioxy-β-nitrostyrene (MNS) as NLRP3 inhibitor, termed C@MN@DMBe-S, limitation of free MNS sinapic acid. Formulated by thin-film hydration method processed through extrusion, unilamellar liposomes demonstrated structural stability mucoadhesive properties due chitosan coating. This configuration protected from acidic environment allowed retention in inflamed colon 48 h. The enzyme-responsive C@MN@DMBe-S nanoliposome releases at site via esterase activity, providing sustained controlled release MNS. synergistic action delivers antioxidant anti-inflammatory effects while influencing gut microbiota composition releasing short-chain fatty acids. Moreover, investigations revealed exhibited superior compared when administered orally. effectively downregulated NF-κB, NLRP3, Caspase-1, IL-1β expression upregulating MUC5AC expression, indicating enhanced protective thereby promoting mucosal healing. In addition, was found regulate immune cell downregulate neutrophil infiltration. armor- strategy elucidates impact nanomedicines on mitigating UC an effective treatment.

Язык: Английский

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Leveraging thiol-functionalized biomucoadhesive hybrid nanoliposome for local therapy of ulcerative colitis

Biomaterials, Год журнала: 2024, Номер 312, С. 122747 - 122747

Опубликована: Авг. 6, 2024

Язык: Английский

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Oral chondroitin sulfate functionalized natural polyphenol for targeted therapy of ulcerative colitis

Materials & Design, Год журнала: 2024, Номер 238, С. 112645 - 112645

Опубликована: Янв. 6, 2024

Ulcerative colitis (UC) is an idiopathic, chronic, and progressive inflammatory set of conditions that affects the colonic mucosa. Natural Polyphenols are well documented for their excellent antioxidant properties have obvious advantages in strategy anti-oxidation treatment UC. However, poor water solubility, low bioavailability, unstable nature hindered clinical application. Therefore, we efficiently encapsulated bioactive polyphenol epigallocatechin gallate (EGCG) with poly(N-vinylpyrrolidone) (PVP) via reliable intermolecular hydrogen-bonded interactions, conjugated polysaccharide chondroitin sulfate (CS) gastrointestinal stability CD44 active targeting capability onto surfaces to achieve targeted delivery (EPC). The obtained EPC system showed average diameter 54 nm, monodisperse size distribution negatively charged surface. In vitro studies demonstrated reactive oxygen species (ROS)-scavenging anti-inflammatory ability system. After oral administration, localized inflamed colon effectively alleviated symptoms dextran sodium salt (DSS)-induced UC mice. Specifically, down-regulated expression cytokines, up-regulated tight junction-associated proteins restore intestinal barrier, modulated gut microbiota. This drug a simple self-assembling process may pave new polyphenol-based therapy

Язык: Английский

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Conjugation, Prodrug, and Co-Administration Strategies in Support of Nanotechnologies to Improve the Therapeutic Efficacy of Phytochemicals in the Central Nervous System

Pharmaceutics, Год журнала: 2023, Номер 15(6), С. 1578 - 1578

Опубликована: Май 23, 2023

Phytochemicals, produced as secondary plant metabolites, have shown interesting potential therapeutic activities against neurodegenerative diseases and cancer. Unfortunately, poor bioavailability rapid metabolic processes compromise their use, several strategies are currently proposed for overcoming these issues. The present review summarises enhancing the central nervous system's phytochemical efficacy. Particular attention has been paid to use of phytochemicals in combination with other drugs (co-administrations) or administration prodrugs conjugates, particularly when approaches supported by nanotechnologies exploiting conjugation appropriate targeting molecules. These aspects described polyphenols essential oil components, which can improve loading nanocarriers, be part nanocarriers designed targeted co-delivery achieve synergistic anti-glioma anti-neurodegenerative effects. vitro models, able simulate blood-brain barrier, neurodegeneration glioma, useful optimizing innovative formulations before vivo via intravenous, oral, nasal routes, is also summarised. Among compounds, quercetin, curcumin, resveratrol, ferulic acid, geraniol, cinnamaldehyde efficaciously formulated attain brain-targeting characteristics, may therefore therapeutically glioma diseases.

Язык: Английский

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Research advancements and perspectives of inflammatory bowel disease: A comprehensive review

Science Progress, Год журнала: 2024, Номер 107(2)

Опубликована: Апрель 1, 2024

Inflammatory bowel disease (IBD) is a chronic inflammatory with increasing incidence, such as Crohn's and ulcerative colitis. The accurate etiology pathogenesis of IBD remain unclear, it generally believed that related to genetic susceptibility, gut microbiota, environmental factors, immunological abnormalities, potentially other factors. Currently, the mainstream therapeutic drugs are amino salicylic acid agents, corticosteroids, immunomodulators, biological but remission rates do not surpass 30-60% patients in real-life setting. As consequence, there many studies focusing on emerging bioactive ingredients have higher efficacy long-term safety for achieving complete deep healing. This article begins review latest, systematic, credible summaries IBD. In addition, we provide summary current treatments Finally, focus effects microRNAs lncRNAs, nanoparticles-mediated natural products their mechanisms action.

Язык: Английский

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Caffeic acid inhibits Staphylococcus aureus‐induced endometritis through regulating AMPKα/mTOR/HIF‐1α signalling pathway

Journal of Cellular and Molecular Medicine, Год журнала: 2024, Номер 28(20)

Опубликована: Окт. 1, 2024

Abstract Endometritis is mostly caused by childbirth or postpartum uterine infection. It one of the important reasons leading to female infertility. Caffeic acid (CA) and its derivatives are widely found in some foods traditional Chinese medicine, have biological activities such as antioxidant, free radical scavenging, anti‐inflammatory, anti‐infection. In this study, we aimed explore effect CA on Staphylococcus aureus ‐induced endometritis. The contents TNF‐α IL‐1β were detected ELISA S. endometritis model. Western blot assay was used detect expression AMPKα/mTOR/HIF‐1α pathway related proteins GPX4 expression. addition, concentrations MDA, GSH, iron tested kits. Compared with model group, treatment significantly alleviated injury, MPO activity, inflammatory factors IL‐1β, NF‐κB activation. Meanwhile, inhibited ferroptosis, confirmed decreased MDA concentration up‐regulated GSH level. Furthermore, attenuated HIF‐1α phosphorylated mTOR increased AMPK conclusion, inhibits inflammation ferroptosis regulating signalling alleviate mice.

Язык: Английский

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Colon delivery of agomelatine nanoparticles in the treatment of TNBS induced ulcerative colitis

Drug Delivery and Translational Research, Год журнала: 2025, Номер unknown

Опубликована: Янв. 24, 2025

Язык: Английский

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Classification of Nanomaterial Drug Delivery Systems for Inflammatory Bowel Disease

International Journal of Nanomedicine, Год журнала: 2025, Номер Volume 20, С. 1383 - 1399

Опубликована: Фев. 1, 2025

Abstract: Inflammatory bowel disease (IBD), including Crohn's and ulcerative colitis, primarily arises from defects in the colonic barrier, imbalances of gut microbiota, immune response issues. These complex causes make it difficult to achieve a complete cure. Patients with IBD frequently experience recurrent abdominal pain bloody diarrhea, while severe cases may result intestinal obstruction, perforation, cancer. Lifelong maintenance therapy thus be needed manage these symptoms; however, traditional drugs, such as 5-aminosalicylic acid, glucocorticoids, immunosuppressants, biological agents, are often associated problems poor solubility, instability, ineffective targeting, well causing serious side effects non-target tissues. Nanomaterial drug delivery systems (NDDS) have recently shown great promise optimizing distribution, solubility through biocompatible coatings, enhancing bioavailability via PEGylation reducing effects. formulations can enhance drug's pharmacokinetics by modifying its properties, improve ability cross barriers, boost bioavailability. In addition, NDDS enable targeted delivery, increase local concentrations, efficacy, reduce effects, protecting active molecules recognition protease degradation. The clinical use for treating IBD, requires further research. This review summarizes classification concludes that, despite ongoing challenges, represent an effective treatment approach IBD. summary, therapeutic agents specific cells or tissues, thereby improving efficacy. effectively surmount facilitating efficient sites, which is crucial attaining optimal outcomes. contributes deeper understanding how physicochemical properties influence pharmacological behavior vivo expedite their translation. Keywords: inflammatory disease, nanomaterials, nano-delivery systems, nanomedicine applications

Язык: Английский

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The Modulation of Cell Plasticity by Budesonide: Beyond the Metabolic and Anti-Inflammatory Actions of Glucocorticoids

Pharmaceutics, Год журнала: 2025, Номер 17(4), С. 504 - 504

Опубликована: Апрель 11, 2025

The synthetic cortisol analog budesonide (BUD) is an essential drug employed to manage chronic inflammatory diseases in humans, mainly those involving gastroenteric and airway mucosa, such as rhinitis, laryngitis, bronchitis, esophagitis, gastritis, colitis, with high levels of success. As a glucocorticoid, BUD prevents the expression pro-inflammatory cytokines/chemokines recruitment immune cells into inflamed mucosa. However, emerging evidence indicates that BUD, unlike classical glucocorticoids, also potent modulator stem cancer cell behavior/plasticity. Certainly, stabilizes cell–cell adhesions, preventing embryonic differentiation inhibiting development 3D gastruloids. In addition, inhibits motile/invasive propensity different cells, including breast, lung, pancreatic cancer. Finally, it infection positive single-stranded human-infecting RNA viruses SARS-CoV-2. At molecular level, induces epigenetic changes modifies transcriptome epithelial, stem, providing support cell-independent activity BUD. Here, we performed in-depth review these unexpected activities identified by unbiased screening programs, emphasize mechanisms modulated this efficacious deserve further research.

Язык: Английский

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Zinc pyrithione ameliorates colitis in mice by interacting on intestinal epithelial TRPA1 and TRPV4 channels

Life Sciences, Год журнала: 2024, Номер 358, С. 123090 - 123090

Опубликована: Окт. 9, 2024

Язык: Английский

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