Novel thiolated pluronic anchored gastro-retentive SEDDS of azithromycin against peptic ulcer
[Display omitted] •Azithromycin was integrated in a thiolated pluronic nanoemulsion drug-delivery system.•The novel formulation was extremely potent in eradicating bacterial load.•Azithromycin solubility, mucoadhesion, stability and targeted drug delivery was attained.•The novel formulation shows gr...
Gespeichert in:
Veröffentlicht in: | Inorganic chemistry communications 2024-09, Vol.167, p.112755, Article 112755 |
---|---|
Hauptverfasser: | , , , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
Online-Zugang: | Volltext |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
Zusammenfassung: | [Display omitted]
•Azithromycin was integrated in a thiolated pluronic nanoemulsion drug-delivery system.•The novel formulation was extremely potent in eradicating bacterial load.•Azithromycin solubility, mucoadhesion, stability and targeted drug delivery was attained.•The novel formulation shows great potential for peptic ulcer treatment.
Peptic ulcer disease is a substantial health issue worldwide, owing to excessive use of non-steroidal anti-inflammatory drugs (NSAIDs) and poor hygienic conditions. Numerous therapeutic approaches including antibiotics and PPIs are commonly used, but these therapies are rendered with multi-drug resistance, increased frequency of dosing, less retention time, deceased safety, efficacy, and non-patient compliance. Herein, azithromycin (AZM), an expansive-spectrum antibiotic with notable anti-ulcer efficiency was integrated into a thiolated pluronic self- emulsifying drug delivery system (SEDDS) to enhance its solubility, mucoadhesion, stability, gastro-retention, and targeted drug delivery. Pluronics are triblock copolymers with excellent biocompatibility and amphiphilic properties, widely used in drug delivery, disease diagnosis, and treatment, among other applications. In vitro and in vivo tests were performed to assess the drug-release kinetics, H-pylori clearance, and efficacy. The optimized formulation possessed a size of 357 nm, PDI ≤ 0.5 and a zeta potential of 30 mV. Drug release was 85 % in 72 h, following Korsmeyer-Peppas model. Thiolated SEDDS proved to be extremely potent in eradicating bacterial load (40-load) when compared to alternative formulations. Furthermore, the retention duration, biofilm elimination and nanoparticle uptake were maximized. This novel thiolated SEDDS composition is highly recommended as it holds promising potential to markedly enhance the therapeutic outcomes of AZM in peptic ulcer treatment and overcomes the restrictions of current methodologies. The study not only boosts scientific comprehension of more effective drug-delivery techniques but also recommends significant implications for the broader disciplines of gastroenterology and personalized medicine. |
---|---|
ISSN: | 1387-7003 1879-0259 |
DOI: | 10.1016/j.inoche.2024.112755 |