Abstract
The current study aimed to develop a luteolin gastric floating microsponge for targeting Helicobacter pylori. The microsponge formulations were prepared by a quasi-emulsion method, and then evaluated for various physicochemical variables. The best microsponge was further assessed for drug-polymer interactions, surface morphology, in vivo floating, and in vitro anti H. pylori activity. The formulation which exhibited comparatively good production yield (64.45% ± 0.83), high entrapment efficiency (67.33% ± 3.79), prolonged in vitro floating time (>8 h), and sustained in-vitro drug release was selected as the best microsponge. The SEM study revealed that the best microsponge was spherical in shape and has a porous surface with interconnecting channels. DSC and XRD studies demonstrated the dispersion of luteolin in the polymeric matrix of the microsponge. Ultrasonography confirmed that the best microsponge could in the rat stomach for 4 h. The in vitro MIC results indicate that the anti H. pylori activity of the best microsponge was almost doubled and more sustained compared to pure luteolin. To conclude, it can be said that the developed luteolin gastric floating microsponge could be a better option to effectively eradicate H. pylori infections and the histopathological and pharmacodynamic assessments of our best microsponge can be expected to provide a rewarding outcome.
Highlights
Helicobacter pylori (H. pylori) is a bacterium that colonizes the human stomach
All microsponge formulations floated within no time after placing them in the medium and they remained floating in the medium for more than 8 h
The emergence of antibiotic resistance in H. pylori has reduced the efficacy of conventional drugs such clarithromycin, amoxicillin, metronidazole, tetracycline and levofloxacin [36]
Summary
70% of the world’s population are infected with H. pylori and are asymptomatic [1]. H. pylori infection is the main cause of gastric ulcers and gastritis that can lead to gastric cancer [2,3,4]. Even though more than half of the human population is infected with. H. pylori only 10–20% will develop a peptic ulcer, and only 1–2% are at risk to develop gastric cancer or MALT lymphoma. The antibiotics which are currently in use in the treatment of H. pylori infections are amoxicillin, tetracycline, metronidazole and macrolides (azithromycin or clarithromycin). Despite the successful use of these treatments, 20% of patients fail to respond positively to therapy. Therapy failure is mostly due to the reduced efficacy of the above antibiotics. H. pylori develop resistance by point mutations
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
