Development of novel pH-sensitive thiolated chitosan/PMLA nanoparticles for amoxicillin delivery to treat Helicobacter pylori

Mater Sci Eng C Mater Biol Appl. 2018 Feb 1:83:17-24. doi: 10.1016/j.msec.2017.08.038. Epub 2017 Aug 12.

Abstract

The cysteine conjugated chitosan/PMLA multifunctional nanoparticles were synthesized as targeted Nano-drug delivery system to eradicate Helicobacter pylori. Helicobacter pylori specifically express urea transport protein on its membrane to carrying urea to the cytoplasm urease to supply ammonia that protects bacteria in the acid environment of the stomach. The clinical suitability of topical antimicrobial agents is required to get rid of Helicobacter pylori inside the inflamed basal region. In this work, cysteine conjugated chitosan derivative, Cys-CS for their mucoadhesive and anticoagulant properties was designed and synthesized, for the preparation of multifunctional nanoparticles. The technique turned into optimized to prepare Cys-CS/PMLA nanoparticles for encapsulation of amoxicillin. The results showed that amoxicillin-Cys-CS/PMLA nanoparticles exhibit favorable pH-sensitive properties that could procrastinate the release of amoxicillin at gastric acid and allow the drug to deliver and target to Helicobacter pylori at its survival region efficiently. In comparison with unmodified amoxicillin-chitosan/PMLA nanoparticles, effective inhibition of Helicobacter pylori growth was observed for amoxicillin-Cys-CS/PMLA nanoparticles. These results indicate that the multifunctional amoxicillin-loaded nanoparticles have great potential for the effective treatment of Helicobacter pylori infection. They can also be used as pharmacologically powerful nanocarriers for oral targeted delivery of different therapeutic drugs to treat Helicobacter pylori.

Keywords: Chitosan; Helicobacter pylori; Mucoadhesive; Multifunctional nanoparticles; Poly (malic acid) (PMLA); Targeted delivery; pH-sensitive.

MeSH terms

  • Amoxicillin / chemistry*
  • Amoxicillin / pharmacology
  • Chitosan / chemistry*
  • Drug Carriers / chemistry
  • Drug Delivery Systems / methods
  • Helicobacter pylori / drug effects
  • Hydrogen-Ion Concentration
  • Nanoparticles / chemistry*
  • Polymers / chemistry

Substances

  • Drug Carriers
  • Polymers
  • Amoxicillin
  • Chitosan