Preformulation studies and optimization of sodium alginate based floating drug delivery system for eradication of Helicobacter pylori

Péter Diós, Sándor Nagy, Szilárd Pál, Tivadar Pernecker, Béla Kocsis, Ferenc Budán, Ildikó Horváth, Krisztián Szigeti, Kata Bölcskei, Domokos Máthé, Attila Dévay

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21 Citations (Scopus)

Abstract

Abstract The aim of this study was to design a local, floating, mucoadhesive drug delivery system containing metronidazole for Helicobacter pylori eradication. Face-centered central composite design (with three factors, in three levels) was used for evaluation and optimization of in vitro floating and dissolution studies. Sodium alginate (X1), low substituted hydroxypropyl cellulose (L-HPC B1, X2) and sodium bicarbonate (X3) concentrations were the independent variables in the development of effervescent floating tablets. All tablets showed acceptable physicochemical properties. Statistical analysis revealed that tablets with 5.00% sodium alginate, 38.63% L-HPC B1 and 8.45% sodium bicarbonate content showed promising in vitro floating and dissolution properties for further examinations. Optimized floating tablets expressed remarkable floating force. Their in vitro dissolution studies were compared with two commercially available non-floating metronidazole products and then microbiologically detected dissolution, ex vivo detachment force, rheological mucoadhesion studies and compatibility studies were carried out. Remarkable similarity (f1, f2) between in vitro spectrophotometrically and microbiologically detected dissolutions was found. Studies revealed significant ex vivo mucoadhesion of optimized tablets, which was considerably increased by L-HPC. In vivo X-ray CT studies of optimized tablets showed 8 h gastroretention in rats represented by an animation prepared by special CT technique.

Original languageEnglish
Article number12007
Pages (from-to)196-206
Number of pages11
JournalEuropean Journal of Pharmaceutics and Biopharmaceutics
Volume96
DOIs
Publication statusPublished - Oct 1 2015

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Keywords

  • Ex vivo mucoadhesion
  • Floating force
  • Gastroretention
  • Low substituted hydroxypropyl cellulose
  • Sodium alginate
  • X-ray CT imaging

ASJC Scopus subject areas

  • Biotechnology
  • Pharmaceutical Science

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