Development of gastroretentive metronidazole floating raft system for targeting Helicobacter pylori

Nancy Abdel Hamid Abou Youssef, Abeer Ahmed Kassem, Magda Abd Elsamea El-Massik, Nabila Ahmed Boraie

Research output: Contribution to journalArticleResearchpeer-review

14 Citations (Scopus)

Abstract

The study demonstrates the feasibility of prolonging gastric residence time and release rate of metronidazole (Mz) by preparing floating raft system (FRS) using ion-sensitive in situ gel forming polymers. FRSs contained 3, 4, 5 and 0.5, 0.75, 1% w/v sodium alginate (Alg) and gellan gum (G), respectively, 0.25% w/v sodium citrate and calcium carbonate (C). Lipids: glyceryl mono stearate (GMS), Precirol® and Compritol® were incorporated into G-based formulations (G1%C1%). Mz:lipid ratio was 1:1, except for Mz:GMS, ratios of 1:1.5 and 1:2 were also investigated. Buoyancy, gelation capacity and viscosity parameters were evaluated. Drug release and kinetics for selected formulae were examined. The selected lipid containing formula was subjected to an accelerated stability testing. Alg4%C2% FRS exhibited short gelation lag time (3 s), long duration (>24 h), floating lag time 1 min and duration >24 h, and a reliable sustained drug release (MDT 6 h). Gellan gum FRSs achieved successful floating gastroretention, but failed to achieve the required gelation capacity. Incorporation of GMS (Mz:GMS 1:1) enhanced the gelation lag time and duration (6 s and >24 h, respectively), keeping sustained drug release and formulation stability. The improved characteristics of the selected FRS make them excellent candidates for gastric targeting to eradicate Helicobacter pylori.

Original languageEnglish
Pages (from-to)297-305
Number of pages9
JournalInternational Journal of Pharmaceutics
Volume486
Issue number1-2
DOIs
Publication statusPublished - 30 May 2015

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Stearates
Metronidazole
Helicobacter pylori
Lipids
Stomach
Drug Compounding
Calcium Carbonate
Feasibility Studies
Viscosity
Polymers
Pharmacokinetics
Gels
Ions
Drug Liberation
gellan gum

Keywords

  • Compritol<sup>®</sup>
  • Gelation capacity
  • Gellan gum
  • Glyceryl mono stearate
  • Precirol<sup>®</sup>
  • Sodium alginate

Cite this

Abou Youssef, Nancy Abdel Hamid ; Kassem, Abeer Ahmed ; El-Massik, Magda Abd Elsamea ; Boraie, Nabila Ahmed. / Development of gastroretentive metronidazole floating raft system for targeting Helicobacter pylori. In: International Journal of Pharmaceutics. 2015 ; Vol. 486, No. 1-2. pp. 297-305.
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Development of gastroretentive metronidazole floating raft system for targeting Helicobacter pylori. / Abou Youssef, Nancy Abdel Hamid; Kassem, Abeer Ahmed; El-Massik, Magda Abd Elsamea; Boraie, Nabila Ahmed.

In: International Journal of Pharmaceutics, Vol. 486, No. 1-2, 30.05.2015, p. 297-305.

Research output: Contribution to journalArticleResearchpeer-review

TY - JOUR

T1 - Development of gastroretentive metronidazole floating raft system for targeting Helicobacter pylori

AU - Abou Youssef, Nancy Abdel Hamid

AU - Kassem, Abeer Ahmed

AU - El-Massik, Magda Abd Elsamea

AU - Boraie, Nabila Ahmed

PY - 2015/5/30

Y1 - 2015/5/30

N2 - The study demonstrates the feasibility of prolonging gastric residence time and release rate of metronidazole (Mz) by preparing floating raft system (FRS) using ion-sensitive in situ gel forming polymers. FRSs contained 3, 4, 5 and 0.5, 0.75, 1% w/v sodium alginate (Alg) and gellan gum (G), respectively, 0.25% w/v sodium citrate and calcium carbonate (C). Lipids: glyceryl mono stearate (GMS), Precirol® and Compritol® were incorporated into G-based formulations (G1%C1%). Mz:lipid ratio was 1:1, except for Mz:GMS, ratios of 1:1.5 and 1:2 were also investigated. Buoyancy, gelation capacity and viscosity parameters were evaluated. Drug release and kinetics for selected formulae were examined. The selected lipid containing formula was subjected to an accelerated stability testing. Alg4%C2% FRS exhibited short gelation lag time (3 s), long duration (>24 h), floating lag time 1 min and duration >24 h, and a reliable sustained drug release (MDT 6 h). Gellan gum FRSs achieved successful floating gastroretention, but failed to achieve the required gelation capacity. Incorporation of GMS (Mz:GMS 1:1) enhanced the gelation lag time and duration (6 s and >24 h, respectively), keeping sustained drug release and formulation stability. The improved characteristics of the selected FRS make them excellent candidates for gastric targeting to eradicate Helicobacter pylori.

AB - The study demonstrates the feasibility of prolonging gastric residence time and release rate of metronidazole (Mz) by preparing floating raft system (FRS) using ion-sensitive in situ gel forming polymers. FRSs contained 3, 4, 5 and 0.5, 0.75, 1% w/v sodium alginate (Alg) and gellan gum (G), respectively, 0.25% w/v sodium citrate and calcium carbonate (C). Lipids: glyceryl mono stearate (GMS), Precirol® and Compritol® were incorporated into G-based formulations (G1%C1%). Mz:lipid ratio was 1:1, except for Mz:GMS, ratios of 1:1.5 and 1:2 were also investigated. Buoyancy, gelation capacity and viscosity parameters were evaluated. Drug release and kinetics for selected formulae were examined. The selected lipid containing formula was subjected to an accelerated stability testing. Alg4%C2% FRS exhibited short gelation lag time (3 s), long duration (>24 h), floating lag time 1 min and duration >24 h, and a reliable sustained drug release (MDT 6 h). Gellan gum FRSs achieved successful floating gastroretention, but failed to achieve the required gelation capacity. Incorporation of GMS (Mz:GMS 1:1) enhanced the gelation lag time and duration (6 s and >24 h, respectively), keeping sustained drug release and formulation stability. The improved characteristics of the selected FRS make them excellent candidates for gastric targeting to eradicate Helicobacter pylori.

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KW - Gelation capacity

KW - Gellan gum

KW - Glyceryl mono stearate

KW - Precirol<sup>®</sup>

KW - Sodium alginate

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U2 - 10.1016/j.ijpharm.2015.04.004

DO - 10.1016/j.ijpharm.2015.04.004

M3 - Article

VL - 486

SP - 297

EP - 305

JO - International Journal of Pharmaceutics

JF - International Journal of Pharmaceutics

SN - 0378-5173

IS - 1-2

ER -