Open AccessEvaluation of the Factors Influencing Stomach‐specific Delivery of Antibacterial Agents for Helicobacter pylori Infection
Author(s) -
SHAH SWETA,
QAQISH ROULA,
PATEL VIJAY,
AMIJI MANSOOR
Publication year - 1999
Publication title -
journal of pharmacy and pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.745
H-Index - 118
eISSN - 2042-7158
pISSN - 0022-3573
DOI - 10.1211/0022357991772952
Subject(s) - metronidazole , helicobacter pylori , mucus , chitosan , antibacterial agent , mucin , stomach , drug delivery , chemistry , microbiology and biotechnology , chromatography , antibiotics , medicine , biochemistry , gastroenterology , biology , ecology , organic chemistry
Because Helicobacter pylori infection is localized in the gastric mucus layer and at the mucus layer‐epithelial cell interface, we have developed amoxycillin‐ and metronidazole‐containing chitosan microspheres for stomach‐specific drug delivery. Drug‐loaded porous chitosan microspheres were prepared by simultaneous crosslinking and precipitation with sodium tripolyphosphate. The release of antibacterial agents into simulated gastric fluid (SGF, pH 1.2), and the stability and permeability through gastric mucin, were examined at 37°C. Because of the high porosity of drug‐loaded chitosan microspheres, all the amoxycillin and metronidazole were released in 2 h. High‐performance liquid chromatography assays of the antibacterial agents in SGF at 37°C indicated 40% degradation of amoxycillin after 10h. Metronidazole was completely stable for up to 24h in SGF. Amoxycillin and metronidazole were highly permeable through the gastric mucin gel layer. The results of this study show that acid‐stable antibacterial agents, such as metronidazole, that rapidly permeate the gastric mucus layer would be very effective for the complete eradication of H. pylori infection when delivered specifically at the site of infection in the stomach.