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Mucoadhesive microspheres containing amoxicillin for clearance of Helicobacter pylori
N Nagahara1, Y Akiyama, M Nakao
1DDS Research Laboratories, Pharmaceutical Research Division, Takeda Chemical Industries, Ltd., Osaka, Japan. Nagahara_Naoki@Takeda.co.jp
Abstract:
In an effort to augment the anti-Helicobacter pylori effect of amoxicillin, mucoadhesive microspheres, which have the ability to reside in the gastrointestinal tract for an extended period, were prepared. The microspheres contained the antimicrobial agent and an adhesive polymer (carboxyvinyl polymer) powder dispersed in waxy hydrogenated castor oil. The percentage of amoxicillin remaining in the stomach both 2 and 4 h after oral administration of the mucoadhesive microspheres to Mongolian gerbils under fed conditions was about three times higher than that after administration in the form of a 0.5% methylcellulose suspension. The in vivo clearance of H. pylori following oral administration of the mucoadhesive microspheres and the 0.5% methylcellulose suspension to infected Mongolian gerbils was examined under fed conditions. The mucoadhesive microspheres and the 0.5% methylcellulose suspension both showed anti-H. pylori effects in this experimental model of infection, but the required dose of amoxicillin was effectively reduced by a factor of 10 when the mucoadhesive microspheres were used. In conclusion, the mucoadhesive microspheres more effectively cleared H. pylori from the gastrointestinal tract than the 0.5% methylcellulose suspension due to the prolonged gastrointestinal residence time resulting from mucoadhesion. A dosage form consisting of mucoadhesive microspheres containing an appropriate antimicrobial agent should be useful for the eradication of H. pylori.
Insights
Mucoadhesive microspheres significantly enhanced amoxicillin's anti-Helicobacter pylori effect by prolonging drug residence time in the gastrointestinal tract, reducing required dosage for effective bacterial clearance.
Area of Science:
- Pharmaceutical Sciences
- Gastroenterology
- Microbiology
Background:
- Amoxicillin is an antibiotic used to treat bacterial infections.
- Helicobacter pylori (H. pylori) is a bacterium that infects the stomach, causing gastritis and ulcers.
- Conventional amoxicillin formulations may have limited efficacy due to rapid clearance from the gastrointestinal tract.
Purpose of the Study:
- To develop mucoadhesive microspheres to augment the anti-H. pylori effect of amoxicillin.
- To evaluate the gastrointestinal residence time and H. pylori clearance efficacy of these microspheres.
Main Methods:
- Mucoadhesive microspheres were prepared using carboxyvinyl polymer and hydrogenated castor oil, encapsulating amoxicillin.
- Amoxicillin levels in the stomach were measured in Mongolian gerbils at 2 and 4 hours post-administration.
- In vivo H. pylori clearance was assessed in infected Mongolian gerbils comparing microspheres to a methylcellulose suspension.
Main Results:
- Microspheres significantly increased amoxicillin's gastric residence time (approximately threefold higher at 2 and 4 hours).
- Both formulations showed anti-H. pylori activity, but microspheres reduced the effective amoxicillin dose by a factor of 10.
- Mucoadhesive microspheres demonstrated superior H. pylori clearance compared to the methylcellulose suspension.
Conclusions:
- Mucoadhesive microspheres provide prolonged gastrointestinal residence, enhancing amoxicillin's efficacy against H. pylori.
- This novel dosage form offers a promising strategy for H. pylori eradication.
- The mucoadhesive approach warrants further investigation for antimicrobial drug delivery.