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Preparation and evaluation of floating‐bioadhesive microparticles containing clarithromycin for the eradication of Helicobacter pylori
Author(s) -
Zheng Jianhua,
Liu Chaowu,
Bao Decai,
Zhao Yanjun,
Ma Xiaojun
Publication year - 2006
Publication title -
journal of applied polymer science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.575
H-Index - 166
eISSN - 1097-4628
pISSN - 0021-8995
DOI - 10.1002/app.24319
Subject(s) - bioadhesive , clarithromycin , chitosan , drug delivery , chemistry , chromatography , drug carrier , omeprazole , nuclear chemistry , materials science , pharmacology , organic chemistry , medicine , antibiotics , biochemistry
The development of a gastric floating‐bioadhesive drug delivery system to increase the efficacy of clarithromycin against Helicobacter pylori is described. Floating‐bioadhesive microparticles containing clarithromycin were prepared by a combined method of emulsification/evaporation and internal/ion gelation for the treatment of H. pylori infection. Ethylcellulose microspheres (EMs) were prepared by the dispersion of clarithromycin, ethylcellulose, and chitosan in dichloromethane and subsequent solvent evaporation. EMs were coated with alginate by the internal gelation process to obtain alginate–ethylcellulose microparticles (AEMs); then, AEMs were dispersed in a chitosan solution, and chitosan–alginate–ethylcellulose microparticles (CAEMs) were obtained by ion gelation to enhance the bioadhesive properties. The morphologies of EMs and CAEMs were investigated under optical and scanning electron microscopes. In vitro buoyancy and drug‐release testing confirmed the good floating and sustained‐release properties of CAEMs. About 74% of the CAEMs floated in an acetate buffer solution for 8 h, and 90% of the clarithromycin contained in the CAEMs was released within 8 h in a sustained manner. In vivo mucoadhesive testing showed that 61% of the CAEMs could be retained in the stomach for 4 h. Under a pretreatment with omeprazole, the clarithromycin concentration in gastric mucosa of the CAEM group was higher than that of the clarithromycin solution group. These results suggest that CAEMs might be a promising drug delivery system for the treatment of H. pylori infection. © 2006 Wiley Periodicals, Inc. J Appl Polym Sci 102: 2226–2232, 2006