CLARITHROMYCIN MUCOADHESIVE MICROSPHERES FOR ANTI­ HELICOBACTER PYLORI THERAPY: FORMULATION AND INVITRO EVALUATION

Helicobacter pylori (H.pylori) is a gram‐negative bacillus responsible for one of the most common infections found in humans worldwide. H pylori causes gastric diseases, such as peptic ulcer, gastric mucosa associated lymphoma. Recent studies showsnthat, decreasing efficacy of  therapies worldwide. One reason for the incomplete eradication of H. pylori is probably due to the short residence time of antimicrobial agents in the stomach so that effective antimicrobial concentration cannot be achieved in the gastric mucous layer or epithelial cell surfaces where H. pylori exists. The purpose of this study was to design mucoadhesive microspheres containing Clarithromycin as an anti‐H. pylori agent to deliver the drug specifically to mucus layer where H.pylori resides and evaluate  the effectiveness of the mucoadhesive microspheres for H. pylori eradication therapy. Microspheres were prepared by using Eudragit RL100 as matrix and Carbopol 974P as a mucoadhesive polymer. The microspheres were prepared by emulsion solvent evaporation technique. The prepared microspheres were evaluated with respect to the particle size, production yield, encapsulation efficiency, shape and surface properties, mucoadhesive property, in vitro drug release and suitability for anti Helicobactor pylori effect. The preliminary results show great promise for this delivery strategy in the treatment of H. Pylori infection.

[1]  Hoo-Kyun Choi,et al.  Preparation of mucoadhesive microspheres containing antimicrobial agents for eradication of H. pylori. , 2005, International journal of pharmaceutics.

[2]  Zhepeng Liu,et al.  In vitro and in vivo studies on mucoadhesive microspheres of amoxicillin. , 2005, Journal of controlled release : official journal of the Controlled Release Society.

[3]  E. Fontham,et al.  Age at Acquisition of Helicobacter pylori Infection: Comparison of Two Areas with Contrasting Risk of Gastric Cancer , 2004, Helicobacter.

[4]  N. Uemura [The trend of the research on H. pylori eradication and gastric cancer prevention]. , 2004, Nihon rinsho. Japanese journal of clinical medicine.

[5]  P. Rozen Cancer of the gastrointestinal tract: early detection or early prevention? , 2004, European journal of cancer prevention : the official journal of the European Cancer Prevention Organisation.

[6]  A. Shrivastava,et al.  Development and Characterization of Mucoadhesive Microspheres Bearing Salbutamol for Nasal Delivery , 2004, Drug delivery.

[7]  K. Ozasa,et al.  Helicobacter pylori Infection and Atrophic Gastritis (A Nested Case-Control Study in a Rural Town in Japan) , 1999, Digestive Diseases and Sciences.

[8]  P. Correa The biological model of gastric carcinogenesis. , 2004, IARC scientific publications.

[9]  H. Tseng,et al.  One-Week Quadruple Therapy Is an Effective Salvage Regimen for Helicobacter pylori Infection in Patients After Failure of Standard Triple Therapy , 2002, Journal of clinical gastroenterology.

[10]  A. Kokkola,et al.  The effect of Helicobacter pylori eradication on the natural course of atrophic gastritis with dysplasia , 2002, Alimentary pharmacology & therapeutics.

[11]  R. Peek,et al.  Review article: pathogenesis of Helicobacter pylori‐induced gastric inflammation , 2001, Alimentary pharmacology & therapeutics.

[12]  S. K. Ogata,et al.  Triple therapy with clarithromycin, amoxicillin and omeprazole for Helicobacter pylori eradication in children and adolescents. , 2001, Arquivos de gastroenterologia.

[13]  M F Dixon,et al.  Classification and grading of gastritis. The updated Sydney System. International Workshop on the Histopathology of Gastritis, Houston 1994. , 1996, The American journal of surgical pathology.

[14]  R. Spiller,et al.  Detection of the intragastric sites at which Helicobacter pylori evades treatment with amoxycillin and cimetidine. , 1995, Gut.

[15]  M. Cooreman,et al.  Local gastric and serum amoxicillin concentrations after different oral application forms , 1993, Antimicrobial Agents and Chemotherapy.

[16]  Alter Mj,et al.  Association between infection with Helicobacter pylori and risk of gastric cancer: evidence from a prospective investigation. , 1991, BMJ.

[17]  M. Caruso,et al.  Histological identification of Helicobacter pylori in early and advanced gastric cancer. , 1990, Journal of clinical gastroenterology.

[18]  P. Correa,et al.  A human model of gastric carcinogenesis. , 1988, Cancer research.

[19]  P. Sipponen,et al.  Chronic gastritis: dynamic and clinical aspects. , 1985, Scandinavian journal of gastroenterology. Supplement.