Development and characterization of colon specific drug delivery system bearing 5-ASA and camylofine dihydrochloride for the treatment of ulcerative colitis

Abstract

The treatment of ulcerative colitis (inflammatory bowel disease, IBD) has been achieved by using colon specific drug delivery system bearing 5-ASA and Camylofine dihydrochloride. Chitosan microspheres were prepared separately for both the drugs using emulsion method followed by enteric coating with Eudragit^®S-100. The in vitro drug release was investigated in different simulated GIT medium. The drug release in PBS (pH7.4) and simulated gastric fluid has shown almost similar pattern and rate, whereas a significant increase in drug release (70.3 ± 1.36 and 72.5 ± 1.33% of 5-ASA and Camylofine, respectively) was observed in medium containing 3% rat caecal matter, after 24 h. In control study, 57.1 ± 1.13% of 5-ASA and 59.2 ± 1.2% of Camylofine release was observed in 24 h. For enzyme induction, rats were orally administered with 1 mL of 1% w/v dispersion of chitosan for 5 days and release rate studies were conducted in SCF with 3% w/v of caecal matter. An enhanced drug release (i.e., 92.3 ± 3.81 and 95.5 ± 3.52% 5-ASA and Camylofine, respectively) was observed after 24 h in dissolution medium containing 3% caecal content obtained from enzyme induced animals. In vivo data showed that microspheres delivered most of its drug load (76.55 ± 2.13%) to the colon after 9 h, which reflects its targeting potential to the colon. It is concluded that orally administered microspheres of both drugs can be used together for the specific delivery of drug to the colon and reduce symptoms of ulcerative colitis.

Keywords::

• Chitosan microspheres
• ulcerative colitis
• Eudragit^®S-100
• 5-ASA
• camylofine dihydrochloride

Acknowledgements

Authors are thankful to Head, Department of pharmaceutical sciences, Dr.H.S.Gour Central University, Sagar for providing necessary facilities, Khandelwal laboratory, Mumbai, India for generously supplying 5-ASA, Camylofine dihydrochloride and TNBS, Indian Institute of chemical biology, Kolkata and Ms.Rounak Dubey for carrying out SEM studies.

Declaration of interest

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of the paper.