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Published on:December 2015
Indian Journal of Pharmaceutical Education and Research, 2016; 50(2s):S106-S114
Original Article | doi:10.5530/ijper.50.2.25

Colon Targeting Guar Gum Microspheres of 5-Aminosalicylic Acid: Evaluation of Various Process Variables, Characterization and In-Vitro Drug Release


Authors and affiliation (s):

Dinesh Kaushik, Kavita Sharma, Satish Sardana

Department of Pharmaceutics, Hindu College of Pharmacy, Sonepat (Haryana) INDIA.

Abstract:

Background and objectives: 5-Amino salicylic acid (5-ASA), a drug of choice for the treatment of crohn’s disease and ulcerative colitis, rapidly absorbs from the small intestine and there is little localization of 5-ASA in the colon. Thus, we have developed a colon-specific delivery cargo of 5-ASA to release the maximum drug in colon. Methods and Results: 5-ASA loaded guar gum microspheres were prepared by emulsion polymerization technique and optimized for particle size, entrapment efficiency and in-vitro drug release in colonic environment. FTIR, PXRD and DSC were used as the techniques to characterize the drug-polymer interaction. 5-ASA-loaded microspheres offer high entrapment efficiency of 82.39 ± 1.06% with a mean particle size of 150.32 ± 11.8 μm. In-vitro release of optimized formulation indicated 9.32 ± 0.63 % release of drug in SGF (pH 1.2; without pepsin); 13.93 ± 0.90 % in SIF (pH 7.5), 32.11 ± 2.80 % in SCF (pH 7.0; without rat caecal contents) while a significant increase in drug release (94.62 ± 4.50%) was observed in SCF (pH 7.0) medium containing 4% rat caecal content after 6 days of enzyme induction. Conclusion: 5-ASA loaded guar gum microspheres can be used as therapeutic agent for the treatment of ulcerative colitis.

Key words: 5-ASA, 5-aminosalicylic acids, Colon, Guar gum, In vitro drug release.

 

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The Official Journal of Association of Pharmaceutical Teachers of India (APTI)
(Registered under Registration of Societies Act XXI of 1860 No. 122 of 1966-1967, Lucknow)

Indian Journal of Pharmaceutical Education and Research (IJPER) [ISSN-0019-5464] is the official journal of Association of Pharmaceutical Teachers of India (APTI) and is being published since 1967.

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