MULTIPARTICULATE DRUG DELIVERY SYSTEM FOR COLON TARGETING
Keywords:
5-Aminosalicylic acid, Colon targeting, Microspheres, PectinAbstract
Objective: The objective of the present investigation was to design a multi particulate delivery system for site-specific delivery of 5-aminosalicylic acid (ASA) using natural polysaccharides (pectin) and pH-sensitive polymer (Eudragit S100) for the treatment of ulcerative colitis. This system is anticipated to protect the drug loss in the upper GI tract, which results from the inherent property of Eudragit S100 (ES), and deliver ASA in the colon only.
Methods: The use of enteric polymers (ES) as the protective coating on the microspheres makes them able to release the drug at the particular pH of colonic fluid. A combined mechanism of release is used, which combines specific biodegradability of polymer and pH-dependent drug release from the coated microspheres. The effects of polymer concentration, stirring rate, and concentration of emulsifier on particle size and drug loading were studied. Pectin microspheres were prepared by emulsion dehydration method using different ratios of drug and polymer (1:2 to 1:4), stirring speeds (1000-3000 rpm) and emulsifier concentrations (1%-3% wt/vol). Eudragit -coating of pectin microspheres was prepared by oil-in-oil solvent evaporation method. Both the pectin microspheres and Eudragit-coated pectin microspheres were evaluated for surface morphology, particle size and size distribution, percentage drug entrapment, swell ability and In vitro drug release in pH progression media.
Result: The release profile of 5-ASA from Eudragit-coated pectin microspheres was pH dependent. Hence, the drug released quickly at pH 7.5 but the release rate was much slower in acidic medium.
Conclusion: The designed drug delivery system can be used as a tool for colon targeting of drugs.
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References
Rubinstein I. Effect of mouthpiece, nose clips, and head position on airway area measured y acoustic reflections. J Appl Physiol 1987;63(4):1469-74.
Ashford M. Studies on pectin formulations for colonic drug delivery. J Controlled Release 1994;30:225-32.
Riley SA, Turn berg LA. Sulphasalazine and amino Salicylate in the treatment of inflammatory bowel disease. Q J Med 1990;75:561-2.
Bartalsky A. Salicylazobenzoic acid in ulcerative colitis. Lancet 1982;319:960-4.
Ashford M, Fell J, Attwood D, Sharma H, Wood head P. In vitro investigation into the suitability of pH dependent polymer for colonic targeting. Int J Pharm 1993;95:193-9.
Marvola M, Nykanen P, Rautio S, Isonen N, Austere AM. Enteric polymer as binder and coating material in multiple unit site-specific drug delivery systems. Eur J Pharm Sci 1999;7:259-67.
Gazzaniga A, Busetti C, Sangali ME, Giordano ME. Time-dependent oral delivery system for colonic targeting system for the colon targeting. STP Pharm Sci 1995;5:83-8.
Gazzaniga A, Lamartine P, Maffione G, Sangal ME. Oral delayed release System for colonic specific delivery. Int J Pharm 1994;108:77-83.
Hovgaard L, Brondsted H. Dextran hydro gels for colon-specific drug delivery. J Control Release 1995;36:159-66.
Watts PJ, Lllum L. Colonic drug delivery. Drug Dev Ind Pharm 1997;23:893-913.
Ashford M, Fell T. Targeting drugs to colon: delivery system for oral administration. J Drug Target 1994;2:241-58.
Kudela V. Hydro gels. In: Mark HF, Bikales N, Overberg CG, Menges G, Kroschwitz JI, eds. Encyclopedia of Polymer Science and Engineering. vol. 7. New York NY: John Wiley & Sons; 1987. p. 703-807.
Tiwari SB, Murthy TK, Pai MR, Mehta PR, Chowdary PB. Controlled release formulation of Tramadol hydrochloride using hydrophilic and hydrophobic matrix system. AAPS Pharm Sci Tech 2003;4:E31.
Graham NB, McNeill ME. Hydro gels for controlled drug delivery. Biomaterials 1984;5:27-36.
Tiwari SB, Murthy TK, Pai MR, Mehta PR, Chowdary PB. Controlled release formulation of Tramadol hydrochloride using hydrophilic and hydrophobic matrix system. AAPS Pharm Sci Tech 2003;4:E31-E37.
Krusteva S, Lambov N, Velinov G. Pharmaceutical investigation of a bio erodible nystatin system. Pharm 1990;45:195-7.