DEVELOPMENT OF COLON-SPECIFIC MULTI PARTICULATE DRUG DELIVERY SYSTEM OF FENOVERINE
Keywords:Fenoverine, Multiparticulate system, Colon specific system, Eudragit S 100
Objective: The main objective of this study was to formulate and evaluate colon-specific multi- particulate drug delivery system of fenoverine, using Eudragit S 100 as enteric coating polymer.
Methods: Microparticles were prepared by oil/water emulsion solvent evaporation technique and characterized for micromeritic properties, encapsulation efficiency, percentage yield and particle size. Various analytical techniques such as FTIR, DSC, PXRD, and SEM were used to characterize microparticles. In vitro release studies were performed in 900 ml of enzyme free SGF (pH 1.2) for 2 h followed by enzyme free SIF (pH 7.4) containing 2% Tween 80 till the end of test using USP paddle apparatus. Drug release data was subjected to release kinetic studies and effect of stirring rate on particle size and percent entrapment of microparticles was also studied.
Results: In vitro release studies showed that microparticles were able to release the drug in a controlled manner with zero order rate kinetics; â€˜n' values obtained from the Korsmeyer Peppas model showed that the release mechanism was non-fickian type. SEM studies revealed that microparticles were smooth and spherical in shape. The DSC and PXRD studies of drug loaded microparticles showed amorphous state of the drug in the microparticles. Mean particle size was reduced with increase in stirring rate but percent drug entrapment of was found to be high 72.12 Â± 1.63.
Conclusion: Colon specific microparticles prevent premature drug release in simulated upper GIT and maximize the drug release in simulated intestinal environment at controlled rate over a period of 24h.
Chourasia MK, Jain SK. Pharmaceutical approaches to colon targeted drug delivery systems. J Pharm Pharma Sci 2003;6(1):33-66.
Meissner Y, Lamprecht A. Alternative drug delivery approaches for the therapy of inflammatory bowel disease. J Pharm Sci 2008;97:2878-91.
Haupt S, Rubinstein A. The colon as a possible target for orally administered peptides and proteins. J Crit Rev Ther Drug Carrier Sys 2002;19:499-542.
Bondesen S. Intestinal fate of 5-aminosalicylic acid:regional and systemic kinetic studies in relation to inflammatory bowel disease. J Pharmacol Toxic 1997;81 (2):1-28.
Lamprecht A, Hiromitsu Y, Hirofumi T, Yoshiaki K. Design of pH sensitive microparticles for the colonic delivery of the immunosuppressive drug tacrolimus. Eur J Pharm Biopharm 2004;58:37-43.
Sahoo SK, Mallick AA, Barik BB, Senapati PC. Formulation and in vitro evaluation of eudragit microparticles of stavudine. Trop J Pharm Res 2005;4(1):369-75.
Bandari S, Eaga CM, Madhisudan Rao Y. Formulation and evaluation of multiple tablets as a biphasic gastroretentive floating drug delivery system for fenoverine. J Acta Pharm 2010;60:89-97.
Sonali NR, Amrita BN. Development and evaluation of once a day oral controlled multiparticulate drug delivery systems of cefixime trihydrate. Indian J Pharm Edu Res 2008;42(3):283-93.
Alex R, Bodmeier R. Encapsulation of water-soluble drugs by a modified solvent evaporation method, effect of process and formulation variables on drug entrapment. J Microencapsul 1990;7(3):347-55.
Behera BC, Sahoo SK, Dhal S, Barik BB, Gupta BK. Characterization of glipizide-loaded polymethacrylate microparticles prepared by an emulsion solvent evaporation method. Trop J Pharm Res 2008;7(1):879-85.
Basu SK, Adhiyaman R. Preparation and characterization of nitrendipine loaded eudragit RL 100 microparticles prepared by an emulsion-solvent evaporation method. Trop J Pharm Res 2008;7(3):1033-41.
Bhagwat DA, Bhutkar MA,Todkar SS, Mohite SK, Gattani YS. Formulation and evaluation of controlled release microparticles of isosorbided initrate. Int J Pharm Tech Res 2009;1(2):125-8.
Gattani YS, Kawtikwar PS, Sakarkar DM. Formulation and evaluation of gastro retentive multiparticulate drug delivery system of aceclofenac. Int J Chem Tech Res 2009;1(1):1-10.
Devrim B, Canefe K. Preparation and evaluation of modified release ibuprofen microparticles with acrylic polymers (eudragit) by quasi emulsion solvent diffusion method:effect of variables. J Acta Poloniae Pharm Drug Res 2006;63(6):521-34.
Carrette O, Favier C, Mizon C, Neut C, Cortot A, Colombel JF, et al. Bacterial enzymes used for colon-specific drug delivery are decreased in active Crohnâ€™s diseases. J Dig Dis Sci 1995;40 (12):2641-6.
Deepthi J, Amulya KP, Dipak KM. Eudragit S 100 entrapped insulin microparticles for oral delivery. J AAPS Pharm Sci Tech 2005;6(1):Article 16.
Haznedar S, DortunÃ§ B. Preparation and in vitro evaluation of eudragit microparticles containing acetazolamide. J Pharm Tech Res 2003;7(1):79-85.