IN VIVO EVALUATION OF BUDESONIDE MICROSPHERES FOR COLON SPECIFIC DRUG DELIVERY
Objective: The aim of the present study was to evaluate the in vivo behaviour of budesonide microspheres for colon targeted delivery.
Methods: In vivo therapeutic effect was evaluated using trinitrobenzene sulfonic acid (TNBS) induced colitis in rats. The therapeutic effect was assessed by determining the damage score, clinical activity score, colon/body weight(C/B) ratio and myeloperoxidase (MPO) activity measurement. The data were compared with standard drug 5-aminosalicylic acid (5-ASA). The targeting efficiency of the formulation was assessed by X-ray studies on the rabbit.
Results: The study showed that oral administration of budesonide microspheres exerted an affirmative impact on the colonic ulcer healing by decreasing the area of ulceration, reducing the mass of colon by improving the symptoms of colitis. MPO activity decreased significantly after oral administration of microspheres. Histopathological studies carried out also confirmed the result. The X-ray studies revealed that the formulations were able to target the colon.
Conclusion: The in vivo study confirmed the ability of budesonide microspheres in targeting the colonic region.
Keywords: Budesonide, Colitis, Targeted delivery, Myeloperoxidase, Ulceration, Clinical activity score
Sarasija S, Hota A. Colon-specific drug delivery system. Indian J Pharm Sci 2000;62:1-8.
Vermula SK, Prabhakar R, Veera R. Different approaches to design and evaluation of a colon-specific drug delivery systems. Int J Pharm Technol 2009;1:1-35.
Solanki R, Madat D, Chauhan K, Parmar L. Recent approaches in the pathogenesis of inflammatory bowel disease. Int J PharmTech Res 2010;2:1796-809.
Taylor KM, Irving PM. Optimization of conventional therapy in patients with IBD. Nat Rev Gastroenterol Hepatol 2011;8:646-56.
Varshosaz J, Emami J, Tavakoli N, Minaiyan M, Rahmani N, Dorkoosh F, et al. Colon-specific delivery of budesonide based on triple coated pellets: In vitro/in vivo evaluation. Acta Pharm 2012;62:341-56.
Baumgart DC. Treatment of inflammatory bowel disease: a review of medical therapy. World J Gastroenterol 2008;21:354-77.
Bodmeier R, Paerathakul O. Spherical agglomerates of water-insoluble drugs. J Pharm Sci 1989;78:964-7.
Dhawan S, Singla AK, Sinha VR. Evaluation of mucoadhesive properties of chitosan microspheres prepared by different methods. AAPS PharmSciTech 2004;5:1-7.
Vasir JK, Tambwekar K, Garg S. Bioadhesive microspheres as a controlled drug delivery system. Int J Pharm 2003;255:13â€32.
Kala D, Nair CRS. Formulation and in vitro evaluation of budesonide microspheres for colon targeting. Int J Pharm Sci Res 2016;7:1000-6.
Morris GP, Beck PL, Herridge MS, Depew WT, Szewczuk MR, Wallace JL. Hapten-induced model of chronic inflammation and ulceration in the rat colon. Gastroenterology 1989;96:795-803.
Paget GE, Barnes JM. Toxicity tests in the evaluation of drug activities pharmacometrics Academic Press: London and New York; 1964, p. 135-66.
Zhou SY, Mei QB, Lilu L, Guo X, Qiu BS, Zhao DH, et al. Delivery of glucocorticoid conjugates in rat gastrointestinal tract and its treatment for ulcerative colitis. Acta Pharmacol Sin 2001;22:761-4.
Hartmann G, Bidlingmaier C, Siegmund B, Albrich S, Schulze J, Tschoep K, et al. Specific type IV phosphodiesterase inhibitor rolipram mitigates experimental colitis in mice. J Pharmacol Exp Ther 2000;292:22-30.
Krawisz JE, Sharon P, Stenson WF. Quantitative assay for acute intestinal inflammation based on myeloperoxidase activity. Gastroenterology 1984;87:1344-50.
Appleyard CB, Wallace JL. Reactivation of hapten-induced colitis and its prevention by anti-inflammatory drugs. Am J Physiol 1995;269:119-25.
Fell JT, Digenis GA. Imaging and behaviour of solid oral dosage form in vivo. Int J Pharm 1984;22:1-15.
Muzib YI, Kadiyam R. Colon-specific drug delivery of tramadol hydrochloride for chronotherapeutics of arthritis. Int J Pharm 2015;1:43-9.
Nakamura K, Maitani Y, Lowman AM, Takayama K, Peppas NA, Nagai T. Uptake and release of budesonide from mucoadhesive, pH-sensitive copolymers and their application to nasal delivery. J Contolled Release 1999;61:329-35.
Gouda M, Shabaraya R, Shantakumar SM, Shyale S, Kumar PR. Development and validation of selective UV spectrophotometric analytical method for budesonide pure sample. J Appl Pharm Sci 2011;1:158-61.
Patriarca P, Cramer R, Marussi M, Ross F, Romeo D. Mode of activation of granule-bound NADPH oxidase in leukocytes during phagocytosis. Biochem Biophys Acta 1971;237:335-8.
Dasankoppa FS, Patwa S, Sholapur H, Arunkumar GR. Formulation and characterization of colon specific drug delivery system of Prednisolone. Saudi J Health Sci 2012;1:143-50.