Budesonide-Loaded Eudragit S 100 Nanocapsules for the Treatment of Acetic Acid-Induced Colitis in Animal Model
Nanoparticles for colon-drug delivery were designed and evaluated to solve many discrepancy issues as insufficient drug amount at diseased regions, high adverse effects of released drugs, and unintentionally premature drug release to noninflamed gastrointestinal regions. Herein, the prepared budesonide-loaded Eudragit S 100/Capryol 90 nanocapsules for the treatment of inflammatory bowel disease. Nanocapsules were prepared efficiently by nanoprecipitation technique and composed mainly of the pH-sensitive Eudragit S 100 polymeric coat with a semisynthetic Capryol 90 oily core. Full 31 × 21 factorial design was applied to obtain optimized nanocapsules. Optimal nanocapsules showed mean particle size of 171 nm with lower polydispersity index indicating the production of monodispersed system and negative zeta-potential of − 37.6 mV. Optimized nanocapsules showed high encapsulation efficiency of 83.4% with lower initial rapid release of 10% for first 2 h and higher rapid cumulative release of 72% after 6 h. The therapeutic activity of the prepared budesonide-loaded nanocapsules was evaluated using a rat colitis model. Disease activity score, macroscopical examination, blood glucose level, and histopathological assessment showed marked improvements over that free drug suspension. Obtained results demonstrate that the budesonide-loaded Eudragit S 100 nanocapsules are an effective colon-targeting nanosystem for the treatment of inflammatory bowel disease. Capryol 90 was found to be a successful, and even preferred, alternative to benzyl benzoate, which is commonly employed as the oil core of such nanocapsules.
KEY WORDSBudesonide Nanocapsules Inflammatory bowel disease Capryol 90 Acetic-acid induced colitis Eudragit S 100
Authors thank MUP (Egypt), Gattefosé (France), Cremer Oleo division (Germany), and Evonik (Germany) for generously providing gift samples. We would to greatly thank DR. Mina Ezzat for his help in the part of histopathological examination.
Compliance with Ethical Standards
Conflict of Interest
The authors declare that they have no conflict of interest.
- 1.Rathbone MJ. In: Rathbone MJ, editor. Controlled release in Oral drug delivery, vol. 2011. New York: Springer; 2013. p. 415.Google Scholar
- 7.Walker BR, Colledge NR. Davidson's principles and practice of medicine e-book: With STUDENT CONSULT Online Access, 22th edition. Elsevier Health Sciences; 2013 Dec 6.Google Scholar
- 8.Wiener C, Fauci AS, Braunwald E, Kasper DL, Hauser SL, Longo DL, Jameson JL, Loscalzo J. Harrison's principles of internal medicine, selfassessment and board review. McGraw Hill Professional; 2008 Jul 20.Google Scholar
- 12.Sweetman SC. Martindale: the complete drug reference, 36th edition. London: Pharmaceutical press; 2009 Jun 29.Google Scholar
- 13.Ulbrich W, Lamprecht A. Targeted drug-delivery approaches by nanoparticulate carriers in the therapy of inflammatory diseases. J R Soc Interface. 2009 Nov 25;7(suppl_1):S55-66.Google Scholar
- 18.Ahmed N, Mora-Huertas C, Jaafar-Maalej C, Fessi H, Elaissari A. Polymeric drug delivery systems for encapsulating hydrophobic drugs. Drug delivery strategies for poorly water-soluble drugs. West Sussex: Wiley; 2012. p. 151–97.Google Scholar
- 31.Santos SS, Lorenzoni A, Ferreira LM, Mattiazzi J, Adams AI, Denardi LB, et al. Clotrimazole-loaded Eudragit® RS100 nanocapsules: preparation, characterization and in vitro evaluation of antifungal activity against Candida species. J Mater Sci. 2013;33(3):1389–94.Google Scholar
- 48.Dumanli I. Mechanistic studies to elucidate the role of lipid vehicles on solubility, formulation and bioavailability of poorly soluble compounds. [PhD]. USA: University of Rhode Island; 2002.Google Scholar