A Comparison of Aerosolization and Homogenization Techniques for Production of Alginate Microparticles for Delivery of Corticosteroids to the Colon |
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Authors: | Yassmin O Samak Magda El Massik Allan GA Coombes |
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Institution: | 1. Department of Pharmaceutics, Pharmacy Australia Centre of Excellence, University of Queensland, Brisbane, Queensland 4102, Australia;2. Department of Pharmaceutics, Faculty of Pharmacy and Drug Manufacturing, Pharos University, Alexandria, Egypt;3. Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Thailand |
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Abstract: | Alginate microparticles incorporating hydrocortisone hemisuccinate were produced by aerosolization and homogenization methods to investigate their potential for colonic drug delivery. Microparticle stabilization was achieved by CaCl2 crosslinking solution (0.5 M and 1 M), and drug loading was accomplished by diffusion into blank microparticles or by direct encapsulation. Homogenization method produced smaller microparticles (45-50 μm), compared to aerosolization (65-90 μm). High drug loadings (40% wt/wt) were obtained for diffusion-loaded aerosolized microparticles. Aerosolized microparticles suppressed drug release in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) prior to drug release in simulated colonic fluid (SCF) to a higher extent than homogenized microparticles. Microparticles prepared using aerosolization or homogenization (1 M CaCl2, diffusion loaded) released 5% and 17% of drug content after 2 h in SGF and 4 h in SIF, respectively, and 75% after 12 h in SCF. Thus, aerosolization and homogenization techniques show potential for producing alginate microparticles for colonic drug delivery in the treatment of inflammatory bowel disease. |
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Keywords: | alginate microparticles aerosolization homogenization colonic drug delivery Hydrocortisone hemisuccinate inflammatory bowel disease |
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