A Comparison of Aerosolization and Homogenization Techniques for Production of Alginate Microparticles for Delivery of Corticosteroids to the Colon.
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 CaCl2crosslinking 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.
Department of Pharmaceutics, Pharmacy Australia Centre of Excellence, University of Queensland, Brisbane, Queensland 4102, Australia. Electronic address: y.samak@uq.edu.au.
Yassmin O
YO
Samak
Department of Pharmaceutics, Faculty of Pharmacy and Drug Manufacturing, Pharos University, Alexandria, Egypt.
Magda
M
El Massik
Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Thailand.
Allan G A
AGA
Coombes
D000305:Adrenal Cortex Hormones / Q000008:administration & dosage* / Q000737:chemistry; D000336:Aerosols / Q000737:chemistry*; D000464:Alginates / Q000737:chemistry*; D002122:Calcium Chloride / Q000737:chemistry; D003106:Colon / Q000378:metabolism; D003432:Cross-Linking Reagents / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D065546:Drug Liberation; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D006801:Humans; D015212:Inflammatory Bowel Diseases / Q000188:drug therapy; D010316:Particle Size
D000305:Adrenal Cortex Hormones; D000336:Aerosols; D000464:Alginates; D003432:Cross-Linking Reagents; D004337:Drug Carriers; D006603:Hexuronic Acids; D020723:Glucuronic Acid; D002122:Calcium Chloride
Hydrocortisone hemisuccinate; aerosolization; alginate microparticles; colonic drug delivery; homogenization; inflammatory bowel disease