A comparison of aerosolization and homogenization techniques for production of alginate microparticles for delivery of corticosteroids to the colon

Samak, Yassmin O., El Massik, Magda and Coombes, Allan G. A. (2017) A comparison of aerosolization and homogenization techniques for production of alginate microparticles for delivery of corticosteroids to the colon. Journal of Pharmaceutical Sciences, 106 1: 208-216. doi:10.1016/j.xphs.2016.08.015


Author Samak, Yassmin O.
El Massik, Magda
Coombes, Allan G. A.
Title A comparison of aerosolization and homogenization techniques for production of alginate microparticles for delivery of corticosteroids to the colon
Journal name Journal of Pharmaceutical Sciences   Check publisher's open access policy
ISSN 1520-6017
0022-3549
Publication date 2017-01-01
Year available 2016
Sub-type Article (original research)
DOI 10.1016/j.xphs.2016.08.015
Open Access Status Not yet assessed
Volume 106
Issue 1
Start page 208
End page 216
Total pages 9
Place of publication New York, NY, United States
Publisher Elsevier
Language eng
Subject 2700 Medicine
3003 Pharmaceutical Science
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 CaCl 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 CaCl, 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.
Formatted 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.
Keyword Aerosolization
Alginate microparticles
Colonic drug delivery
Homogenization
Hydrocortisone hemisuccinate
Inflammatory bowel disease
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: HERDC Pre-Audit
School of Pharmacy Publications
 
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