Abstract
Core-shell beads loaded with betamethasone were developed using co-axial prilling as production technique and pectin plus alginate as polymeric carriers. During this study, many operative conditions were intensively investigated to find the best ones necessary to produce uniform core-shell particle systems in a reproducible way. Particularly, feed solutions’ composition, polymers mass ratios and the effect of the main process parameters on particles production, micromeritics, inner structure, drug loading and drug-release/swelling profiles in simulated biological fluids were studied. The optimized core-shell formulation F5 produced with a pectin core concentration of 4.0% w/v and an alginate shell concentration of 2.0% w/v (2:1 core:shell ratio) acted as a sustained drug delivery system. It was able to reduce the early release of the drug in the upper part of the gastro-intestinal tract for the presence of the zinc-alginate gastro-resistant outer layer and to specifically deliver it in the colon, thanks to the selectivity of amidated low methoxy pectin core for this district. Therefore, these particles may be proposed as colon targeted drug delivery systems useful for inflammatory bowel disease (IBD) therapy.
Highlights
Inflammatory bowel disease (IBD) includes almost two disorders: ulcerative colitis and Crohn’s disease [1,2]
Core-shell beads consisting of zinc pectinate and betamethasone (B) in the core and zinc alginate in the shell were manufactured by prilling technology in co-axial configuration
The polymeric jet is broken-up by radiofrequency into uniform core-shell droplets that drip into a Zn2+ gelling solution and “solidify”
Summary
Inflammatory bowel disease (IBD) includes almost two disorders: ulcerative colitis and Crohn’s disease [1,2]. Several innovative drug delivery systems have been developed to achieve a selective drug delivery to the inflamed tissues [6,7,8,9] With this aim, several approaches can be followed, i.e., the use of prodrugs becoming active after the hydrolysis by specific colon enzymes [10], bioadhesive delivery systems [11], timed-dependent delivery systems [12] and drug coating with pH dependent polymers [13,14]. The use of pH-sensitive polymers protects the drug from the early release in the acidic pH of the stomach and small intestine, increasing the amount of active compound in the colon region
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