Exploiting the versatility of oral capsule formulations based on high M-alginate for targeted delivery of poorly water soluble drugs to the upper and lower GI tract

Autor: Allan G.A. Coombes, Loo Yee Teng, Foo Siang Sheng, Diviya Santhanes
Rok vydání: 2018
Předmět:
Zdroj: Journal of Drug Delivery Science and Technology. 46:384-391
ISSN: 1773-2247
DOI: 10.1016/j.jddst.2018.05.024
Popis: Capsules containing indomethacin as a model, poorly water-soluble drug, were produced using the unconventional high-M alginate polymer for site-specific drug delivery in the GI tract. Hydrated Calcium (Ca)-alginate capsules (3 mm diameter), produced by ionotropic gelation permitted almost complete release in simulated gastric fluid (SGF), at 37 °C in 2 h, offering a facile approach for extemporaneous preparation of immediate release formulations. Hydrated Zinc (Zn)-alginate capsules delivered 50% of the drug in SGF but almost zero in simulated intestinal fluid (SIF) over 6 h. Ca-alginate capsules dried at room temperature, hydrated Barium (Ba)-alginate capsules and hydrated Ca-alginate/guar gum capsules released 70% of the drug load in SIF, providing options for improving delivery efficiency in the small intestine. Hydrated Ba-alginate capsules resulted in a significant reduction in indomethacin release compared with Ca-alginate due to the binding affinity of Ba2+ for both M and G blocks in the high-M alginate chain. Ca-alginate capsules dried at 45 °C or freeze dried, restricted release to below 25% on sequential exposure to SGF and SIF and are potentially useful for targeting the diseased colon.
Databáze: OpenAIRE
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