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Published on: August 15, 2016
Formulation buoyancy of nanoencapsulated gliclazide using primary, conjugated and deconjugated bile acids
Sangeetha Mathavan1, Corina M Ionescu2, Bozica Kovacevic1
1Biotechnology & Drug Development Research Laboratory, School of Pharmacy & Biomedical Science, Curtin Health Innovation Research Institute, Curtin University, Kent Street, Bentley 6102, Perth, WA, Australia.
Abstract:
Aim: Recent studies suggest potential applications of endogenously produced human bile acids as formulation-excipient and drug tissue permeation enhancers in Type 1 diabetes. We aimed to examine the stability, tissue permeation and ex vivo muscle-cell effects of microencapsulated gliclazide (G) incorporated with a primary (chenodeoxycholic acid [CDCA]), a secondary (ursodeoxycholic acid [UDCA]) or a tertiary (taurocholic acid [TCA]) bile acid. Materials & methods: Four formulations made of sodium alginate, CDCA, UDCA and TCA were examined for buoyancy, tissue-enhancing effects (in vivo) and local (ex vivo) viability effects. Results & conclusion: CDCA, UDCA and TCA improved buoyancy and cell viability but not tissue-specific uptake. G-TCA-sodium alginate microcapsules exerted hypoglycemic effects, suggesting significant improvement of G gut-uptake by TCA, possibly via improving buoyancy.
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