Formulation buoyancy of nanoencapsulated gliclazide using primary, conjugated and deconjugated bile acids

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.