Formulation Buoyancy of Nanoencapsulated Gliclazide Using primary, Conjugated and Deconjugated Bile Acids

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.

Graphical abstract

Keywords:

• buoyancy
• cell viability
• drug tissue permeation
• excipient stabilizing
• gliclazide
• muscle cells

Author contributions

S Mathavan concept and designed the project, analysed and interpreted research data, drafted significant parts of the work or critically revised it, which contributed to the interpretation, significant contribution to data interpretation and presentation resulting in significant improvement of quality. CM Ionescu performed analysis and interpretation of research data, drafted significant parts of the work or critically revised it, which contributed to the interpretation, significant contribution to data interpretation and presentation resulting in significant improvement of quality. B Kovacevic performed analysis and interpretation of research data, drafted significant parts of the work or critically revised it, which contributes to the interpretation. M Mikov concept and designed the project, drafted significant parts of the work or critically revised it, which contributed to the interpretation. S Golocorbin-Kon concept and designed the project, drafted significant parts of the work or critically revised it, which contributed to the interpretation. A Mooranian performed analysis and interpretation of research data, drafted significant parts of the work or critically revised it, which contributed to the interpretation. CR Dass performed analysis and interpretation of research data, drafted significant parts of the work or critically revised it, which contributed to the interpretation. H Al-Salami concept and designed the project, analysis and interpretated research data, drafted significant parts of the work or critically revised it, which contributed to the interpretation, significantly contributed to data interpretation and presentation resulting in significant improvement of quality.

Acknowledgments

The authors acknowledge the use of equipment, scientific and technical assistance of the Curtin University Electron Microscope Facility, which has been partially funded by the University, State and Commonwealth Governments. H Al-Salami is partially supported by the European Union's Horizon 2020 research and innovation program under the Marie Skłodowska-Curie grant agreement no. 690876.

Financial & competing interests disclosure

H Al-Salami has been and is currently receiving funding from Beijing Nat-Med Biotechnology Co., Ltd. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.