Bio Micro-Nano Technologies of Antioxidants Optimised Their Pharmacological and Cellular Effects, ex vivo, in Pancreatic β-Cells

Abstract

Introduction

Recent formulation and microencapsulation studies of probucol (PB) using the polymer sodium alginate (SA) and bile acids have shown promising results but PB stability, and pharmacology profiles remain suboptimal. This study aimed to investigate novel polymers for the nano and micro encapsulation of PB, with the anti-inflammatory bile acid ursodeoxycholic acid (UDCA).

Material and methods

Six formulations using three types of polymers were investigated with and without UDCA. The polymers were NM30D, RL30D, and RS30D and they were mixed with SA and PB at set ratios and microencapsulated using oscillating-voltage-mediated nozzle technology coupled with ionic gelation. The microcapsules were examined for physical and biological effects using pancreatic β-cells.

Results and discussion

UDCA addition did not adversely affect the morphology and physical features of the microcapsules. Despite thermal stability remaining unchanged, bile acid incorporation did enhance the electrokinetic stability of the formulation system for NM30D and RL30D polymers. Mechanical stability remained similar in all groups. Enhanced uptake of PB from the microcapsule by pancreatic β-cells was only seen with NM30D-UDCA-intercalated microcapsules and this effect was sustained at both glucose levels of 5.5 and 35.5 mM.

Conclusion

UDCA addition enhanced PB delivery and biological effects in a formulation-dependent manner.

Keywords:

• probucol
• microencapsulation
• NM30D
• ursodeoxycholic acid
• diabetes
• oxidative stress

Acknowledgments

The authors acknowledge the use of laboratory equipment, and the scientific and technical assistance of the Microscopy and Microanalysis Facility at Curtin University, which has been partially funded by the University, State and Commonwealth Governments. Al-Salami’s work is partially supported by the European Union’s Horizon 2020 research and innovation programme under the Marie Skłodowska-Curie grant agreement No 872370. The NIT-1 cells were a generous donation from Professor Grant Morahan at the University of Western Australia and were approved by Curtin.

Author Contributions

All authors contributed towards data analysis, drafting and critically revising the paper, gave final approval of the version to be published, and agreed to be accountable for all aspects of the work.

Disclosure

H Al-Salami has been, and is currently receiving, funding from Beijing Nat-Med Biotechnology Co., Ltd., and reports grants from EU Horizon 2020, outside the submitted work. The authors report no other conflicts of interest in this work.