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Original Articles

Two-level delivery systems based on CaCO3 cores for oral administration of therapeutic peptides

, , , , , , & show all
Pages 619-634 | Received 31 Jul 2018, Accepted 12 Dec 2018, Published online: 31 Jan 2019
 

Abstract

Two-level systems for oral delivery of therapeutic peptides were developed; the carriers consist of CaCO3 cores included into alginate granules. Such systems were first used for the delivery of low molecular weight drugs. It was shown that efficiency of encapsulation of peptides depends on their pI value, hydrophobicity, characteristics of the compounds used for doping CaCO3 cores, their surface potential and the techniques employed for loading peptides into the first-level carriers. Doping CaCO3 cores with dextran sulphate save their viability compared to the pristine CaCO3 cores, but ensures delivery of the desired quantity of peptide when using a smaller amount of delivery systems. Introducing the inhibitor of peptidases leads to an increase in the concentration of peptide in rat blood after intragastric administration of the developed delivery systems. Scanning electron microscopy and energy-dispersive X-ray spectroscopy demonstrated the presence of fragments of destructed first-level carriers in blood and plasma of experimental animals.

Acknowledgements

We gratefully acknowledge Dr. Vadim Baigildin for determination of ξ potential of doped and pristine CaCO3 cores.

Disclosure statement

The authors report no declarations of interest.

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