TY - JOUR

T1 - Hyaluronan/B12-chitosan polyelectrolyte complex for oral colistin administration

AU - Dubashynskaya, N.V.

AU - Bokatyi, A.N.

AU - Sall, T.S.

AU - Egorova, T.S.

AU - Demyanova, E.V.

AU - Dubrovskii, Y.A.

AU - Murashko, E.A.

AU - Anufrikov, Y.A.

AU - Shasherina, A.Y.

AU - Vlasova, E.N.

AU - Skorik, Y.A.

N1 - Export Date: 04 March 2024; Cited By: 0; CODEN: IJBMD

PY - 2024/4/1

Y1 - 2024/4/1

N2 - Polyelectrolyte complexes (PECs) based on polysaccharides, including hyaluronic acid (HA) and chitosan (CS), are promising delivery systems for antimicrobial agents, including oral administration of the peptide antibiotic colistin (CT). Modification of CS with different targeting ligands to improve intestinal permeability is a suitable way to improve the oral bioavailability of polyelectrolyte particles. This study describes the procedure for obtaining CT-containing PECs based on HA and CS modified with cyanocobalamin (vitamin B12). In this case, vitamin B12 is used as a targeting ligand because it is absorbed in the ileum via specific transporter proteins. The resulting PECs had a hydrodynamic size of about 284 nm and a positive ζ-potential of about 26 mV; the encapsulation efficiency was 88.2 % and the CT content was 42.2 μg/mg. The developed systems provided a two-phase drug release: about 50 % of the CT was released in 0.5–1 h, and about 60 % of the antibiotic was cumulatively released in 5 h. The antimicrobial activity of encapsulated CT was maintained at the same level as the pure drug for at least 24 h (minimum inhibitory concentration against Pseudomonas aeruginosa was 2 μg/mL for both). In addition, the apparent permeability coefficient of CT in the PEC formulation was 2.4 × 10−6 cm/s. Thus, the incorporation of CT into HA- and vitamin B12-modified CS-based PECs can be considered as a simple and convenient method to improve the oral delivery of CT. © 2024

AB - Polyelectrolyte complexes (PECs) based on polysaccharides, including hyaluronic acid (HA) and chitosan (CS), are promising delivery systems for antimicrobial agents, including oral administration of the peptide antibiotic colistin (CT). Modification of CS with different targeting ligands to improve intestinal permeability is a suitable way to improve the oral bioavailability of polyelectrolyte particles. This study describes the procedure for obtaining CT-containing PECs based on HA and CS modified with cyanocobalamin (vitamin B12). In this case, vitamin B12 is used as a targeting ligand because it is absorbed in the ileum via specific transporter proteins. The resulting PECs had a hydrodynamic size of about 284 nm and a positive ζ-potential of about 26 mV; the encapsulation efficiency was 88.2 % and the CT content was 42.2 μg/mg. The developed systems provided a two-phase drug release: about 50 % of the CT was released in 0.5–1 h, and about 60 % of the antibiotic was cumulatively released in 5 h. The antimicrobial activity of encapsulated CT was maintained at the same level as the pure drug for at least 24 h (minimum inhibitory concentration against Pseudomonas aeruginosa was 2 μg/mL for both). In addition, the apparent permeability coefficient of CT in the PEC formulation was 2.4 × 10−6 cm/s. Thus, the incorporation of CT into HA- and vitamin B12-modified CS-based PECs can be considered as a simple and convenient method to improve the oral delivery of CT. © 2024

UR - https://www.mendeley.com/catalogue/bdd53741-f061-304f-8214-0382f904480f/

U2 - 10.1016/j.ijbiomac.2024.130177

DO - 10.1016/j.ijbiomac.2024.130177

M3 - статья

VL - 263

JO - International Journal of Biological Macromolecules

JF - International Journal of Biological Macromolecules

SN - 0141-8130

M1 - 130177

ER -