Surface Layer Modification of Poly(d,l-lactic- co-glycolic acid) Nanoparticles with TargetingPeptide: A Convenient Synthetic Route for Pluronic F127-Tuftsin Conjugate

Horváti, Kata and Gyulai, Gergő and Csámpai, Antal and Rohonczy, János and Kiss, Éva and Bősze, Szilvia (2018) Surface Layer Modification of Poly(d,l-lactic- co-glycolic acid) Nanoparticles with TargetingPeptide: A Convenient Synthetic Route for Pluronic F127-Tuftsin Conjugate. Bioconjugate Chemistry, 29 (5). pp. 1495-1499. ISSN 1043-1802 (print), 1520-4812 (online)

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Abstract

Nanoparticles consisting of biodegradable poly(d,l-lactic- co-glycolic acid) (PLGA) are promising carriers for drug molecules to improve the treatment of tuberculosis. Surface modifiers, such as Pluronic F127, are essential for biocompatibility and for the protection against particle aggregation. This study demonstrates a successful approach to conjugate Pluronic F127 coated PLGA nanoparticles with Tuftsin, which has been reported as a macrophage-targeting peptide. Transformation of Pluronic F127 hydroxyl groups-which have limited reactivity-into aldehyde groups provide a convenient way to bind aminooxy-peptide derivatives in a one-step reaction. We have also investigated that this change has no effect on the physicochemical properties of the nanoparticles. Our data showed that coating nanoparticles with Pluronic-Tuftsin conjugate markedly increased the internalization rate and the intracellular activity of the encapsulated drug candidate against Mycobacterium tuberculosis. By employing this approach, a large variety of peptide targeted PLGA nanoparticles can be designed for drug delivery.

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