Pyrazinoic acid-Poly(malic acid) biodegradable nanoconjugate for efficient intracellular delivery - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue Precision Nanomedicine Année : 2019

Pyrazinoic acid-Poly(malic acid) biodegradable nanoconjugate for efficient intracellular delivery

Pyrazinoic acid-Poly(malic acid) biodegradable nanoconjugate for efficient intracellular delivery

Résumé

Tuberculosis is an infectious disease affecting mostly lungs, that is still considered a health global problem as it causes millions of deaths worldwide. Current treatment is effective but associated with severe adverse effects due to the high doses of each anti-tuberculosis drug daily administrated by oral therapy. For the first time, a pyrazinoic acid (PA) biodegradable nanoconjugate was synthesized and developed for pulmonary administration in an attempt to reduce the administered doses by achieving a high drug payload and controlled release at the target site. The conjugate was synthesized by coupling pyrazinoic acid on carboxylic groups of poly(malic acid), which is a biodegradable and biocompatible polymer, and posteriorly self-assembled into nanoconjugates. Characterization confirmed the formation of nanometric, spherical and negatively charged pyrazinoic acid nanoconjugate (NC-PA). NC-PA was stable for 60 days at 4 and 37°C and able to deliver PA in a sustained release manner over time. On macrophages, they exhibited no cell toxicity for a wide range of concentrations (from 1 to 100 µg/mL), demonstrating the safety of NC-PA. In addition, the nanoconjugate was efficiently taken up by RAW 264.7 cells over 6 hours reaching a maximum value after 3 hours of incubation. In conclusion, innovative nanoconjugates are a promising alternative to deliver drugs directly to the lungs and contributing to improving tuberculosis therapy.

Domaines

Biomatériaux
Fichier principal
Vignette du fichier
Article PRNanorevisedV2.pdf (600.9 Ko) Télécharger le fichier
Origine : Fichiers produits par l'(les) auteur(s)
Loading...

Dates et versions

hal-02331736 , version 1 (24-10-2019)

Identifiants

Citer

Simone Pinto Carneiro, Laurence Moine, Barbara Tessier, Valérie Nicolas, Orlando David Henrique dos Santos, et al.. Pyrazinoic acid-Poly(malic acid) biodegradable nanoconjugate for efficient intracellular delivery. Precision Nanomedicine, 2019, 2 (3), pp.303-317. ⟨10.33218/prnano2(3).190523.1⟩. ⟨hal-02331736⟩
26 Consultations
76 Téléchargements

Altmetric

Partager

Gmail Facebook X LinkedIn More