Targeted delivery of rifampicin to tuberculosis-infected macrophages: design, in-vitro, and in-vivo performance of rifampicin-loaded poly(ester amide)s nanocarriers

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• 作者：Rajendran Amarnath Praphakar^a ; ^{amarnathyuvi@gmail.com" class="auth_mail" title="E-mail the corresponding author} ; Murugan A. Munusamy^b ; Kishor Kumar Sadasivuni^c ; Mariappan Rajan^a ; ^{rajanm153@gmail.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Alveolar macrophages ; Mycobacterium smegmatis ; Nanoparticles ; Polyesteramides ; Rifampicin ; Tuberculosis
• 刊名：International Journal of Pharmaceutics
• 出版年：2016
• 出版时间：20 November 2016
• 年：2016
• 卷：513
• 期：1-2
• 页码：628-635
• 全文大小：2446 K

文摘

We have developed a nano drug delivery system for the treatment of tuberculosis (TB) using rifampicin (RF) encapsulated in poly(ester amide)s nanoparticles (PEA-RF-NPs), which are biocompatible polymers. In this study, biodegradable amino acid based poly(ester amide)s (PEAs) were synthesized by the poly condensation reaction and RF-loaded NPs were fabricated by the dialysis method. The surface morphology and in-vitro drug release efficiency were examined. The effect of time and temperature on the cellular uptake of PEA-RF-NPs in NR8383 cells was evaluated. Fluorescence microscopic results of PEA-RF-NPs from NR8383 cell lines suggest its potential application in treating TB. The antibacterial activity of RF against Mycobacterium smegmatis was also evaluated. Based on these results, this approach provides a new means for controlled and efficient release of RF using the PEA-NPs delivery system and is promising for the treatment of TB.