Targeted delivery of rifampicin to tuberculosis-infected macrophages: design, in-vitro, and in-vivo performance of rifampicin-loaded poly(ester amide)s nanocarriers.
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.
Biomaterials in Medicinal Chemistry Laboratory, Department of Natural Products Chemistry, School of Chemistry, Madurai Kamaraj University, Madurai-21, Tamil Nadu, India. Electronic address: amarnathyuvi@gmail.com.
Rajendran
R
Amarnath Praphakar
Department of Botany and Microbiology, College of Science, King Saud University, Riyadh, Saudi Arabia.
Murugan A
MA
Munusamy
Department of Mechanical & Industrial Engineering, College of Engineering, Qatar University, PO Box 2713, Doha, Qatar.
Kishor Kumar
KK
Sadasivuni
Biomaterials in Medicinal Chemistry Laboratory, Department of Natural Products Chemistry, School of Chemistry, Madurai Kamaraj University, Madurai-21, Tamil Nadu, India. Electronic address: rajanm153@gmail.com.
Mariappan
M
Rajan
D000577:Amides / Q000008:administration & dosage / Q000737:chemistry; D000818:Animals; D000904:Antibiotics, Antitubercular / Q000008:administration & dosage / Q000737:chemistry; D002460:Cell Line; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry; D015195:Drug Design; D065546:Drug Liberation; D008264:Macrophages / Q000187:drug effects / Q000382:microbiology; D008855:Microscopy, Electron, Scanning; D009161:Mycobacterium / Q000187:drug effects / Q000254:growth & development; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry / Q000648:ultrastructure; D011091:Polyesters / Q000008:administration & dosage / Q000737:chemistry; D051381:Rats; D012293:Rifampin / Q000008:administration & dosage / Q000737:chemistry
D000577:Amides; D000904:Antibiotics, Antitubercular; D004337:Drug Carriers; D011091:Polyesters; D012293:Rifampin
Alveolar macrophages; Mycobacterium smegmatis; Nanoparticles; Polyesteramides; Rifampicin; Tuberculosis