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pH-driven enhancement of anti-tubercular drug loading on iron oxide nanoparticles for drug delivery in macrophages
- Source :
- Beilstein Journal of Nanotechnology, Beilstein Journal of Nanotechnology, Vol 12, Iss 1, Pp 1127-1139 (2021)
- Publication Year :
- 2021
- Publisher :
- Beilstein Institut, 2021.
-
Abstract
- Nanoparticle deployment in drug delivery is contingent upon controlled drug loading and a desired release profile, with simultaneous biocompatibility and cellular targeting. Iron oxide nanoparticles (IONPs), being biocompatible, are used as drug carriers. However, to prevent aggregation of bare IONPs, they are coated with stabilizing agents. We hypothesize that, zwitterionic drugs like norfloxacin (NOR, a fluoroquinolone) can manifest dual functionality β nanoparticle stabilization and antibiotic activity, eliminating the need of a separate stabilizing agent. Since these drugs have different charges, depending on the surrounding pH, drug loading enhancement could be pH dependent. Hence, upon synthesizing IONPs, they were coated with NOR, either at pH 5 (predominantly as cationic, NOR+) or at pH 10 (predominantly as anionic, NORβ). We observed that, drug loading at pH 5 exceeded that at pH 10 by 4.7β5.7 times. Furthermore, only the former (pH 5 system) exhibited a desirable slower drug release profile, compared to the free drug. NOR-coated IONPs also enable a 22 times higher drug accumulation in macrophages, compared to identical extracellular concentrations of the free drug. Thus, lowering the drug coating pH to 5 imparts multiple benefits β improved IONP stability, enhanced drug coating, higher drug uptake in macrophages at reduced toxicity and slower drug release.
- Subjects :
- Drug
Technology
Biocompatibility
medicine.drug_class
Science
QC1-999
media_common.quotation_subject
Antibiotics
General Physics and Astronomy
Nanoparticle
norfloxacin
TP1-1185
Full Research Paper
chemistry.chemical_compound
drug uptake
medicine
Nanotechnology
General Materials Science
Electrical and Electronic Engineering
Norfloxacin
media_common
Chemistry
Chemical technology
Physics
iron oxide nanoparticles
Nanoscience
intra-macrophage
Drug delivery
drug-nanoparticle interactions
Biophysics
Drug carrier
Iron oxide nanoparticles
medicine.drug
Subjects
Details
- ISSN :
- 21904286
- Volume :
- 12
- Database :
- OpenAIRE
- Journal :
- Beilstein Journal of Nanotechnology
- Accession number :
- edsair.doi.dedup.....95d0456ce85f7350494602f5b22164a8