ArticlePharmaceutical research2018
Functionalization of PLGA Nanoparticles with 1,3-β-glucan Enhances the Intracellular Pharmacokinetics of Rifampicin in Macrophages.
Article in Pharmaceutical research, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers, 1 of them a synthesis that pooled it.
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Who cites it
15 citing papers in PubMed, 1 synthesis or guideline pooled it, 24 citations in OpenAlex.
- Actively Targeted Nanoparticles for Enhanced Diagnosis, Treatment, and Vaccination of Tuberculosis: A Systematic Review.International journal of nanomedicine · 2025Pooled it
- Fucoidan-Functionalized Nanoparticles for Antimycobacterial Therapy: A Promising Approach against Drug-ResistantACS omega · 2026Article
- Weekly pulmonary delivery of β-glucan-chitosan-poly(lactic co-glycolic) acid (β-C-P) nanoparticles with daily standard oral therapy achieves control ofAntimicrobial agents and chemotherapy · 2026Article
- Antimicrobial Resistance inAntibiotics (Basel, Switzerland) · 2026Review
- Formulation and clinical translation of inhalable nanomedicines for the treatment and prevention of pulmonary infectious diseases.Drug delivery and translational research · 2025Review
- Inhalational Delivery ofAdvanced therapeutics · 2025Article
- Immunomodulatory Nanoparticles Induce Autophagy in Macrophages and ReduceACS infectious diseases · 2025Article
- Recent Advances in Nanotechnology-Based Strategies for Bone Tuberculosis Management.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Physicochemical and Biological Evaluation of Curdlan-Poly(Lactic-Co-Glycolic Acid) Nanoparticles as a Host-Directed Therapy Against Mycobacterium Tuberculosis.Journal of pharmaceutical sciences · 2022Article
- It Takes a Village: The Multifaceted Immune Response toFrontiers in immunology · 2022Review
- Recent Advances in Polymeric Nanoparticle-Encapsulated Drugs against Intracellular Infections.Molecules (Basel, Switzerland) · 2020Review
- Therapies and Vaccines Based on Nanoparticles for the Treatment of Systemic Fungal Infections.Frontiers in cellular and infection microbiology · 2020Review
- Development of Rifapentine-Loaded PLGA-Based Nanoparticles: In vitro Characterisation and in vivo Study in Mice.International journal of nanomedicine · 2020Article
- The Macrophage Response toFrontiers in cellular and infection microbiology · 2020Review
- Inhalable Fucoidan Microparticles Combining Two Antitubercular Drugs with Potential Application in Pulmonary Tuberculosis Therapy.Polymers · 2018Article
Corrections and comments
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Authors and funding
6 authors at 5 institutions in 2 countries.
Funding
Abstract
purposeMycobacterium tuberculosis which causes tuberculosis, is primarily resident within macrophages. 1,3-β-glucan has been proposed as a ligand to target drug loaded nanoparticles (NPs) to macrophages. In this study we characterized the intracellular pharmacokinetics of the anti-tubercular drug rifampicin delivered by 1,3-β-glucan functionalized PLGA NPs (Glu-PLGA). We hypothesized that Glu-PLGA NPs would be taken up at a faster rate than PLGA NPs, and consequently deliver higher amounts of rifampicin into the macrophages.
methodsCarbodiimide chemistry was employed to conjugate 1,3-β-glucan and rhodamine to PLGA. Rifampicin loaded PLGA and Glu-PLGA NPs as well as rhodamine functionalized PLGA and Glu-PLGA NPs were synthesized using an emulsion solvent evaporation technique. Intracellular pharmacokinetics of rifampicin and NPs were evaluated in THP-1 derived macrophages. A pharmacokinetic model was developed to describe uptake, and modelling was performed using ADAPT 5 software.
resultsThe NPs increased the rate of uptake of rifampicin by a factor of 17 and 62 in case of PLGA and Glu-PLGA, respectively. Expulsion of NPs from the macrophages was also observed, which was 3 fold greater for Glu-PLGA NPs than for PLGA NPs. However, the ratio of uptake to expulsion was similar for both NPs. After 24 h, the amount of rifampicin delivered by the PLGA and Glu-PLGA NPs was similar. The NPs resulted in at least a 10-fold increase in the uptake of rifampicin.
conclusionsFunctionalization of PLGA NPs with 1,3-β-glucan resulted in faster uptake of rifampicin into macrophages. These NPs may be useful to achieve rapid intracellular eradication of Mycobacterium tuberculosis.
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Registered trials
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