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In vitro phagocytosis and monocyte-macrophage activation with poly(lactide) and poly(lactide-co-glycolide) microspheres
Abstract
Treatment of many intracellular infections in the mononuclear phagocytic system (MPS), requires targeting of antibiotics by a drug delivery system. The objective of this study was to examine whether the particular nature of microspheres, made of end-group capped and uncapped poly(lactide) [PLA] and poly(lactide-co-glycolide) [PLGA 50:50 and PLGA 75:25], affect the uptake into and also the activation of monocyte-macrophages. Placebo and gentamicin sulfate containing microspheres were incubated with J774 murine monocyte-macrophages and fresh human blood monocytes. Phagocytosis became more efficient with increasing polymer hydrophobicity, whereas opsonization of the particles in serum exerted inconsistent effects. Monocyte activation was determined by flow cytometry and measured as oxidative burst. The cellular oxidative burst induced by the particles was higher for end-group uncapped polymers. Opsonization increased significantly the oxidative activity of J774 monocytes, but affected inconsistently that of human blood monocytes. The results demonstrate that PLA and PLGA microspheres loaded with gentamicin sulfate were efficiently phagocytosed in vitro. The end-group uncapped polymer-type microspheres promoted significantly cell activation, which may be of importance for drug delivery and targeting to intracellular infections.
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Metadata
- Authors
- Prior, S., Gander, B., Blarer, N., Merkle, H. P., Subirá, M. L., Irache, J. M., & Gamazo, C.
- Affiliations
- Universidad de Navarra (ES)
- ETH Zurich (CH)
- Corresponding author
- Gamazo, Carlos
- Venue
- European Journal of Pharmaceutical Sciences
- Publisher
- Elsevier BV
- Published
- 2002-03
- Volume
- 15
- Issue
- 2
- Pages
- 197-207
- ISSN
- 0928-0987 (ISSN-L)
- OpenAlex
- W2057572412
- Cited by
- 138
- References
- 42
- Citations by year
- 2026: 2 · 2025: 2 · 2024: 1 · 2023: 3 · 2022: 3 · 2021: 3 · 2020: 6 · 2019: 4 · 2018: 3 · 2017: 1 · 2016: 9 · 2015: 5 · 2014: 9 · 2013: 8 · 2012: 6
- FWCI
- 4.30
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- European Journal of Pharmaceutical Sciences (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Inhalation and Respiratory Drug Delivery
- Keywords
- polylactic acid, poly(lactic-co-glycolic acid), microspheres, phagocytosis, monocyte/macrophage activation, polymer hydrophobicity, opsonization, respiratory burst, gentamicin sulfate, intracellular drug delivery, J774 cells, blood monocytes
- MeSH terms
- Polylactic Acid-Polyglycolic Acid Copolymer, Aminoglycosides, Animals, Biocompatible Materials, Cells, Cultured, Gentamicins, Humans, Macrophage Activation, Macrophages, Microspheres, Monocytes, Phagocytosis, Polyesters, Polyglycolic Acid, Polymers, Drug Delivery Systems, Respiratory Burst, Lactic Acid, Mice, Static Electricity, Hydrophobic and Hydrophilic Interactions
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