Macrophage Targeting pH Responsive Polymersomes for Glucocorticoid Therapy.
Virgínia M Gouveia1,2,3,4, Loris Rizzello3,4,5, Claudia Nunes1
1LAQV/REQUIMTE, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal.
Pharmaceutics
|November 17, 2019
Summary
pH responsive polymersomes offer a novel nanocarrier for precise glucocorticoid (GC) delivery, enhancing anti-inflammatory effects in macrophages and overcoming therapeutic limitations.
Area of Science:
- Biomaterials Science
- Nanotechnology
- Pharmacology
Background:
- Glucocorticoids (GCs) are primary treatments for inflammatory diseases.
- Current GC therapies face limitations in precise delivery and side effects.
- Targeted drug delivery systems are needed to improve GC efficacy.
Purpose of the Study:
- To develop and evaluate pH responsive polymersomes for targeted GC delivery.
- To assess the stability, selectivity, and bioavailability of GCs within macrophages.
- To investigate the enhancement of anti-inflammatory effects using these nanocarriers.
Main Methods:
- Synthesis of poly(2-methacryloyloxyethyl phosphorylcholine)-poly(2-(diisopropylamino)ethyl methacrylate) (PMPC-PDPA) polymersomes.
- Loading of glucocorticoid drugs into the polymersomes.
- In vitro cellular studies using macrophages to assess drug delivery and efficacy.
- Molecular analysis of inflammation markers: nuclear factor-κB, tumour necrosis factor-α, interleukin-1β, and interleukin-6.
Main Results:
- PMPC-PDPA polymersomes demonstrated stability, selectivity, and enhanced bioavailability of loaded GCs in macrophages.
- Polymersomes significantly improved the anti-inflammatory activity of GCs.
- GC-loaded polymersomes effectively reduced key inflammation markers.
Conclusions:
- pH responsive PMPC-PDPA polymersomes are effective nanoscopic carriers for controlled GC delivery.
- This approach enhances anti-inflammatory effects and mitigates GC therapeutic limitations.
- PMPC-PDPA polymersomes show potential for improved inflammation management.
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