Fast Release of Lipophilic Agents from Circulating PEG-PDLLA Micelles Revealed by in Vivo Förster Resonance Energy Transfer Imaging
Abstract
Understanding the in vivo behavior of nanoparticles is critical for the translation of nanomedicine from laboratory research to clinical trials. In this work, in vivo Forster resonance energy transfer (FRET) imaging was employed to monitor the release of hydrophobic molecules from circulating poly(ethylene glycol)-poly( D, L-lactic acid) (PEG-PDLLA) micelles. A lipophilic FRET pair (DiIC(18) and DiOC(18)) was physically entrapped into micelle cores by mimicking the loading of hydrophobic drugs. The FRET efficiency was found significantly reduced within 15 min after intravenous injection, implying that DiIC(18) and DiOC(18) quickly escaped from the circulating micelles. FRET spectroscopy studies further demonstrated that alpha- and beta-globulins were major factors for the observed fast release, while gamma-globulins, albumin, and red blood cells played minor roles. These results provide useful information for developing blood-stable micelles to deliver hydrophobic drugs to the target site via prolonged circulation and extravasation from the vascular system.
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The low stability of micelles in plasma is also supported by data previously published by Chen et al., focused on PEG-PDLLA micelles.
“The low stability of micelles in plasma is also supported by the data previously published by Chen et al. [235], focused on poly(ethylene glycol)-poly(d, l-lactic acid) (PEG-PDLLA) micelles.”
From Polymeric micelles in drug delivery: An insight of the techniques for their characterization and assessment in biorelevant conditions (2021) · cites this paper as [235]
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- Authors
- Chen, H., Kim, S., He, W., Wang, H., Low, P. S., Park, K., & Cheng, J.-X.
- Affiliations
- Purdue University West Lafayette (US)
- Houston Methodist (US)
- Corresponding author
- Cheng, Ji-Xin
- Venue
- Langmuir
- Publisher
- American Chemical Society (ACS)
- Published
- 2008-02-08
- Volume
- 24
- Issue
- 10
- Pages
- 5213-5217
- ISSN
- 0743-7463 (ISSN-L)
- 1520-5827
- OpenAlex
- W2022646304
- Cited by
- 311
- References
- 0
- Citations by year
- 2026: 1 · 2025: 6 · 2024: 8 · 2023: 4 · 2022: 18 · 2021: 13 · 2020: 26 · 2019: 18 · 2018: 22 · 2017: 18 · 2016: 25 · 2015: 21 · 2014: 31 · 2013: 29 · 2012: 31
- FWCI
- 5.71
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Langmuir (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Heart, Lung, and Blood Institute (HL078715)
- National Institute of General Medical Sciences (R01GM065284, GM065284)
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › RNA Interference and Gene Delivery
- Keywords
- hydrophobic drug delivery, globulin, albumin, erythrocytes, extravasation
- MeSH terms
- Alpha-Globulins, Animals, Beta-Globulins, Biophysics, Cattle, Drug Carriers, Erythrocytes, Mice, Inbred BALB C, Micelles, Polyesters, Polyethylene Glycols, Polymers, Serum Albumin, Spectrometry, Fluorescence, Fluorescence Resonance Energy Transfer, Nanotechnology, Mice
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