The effect of drug loading on micelle properties: solid-state NMR as a tool to gain structural insight
Open accessAbstract
The present study highlights the importance of understanding the structural changes of micelles induced by drug loading on their physico‐chemical properties. A block copolymer with attached fructose, which interacts with GLUT5 receptor, was used and conjugated with a low and a high amount of platinum drugs. Against expectations, the low‐loading micelle, despite having a less defined morphology and larger nanoparticle size according to TEM, displays higher cellular uptake and higher toxicity. This behaviour can only be understood when elucidating additional information on the structure of micelles. Extensive solid‐state NMR measurements were therefore employed to reveal that the drug loading affected swelling and mobility of core and shell of the micelle. The results obtained from solid‐state NMR spectroscopy could explain all the observations on this system. In summary, solid‐state NMR spectroscopy is an excellent tool to understand the effects of drug loading on the behavior of micelles.
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In Callari et al.'s micelles, as drug loading increased, chain mobility and swelling in the core and shell decreased.
“They compared micelles with varied drug loading and from ssNMR analysis concluded that as the drug loading increased the chain mobility and swelling in the core and shell of the micelle decreased.”
From Polymeric micelles for the delivery of poorly soluble drugs: From nanoformulation to clinical approval. (2020) · cites this paper as [226]
In the main discussion (pp. 8441–8445), solid-state NMR describes the high-loading micelles as rigid and the low-loading micelles as having a mobile outer corona; the low-loading micelles also absorb more water. This supports reduced mobility and hydration with higher loading overall, but the text does not establish that mobility and swelling each decreased in both the core and shell: it describes the low-loading core as rigid too. (LLM, conf=0.78)
Experimental — accuracy not yet measuredCallari et al. used 1D and 2D ssNMR to investigate the correlation between drug loading and size of polymeric micelles.
“Callari et al. showcased the utility of 1D and 2D ssNMR to investigate the correlation between drug loading and size of polymeric micelles [226].”
From Polymeric micelles for the delivery of poorly soluble drugs: From nanoformulation to clinical approval. (2020) · cites this paper as [226]
In the section beginning “Polymer micelles are widely applied as nanocarriers for drug” (page not supplied), the paper says 1D and 2D solid-state NMR revealed micelle structure and dynamics. It also reports that low-loading micelles were larger than high-loading micelles, but says their sizes were measured by TEM and dynamic light scattering, not NMR. Thus the cited work supports the use of NMR to compare micelles at different drug loadings, but not the claim that NMR investigated the loading–size relationship. (LLM, conf=0.86)
Experimental — accuracy not yet measuredLower-loaded Callari et al. micelles had greater uptake and in vitro cytotoxicity than higher-loaded micelles.
“The lower loaded micelle had greater uptake and in vitro cytotoxicity, presumably due to the softer micellar structure facilitating interactions between the micelles and the cells.”
From Polymeric micelles for the delivery of poorly soluble drugs: From nanoformulation to clinical approval. (2020) · cites this paper as [226]
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References 20 · Cited by 68
Research works printed but not linked: 19
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- Authors
- Callari, M., De Souza, P. L., Rawal, A., & Stenzel, M. H.
- Affiliations
- Liverpool Hospital (AU)
- Liverpool Hospital Clinical School, and Molecular Medicine Research Group University of Western Sydney Sydney NSW 2170 Australia
- UNSW Sydney (AU)
- Corresponding author
- Rawal, Aditya
- Stenzel, Martina H.
- Venue
- Angewandte Chemie International Edition
- Publisher
- Wiley
- Published
- 2017-06
- Volume
- 56
- Issue
- 29
- Pages
- 8441-8445
- ISSN
- 1433-7851 (ISSN-L)
- 1521-3773
- OpenAlex
- W2620987407
- Cited by
- 68
- References
- 20
- Citations by year
- 2026: 4 · 2025: 5 · 2024: 8 · 2023: 7 · 2022: 5 · 2021: 10 · 2020: 13 · 2019: 7 · 2018: 8 · 2017: 1
- FWCI
- 2.86
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Licence
- Locations
- Angewandte Chemie International Edition (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Australian Research Council (DP130101625)
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Physical Sciences › Chemistry › Organic Chemistry › Surfactants and Colloidal Systems
- Physical Sciences › Chemistry › Organic Chemistry › Advanced Polymer Synthesis and Characterization
- Keywords
- drug loading, micelles, block copolymer micelles, fructose, platinum drugs, solid-state NMR, micelle structure, micelle swelling, cellular uptake, drug toxicity, nanoparticle size
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